Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name |
GPCRdb ID |
Reference ligand |
Vendors |
Species |
Assay Type |
Activity Type |
Activity Relation |
Activity Value |
p-value (-log) |
Fold selectivity |
Tested GPCRs |
Assay Description |
Source |
Mol weight |
Rot Bonds |
H don |
H acc |
LogP |
Smiles |
DOI |
|
137642920 | 158207 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 390 | 7 | 1 | 3 | 5.5 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c(Cl)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4086893 | 158207 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 390 | 7 | 1 | 3 | 5.5 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c(Cl)c1 | 10.1016/j.bmcl.2017.01.034 | |||
134157586 | 154252 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -3 | 3 | ChEMBL | 366 | 8 | 1 | 3 | 5.5 | O=C(O)CCCOc1ccc(-c2cc(Oc3ccccc3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3985509 | 154252 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | -3 | 3 | ChEMBL | 366 | 8 | 1 | 3 | 5.5 | O=C(O)CCCOc1ccc(-c2cc(Oc3ccccc3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
90407037 | 157380 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 377 | 8 | 1 | 3 | 5.3 | CCc1ccc(-n2cccc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4076902 | 157380 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 377 | 8 | 1 | 3 | 5.3 | CCc1ccc(-n2cccc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
90405670 | 164789 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 425 | 7 | 1 | 3 | 5.4 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccccc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4217143 | 164789 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 425 | 7 | 1 | 3 | 5.4 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccccc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
118707082 | 113071 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 309 | 4 | 1 | 3 | 3.3 | COc1ccc(S(=O)(=O)Nc2c(C)cc(F)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311196 | 113071 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 309 | 4 | 1 | 3 | 3.3 | COc1ccc(S(=O)(=O)Nc2c(C)cc(F)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
925016 | 113093 | None | 13 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 289 | 3 | 1 | 2 | 3.7 | Cc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311314 | 113093 | None | 13 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 289 | 3 | 1 | 2 | 3.7 | Cc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
137649416 | 157611 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 338 | 6 | 1 | 2 | 4.6 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4079893 | 157611 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 338 | 6 | 1 | 2 | 4.6 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2017.01.034 | |||
82051616 | 159551 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | 12 | 2 | ChEMBL | 304 | 6 | 1 | 2 | 4.2 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4101323 | 159551 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | 12 | 2 | ChEMBL | 304 | 6 | 1 | 2 | 4.2 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl | 10.1016/j.bmcl.2017.01.034 | |||
975397 | 113099 | None | 6 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 335 | 5 | 1 | 4 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1OC | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311324 | 113099 | None | 6 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 335 | 5 | 1 | 4 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1OC | 10.1016/j.bmcl.2014.05.012 | |||
137634844 | 156207 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 412 | 9 | 1 | 3 | 6.1 | CC(C)Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4063239 | 156207 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 412 | 9 | 1 | 3 | 6.1 | CC(C)Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
137640323 | 157070 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 358 | 7 | 1 | 4 | 4.3 | O=C(O)COc1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4073013 | 157070 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 358 | 7 | 1 | 4 | 4.3 | O=C(O)COc1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
137653973 | 158776 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 354 | 6 | 2 | 3 | 4.3 | Cc1cc(CCC(=O)O)ccc1OCc1cc(C(F)(F)F)ccc1O | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4093067 | 158776 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 354 | 6 | 2 | 3 | 4.3 | Cc1cc(CCC(=O)O)ccc1OCc1cc(C(F)(F)F)ccc1O | 10.1016/j.bmcl.2017.01.034 | |||
134133275 | 143730 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -8 | 2 | ChEMBL | 384 | 5 | 1 | 3 | 5.7 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3Cl)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3899885 | 143730 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -8 | 2 | ChEMBL | 384 | 5 | 1 | 3 | 5.7 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3Cl)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
85472225 | 162856 | None | 0 | Mouse | Functional | pEC50 | = | 7.0 | 7.0 | -2 | 3 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4171724 | 162856 | None | 0 | Mouse | Functional | pEC50 | = | 7.0 | 7.0 | -2 | 3 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
134133797 | 143655 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 338 | 3 | 0 | 4 | 3.6 | O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3899190 | 143655 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 338 | 3 | 0 | 4 | 3.6 | O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
85472621 | 162898 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4172392 | 162898 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
145955668 | 162520 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 415 | 7 | 1 | 4 | 6.0 | Cc1snc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4166208 | 162520 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 415 | 7 | 1 | 4 | 6.0 | Cc1snc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1021/acsmedchemlett.7b00233 | |||
134149615 | 148664 | None | 0 | Mouse | Functional | pEC50 | = | 7.0 | 7.0 | 1 | 3 | ChEMBL | 370 | 5 | 1 | 3 | 4.6 | O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3939004 | 148664 | None | 0 | Mouse | Functional | pEC50 | = | 7.0 | 7.0 | 1 | 3 | ChEMBL | 370 | 5 | 1 | 3 | 4.6 | O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1016/j.bmcl.2016.10.054 | |||
137640701 | 157181 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 427 | 9 | 1 | 4 | 6.2 | CCCc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4074388 | 157181 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 427 | 9 | 1 | 4 | 6.2 | CCCc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
137636217 | 156184 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 425 | 8 | 1 | 4 | 6.1 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2C2CC2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4063013 | 156184 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 425 | 8 | 1 | 4 | 6.1 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2C2CC2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
137642920 | 158207 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 390 | 7 | 1 | 3 | 5.5 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c(Cl)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4086893 | 158207 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 390 | 7 | 1 | 3 | 5.5 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c(Cl)c1 | 10.1016/j.bmcl.2017.01.034 | |||
90418476 | 162881 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 511 | 7 | 1 | 4 | 6.7 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C(F)(F)F)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4172136 | 162881 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 511 | 7 | 1 | 4 | 6.7 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C(F)(F)F)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
57521919 | 76304 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 23 | 2 | ChEMBL | 350 | 7 | 1 | 2 | 5.1 | O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058532 | 76304 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 23 | 2 | ChEMBL | 350 | 7 | 1 | 2 | 5.1 | O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL4207911 | 76304 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 23 | 2 | ChEMBL | 350 | 7 | 1 | 2 | 5.1 | O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
137636217 | 156184 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 425 | 8 | 1 | 4 | 6.1 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2C2CC2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4063013 | 156184 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 425 | 8 | 1 | 4 | 6.1 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2C2CC2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
134138099 | 147910 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 4 | 2 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3932897 | 147910 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 4 | 2 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
60195036 | 81752 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -630 | 2 | ChEMBL | 481 | 12 | 2 | 5 | 5.1 | Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm3002026 | |||
CHEMBL2163924 | 81752 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -630 | 2 | ChEMBL | 481 | 12 | 2 | 5 | 5.1 | Cc1cc(OCCCS(C)(=O)=O)ccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm3002026 | |||
137632299 | 156558 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 455 | 7 | 1 | 4 | 5.8 | Cc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CC(C)C(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4067368 | 156558 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 455 | 7 | 1 | 4 | 5.8 | Cc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CC(C)C(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
90406631 | 164529 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 503 | 7 | 1 | 3 | 6.1 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Br)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4213709 | 164529 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 503 | 7 | 1 | 3 | 6.1 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Br)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
137643228 | 158348 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 457 | 8 | 1 | 5 | 5.2 | COc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4088620 | 158348 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 457 | 8 | 1 | 5 | 5.2 | COc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
137647721 | 157922 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | 1 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.5 | CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4083440 | 157922 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | 1 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.5 | CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
59455584 | 157133 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 378 | 8 | 1 | 4 | 4.6 | CCc1ccc(-n2nccc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4073815 | 157133 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 378 | 8 | 1 | 4 | 4.6 | CCc1ccc(-n2nccc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
90406228 | 163797 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 453 | 8 | 1 | 3 | 5.9 | CCc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4204928 | 163797 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 453 | 8 | 1 | 3 | 5.9 | CCc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
561372 | 58844 | None | 46 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -20 | 2 | ChEMBL | 256 | 6 | 1 | 2 | 3.3 | O=C(O)CCc1ccc(OCc2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL1688452 | 58844 | None | 46 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -20 | 2 | ChEMBL | 256 | 6 | 1 | 2 | 3.3 | O=C(O)CCc1ccc(OCc2ccccc2)cc1 | 10.1021/jm300215x | |||
11717831 | 585 | None | 42 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -38 | 2 | ChEMBL | 379 | 7 | 2 | 7 | 2.4 | N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N | 10.6019/CHEMBL5442687 | |||
3289 | 585 | None | 42 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -38 | 2 | ChEMBL | 379 | 7 | 2 | 7 | 2.4 | N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N | 10.6019/CHEMBL5442687 | |||
CHEMBL4202825 | 585 | None | 42 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -38 | 2 | ChEMBL | 379 | 7 | 2 | 7 | 2.4 | N#Cc1c(N)nc(c(c1c1ccc(cc1)OCC1CC1)C#N)SCC(=O)N | 10.6019/CHEMBL5442687 | |||
86343591 | 163798 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 457 | 7 | 1 | 3 | 5.8 | Cc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4204946 | 163798 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 457 | 7 | 1 | 3 | 5.8 | Cc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
134133275 | 143730 | None | 0 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | 8 | 2 | ChEMBL | 384 | 5 | 1 | 3 | 5.7 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3Cl)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3899885 | 143730 | None | 0 | Mouse | Functional | pEC50 | = | 7.9 | 7.9 | 8 | 2 | ChEMBL | 384 | 5 | 1 | 3 | 5.7 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3Cl)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
137643958 | 158371 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 505 | 7 | 1 | 4 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Br)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4088889 | 158371 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 505 | 7 | 1 | 4 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Br)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
137657488 | 159774 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 441 | 7 | 1 | 4 | 5.5 | Cc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4104082 | 159774 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 441 | 7 | 1 | 4 | 5.5 | Cc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
90418753 | 162491 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 463 | 8 | 1 | 4 | 6.6 | CCc1ccc(-c2nsc(C(F)(F)F)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4165803 | 162491 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 463 | 8 | 1 | 4 | 6.6 | CCc1ccc(-c2nsc(C(F)(F)F)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
73777111 | 149798 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -1 | 2 | ChEMBL | 373 | 3 | 1 | 2 | 5.1 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3947837 | 149798 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -1 | 2 | ChEMBL | 373 | 3 | 1 | 2 | 5.1 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
25098573 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 8 | 2 | ChEMBL | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 10.1021/jm800970b | |||
5587 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 8 | 2 | ChEMBL | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 10.1021/jm800970b | |||
CHEMBL463785 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 8 | 2 | ChEMBL | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 10.1021/jm800970b | |||
134141270 | 146898 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -3 | 3 | ChEMBL | 334 | 8 | 1 | 3 | 4.6 | CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3924759 | 146898 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -3 | 3 | ChEMBL | 334 | 8 | 1 | 3 | 4.6 | CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
90418849 | 162791 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 473 | 7 | 1 | 4 | 6.5 | Cc1cc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)cc1CCC(=O)O | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4170501 | 162791 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 473 | 7 | 1 | 4 | 6.5 | Cc1cc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)cc1CCC(=O)O | 10.1021/acsmedchemlett.7b00233 | |||
11316919 | 3068 | None | 31 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -2 | 8 | ChEMBL | 451 | 4 | 0 | 4 | 5.3 | Clc1c(cccc1)n1nc2C(=O)N(CCOc2c1c1ccc(cc1)Cl)CC(C)(F)F | 10.6019/CHEMBL5442687 | |||
11693 | 3068 | None | 31 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -2 | 8 | ChEMBL | 451 | 4 | 0 | 4 | 5.3 | Clc1c(cccc1)n1nc2C(=O)N(CCOc2c1c1ccc(cc1)Cl)CC(C)(F)F | 10.6019/CHEMBL5442687 | |||
CHEMBL484929 | 3068 | None | 31 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -2 | 8 | ChEMBL | 451 | 4 | 0 | 4 | 5.3 | Clc1c(cccc1)n1nc2C(=O)N(CCOc2c1c1ccc(cc1)Cl)CC(C)(F)F | 10.6019/CHEMBL5442687 | |||
8190724 | 113092 | None | 5 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 359 | 4 | 1 | 3 | 4.3 | Cc1cc(C)c(NS(=O)(=O)c2ccc(OC(F)(F)F)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311313 | 113092 | None | 5 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 359 | 4 | 1 | 3 | 4.3 | Cc1cc(C)c(NS(=O)(=O)c2ccc(OC(F)(F)F)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
258072 | 80119 | None | 21 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 275 | 3 | 1 | 2 | 3.4 | Cc1cc(C)c(NS(=O)(=O)c2ccccc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL2131154 | 80119 | None | 21 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 275 | 3 | 1 | 2 | 3.4 | Cc1cc(C)c(NS(=O)(=O)c2ccccc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
91824000 | 113091 | None | 6 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1cccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311312 | 113091 | None | 6 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1cccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
137647721 | 157922 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | 1 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.5 | CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4083440 | 157922 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | 1 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.5 | CC(CC(=O)O)c1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
57521919 | 76304 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 23 | 2 | ChEMBL | 350 | 7 | 1 | 2 | 5.1 | O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
CHEMBL2058532 | 76304 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 23 | 2 | ChEMBL | 350 | 7 | 1 | 2 | 5.1 | O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
CHEMBL4207911 | 76304 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 23 | 2 | ChEMBL | 350 | 7 | 1 | 2 | 5.1 | O=C(O)CCc1ccc(OCc2cc(F)ccc2-c2ccccc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
54586011 | 61828 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -14 | 2 | ChEMBL | 324 | 6 | 1 | 2 | 4.3 | O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 | 10.1021/jm300215x | |||
CHEMBL1773257 | 61828 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -14 | 2 | ChEMBL | 324 | 6 | 1 | 2 | 4.3 | O=C(O)CCc1ccc(OCc2cccc(C(F)(F)F)c2)cc1 | 10.1021/jm300215x | |||
137640701 | 157181 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 427 | 9 | 1 | 4 | 6.2 | CCCc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4074388 | 157181 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 427 | 9 | 1 | 4 | 6.2 | CCCc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
134151903 | 153445 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 438 | 6 | 1 | 6 | 4.2 | COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3978465 | 153445 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 438 | 6 | 1 | 6 | 4.2 | COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
73777069 | 142756 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 2 | ChEMBL | 389 | 4 | 1 | 3 | 5.0 | O=C(O)CC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3891920 | 142756 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 2 | ChEMBL | 389 | 4 | 1 | 3 | 5.0 | O=C(O)CC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
73777174 | 150542 | None | 0 | Mouse | Functional | pEC50 | = | 5.9 | 5.9 | 2 | 2 | ChEMBL | 356 | 3 | 1 | 3 | 4.4 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccn1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3954140 | 150542 | None | 0 | Mouse | Functional | pEC50 | = | 5.9 | 5.9 | 2 | 2 | ChEMBL | 356 | 3 | 1 | 3 | 4.4 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccn1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
11498 | 3019 | None | 34 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -18 | 8 | ChEMBL | 392 | 3 | 1 | 5 | 4.1 | CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC | 10.6019/CHEMBL5442687 | |||
4995951 | 3019 | None | 34 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -18 | 8 | ChEMBL | 392 | 3 | 1 | 5 | 4.1 | CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC | 10.6019/CHEMBL5442687 | |||
CHEMBL59898 | 3019 | None | 34 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -18 | 8 | ChEMBL | 392 | 3 | 1 | 5 | 4.1 | CCOC(=O)c1c(C)[nH]c2c1c1CN3CCc4c(C3Oc1cc2)ccc(c4)OC | 10.6019/CHEMBL5442687 | |||
134136175 | 142767 | None | 0 | Mouse | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 3 | ChEMBL | 388 | 7 | 1 | 3 | 5.5 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)ccc1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3892019 | 142767 | None | 0 | Mouse | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 3 | ChEMBL | 388 | 7 | 1 | 3 | 5.5 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)ccc1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
643684 | 107571 | None | 40 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 8 | 2 | ChEMBL | 298 | 15 | 2 | 2 | 5.1 | CCCCCC[C@@H](O)C/C=C\CCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
CHEMBL3186422 | 107571 | None | 40 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 8 | 2 | ChEMBL | 298 | 15 | 2 | 2 | 5.1 | CCCCCC[C@@H](O)C/C=C\CCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
86343965 | 163906 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 443 | 7 | 1 | 3 | 5.5 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4206168 | 163906 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 443 | 7 | 1 | 3 | 5.5 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
90418650 | 157447 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2csnc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4077787 | 157447 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2csnc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
85470884 | 164099 | None | 3 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 5 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4208325 | 164099 | None | 3 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 5 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
134149615 | 148664 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 3 | ChEMBL | 370 | 5 | 1 | 3 | 4.6 | O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3939004 | 148664 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 3 | ChEMBL | 370 | 5 | 1 | 3 | 4.6 | O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1016/j.bmcl.2016.10.054 | |||
90406583 | 164756 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 416 | 7 | 1 | 4 | 4.9 | N#Cc1ccn(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(F)c1F | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4216721 | 164756 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | ChEMBL | 416 | 7 | 1 | 4 | 4.9 | N#Cc1ccn(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(F)c1F | 10.1016/j.bmcl.2018.02.013 | |||
134144000 | 150297 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | -1 | 2 | ChEMBL | 431 | 8 | 1 | 6 | 4.0 | COc1cc(O[C@H]2C[C@H](OC)C2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3952043 | 150297 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | -1 | 2 | ChEMBL | 431 | 8 | 1 | 6 | 4.0 | COc1cc(O[C@H]2C[C@H](OC)C2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134154415 | 152783 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 447 | 6 | 1 | 5 | 6.3 | Cc1cnc(Oc2cc(Cl)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)c2)s1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3972870 | 152783 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | ChEMBL | 447 | 6 | 1 | 5 | 6.3 | Cc1cnc(Oc2cc(Cl)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)c2)s1 | 10.1021/acsmedchemlett.6b00394 | |||
137640328 | 157076 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 461 | 7 | 1 | 4 | 5.9 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)c1F | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4073078 | 157076 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 461 | 7 | 1 | 4 | 5.9 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)c1F | 10.1016/j.bmcl.2017.06.028 | |||
134133675 | 143349 | None | 0 | Mouse | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 3 | ChEMBL | 318 | 8 | 1 | 3 | 4.1 | CCOc1ccc(F)c(-c2ccc(OCCCC(=O)O)cc2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3896714 | 143349 | None | 0 | Mouse | Functional | pEC50 | = | 6.9 | 6.9 | 2 | 3 | ChEMBL | 318 | 8 | 1 | 3 | 4.1 | CCOc1ccc(F)c(-c2ccc(OCCCC(=O)O)cc2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
1050 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1021/jm300215x | |||
11595431 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1021/jm300215x | |||
CHEMBL207881 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1021/jm300215x | |||
85471695 | 158761 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 394 | 8 | 1 | 3 | 6.2 | CCc1ccc(-c2cscc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4092882 | 158761 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | ChEMBL | 394 | 8 | 1 | 3 | 6.2 | CCc1ccc(-c2cscc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
57522038 | 3887 | None | 48 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.ejmech.2023.115267 | |||
6490 | 3887 | None | 48 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.ejmech.2023.115267 | |||
CHEMBL2058533 | 3887 | None | 48 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.ejmech.2023.115267 | |||
137657736 | 159732 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 385 | 7 | 1 | 4 | 5.2 | Cc1c(CCC(=O)O)ccc(OCc2conc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4103573 | 159732 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 385 | 7 | 1 | 4 | 5.2 | Cc1c(CCC(=O)O)ccc(OCc2conc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
90405989 | 156051 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 383 | 7 | 1 | 3 | 5.3 | Cc1c(CCC(=O)O)ccc(OCc2cccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4061340 | 156051 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 383 | 7 | 1 | 3 | 5.3 | Cc1c(CCC(=O)O)ccc(OCc2cccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
137653883 | 158614 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 493 | 7 | 1 | 4 | 6.6 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)cc1C(F)(F)F | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4091291 | 158614 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 493 | 7 | 1 | 4 | 6.6 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)cc1C(F)(F)F | 10.1016/j.bmcl.2017.06.028 | |||
11195 | 3882 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
86280676 | 3882 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3941880 | 3882 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
87055315 | 165852 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 349 | 8 | 2 | 3 | 4.7 | CC(C)Nc1ccccc1-c1cc(F)c(OCCCC(=O)O)c(F)c1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4246850 | 165852 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 349 | 8 | 2 | 3 | 4.7 | CC(C)Nc1ccccc1-c1cc(F)c(OCCCC(=O)O)c(F)c1 | 10.1016/j.bmcl.2018.06.047 | |||
145986046 | 166007 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 19 | 2 | ChEMBL | 437 | 10 | 1 | 6 | 4.3 | CO[C@H]1C[C@H](Oc2ccc([N+](=O)[O-])c(-c3cc(F)c(OCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4250196 | 166007 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 19 | 2 | ChEMBL | 437 | 10 | 1 | 6 | 4.3 | CO[C@H]1C[C@H](Oc2ccc([N+](=O)[O-])c(-c3cc(F)c(OCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
3038495 | 708 | None | 33 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -2754 | 8 | ChEMBL | 417 | 8 | 1 | 4 | 4.2 | COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 | 10.6019/CHEMBL5442687 | |||
7625 | 708 | None | 33 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -2754 | 8 | ChEMBL | 417 | 8 | 1 | 4 | 4.2 | COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 | 10.6019/CHEMBL5442687 | |||
CHEMBL25236 | 708 | None | 33 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -2754 | 8 | ChEMBL | 417 | 8 | 1 | 4 | 4.2 | COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 | 10.6019/CHEMBL5442687 | |||
142738582 | 184626 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -42 | 2 | ChEMBL | 293 | 4 | 2 | 1 | 4.5 | Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 | 10.1021/acs.jmedchem.1c00031 | |||
CHEMBL4847662 | 184626 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -42 | 2 | ChEMBL | 293 | 4 | 2 | 1 | 4.5 | Cc1ccc(C)c(-c2cc3cc(CCC(=O)O)ccc3[nH]2)c1 | 10.1021/acs.jmedchem.1c00031 | |||
134157207 | 154300 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -3 | 2 | ChEMBL | 386 | 7 | 1 | 3 | 5.3 | Cc1cc(-c2cc(OC(F)(F)F)ccc2F)cc(C)c1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3985939 | 154300 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -3 | 2 | ChEMBL | 386 | 7 | 1 | 3 | 5.3 | Cc1cc(-c2cc(OC(F)(F)F)ccc2F)cc(C)c1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
134135468 | 144563 | None | 0 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -1 | 2 | ChEMBL | 389 | 4 | 1 | 3 | 4.8 | O=C(O)C1CCC(C2CCN(c3cc(OC(F)(F)F)ccc3F)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3906716 | 144563 | None | 0 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -1 | 2 | ChEMBL | 389 | 4 | 1 | 3 | 4.8 | O=C(O)C1CCC(C2CCN(c3cc(OC(F)(F)F)ccc3F)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
134145700 | 148839 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 400 | 7 | 1 | 4 | 5.0 | COc1cc(OC2CCC2)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3940429 | 148839 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 400 | 7 | 1 | 4 | 5.0 | COc1cc(OC2CCC2)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134155067 | 151395 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 401 | 7 | 1 | 5 | 4.4 | COc1cc(OC2CCC2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3960738 | 151395 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 401 | 7 | 1 | 5 | 4.4 | COc1cc(OC2CCC2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
137646995 | 157925 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 391 | 7 | 1 | 4 | 5.0 | O=C(O)CCc1ccc(OCc2c(-c3ccccc3)noc2C(F)(F)F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4083499 | 157925 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 391 | 7 | 1 | 4 | 5.0 | O=C(O)CCc1ccc(OCc2c(-c3ccccc3)noc2C(F)(F)F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
137660451 | 159338 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 445 | 7 | 1 | 4 | 5.4 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(F)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4099026 | 159338 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 445 | 7 | 1 | 4 | 5.4 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(F)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
134151115 | 152288 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -4 | 3 | ChEMBL | 336 | 6 | 1 | 3 | 5.0 | O=C(O)CCc1cc2cc(-c3cccc(OC4CCC4)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3968537 | 152288 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -4 | 3 | ChEMBL | 336 | 6 | 1 | 3 | 5.0 | O=C(O)CCc1cc2cc(-c3cccc(OC4CCC4)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
90418653 | 137600 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 469 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c1C | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL3754160 | 137600 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 469 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c1C | 10.1021/acsmedchemlett.7b00233 | |||
86343594 | 163692 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 461 | 7 | 1 | 3 | 5.6 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2F)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4203544 | 163692 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 461 | 7 | 1 | 3 | 5.6 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2F)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
137641343 | 157149 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 117 | 2 | ChEMBL | 342 | 8 | 1 | 3 | 4.7 | Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4074009 | 157149 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 117 | 2 | ChEMBL | 342 | 8 | 1 | 3 | 4.7 | Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
134132142 | 144957 | None | 0 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | 13 | 2 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3909872 | 144957 | None | 0 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | 13 | 2 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1021/acsmedchemlett.6b00360 | |||
134132142 | 144957 | None | 0 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | 13 | 2 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3909872 | 144957 | None | 0 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | 13 | 2 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
57522038 | 3887 | None | 48 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | 13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
6490 | 3887 | None | 48 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | 13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
CHEMBL2058533 | 3887 | None | 48 | Mouse | Functional | pEC50 | = | 7.8 | 7.8 | 13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
137635671 | 156082 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 461 | 7 | 1 | 4 | 5.9 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4061699 | 156082 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 461 | 7 | 1 | 4 | 5.9 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
137632299 | 156558 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 455 | 7 | 1 | 4 | 5.8 | Cc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CC(C)C(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4067368 | 156558 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 455 | 7 | 1 | 4 | 5.8 | Cc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CC(C)C(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
137661886 | 159421 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 453 | 7 | 1 | 4 | 6.2 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4099943 | 159421 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 453 | 7 | 1 | 4 | 6.2 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c1C | 10.1016/j.bmcl.2017.06.028 | |||
137657968 | 159686 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 394 | 8 | 1 | 3 | 6.2 | CCc1ccc(-c2ccsc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4103081 | 159686 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 394 | 8 | 1 | 3 | 6.2 | CCc1ccc(-c2ccsc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
90418139 | 162676 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 443 | 7 | 1 | 4 | 5.7 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccccc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4168786 | 162676 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 443 | 7 | 1 | 4 | 5.7 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccccc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
90406219 | 164409 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 469 | 7 | 1 | 3 | 5.8 | O=C(O)CCc1ccc(OCc2c(Br)ccn2-c2ccc(Cl)cc2)c(F)c1F | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4212281 | 164409 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 469 | 7 | 1 | 3 | 5.8 | O=C(O)CCc1ccc(OCc2c(Br)ccn2-c2ccc(Cl)cc2)c(F)c1F | 10.1016/j.bmcl.2018.02.013 | |||
90406961 | 163877 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 445 | 7 | 1 | 3 | 5.9 | OCCCc1ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1F | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4205879 | 163877 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 445 | 7 | 1 | 3 | 5.9 | OCCCc1ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1F | 10.1016/j.bmcl.2018.02.013 | |||
90406842 | 164801 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 427 | 7 | 1 | 3 | 5.5 | Cc1c(CCC(=O)O)ccc(OCc2cccn2-c2ccc(Br)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4217252 | 164801 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 427 | 7 | 1 | 3 | 5.5 | Cc1c(CCC(=O)O)ccc(OCc2cccn2-c2ccc(Br)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
85472222 | 163161 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 437 | 9 | 1 | 4 | 6.7 | CCc1ccc(-c2nsc(C(C)C)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4176414 | 163161 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 437 | 9 | 1 | 4 | 6.7 | CCc1ccc(-c2nsc(C(C)C)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
51349861 | 58846 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -77 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.1 | O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL1688454 | 58846 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -77 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.1 | O=C(O)CCc1ccc(OCc2ccc(Oc3ccccc3)cc2)cc1 | 10.1021/jm300215x | |||
10466 | 166765 | None | 59 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 12 | 2 | ChEMBL | 272 | 15 | 2 | 2 | 4.5 | O=C(O)CCCCCCCCCCCCCCCO | 10.1039/C7MD00130D | |||
CHEMBL4281719 | 166765 | None | 59 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 12 | 2 | ChEMBL | 272 | 15 | 2 | 2 | 4.5 | O=C(O)CCCCCCCCCCCCCCCO | 10.1039/C7MD00130D | |||
134153222 | 152614 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccncc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3971461 | 152614 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccncc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
134134149 | 143462 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -2 | 3 | ChEMBL | 348 | 8 | 1 | 3 | 5.4 | O=C(O)CCCOc1ccc(-c2cccc(Oc3ccccc3)c2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3897776 | 143462 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | -2 | 3 | ChEMBL | 348 | 8 | 1 | 3 | 5.4 | O=C(O)CCCOc1ccc(-c2cccc(Oc3ccccc3)c2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
134155480 | 151340 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 38 | 2 | ChEMBL | 384 | 5 | 1 | 3 | 5.0 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3960231 | 151340 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 38 | 2 | ChEMBL | 384 | 5 | 1 | 3 | 5.0 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
137648785 | 157702 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 427 | 7 | 1 | 4 | 5.2 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccccc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4080995 | 157702 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 427 | 7 | 1 | 4 | 5.2 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccccc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
137655521 | 159081 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 467 | 8 | 1 | 4 | 6.1 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C4CC4)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4096332 | 159081 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 467 | 8 | 1 | 4 | 6.1 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C4CC4)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
25109512 | 189873 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 12 | 2 | ChEMBL | 382 | 10 | 1 | 5 | 4.8 | O=C(O)CCCc1ccc(OCCN(c2ccccc2)c2nccs2)cc1 | 10.1021/jm800970b | |||
CHEMBL515995 | 189873 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 12 | 2 | ChEMBL | 382 | 10 | 1 | 5 | 4.8 | O=C(O)CCCc1ccc(OCCN(c2ccccc2)c2nccs2)cc1 | 10.1021/jm800970b | |||
137641343 | 157149 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 117 | 2 | ChEMBL | 342 | 8 | 1 | 3 | 4.7 | Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4074009 | 157149 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 117 | 2 | ChEMBL | 342 | 8 | 1 | 3 | 4.7 | Cc1ccc(OC(C)C)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
90418782 | 163178 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 513 | 7 | 1 | 4 | 6.6 | O=C(O)CCc1c(F)c(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4176642 | 163178 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 513 | 7 | 1 | 4 | 6.6 | O=C(O)CCc1c(F)c(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
90407441 | 163809 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 417 | 7 | 1 | 3 | 6.0 | Cc1c(CCC(=O)O)ccc(OCc2c(Cl)ccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4205035 | 163809 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 417 | 7 | 1 | 3 | 6.0 | Cc1c(CCC(=O)O)ccc(OCc2c(Cl)ccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
54580132 | 61824 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -3 | 2 | ChEMBL | 334 | 6 | 1 | 2 | 4.0 | O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 | 10.1021/jm300215x | |||
CHEMBL1773253 | 61824 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -3 | 2 | ChEMBL | 334 | 6 | 1 | 2 | 4.0 | O=C(O)CCc1ccc(OCc2ccccc2Br)cc1 | 10.1021/jm300215x | |||
7789 | 100739 | None | 56 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 300 | 16 | 2 | 2 | 5.3 | CCCCCCC(O)CCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
CHEMBL292352 | 100739 | None | 56 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 300 | 16 | 2 | 2 | 5.3 | CCCCCCC(O)CCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
86343595 | 164790 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 461 | 7 | 1 | 3 | 5.6 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(F)c(F)c2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4217161 | 164790 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 461 | 7 | 1 | 3 | 5.6 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(F)c(F)c2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
137646145 | 158116 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 385 | 7 | 1 | 4 | 5.2 | Cc1c(CCC(=O)O)ccc(OCc2ncoc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4085643 | 158116 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 385 | 7 | 1 | 4 | 5.2 | Cc1c(CCC(=O)O)ccc(OCc2ncoc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
57521809 | 76291 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 13 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058520 | 76291 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 13 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL4210970 | 76291 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 13 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
86294762 | 164210 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 477 | 7 | 1 | 3 | 6.2 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2F)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4209823 | 164210 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 477 | 7 | 1 | 3 | 6.2 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2F)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
134133355 | 143623 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 413 | 6 | 1 | 5 | 4.2 | COc1cc(OC2CCC2)nc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3898962 | 143623 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | ChEMBL | 413 | 6 | 1 | 5 | 4.2 | COc1cc(OC2CCC2)nc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
137657488 | 159774 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 441 | 7 | 1 | 4 | 5.5 | Cc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4104082 | 159774 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 441 | 7 | 1 | 4 | 5.5 | Cc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
134146386 | 148995 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 384 | 5 | 1 | 3 | 5.0 | O=C(O)CC[C@@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3941726 | 148995 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | ChEMBL | 384 | 5 | 1 | 3 | 5.0 | O=C(O)CC[C@@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
46892131 | 144759 | None | 3 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -3 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3908362 | 144759 | None | 3 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -3 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
134143163 | 145832 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.7 | Cc1ccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3916564 | 145832 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.7 | Cc1ccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
90406575 | 164449 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 455 | 8 | 1 | 4 | 5.4 | COc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4212717 | 164449 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 455 | 8 | 1 | 4 | 5.4 | COc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
134136175 | 142767 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -1 | 3 | ChEMBL | 388 | 7 | 1 | 3 | 5.5 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)ccc1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3892019 | 142767 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -1 | 3 | ChEMBL | 388 | 7 | 1 | 3 | 5.5 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)ccc1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
145983493 | 165599 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 371 | 2 | ChEMBL | 442 | 10 | 1 | 4 | 5.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4240607 | 165599 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 371 | 2 | ChEMBL | 442 | 10 | 1 | 4 | 5.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
134146021 | 149152 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -5 | 2 | ChEMBL | 392 | 7 | 1 | 3 | 5.3 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)c(F)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3942922 | 149152 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -5 | 2 | ChEMBL | 392 | 7 | 1 | 3 | 5.3 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)c(F)c1 | 10.1016/j.bmcl.2016.10.054 | |||
134154330 | 152969 | None | 0 | Mouse | Functional | pEC50 | = | 5.7 | 5.7 | 1 | 2 | ChEMBL | 340 | 7 | 1 | 3 | 4.5 | O=C(O)CCCOc1ccc(-c2ccccc2OC(F)(F)F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3974501 | 152969 | None | 0 | Mouse | Functional | pEC50 | = | 5.7 | 5.7 | 1 | 2 | ChEMBL | 340 | 7 | 1 | 3 | 4.5 | O=C(O)CCCOc1ccc(-c2ccccc2OC(F)(F)F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137638355 | 156921 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 97 | 2 | ChEMBL | 318 | 6 | 1 | 2 | 4.6 | Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4071290 | 156921 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 97 | 2 | ChEMBL | 318 | 6 | 1 | 2 | 4.6 | Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
134147174 | 149791 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 2 | ChEMBL | 370 | 6 | 1 | 3 | 5.7 | O=C(O)CCc1cc2cc(-c3cc(Cl)cc(OC4CCC4)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3947787 | 149791 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 2 | ChEMBL | 370 | 6 | 1 | 3 | 5.7 | O=C(O)CCc1cc2cc(-c3cc(Cl)cc(OC4CCC4)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
137649360 | 157478 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 495 | 7 | 1 | 4 | 6.3 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C(F)(F)F)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4078286 | 157478 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 495 | 7 | 1 | 4 | 6.3 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C(F)(F)F)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
90418662 | 159033 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 395 | 8 | 1 | 4 | 5.6 | CCc1ccc(-c2sncc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4095819 | 159033 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 395 | 8 | 1 | 4 | 5.6 | CCc1ccc(-c2sncc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
73777175 | 143996 | None | 0 | Mouse | Functional | pEC50 | = | 6.7 | 6.7 | 1 | 3 | ChEMBL | 357 | 3 | 1 | 2 | 4.9 | O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3901994 | 143996 | None | 0 | Mouse | Functional | pEC50 | = | 6.7 | 6.7 | 1 | 3 | ChEMBL | 357 | 3 | 1 | 2 | 4.9 | O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
57521814 | 76296 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 10 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.0 | COc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058525 | 76296 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 10 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.0 | COc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
90418662 | 159033 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 395 | 8 | 1 | 4 | 5.6 | CCc1ccc(-c2sncc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4095819 | 159033 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 395 | 8 | 1 | 4 | 5.6 | CCc1ccc(-c2sncc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
85470884 | 164099 | None | 3 | Mouse | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 5 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4208325 | 164099 | None | 3 | Mouse | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 5 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
57521808 | 76290 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -3 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1cccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm300215x | |||
CHEMBL2058519 | 76290 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -3 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1cccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm300215x | |||
57521809 | 76291 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 13 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
CHEMBL2058520 | 76291 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 13 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
CHEMBL4210970 | 76291 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 13 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
90442468 | 164577 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 456 | 8 | 1 | 5 | 4.8 | COc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cn1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4214224 | 164577 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 456 | 8 | 1 | 5 | 4.8 | COc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cn1 | 10.1016/j.bmcl.2018.02.013 | |||
134156096 | 151536 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -5 | 3 | ChEMBL | 400 | 8 | 1 | 3 | 6.2 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3961950 | 151536 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -5 | 3 | ChEMBL | 400 | 8 | 1 | 3 | 6.2 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137638355 | 156921 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 97 | 2 | ChEMBL | 318 | 6 | 1 | 2 | 4.6 | Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4071290 | 156921 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 97 | 2 | ChEMBL | 318 | 6 | 1 | 2 | 4.6 | Cc1ccc(Cl)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
137642604 | 158609 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 41 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.2 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4091228 | 158609 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 41 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.2 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
137632403 | 156395 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 386 | 8 | 1 | 4 | 4.9 | COc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4065447 | 156395 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 386 | 8 | 1 | 4 | 4.9 | COc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
84481843 | 113098 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 333 | 5 | 1 | 3 | 4.2 | Cc1cc(C)c(NS(=O)(=O)c2ccc(OC(C)C)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311322 | 113098 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 333 | 5 | 1 | 3 | 4.2 | Cc1cc(C)c(NS(=O)(=O)c2ccc(OC(C)C)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
8190727 | 113101 | None | 2 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 347 | 3 | 1 | 4 | 3.6 | Cc1cc(C)c(NS(=O)(=O)c2ccc3c(c2)OCCCO3)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311326 | 113101 | None | 2 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 347 | 3 | 1 | 4 | 3.6 | Cc1cc(C)c(NS(=O)(=O)c2ccc3c(c2)OCCCO3)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
137632403 | 156395 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 386 | 8 | 1 | 4 | 4.9 | COc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4065447 | 156395 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 386 | 8 | 1 | 4 | 4.9 | COc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
134153562 | 152812 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | -2 | 3 | ChEMBL | 394 | 7 | 1 | 3 | 4.9 | O=C(O)CCCOc1c(F)cc(-c2cc(OC(F)(F)F)ccc2F)cc1F | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3973101 | 152812 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | -2 | 3 | ChEMBL | 394 | 7 | 1 | 3 | 4.9 | O=C(O)CCCOc1c(F)cc(-c2cc(OC(F)(F)F)ccc2F)cc1F | 10.1016/j.bmcl.2016.10.054 | |||
87055315 | 165852 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 349 | 8 | 2 | 3 | 4.7 | CC(C)Nc1ccccc1-c1cc(F)c(OCCCC(=O)O)c(F)c1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4246850 | 165852 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 349 | 8 | 2 | 3 | 4.7 | CC(C)Nc1ccccc1-c1cc(F)c(OCCCC(=O)O)c(F)c1 | 10.1016/j.bmcl.2018.06.047 | |||
73777156 | 152804 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -1 | 3 | ChEMBL | 396 | 4 | 1 | 4 | 4.7 | N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3973034 | 152804 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -1 | 3 | ChEMBL | 396 | 4 | 1 | 4 | 4.7 | N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
137642604 | 158609 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 41 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.2 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4091228 | 158609 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 41 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.2 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
90418651 | 162508 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 469 | 8 | 1 | 4 | 6.6 | CCc1cc(CCC(=O)O)ccc1OCc1c(-c2ccc(Cl)cc2)nsc1C(F)(F)F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4166012 | 162508 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 469 | 8 | 1 | 4 | 6.6 | CCc1cc(CCC(=O)O)ccc1OCc1c(-c2ccc(Cl)cc2)nsc1C(F)(F)F | 10.1021/acsmedchemlett.7b00233 | |||
59455552 | 156132 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 384 | 7 | 1 | 4 | 4.7 | Cc1c(CCC(=O)O)ccc(OCc2ccnn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4062462 | 156132 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 384 | 7 | 1 | 4 | 4.7 | Cc1c(CCC(=O)O)ccc(OCc2ccnn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
134154417 | 152793 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 2 | ChEMBL | 374 | 7 | 1 | 3 | 4.6 | O=C(O)CCCOc1ccc(-c2cc(-[n+]3ccsc3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3972973 | 152793 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 2 | ChEMBL | 374 | 7 | 1 | 3 | 4.6 | O=C(O)CCCOc1ccc(-c2cc(-[n+]3ccsc3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
57521813 | 76295 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | ChEMBL | 400 | 7 | 1 | 2 | 6.0 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(C(F)(F)F)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058524 | 76295 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | ChEMBL | 400 | 7 | 1 | 2 | 6.0 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(C(F)(F)F)cc2)cc1 | 10.1021/jm300215x | |||
134134846 | 144327 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -1 | 2 | ChEMBL | 337 | 3 | 0 | 3 | 4.2 | O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3904654 | 144327 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -1 | 2 | ChEMBL | 337 | 3 | 0 | 3 | 4.2 | O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
54582149 | 61826 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -33 | 2 | ChEMBL | 281 | 6 | 1 | 3 | 3.2 | N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm300215x | |||
CHEMBL1773255 | 61826 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -33 | 2 | ChEMBL | 281 | 6 | 1 | 3 | 3.2 | N#Cc1cccc(COc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm300215x | |||
134146958 | 149697 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 388 | 6 | 1 | 3 | 5.1 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cc(F)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3947070 | 149697 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | - | 1 | ChEMBL | 388 | 6 | 1 | 3 | 5.1 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cc(F)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
73777085 | 153319 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | ChEMBL | 351 | 4 | 1 | 3 | 4.6 | COc1ccc(Cl)c(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3977361 | 153319 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | ChEMBL | 351 | 4 | 1 | 3 | 4.6 | COc1ccc(Cl)c(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
91826086 | 115000 | None | 44 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -2398 | 4 | ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.6019/CHEMBL5442687 | |||
CHEMBL3342358 | 115000 | None | 44 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -2398 | 4 | ChEMBL | 418 | 7 | 3 | 7 | 3.2 | CNc1nc(NCc2ccc(NS(C)(=O)=O)cc2Cl)cc(-c2ccccn2)n1 | 10.6019/CHEMBL5442687 | |||
90418650 | 157447 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2csnc2-c2ccc(Cl)cc2)c1C | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4077787 | 157447 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2csnc2-c2ccc(Cl)cc2)c1C | 10.1021/acsmedchemlett.7b00233 | |||
90418650 | 157447 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2csnc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4077787 | 157447 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2csnc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
57521913 | 76297 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | 2 | 2 | ChEMBL | 376 | 9 | 1 | 3 | 5.3 | CCOc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058526 | 76297 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | 2 | 2 | ChEMBL | 376 | 9 | 1 | 3 | 5.3 | CCOc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
134145750 | 149233 | None | 0 | Mouse | Functional | pEC50 | = | 5.7 | 5.7 | 3 | 2 | ChEMBL | 324 | 6 | 1 | 2 | 4.6 | O=C(O)CCCOc1ccc(-c2ccccc2C(F)(F)F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3943430 | 149233 | None | 0 | Mouse | Functional | pEC50 | = | 5.7 | 5.7 | 3 | 2 | ChEMBL | 324 | 6 | 1 | 2 | 4.6 | O=C(O)CCCOc1ccc(-c2ccccc2C(F)(F)F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
134141029 | 147255 | None | 0 | Mouse | Functional | pEC50 | = | 7.7 | 7.7 | 4 | 2 | ChEMBL | 352 | 6 | 1 | 3 | 4.8 | O=C(O)CCc1cc2cc(-c3cc(C(=O)C4CC4)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3927879 | 147255 | None | 0 | Mouse | Functional | pEC50 | = | 7.7 | 7.7 | 4 | 2 | ChEMBL | 352 | 6 | 1 | 3 | 4.8 | O=C(O)CCc1cc2cc(-c3cc(C(=O)C4CC4)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
145984594 | 166028 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 436 | 9 | 1 | 6 | 4.2 | CO[C@H]1C[C@H](Oc2cc3c(c(-c4cc(F)c(OCCCC(=O)O)c(F)c4)c2)OCO3)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4250664 | 166028 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 436 | 9 | 1 | 6 | 4.2 | CO[C@H]1C[C@H](Oc2cc3c(c(-c4cc(F)c(OCCCC(=O)O)c(F)c4)c2)OCO3)C1 | 10.1016/j.bmcl.2018.06.047 | |||
134156455 | 154410 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 394 | 6 | 1 | 5 | 4.3 | Fc1ccc(OC2CCC2)cc1-c1ccc2c(c1)CC[C@H](CCc1nnn[nH]1)O2 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3986721 | 154410 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 394 | 6 | 1 | 5 | 4.3 | Fc1ccc(OC2CCC2)cc1-c1ccc2c(c1)CC[C@H](CCc1nnn[nH]1)O2 | 10.1021/acsmedchemlett.6b00394 | |||
73777153 | 142910 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 3 | ChEMBL | 355 | 3 | 1 | 2 | 5.2 | O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3893026 | 142910 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 3 | ChEMBL | 355 | 3 | 1 | 2 | 5.2 | O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
137645347 | 157894 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 394 | 7 | 1 | 2 | 6.2 | Cc1c(CCC(=O)O)ccc(OCc2ccccc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4083233 | 157894 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | ChEMBL | 394 | 7 | 1 | 2 | 6.2 | Cc1c(CCC(=O)O)ccc(OCc2ccccc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
134147107 | 149964 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 417 | 3 | 1 | 3 | 5.5 | O=C(O)C1CC12CCC1(CCN(c3cc(OC(F)(F)F)ccc3Cl)CC1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3949142 | 149964 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | ChEMBL | 417 | 3 | 1 | 3 | 5.5 | O=C(O)C1CC12CCC1(CCN(c3cc(OC(F)(F)F)ccc3Cl)CC1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
25150014 | 3885 | None | 44 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -44 | 9 | ChEMBL | 264 | 3 | 1 | 1 | 3.4 | OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C | 10.1021/jm300215x | |||
3952 | 3885 | None | 44 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -44 | 9 | ChEMBL | 264 | 3 | 1 | 1 | 3.4 | OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C | 10.1021/jm300215x | |||
CHEMBL449588 | 3885 | None | 44 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -44 | 9 | ChEMBL | 264 | 3 | 1 | 1 | 3.4 | OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C | 10.1021/jm300215x | |||
137646188 | 157697 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 406 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c2ccccc12 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4080936 | 157697 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 406 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c2ccccc12 | 10.1016/j.bmcl.2017.01.034 | |||
137660451 | 159338 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 445 | 7 | 1 | 4 | 5.4 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(F)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4099026 | 159338 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 445 | 7 | 1 | 4 | 5.4 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(F)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
57521915 | 76299 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 15 | 2 | ChEMBL | 378 | 8 | 1 | 3 | 5.7 | CSc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058528 | 76299 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 15 | 2 | ChEMBL | 378 | 8 | 1 | 3 | 5.7 | CSc1ccc(-c2ccccc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
11195 | 3882 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 1 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
86280676 | 3882 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 1 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3941880 | 3882 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 1 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
134152545 | 153566 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -3 | 2 | ChEMBL | 380 | 3 | 0 | 4 | 4.2 | N#Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3979588 | 153566 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -3 | 2 | ChEMBL | 380 | 3 | 0 | 4 | 4.2 | N#Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
137636733 | 156295 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 348 | 6 | 1 | 2 | 4.4 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Br | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4064298 | 156295 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 348 | 6 | 1 | 2 | 4.4 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Br | 10.1016/j.bmcl.2017.01.034 | |||
90442039 | 163004 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 509 | 7 | 1 | 4 | 7.1 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)cc1C(F)(F)F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4173940 | 163004 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 509 | 7 | 1 | 4 | 7.1 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)cc1C(F)(F)F | 10.1021/acsmedchemlett.7b00233 | |||
57521916 | 76300 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 2 | 2 | ChEMBL | 366 | 7 | 1 | 2 | 5.6 | O=C(O)CCc1ccc(OCc2cc(Cl)ccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058529 | 76300 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 2 | 2 | ChEMBL | 366 | 7 | 1 | 2 | 5.6 | O=C(O)CCc1ccc(OCc2cc(Cl)ccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
25098573 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.6 | 5.6 | 8 | 2 | ChEMBL | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 10.1021/jm300215x | |||
5587 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.6 | 5.6 | 8 | 2 | ChEMBL | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 10.1021/jm300215x | |||
CHEMBL463785 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.6 | 5.6 | 8 | 2 | ChEMBL | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 10.1021/jm300215x | |||
23136411 | 58849 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -11 | 2 | ChEMBL | 332 | 7 | 1 | 2 | 5.0 | O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 | 10.1021/jm300215x | |||
CHEMBL1688457 | 58849 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -11 | 2 | ChEMBL | 332 | 7 | 1 | 2 | 5.0 | O=C(O)CCc1ccc(OCc2cccc(-c3ccccc3)c2)cc1 | 10.1021/jm300215x | |||
134143370 | 145891 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 442 | 7 | 1 | 6 | 4.0 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCc3nnn[nH]3)O4)c2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3916986 | 145891 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 442 | 7 | 1 | 6 | 4.0 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCc3nnn[nH]3)O4)c2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
145983824 | 165834 | None | 0 | Human | Functional | pEC50 | = | 4.6 | 4.6 | -6 | 2 | ChEMBL | 484 | 13 | 1 | 4 | 6.3 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4246334 | 165834 | None | 0 | Human | Functional | pEC50 | = | 4.6 | 4.6 | -6 | 2 | ChEMBL | 484 | 13 | 1 | 4 | 6.3 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
134129938 | 142527 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | 263 | 2 | ChEMBL | 414 | 6 | 1 | 4 | 5.0 | COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3890089 | 142527 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | 263 | 2 | ChEMBL | 414 | 6 | 1 | 4 | 5.0 | COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134153298 | 152455 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 412 | 6 | 1 | 4 | 4.8 | COc1cc(OC2CCC2)cc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3970166 | 152455 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | - | 1 | ChEMBL | 412 | 6 | 1 | 4 | 4.8 | COc1cc(OC2CCC2)cc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
85472225 | 162856 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | 2 | 3 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4171724 | 162856 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | 2 | 3 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
134153546 | 152670 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 8 | 2 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ncc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3971857 | 152670 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 8 | 2 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ncc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
137636733 | 156295 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 348 | 6 | 1 | 2 | 4.4 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Br | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4064298 | 156295 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 348 | 6 | 1 | 2 | 4.4 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Br | 10.1016/j.bmcl.2017.01.034 | |||
82051652 | 158690 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 284 | 6 | 1 | 2 | 3.9 | Cc1cccc(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4092090 | 158690 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 284 | 6 | 1 | 2 | 3.9 | Cc1cccc(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
137654721 | 158831 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 328 | 8 | 1 | 3 | 4.4 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1OC(C)C | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4093589 | 158831 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 328 | 8 | 1 | 3 | 4.4 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1OC(C)C | 10.1016/j.bmcl.2017.01.034 | |||
711134 | 113088 | None | 13 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 291 | 4 | 1 | 3 | 3.1 | COc1ccc(S(=O)(=O)Nc2ccc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311305 | 113088 | None | 13 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 291 | 4 | 1 | 3 | 3.1 | COc1ccc(S(=O)(=O)Nc2ccc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
137646188 | 157697 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 406 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c2ccccc12 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4080936 | 157697 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 406 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c2ccccc12 | 10.1016/j.bmcl.2017.01.034 | |||
134155277 | 151414 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | -3 | 2 | ChEMBL | 388 | 7 | 1 | 3 | 5.5 | Cc1cc(OCCCC(=O)O)ccc1-c1cc(OC(F)(F)F)ccc1Cl | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3961009 | 151414 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | -3 | 2 | ChEMBL | 388 | 7 | 1 | 3 | 5.5 | Cc1cc(OCCCC(=O)O)ccc1-c1cc(OC(F)(F)F)ccc1Cl | 10.1016/j.bmcl.2016.10.054 | |||
10531 | 1420 | None | 13 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -3019 | 29 | ChEMBL | 583 | 4 | 3 | 6 | 2.1 | CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O | 10.6019/CHEMBL5442687 | |||
10531.0 | 1420 | None | 13 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -3019 | 29 | ChEMBL | 583 | 4 | 3 | 6 | 2.1 | CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O | 10.6019/CHEMBL5442687 | |||
121 | 1420 | None | 13 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -3019 | 29 | ChEMBL | 583 | 4 | 3 | 6 | 2.1 | CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O | 10.6019/CHEMBL5442687 | |||
888 | 1420 | None | 13 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -3019 | 29 | ChEMBL | 583 | 4 | 3 | 6 | 2.1 | CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O | 10.6019/CHEMBL5442687 | |||
CHEMBL1732 | 1420 | None | 13 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -3019 | 29 | ChEMBL | 583 | 4 | 3 | 6 | 2.1 | CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O | 10.6019/CHEMBL5442687 | |||
DB00320 | 1420 | None | 13 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -3019 | 29 | ChEMBL | 583 | 4 | 3 | 6 | 2.1 | CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O | 10.6019/CHEMBL5442687 | |||
1049 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm800970b | |||
4618 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm800970b | |||
5280934 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm800970b | |||
CHEMBL8739 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm800970b | |||
DB00132 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm800970b | |||
90406335 | 163925 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 457 | 7 | 1 | 3 | 5.8 | Cc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1F | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4206369 | 163925 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 457 | 7 | 1 | 3 | 5.8 | Cc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1F | 10.1016/j.bmcl.2018.02.013 | |||
134138318 | 148107 | None | 0 | Mouse | Functional | pEC50 | = | 6.6 | 6.6 | 1 | 3 | ChEMBL | 378 | 9 | 1 | 4 | 5.4 | COc1cccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3934450 | 148107 | None | 0 | Mouse | Functional | pEC50 | = | 6.6 | 6.6 | 1 | 3 | ChEMBL | 378 | 9 | 1 | 4 | 5.4 | COc1cccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
134144214 | 150446 | None | 0 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | 2 | 3 | ChEMBL | 384 | 8 | 1 | 3 | 5.7 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3953203 | 150446 | None | 0 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | 2 | 3 | ChEMBL | 384 | 8 | 1 | 3 | 5.7 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
59455555 | 158808 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 399 | 7 | 1 | 4 | 5.5 | Cc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4093383 | 158808 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 399 | 7 | 1 | 4 | 5.5 | Cc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
73776979 | 143446 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 419 | 5 | 1 | 3 | 5.9 | O=C(O)CCC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3897637 | 143446 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 419 | 5 | 1 | 3 | 5.9 | O=C(O)CCC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
137654721 | 158831 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 328 | 8 | 1 | 3 | 4.4 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1OC(C)C | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4093589 | 158831 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 328 | 8 | 1 | 3 | 4.4 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1OC(C)C | 10.1016/j.bmcl.2017.01.034 | |||
82051652 | 158690 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 284 | 6 | 1 | 2 | 3.9 | Cc1cccc(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4092090 | 158690 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 284 | 6 | 1 | 2 | 3.9 | Cc1cccc(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
137657736 | 159732 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 385 | 7 | 1 | 4 | 5.2 | Cc1c(CCC(=O)O)ccc(OCc2conc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4103573 | 159732 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 385 | 7 | 1 | 4 | 5.2 | Cc1c(CCC(=O)O)ccc(OCc2conc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
145986262 | 165940 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 428 | 8 | 1 | 4 | 4.7 | O=C(O)CCCOc1c(F)cc(-c2cc(OC3CCOCC3)cc(F)c2F)cc1F | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4248845 | 165940 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 428 | 8 | 1 | 4 | 4.7 | O=C(O)CCCOc1c(F)cc(-c2cc(OC3CCOCC3)cc(F)c2F)cc1F | 10.1016/j.bmcl.2018.06.047 | |||
134154473 | 152463 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | 218 | 2 | ChEMBL | 370 | 6 | 1 | 3 | 5.0 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3970238 | 152463 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | 218 | 2 | ChEMBL | 370 | 6 | 1 | 3 | 5.0 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
134139171 | 146351 | None | 0 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | 2 | 3 | ChEMBL | 350 | 6 | 1 | 3 | 5.4 | Cc1cc(OC2CCC2)cc(-c2ccc3oc(CCC(=O)O)cc3c2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3920591 | 146351 | None | 0 | Mouse | Functional | pEC50 | = | 7.6 | 7.6 | 2 | 3 | ChEMBL | 350 | 6 | 1 | 3 | 5.4 | Cc1cc(OC2CCC2)cc(-c2ccc3oc(CCC(=O)O)cc3c2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
86343964 | 163715 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 421 | 7 | 1 | 3 | 5.5 | Cc1cc(CCC(=O)O)ccc1OCc1c(C(F)(F)F)ccn1-c1ccc(F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4203774 | 163715 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | ChEMBL | 421 | 7 | 1 | 3 | 5.5 | Cc1cc(CCC(=O)O)ccc1OCc1c(C(F)(F)F)ccn1-c1ccc(F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
137647294 | 158044 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 461 | 8 | 1 | 4 | 6.9 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2-c2ccccc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4084679 | 158044 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | ChEMBL | 461 | 8 | 1 | 4 | 6.9 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2-c2ccccc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
24801690 | 98094 | None | 20 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -295 | 5 | ChEMBL | 593 | 9 | 5 | 5 | 4.5 | CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 | 10.6019/CHEMBL5442687 | |||
CHEMBL273083 | 98094 | None | 20 | Human | Functional | pEC50 | = | 5.6 | 5.6 | -295 | 5 | ChEMBL | 593 | 9 | 5 | 5 | 4.5 | CSc1ccc(C(=O)N[C@@H]2CCCC[C@@H]2NC(=O)CNC(=O)c2cc(C(F)(F)F)ccc2NC(=O)NC(C)C)cc1 | 10.6019/CHEMBL5442687 | |||
90407659 | 164328 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 440 | 7 | 1 | 4 | 5.1 | Cc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cn1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4211144 | 164328 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 440 | 7 | 1 | 4 | 5.1 | Cc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cn1 | 10.1016/j.bmcl.2018.02.013 | |||
134157586 | 154252 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 3 | 3 | ChEMBL | 366 | 8 | 1 | 3 | 5.5 | O=C(O)CCCOc1ccc(-c2cc(Oc3ccccc3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3985509 | 154252 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 3 | 3 | ChEMBL | 366 | 8 | 1 | 3 | 5.5 | O=C(O)CCCOc1ccc(-c2cc(Oc3ccccc3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137636575 | 155991 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 479 | 7 | 1 | 4 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(F)cc3Cl)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4060663 | 155991 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 479 | 7 | 1 | 4 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(F)cc3Cl)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
134133675 | 143349 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -2 | 3 | ChEMBL | 318 | 8 | 1 | 3 | 4.1 | CCOc1ccc(F)c(-c2ccc(OCCCC(=O)O)cc2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3896714 | 143349 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -2 | 3 | ChEMBL | 318 | 8 | 1 | 3 | 4.1 | CCOc1ccc(F)c(-c2ccc(OCCCC(=O)O)cc2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
90404813 | 164603 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 473 | 7 | 1 | 3 | 6.3 | CC(Cc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1)C(=O)O | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4214698 | 164603 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 473 | 7 | 1 | 3 | 6.3 | CC(Cc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1)C(=O)O | 10.1016/j.bmcl.2018.02.013 | |||
11374217 | 3597 | None | 38 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -363 | 8 | ChEMBL | 445 | 4 | 1 | 3 | 4.1 | Fc1ccc(cc1)CNC(=O)N1CCN2C(C1)C(OC2=O)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
5813 | 3597 | None | 38 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -363 | 8 | ChEMBL | 445 | 4 | 1 | 3 | 4.1 | Fc1ccc(cc1)CNC(=O)N1CCN2C(C1)C(OC2=O)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
CHEMBL469695 | 3597 | None | 38 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -363 | 8 | ChEMBL | 445 | 4 | 1 | 3 | 4.1 | Fc1ccc(cc1)CNC(=O)N1CCN2C(C1)C(OC2=O)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
57521812 | 76294 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 2 | 2 | ChEMBL | 410 | 7 | 1 | 2 | 5.7 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Br)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058523 | 76294 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 2 | 2 | ChEMBL | 410 | 7 | 1 | 2 | 5.7 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Br)cc2)cc1 | 10.1021/jm300215x | |||
137633536 | 156386 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -4 | 6 | ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4065397 | 156386 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -4 | 6 | ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | |||
134154330 | 152969 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 2 | ChEMBL | 340 | 7 | 1 | 3 | 4.5 | O=C(O)CCCOc1ccc(-c2ccccc2OC(F)(F)F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3974501 | 152969 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 2 | ChEMBL | 340 | 7 | 1 | 3 | 4.5 | O=C(O)CCCOc1ccc(-c2ccccc2OC(F)(F)F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
134148110 | 149658 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3nc(OC4CCC4)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3946820 | 149658 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3nc(OC4CCC4)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
134138802 | 148007 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -4 | 2 | ChEMBL | 383 | 4 | 1 | 3 | 4.7 | O=C(O)C1CCN(c2ccc(-c3cc(OC(F)(F)F)ccc3F)cc2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3933619 | 148007 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -4 | 2 | ChEMBL | 383 | 4 | 1 | 3 | 4.7 | O=C(O)C1CCN(c2ccc(-c3cc(OC(F)(F)F)ccc3F)cc2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
3376937 | 124204 | None | 45 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -70 | 2 | ChEMBL | 365 | 4 | 3 | 4 | 3.3 | COc1cc(OC)cc(C(=O)NNC(=O)Nc2cccc3ccccc23)c1 | 10.6019/CHEMBL5442687 | |||
CHEMBL3633893 | 124204 | None | 45 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -70 | 2 | ChEMBL | 365 | 4 | 3 | 4 | 3.3 | COc1cc(OC)cc(C(=O)NNC(=O)Nc2cccc3ccccc23)c1 | 10.6019/CHEMBL5442687 | |||
46892131 | 144759 | None | 3 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -3 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3908362 | 144759 | None | 3 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -3 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
137661388 | 159333 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 384 | 7 | 1 | 3 | 5.5 | Cc1c(CCC(=O)O)ccc(OCc2ccccc2SC(F)(F)F)c1C | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4098969 | 159333 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 384 | 7 | 1 | 3 | 5.5 | Cc1c(CCC(=O)O)ccc(OCc2ccccc2SC(F)(F)F)c1C | 10.1016/j.bmcl.2017.01.034 | |||
134133297 | 143866 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -3 | 3 | ChEMBL | 372 | 7 | 1 | 3 | 4.9 | Cc1cc(-c2cc(OC(F)(F)F)ccc2F)ccc1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3900990 | 143866 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -3 | 3 | ChEMBL | 372 | 7 | 1 | 3 | 4.9 | Cc1cc(-c2cc(OC(F)(F)F)ccc2F)ccc1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
57521811 | 76293 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 1 | 2 | ChEMBL | 366 | 7 | 1 | 2 | 5.6 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Cl)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058522 | 76293 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 1 | 2 | ChEMBL | 366 | 7 | 1 | 2 | 5.6 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(Cl)cc2)cc1 | 10.1021/jm300215x | |||
24825492 | 149630 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -9 | 2 | ChEMBL | 333 | 6 | 2 | 2 | 4.1 | O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 | 10.1021/jm300215x | |||
CHEMBL394666 | 149630 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -9 | 2 | ChEMBL | 333 | 6 | 2 | 2 | 4.1 | O=C(O)CCc1ccc(NCc2cccc(Br)c2)cc1 | 10.1021/jm300215x | |||
85472227 | 162282 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 519 | 7 | 1 | 4 | 6.8 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(Br)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4162566 | 162282 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 519 | 7 | 1 | 4 | 6.8 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(Br)c1 | 10.1021/acsmedchemlett.7b00233 | |||
134149615 | 148664 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 1 | 3 | ChEMBL | 370 | 5 | 1 | 3 | 4.6 | O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3939004 | 148664 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 1 | 3 | ChEMBL | 370 | 5 | 1 | 3 | 4.6 | O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1016/j.bmcl.2016.10.054 | |||
73777174 | 150542 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -2 | 2 | ChEMBL | 356 | 3 | 1 | 3 | 4.4 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccn1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3954140 | 150542 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -2 | 2 | ChEMBL | 356 | 3 | 1 | 3 | 4.4 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccn1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
145960576 | 162246 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 527 | 8 | 1 | 5 | 6.6 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(OC(F)(F)F)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4161929 | 162246 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 527 | 8 | 1 | 5 | 6.6 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(OC(F)(F)F)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
134145195 | 150511 | None | 0 | Mouse | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 392 | 5 | 1 | 5 | 4.4 | Fc1ccc(OC(F)(F)F)cc1-c1ccc2oc(CCc3nn[nH]n3)cc2c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3953859 | 150511 | None | 0 | Mouse | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 392 | 5 | 1 | 5 | 4.4 | Fc1ccc(OC(F)(F)F)cc1-c1ccc2oc(CCc3nn[nH]n3)cc2c1 | 10.1016/j.bmcl.2016.10.054 | |||
1052 | 2321 | None | 51 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 3 | 4 | ChEMBL | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 10.1016/j.bmcl.2014.05.012 | |||
3323 | 2321 | None | 51 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 3 | 4 | ChEMBL | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 10.1016/j.bmcl.2014.05.012 | |||
5280450 | 2321 | None | 51 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 3 | 4 | ChEMBL | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL267476 | 2321 | None | 51 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 3 | 4 | ChEMBL | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 10.1016/j.bmcl.2014.05.012 | |||
DB14104 | 2321 | None | 51 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 3 | 4 | ChEMBL | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 10.1016/j.bmcl.2014.05.012 | |||
900631 | 113100 | None | 14 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 333 | 3 | 1 | 4 | 3.2 | Cc1cc(C)c(NS(=O)(=O)c2ccc3c(c2)OCCO3)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311325 | 113100 | None | 14 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 333 | 3 | 1 | 4 | 3.2 | Cc1cc(C)c(NS(=O)(=O)c2ccc3c(c2)OCCO3)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
118707173 | 113102 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 331 | 6 | 1 | 3 | 3.8 | C=CCc1cc(C)c(NS(=O)(=O)c2ccc(OC)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311327 | 113102 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 331 | 6 | 1 | 3 | 3.8 | C=CCc1cc(C)c(NS(=O)(=O)c2ccc(OC)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
137633536 | 156386 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -4 | 6 | ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4065397 | 156386 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -4 | 6 | ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | |||
137661388 | 159333 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 384 | 7 | 1 | 3 | 5.5 | Cc1c(CCC(=O)O)ccc(OCc2ccccc2SC(F)(F)F)c1C | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4098969 | 159333 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 384 | 7 | 1 | 3 | 5.5 | Cc1c(CCC(=O)O)ccc(OCc2ccccc2SC(F)(F)F)c1C | 10.1016/j.bmcl.2017.01.034 | |||
1050 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1016/j.bmcl.2020.127650 | |||
11595431 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL207881 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1016/j.bmcl.2020.127650 | |||
825631 | 113089 | None | 11 | Human | Functional | pEC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 291 | 4 | 1 | 3 | 3.1 | COc1ccc(S(=O)(=O)Nc2c(C)cccc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311306 | 113089 | None | 11 | Human | Functional | pEC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 291 | 4 | 1 | 3 | 3.1 | COc1ccc(S(=O)(=O)Nc2c(C)cccc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
841618 | 113096 | None | 12 | Human | Functional | pEC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 309 | 3 | 1 | 2 | 4.1 | Cc1cc(C)c(NS(=O)(=O)c2ccc(Cl)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311318 | 113096 | None | 12 | Human | Functional | pEC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 309 | 3 | 1 | 2 | 4.1 | Cc1cc(C)c(NS(=O)(=O)c2ccc(Cl)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
134141270 | 146898 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 3 | 3 | ChEMBL | 334 | 8 | 1 | 3 | 4.6 | CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3924759 | 146898 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 3 | 3 | ChEMBL | 334 | 8 | 1 | 3 | 4.6 | CCOc1ccc(Cl)c(-c2ccc(OCCCC(=O)O)cc2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
134145412 | 149359 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 2 | 2 | ChEMBL | 330 | 8 | 1 | 3 | 4.3 | O=C(O)CCCOc1ccc(-c2cc(OC3CC3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3944507 | 149359 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 2 | 2 | ChEMBL | 330 | 8 | 1 | 3 | 4.3 | O=C(O)CCCOc1ccc(-c2cc(OC3CC3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
134147601 | 150116 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 396 | 4 | 1 | 3 | 4.8 | O=C(O)[C@H]1C[C@@H]1[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3950444 | 150116 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 396 | 4 | 1 | 3 | 4.8 | O=C(O)[C@H]1C[C@@H]1[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
10204153 | 3533 | None | 31 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -23 | 2 | ChEMBL | 448 | 5 | 0 | 6 | 5.2 | Cc1sc(c(n1)C(=O)N1CCC[C@H]1Cc1nnc(o1)c1ccccc1)c1ccccc1F | 10.6019/CHEMBL5442687 | |||
9136 | 3533 | None | 31 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -23 | 2 | ChEMBL | 448 | 5 | 0 | 6 | 5.2 | Cc1sc(c(n1)C(=O)N1CCC[C@H]1Cc1nnc(o1)c1ccccc1)c1ccccc1F | 10.6019/CHEMBL5442687 | |||
CHEMBL2110363 | 3533 | None | 31 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -23 | 2 | ChEMBL | 448 | 5 | 0 | 6 | 5.2 | Cc1sc(c(n1)C(=O)N1CCC[C@H]1Cc1nnc(o1)c1ccccc1)c1ccccc1F | 10.6019/CHEMBL5442687 | |||
1049 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm300215x | |||
4618 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm300215x | |||
5280934 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm300215x | |||
CHEMBL8739 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm300215x | |||
DB00132 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | ChEMBL | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 10.1021/jm300215x | |||
134143899 | 150327 | None | 0 | Mouse | Functional | pEC50 | = | 6.5 | 6.5 | 1 | 3 | ChEMBL | 350 | 5 | 1 | 3 | 5.0 | O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3952316 | 150327 | None | 0 | Mouse | Functional | pEC50 | = | 6.5 | 6.5 | 1 | 3 | ChEMBL | 350 | 5 | 1 | 3 | 5.0 | O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
73777063 | 1154 | None | 36 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
8418 | 1154 | None | 36 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3919973 | 1154 | None | 36 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
134152336 | 153545 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 408 | 5 | 1 | 5 | 4.2 | Fc1ccc(OC(F)(F)F)cc1-c1ccc2c(c1)CC[C@H](CCc1nnn[nH]1)O2 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3979448 | 153545 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 408 | 5 | 1 | 5 | 4.2 | Fc1ccc(OC(F)(F)F)cc1-c1ccc2c(c1)CC[C@H](CCc1nnn[nH]1)O2 | 10.1021/acsmedchemlett.6b00394 | |||
117886639 | 148538 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 2 | ChEMBL | 391 | 3 | 1 | 3 | 5.3 | CC1(C)Cc2cc(Cl)cc(N3CCC4(CCC(CC(=O)O)CC4)CC3)c2O1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3937916 | 148538 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 2 | ChEMBL | 391 | 3 | 1 | 3 | 5.3 | CC1(C)Cc2cc(Cl)cc(N3CCC4(CCC(CC(=O)O)CC4)CC3)c2O1 | 10.1021/acsmedchemlett.6b00360 | |||
90417528 | 162266 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 513 | 9 | 1 | 4 | 7.2 | CCc1ccc(-c2nsc(C(F)(F)C(F)(F)F)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4162353 | 162266 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 513 | 9 | 1 | 4 | 7.2 | CCc1ccc(-c2nsc(C(F)(F)C(F)(F)F)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
2131 | 3499 | None | 46 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -323 | 5 | ChEMBL | 380 | 5 | 1 | 2 | 6.1 | CC[C@@H](c1ccccc1)NC(=O)c1c(C)c(nc2c1cccc2)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
6604009 | 3499 | None | 46 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -323 | 5 | ChEMBL | 380 | 5 | 1 | 2 | 6.1 | CC[C@@H](c1ccccc1)NC(=O)c1c(C)c(nc2c1cccc2)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
CHEMBL10284 | 3499 | None | 46 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -323 | 5 | ChEMBL | 380 | 5 | 1 | 2 | 6.1 | CC[C@@H](c1ccccc1)NC(=O)c1c(C)c(nc2c1cccc2)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
85472359 | 162223 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 471 | 8 | 1 | 4 | 6.3 | CCc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4161536 | 162223 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | - | 1 | ChEMBL | 471 | 8 | 1 | 4 | 6.3 | CCc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
134148736 | 148642 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 2 | 2 | ChEMBL | 383 | 8 | 1 | 4 | 5.4 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccnc3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3938783 | 148642 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 2 | 2 | ChEMBL | 383 | 8 | 1 | 4 | 5.4 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccnc3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
134156096 | 151536 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 5 | 3 | ChEMBL | 400 | 8 | 1 | 3 | 6.2 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3961950 | 151536 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 5 | 3 | ChEMBL | 400 | 8 | 1 | 3 | 6.2 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137649360 | 157478 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 495 | 7 | 1 | 4 | 6.3 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C(F)(F)F)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4078286 | 157478 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 495 | 7 | 1 | 4 | 6.3 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C(F)(F)F)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
86343961 | 164382 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 435 | 7 | 1 | 3 | 5.8 | Cc1c(CCC(=O)O)ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4211967 | 164382 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 435 | 7 | 1 | 3 | 5.8 | Cc1c(CCC(=O)O)ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
145985748 | 165738 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 444 | 9 | 1 | 4 | 5.4 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(SCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4243863 | 165738 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 444 | 9 | 1 | 4 | 5.4 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(SCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
134156727 | 153723 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | -4 | 2 | ChEMBL | 419 | 7 | 1 | 5 | 4.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)n2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3980898 | 153723 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | -4 | 2 | ChEMBL | 419 | 7 | 1 | 5 | 4.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)n2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
134151115 | 152288 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 4 | 3 | ChEMBL | 336 | 6 | 1 | 3 | 5.0 | O=C(O)CCc1cc2cc(-c3cccc(OC4CCC4)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3968537 | 152288 | None | 0 | Mouse | Functional | pEC50 | = | 7.5 | 7.5 | 4 | 3 | ChEMBL | 336 | 6 | 1 | 3 | 5.0 | O=C(O)CCc1cc2cc(-c3cccc(OC4CCC4)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
137631865 | 156425 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 399 | 7 | 1 | 4 | 5.5 | Cc1noc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4065769 | 156425 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | ChEMBL | 399 | 7 | 1 | 4 | 5.5 | Cc1noc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
1050 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1016/j.bmcl.2018.06.047 | |||
11595431 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL207881 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1016/j.bmcl.2018.06.047 | |||
73777065 | 147344 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC(C(=O)O)C1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3928591 | 147344 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | - | 1 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC(C(=O)O)C1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
134146021 | 149152 | None | 0 | Mouse | Functional | pEC50 | = | 7.4 | 7.4 | 5 | 2 | ChEMBL | 392 | 7 | 1 | 3 | 5.3 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)c(F)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3942922 | 149152 | None | 0 | Mouse | Functional | pEC50 | = | 7.4 | 7.4 | 5 | 2 | ChEMBL | 392 | 7 | 1 | 3 | 5.3 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)c(F)c1 | 10.1016/j.bmcl.2016.10.054 | |||
73777135 | 150458 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | -5 | 2 | ChEMBL | 412 | 4 | 1 | 4 | 5.4 | N#Cc1cc(SC(F)(F)F)cc(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3953289 | 150458 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | -5 | 2 | ChEMBL | 412 | 4 | 1 | 4 | 5.4 | N#Cc1cc(SC(F)(F)F)cc(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
11250647 | 1545 | None | 35 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -999 | 7 | ChEMBL | 631 | 12 | 2 | 7 | 5.5 | COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F | 10.6019/CHEMBL5442687 | |||
11250647.0 | 1545 | None | 35 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -999 | 7 | ChEMBL | 631 | 12 | 2 | 7 | 5.5 | COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F | 10.6019/CHEMBL5442687 | |||
5293 | 1545 | None | 35 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -999 | 7 | ChEMBL | 631 | 12 | 2 | 7 | 5.5 | COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F | 10.6019/CHEMBL5442687 | |||
8362 | 1545 | None | 35 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -999 | 7 | ChEMBL | 631 | 12 | 2 | 7 | 5.5 | COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F | 10.6019/CHEMBL5442687 | |||
CHEMBL1208155 | 1545 | None | 35 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -999 | 7 | ChEMBL | 631 | 12 | 2 | 7 | 5.5 | COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F | 10.6019/CHEMBL5442687 | |||
DB11979 | 1545 | None | 35 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -999 | 7 | ChEMBL | 631 | 12 | 2 | 7 | 5.5 | COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F | 10.6019/CHEMBL5442687 | |||
137643339 | 158135 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 26 | 2 | ChEMBL | 304 | 6 | 1 | 2 | 4.2 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4085843 | 158135 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 26 | 2 | ChEMBL | 304 | 6 | 1 | 2 | 4.2 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 | 10.1016/j.bmcl.2017.01.034 | |||
90406970 | 164871 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 477 | 7 | 1 | 3 | 6.2 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)c(F)c2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4218078 | 164871 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 477 | 7 | 1 | 3 | 6.2 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)c(F)c2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
134146720 | 149219 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 443 | 7 | 1 | 6 | 5.6 | COc1cc(Oc2ncc(C)s2)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3943315 | 149219 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 443 | 7 | 1 | 6 | 5.6 | COc1cc(Oc2ncc(C)s2)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
23136477 | 58847 | None | 2 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 15 | 2 | ChEMBL | 332 | 7 | 1 | 2 | 5.0 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL1688455 | 58847 | None | 2 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 15 | 2 | ChEMBL | 332 | 7 | 1 | 2 | 5.0 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL4213909 | 58847 | None | 2 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 15 | 2 | ChEMBL | 332 | 7 | 1 | 2 | 5.0 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
134132711 | 145026 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 1 | 2 | ChEMBL | 372 | 3 | 0 | 4 | 4.2 | O=S1(=O)c2ccccc2CN1c1cc(Cl)cc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3910333 | 145026 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 1 | 2 | ChEMBL | 372 | 3 | 0 | 4 | 4.2 | O=S1(=O)c2ccccc2CN1c1cc(Cl)cc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
134145778 | 149435 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 13 | 2 | ChEMBL | 355 | 3 | 0 | 3 | 4.3 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccccc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3945213 | 149435 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 13 | 2 | ChEMBL | 355 | 3 | 0 | 3 | 4.3 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccccc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
137657972 | 159698 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 40 | 2 | ChEMBL | 376 | 8 | 1 | 3 | 5.7 | Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4103243 | 159698 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 40 | 2 | ChEMBL | 376 | 8 | 1 | 3 | 5.7 | Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 | 10.1016/j.bmcl.2017.01.034 | |||
5310990 | 166926 | None | 8 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -22 | 4 | ChEMBL | 510 | 12 | 1 | 6 | 4.7 | CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 | 10.6019/CHEMBL5442687 | |||
CHEMBL428504 | 166926 | None | 8 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -22 | 4 | ChEMBL | 510 | 12 | 1 | 6 | 4.7 | CCCCN(CCCC)C(=O)CN1C[C@@H](c2ccc3c(c2)OCO3)[C@H](C(=O)O)[C@H]1c1ccc(OC)cc1 | 10.6019/CHEMBL5442687 | |||
23136477 | 58847 | None | 2 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 15 | 2 | ChEMBL | 332 | 7 | 1 | 2 | 5.0 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
CHEMBL1688455 | 58847 | None | 2 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 15 | 2 | ChEMBL | 332 | 7 | 1 | 2 | 5.0 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
CHEMBL4213909 | 58847 | None | 2 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 15 | 2 | ChEMBL | 332 | 7 | 1 | 2 | 5.0 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccccc2)cc1 | 10.1016/j.bmc.2017.10.040 | |||
118707084 | 113073 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 321 | 5 | 1 | 4 | 3.1 | COc1ccc(S(=O)(=O)Nc2c(C)cc(OC)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311198 | 113073 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 321 | 5 | 1 | 4 | 3.1 | COc1ccc(S(=O)(=O)Nc2c(C)cc(OC)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
8190712 | 113097 | None | 7 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 317 | 5 | 1 | 2 | 4.4 | CCCc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311319 | 113097 | None | 7 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 317 | 5 | 1 | 2 | 4.4 | CCCc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
137643339 | 158135 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 26 | 2 | ChEMBL | 304 | 6 | 1 | 2 | 4.2 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4085843 | 158135 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 26 | 2 | ChEMBL | 304 | 6 | 1 | 2 | 4.2 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(Cl)c1 | 10.1016/j.bmcl.2017.01.034 | |||
956298 | 113087 | None | 11 | Human | Functional | pEC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 319 | 4 | 1 | 4 | 2.9 | COC(=O)c1cccc(NS(=O)(=O)c2ccc(C)cc2)c1C | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311303 | 113087 | None | 11 | Human | Functional | pEC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 319 | 4 | 1 | 4 | 2.9 | COC(=O)c1cccc(NS(=O)(=O)c2ccc(C)cc2)c1C | 10.1016/j.bmcl.2014.05.012 | |||
137657972 | 159698 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 40 | 2 | ChEMBL | 376 | 8 | 1 | 3 | 5.7 | Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4103243 | 159698 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 40 | 2 | ChEMBL | 376 | 8 | 1 | 3 | 5.7 | Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(Oc2ccccc2)c1 | 10.1016/j.bmcl.2017.01.034 | |||
134131874 | 144945 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 404 | 6 | 1 | 3 | 5.6 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cc(Cl)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3909773 | 144945 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 404 | 6 | 1 | 3 | 5.6 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cc(Cl)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
86281122 | 164421 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 453 | 8 | 1 | 3 | 5.9 | CCc1ccc(-n2ccc(C(F)(F)F)c2COc2ccc(CCC(=O)O)c(F)c2F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4212409 | 164421 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 453 | 8 | 1 | 3 | 5.9 | CCc1ccc(-n2ccc(C(F)(F)F)c2COc2ccc(CCC(=O)O)c(F)c2F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
137660302 | 159532 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 413 | 8 | 1 | 4 | 5.8 | CCc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4101135 | 159532 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 413 | 8 | 1 | 4 | 5.8 | CCc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
137638176 | 156825 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 457 | 7 | 1 | 4 | 6.1 | Cc1cc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)cc1CCC(=O)O | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4070355 | 156825 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 457 | 7 | 1 | 4 | 6.1 | Cc1cc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)cc1CCC(=O)O | 10.1016/j.bmcl.2017.06.028 | |||
117873187 | 152433 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC1CC2(CCC1CC(=O)O)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3969920 | 152433 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC1CC2(CCC1CC(=O)O)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
10416 | 1879 | None | 31 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -199 | 3 | ChEMBL | 548 | 9 | 3 | 8 | 4.0 | COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl | 10.6019/CHEMBL5442687 | |||
46861584 | 1879 | None | 31 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -199 | 3 | ChEMBL | 548 | 9 | 3 | 8 | 4.0 | COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl | 10.6019/CHEMBL5442687 | |||
CHEMBL2018969 | 1879 | None | 31 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -199 | 3 | ChEMBL | 548 | 9 | 3 | 8 | 4.0 | COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl | 10.6019/CHEMBL5442687 | |||
87054900 | 148849 | None | 0 | Mouse | Functional | pEC50 | = | 6.4 | 6.4 | 1 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.4 | O=C(O)CCCOc1ccc(-c2ccccc2Oc2ccccc2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3940493 | 148849 | None | 0 | Mouse | Functional | pEC50 | = | 6.4 | 6.4 | 1 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.4 | O=C(O)CCCOc1ccc(-c2ccccc2Oc2ccccc2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
90418278 | 162473 | None | 16 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 1 | 2 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3F)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4165366 | 162473 | None | 16 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 1 | 2 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3F)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
73777175 | 143996 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | -1 | 3 | ChEMBL | 357 | 3 | 1 | 2 | 4.9 | O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3901994 | 143996 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | -1 | 3 | ChEMBL | 357 | 3 | 1 | 2 | 4.9 | O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
60195039 | 81824 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -181 | 2 | ChEMBL | 377 | 8 | 2 | 2 | 5.7 | CCc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/jm3002026 | |||
CHEMBL2164240 | 81824 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -181 | 2 | ChEMBL | 377 | 8 | 2 | 2 | 5.7 | CCc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/jm3002026 | |||
134134229 | 143342 | None | 0 | Mouse | Functional | pEC50 | = | 7.4 | 7.4 | 1 | 3 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3896657 | 143342 | None | 0 | Mouse | Functional | pEC50 | = | 7.4 | 7.4 | 1 | 3 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1021/acsmedchemlett.6b00360 | |||
134134229 | 143342 | None | 0 | Mouse | Functional | pEC50 | = | 7.4 | 7.4 | 1 | 3 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3896657 | 143342 | None | 0 | Mouse | Functional | pEC50 | = | 7.4 | 7.4 | 1 | 3 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
86281125 | 164166 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 445 | 7 | 1 | 3 | 5.9 | OCCCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4209308 | 164166 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 445 | 7 | 1 | 3 | 5.9 | OCCCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
57522038 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.4 | 7.4 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
6490 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.4 | 7.4 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
CHEMBL2058533 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.4 | 7.4 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
117886649 | 152167 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 391 | 4 | 1 | 3 | 5.4 | OCCC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3967504 | 152167 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | - | 1 | ChEMBL | 391 | 4 | 1 | 3 | 5.4 | OCCC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
134142866 | 145730 | None | 0 | Mouse | Functional | pEC50 | = | 6.4 | 6.4 | 2 | 3 | ChEMBL | 358 | 7 | 1 | 3 | 4.6 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3915765 | 145730 | None | 0 | Mouse | Functional | pEC50 | = | 6.4 | 6.4 | 2 | 3 | ChEMBL | 358 | 7 | 1 | 3 | 4.6 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
2705 | 3842 | None | 44 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -676 | 12 | ChEMBL | 325 | 7 | 1 | 2 | 5.3 | Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O | 10.6019/CHEMBL5442687 | |||
360 | 3842 | None | 44 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -676 | 12 | ChEMBL | 325 | 7 | 1 | 2 | 5.3 | Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O | 10.6019/CHEMBL5442687 | |||
443879 | 3842 | None | 44 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -676 | 12 | ChEMBL | 325 | 7 | 1 | 2 | 5.3 | Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O | 10.6019/CHEMBL5442687 | |||
443879.0 | 3842 | None | 44 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -676 | 12 | ChEMBL | 325 | 7 | 1 | 2 | 5.3 | Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O | 10.6019/CHEMBL5442687 | |||
CHEMBL1382 | 3842 | None | 44 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -676 | 12 | ChEMBL | 325 | 7 | 1 | 2 | 5.3 | Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O | 10.6019/CHEMBL5442687 | |||
DB01036 | 3842 | None | 44 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -676 | 12 | ChEMBL | 325 | 7 | 1 | 2 | 5.3 | Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O | 10.6019/CHEMBL5442687 | |||
57521914 | 76298 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -6 | 2 | ChEMBL | 416 | 8 | 1 | 3 | 5.8 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(OC(F)(F)F)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058527 | 76298 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -6 | 2 | ChEMBL | 416 | 8 | 1 | 3 | 5.8 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(OC(F)(F)F)cc2)cc1 | 10.1021/jm300215x | |||
60195125 | 3888 | None | 8 | Human | Functional | pEC50 | = | 4.4 | 4.4 | -1096 | 3 | ChEMBL | 499 | 12 | 2 | 5 | 5.2 | OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C | 10.1021/jm3002026 | |||
9149 | 3888 | None | 8 | Human | Functional | pEC50 | = | 4.4 | 4.4 | -1096 | 3 | ChEMBL | 499 | 12 | 2 | 5 | 5.2 | OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C | 10.1021/jm3002026 | |||
CHEMBL2164242 | 3888 | None | 8 | Human | Functional | pEC50 | = | 4.4 | 4.4 | -1096 | 3 | ChEMBL | 499 | 12 | 2 | 5 | 5.2 | OC(=O)CCc1ccc(cc1F)NCc1cccc(c1)c1ccc(cc1C)OCCCS(=O)(=O)C | 10.1021/jm3002026 | |||
443375 | 210065 | None | 33 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -22387 | 9 | ChEMBL | 408 | 3 | 2 | 3 | 3.7 | CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 | 10.6019/CHEMBL5442687 | |||
CHEMBL9506 | 210065 | None | 33 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -22387 | 9 | ChEMBL | 408 | 3 | 2 | 3 | 3.7 | CN1C(=O)[C@@H](NC(=O)c2cc3ccccc3[nH]2)N=C(c2ccccc2)c2ccccc21 | 10.6019/CHEMBL5442687 | |||
73777135 | 150458 | None | 0 | Mouse | Functional | pEC50 | = | 7.4 | 7.4 | 5 | 2 | ChEMBL | 412 | 4 | 1 | 4 | 5.4 | N#Cc1cc(SC(F)(F)F)cc(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3953289 | 150458 | None | 0 | Mouse | Functional | pEC50 | = | 7.4 | 7.4 | 5 | 2 | ChEMBL | 412 | 4 | 1 | 4 | 5.4 | N#Cc1cc(SC(F)(F)F)cc(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
73776995 | 148830 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC1CC(CC(=O)O)CCC12CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3940359 | 148830 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC1CC(CC(=O)O)CCC12CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
24825509 | 87980 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -29 | 2 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL234057 | 87980 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -29 | 2 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | O=C(O)CCc1ccc(NCc2ccc(Oc3ccccc3)cc2)cc1 | 10.1021/jm300215x | |||
134154953 | 151365 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 7 | 2 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3960369 | 151365 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 7 | 2 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
86343963 | 164839 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 443 | 7 | 1 | 3 | 5.5 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2cccc(F)c2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4217669 | 164839 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | ChEMBL | 443 | 7 | 1 | 3 | 5.5 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2cccc(F)c2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
134155950 | 151179 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 430 | 6 | 1 | 4 | 4.6 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H]([C@@H]3C[C@H]3C(=O)O)O4)c2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3959068 | 151179 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | - | 1 | ChEMBL | 430 | 6 | 1 | 4 | 4.6 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H]([C@@H]3C[C@H]3C(=O)O)O4)c2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
145984009 | 165684 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 418 | 7 | 1 | 4 | 4.7 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4242595 | 165684 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 418 | 7 | 1 | 4 | 4.7 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
57522038 | 3887 | None | 48 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.6019/CHEMBL5442687 | |||
6490 | 3887 | None | 48 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.6019/CHEMBL5442687 | |||
CHEMBL2058533 | 3887 | None | 48 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.6019/CHEMBL5442687 | |||
134157207 | 154300 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 3 | 2 | ChEMBL | 386 | 7 | 1 | 3 | 5.3 | Cc1cc(-c2cc(OC(F)(F)F)ccc2F)cc(C)c1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3985939 | 154300 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 3 | 2 | ChEMBL | 386 | 7 | 1 | 3 | 5.3 | Cc1cc(-c2cc(OC(F)(F)F)ccc2F)cc(C)c1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
57522038 | 3887 | None | 48 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/acsmedchemlett.6b00025 | |||
6490 | 3887 | None | 48 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/acsmedchemlett.6b00025 | |||
CHEMBL2058533 | 3887 | None | 48 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/acsmedchemlett.6b00025 | |||
134157563 | 154096 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 1 | 2 | ChEMBL | 365 | 6 | 1 | 4 | 5.0 | O=C(O)CCCOc1ccc(-c2noc3ccccc23)c(Cl)c1Cl | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3984072 | 154096 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 1 | 2 | ChEMBL | 365 | 6 | 1 | 4 | 5.0 | O=C(O)CCCOc1ccc(-c2noc3ccccc23)c(Cl)c1Cl | 10.1016/j.bmcl.2016.10.054 | |||
2200 | 3311 | None | 35 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -371 | 3 | ChEMBL | 619 | 7 | 2 | 7 | 3.3 | COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl | 10.6019/CHEMBL5442687 | |||
3482 | 3311 | None | 35 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -371 | 3 | ChEMBL | 619 | 7 | 2 | 7 | 3.3 | COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl | 10.6019/CHEMBL5442687 | |||
60943 | 3311 | None | 35 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -371 | 3 | ChEMBL | 619 | 7 | 2 | 7 | 3.3 | COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl | 10.6019/CHEMBL5442687 | |||
CHEMBL419667 | 3311 | None | 35 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -371 | 3 | ChEMBL | 619 | 7 | 2 | 7 | 3.3 | COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl | 10.6019/CHEMBL5442687 | |||
DB13929 | 3311 | None | 35 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -371 | 3 | ChEMBL | 619 | 7 | 2 | 7 | 3.3 | COc1ccc(cc1OC)S(=O)(=O)N1c2ccc(cc2[C@]([C@@H]1C(=O)N1CCC[C@H]1C(=O)N)(O)c1ccccc1Cl)Cl | 10.6019/CHEMBL5442687 | |||
54584098 | 61825 | None | 2 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -5 | 2 | ChEMBL | 334 | 6 | 1 | 2 | 4.0 | O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 | 10.1021/jm300215x | |||
CHEMBL1773254 | 61825 | None | 2 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -5 | 2 | ChEMBL | 334 | 6 | 1 | 2 | 4.0 | O=C(O)CCc1ccc(OCc2cccc(Br)c2)cc1 | 10.1021/jm300215x | |||
54583098 | 61829 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -70 | 2 | ChEMBL | 331 | 7 | 2 | 2 | 5.0 | O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 | 10.1021/jm300215x | |||
CHEMBL1773258 | 61829 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -70 | 2 | ChEMBL | 331 | 7 | 2 | 2 | 5.0 | O=C(O)CCc1ccc(NCc2cccc(-c3ccccc3)c2)cc1 | 10.1021/jm300215x | |||
3036864 | 205211 | None | 16 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -12302 | 13 | ChEMBL | 287 | 1 | 1 | 2 | 3.7 | CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 | 10.6019/CHEMBL5442687 | |||
CHEMBL1256645 | 205211 | None | 16 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -12302 | 13 | ChEMBL | 287 | 1 | 1 | 2 | 3.7 | CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 | 10.6019/CHEMBL5442687 | |||
CHEMBL1814790 | 205211 | None | 16 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -12302 | 13 | ChEMBL | 287 | 1 | 1 | 2 | 3.7 | CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 | 10.6019/CHEMBL5442687 | |||
CHEMBL62 | 205211 | None | 16 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -12302 | 13 | ChEMBL | 287 | 1 | 1 | 2 | 3.7 | CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 | 10.6019/CHEMBL5442687 | |||
134157563 | 154096 | None | 0 | Mouse | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 2 | ChEMBL | 365 | 6 | 1 | 4 | 5.0 | O=C(O)CCCOc1ccc(-c2noc3ccccc23)c(Cl)c1Cl | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3984072 | 154096 | None | 0 | Mouse | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 2 | ChEMBL | 365 | 6 | 1 | 4 | 5.0 | O=C(O)CCCOc1ccc(-c2noc3ccccc23)c(Cl)c1Cl | 10.1016/j.bmcl.2016.10.054 | |||
73777069 | 142756 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 1 | 2 | ChEMBL | 389 | 4 | 1 | 3 | 5.0 | O=C(O)CC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3891920 | 142756 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 1 | 2 | ChEMBL | 389 | 4 | 1 | 3 | 5.0 | O=C(O)CC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
134138318 | 148107 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 3 | ChEMBL | 378 | 9 | 1 | 4 | 5.4 | COc1cccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3934450 | 148107 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 3 | ChEMBL | 378 | 9 | 1 | 4 | 5.4 | COc1cccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
134144000 | 150297 | None | 0 | Mouse | Functional | pEC50 | = | 8.3 | 8.3 | 1 | 2 | ChEMBL | 431 | 8 | 1 | 6 | 4.0 | COc1cc(O[C@H]2C[C@H](OC)C2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3952043 | 150297 | None | 0 | Mouse | Functional | pEC50 | = | 8.3 | 8.3 | 1 | 2 | ChEMBL | 431 | 8 | 1 | 6 | 4.0 | COc1cc(O[C@H]2C[C@H](OC)C2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
86281123 | 163843 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 439 | 7 | 1 | 3 | 5.7 | Cc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4205429 | 163843 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 439 | 7 | 1 | 3 | 5.7 | Cc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2018.02.013 | |||
137646553 | 158006 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 362 | 6 | 1 | 2 | 4.7 | Cc1ccc(Br)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4084333 | 158006 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 362 | 6 | 1 | 2 | 4.7 | Cc1ccc(Br)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
118707083 | 113072 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 325 | 4 | 1 | 3 | 3.8 | COc1ccc(S(=O)(=O)Nc2c(C)cc(Cl)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311197 | 113072 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 325 | 4 | 1 | 3 | 3.8 | COc1ccc(S(=O)(=O)Nc2c(C)cc(Cl)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
743974 | 113090 | None | 54 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 1 | 3 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311308 | 113090 | None | 54 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 1 | 3 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
137638995 | 157057 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 16 | 2 | ChEMBL | 338 | 6 | 1 | 2 | 4.6 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4072885 | 157057 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 16 | 2 | ChEMBL | 338 | 6 | 1 | 2 | 4.6 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
23136401 | 159228 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 7 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.4 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4097919 | 159228 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 7 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.4 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 | 10.1016/j.bmcl.2017.01.034 | |||
145984445 | 165555 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 456 | 9 | 1 | 4 | 5.3 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCC(C)(C)C(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4239572 | 165555 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 456 | 9 | 1 | 4 | 5.3 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCC(C)(C)C(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
134138281 | 147874 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 410 | 7 | 1 | 6 | 3.9 | COc1cc(OC2CC2)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3932664 | 147874 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 410 | 7 | 1 | 6 | 3.9 | COc1cc(OC2CC2)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
90417978 | 162078 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 477 | 7 | 1 | 4 | 6.4 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4159180 | 162078 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 477 | 7 | 1 | 4 | 6.4 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
73777153 | 142910 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 2 | 3 | ChEMBL | 355 | 3 | 1 | 2 | 5.2 | O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3893026 | 142910 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 2 | 3 | ChEMBL | 355 | 3 | 1 | 2 | 5.2 | O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
216237 | 3843 | None | 51 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -724 | 11 | ChEMBL | 448 | 3 | 2 | 3 | 5.7 | Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C | 10.6019/CHEMBL5442687 | |||
216237.0 | 3843 | None | 51 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -724 | 11 | ChEMBL | 448 | 3 | 2 | 3 | 5.7 | Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C | 10.6019/CHEMBL5442687 | |||
2226 | 3843 | None | 51 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -724 | 11 | ChEMBL | 448 | 3 | 2 | 3 | 5.7 | Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C | 10.6019/CHEMBL5442687 | |||
4110 | 3843 | None | 51 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -724 | 11 | ChEMBL | 448 | 3 | 2 | 3 | 5.7 | Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C | 10.6019/CHEMBL5442687 | |||
443894 | 3843 | None | 51 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -724 | 11 | ChEMBL | 448 | 3 | 2 | 3 | 5.7 | Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C | 10.6019/CHEMBL5442687 | |||
443894.0 | 3843 | None | 51 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -724 | 11 | ChEMBL | 448 | 3 | 2 | 3 | 5.7 | Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C | 10.6019/CHEMBL5442687 | |||
CHEMBL344159 | 3843 | None | 51 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -724 | 11 | ChEMBL | 448 | 3 | 2 | 3 | 5.7 | Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C | 10.6019/CHEMBL5442687 | |||
DB06212 | 3843 | None | 51 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -724 | 11 | ChEMBL | 448 | 3 | 2 | 3 | 5.7 | Clc1ccc2c(c1)C(O)CCCN2C(=O)c1ccc(cc1C)NC(=O)c1ccccc1C | 10.6019/CHEMBL5442687 | |||
57521918 | 76303 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 2 | ChEMBL | 380 | 7 | 1 | 2 | 5.9 | Cc1ccc(-c2ccc(Cl)cc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058531 | 76303 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 2 | ChEMBL | 380 | 7 | 1 | 2 | 5.9 | Cc1ccc(-c2ccc(Cl)cc2COc2ccc(CCC(=O)O)cc2)cc1 | 10.1021/jm300215x | |||
54582150 | 61830 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | -22 | 2 | ChEMBL | 331 | 7 | 2 | 2 | 5.0 | O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL1773259 | 61830 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | -22 | 2 | ChEMBL | 331 | 7 | 2 | 2 | 5.0 | O=C(O)CCc1ccc(NCc2ccccc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
59455584 | 157133 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 378 | 8 | 1 | 4 | 4.6 | CCc1ccc(-n2nccc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4073815 | 157133 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 378 | 8 | 1 | 4 | 4.6 | CCc1ccc(-n2nccc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
137646553 | 158006 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 362 | 6 | 1 | 2 | 4.7 | Cc1ccc(Br)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4084333 | 158006 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 362 | 6 | 1 | 2 | 4.7 | Cc1ccc(Br)c(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
134132951 | 144710 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 454 | 8 | 1 | 7 | 3.9 | COc1cc(O[C@H]2C[C@H](OC)C2)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3907996 | 144710 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 454 | 8 | 1 | 7 | 3.9 | COc1cc(O[C@H]2C[C@H](OC)C2)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
137638995 | 157057 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 16 | 2 | ChEMBL | 338 | 6 | 1 | 2 | 4.6 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4072885 | 157057 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 16 | 2 | ChEMBL | 338 | 6 | 1 | 2 | 4.6 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1C(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
90407027 | 164289 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 437 | 7 | 1 | 3 | 6.3 | Cc1c(CCCO)ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4210752 | 164289 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 437 | 7 | 1 | 3 | 6.3 | Cc1c(CCCO)ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
54585039 | 61823 | None | 2 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -17 | 2 | ChEMBL | 334 | 6 | 1 | 2 | 4.0 | O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL1773252 | 61823 | None | 2 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -17 | 2 | ChEMBL | 334 | 6 | 1 | 2 | 4.0 | O=C(O)CCc1ccc(OCc2ccc(Br)cc2)cc1 | 10.1021/jm300215x | |||
134143899 | 150327 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 3 | ChEMBL | 350 | 5 | 1 | 3 | 5.0 | O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3952316 | 150327 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 3 | ChEMBL | 350 | 5 | 1 | 3 | 5.0 | O=C(O)CCc1cc2cc(-c3cccc(OC(F)(F)F)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
87054900 | 148849 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.4 | O=C(O)CCCOc1ccc(-c2ccccc2Oc2ccccc2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3940493 | 148849 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -1 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.4 | O=C(O)CCCOc1ccc(-c2ccccc2Oc2ccccc2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
90406418 | 164672 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 457 | 7 | 1 | 3 | 5.8 | CC(Cc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)c(F)c1)C(=O)O | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4215446 | 164672 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | ChEMBL | 457 | 7 | 1 | 3 | 5.8 | CC(Cc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)c(F)c1)C(=O)O | 10.1016/j.bmcl.2018.02.013 | |||
134131620 | 142519 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 442 | 7 | 1 | 5 | 4.5 | COc1cc(O[C@H]2C[C@H](OC)C2)cc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3890035 | 142519 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 442 | 7 | 1 | 5 | 4.5 | COc1cc(O[C@H]2C[C@H](OC)C2)cc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
23136401 | 159228 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 7 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.4 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4097919 | 159228 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 7 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.4 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(Oc2ccccc2)c1 | 10.1016/j.bmcl.2017.01.034 | |||
90418513 | 162718 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 429 | 8 | 1 | 4 | 6.2 | CCc1ccc(-c2snc(Cl)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4169436 | 162718 | None | 0 | Human | Functional | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 429 | 8 | 1 | 4 | 6.2 | CCc1ccc(-c2snc(Cl)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
23136363 | 58850 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -14 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.1 | O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 | 10.1021/jm300215x | |||
CHEMBL1688458 | 58850 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -14 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.1 | O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 | 10.1021/jm300215x | |||
73777063 | 1154 | None | 36 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.6019/CHEMBL5442687 | |||
8418 | 1154 | None | 36 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.6019/CHEMBL5442687 | |||
CHEMBL3919973 | 1154 | None | 36 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.6019/CHEMBL5442687 | |||
134150245 | 152334 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -6 | 3 | ChEMBL | 374 | 7 | 1 | 3 | 5.1 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3968947 | 152334 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -6 | 3 | ChEMBL | 374 | 7 | 1 | 3 | 5.1 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137643146 | 158156 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 455 | 8 | 1 | 4 | 5.8 | CCc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4086174 | 158156 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 455 | 8 | 1 | 4 | 5.8 | CCc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
73777085 | 153319 | None | 0 | Mouse | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 351 | 4 | 1 | 3 | 4.6 | COc1ccc(Cl)c(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3977361 | 153319 | None | 0 | Mouse | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 351 | 4 | 1 | 3 | 4.6 | COc1ccc(Cl)c(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
73776997 | 154369 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 407 | 4 | 1 | 4 | 4.5 | O=C(O)CC1CCC2(CCN(c3cc(OC(F)(F)F)ccc3Cl)CC2)OC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3986483 | 154369 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 407 | 4 | 1 | 4 | 4.5 | O=C(O)CC1CCC2(CCN(c3cc(OC(F)(F)F)ccc3Cl)CC2)OC1 | 10.1021/acsmedchemlett.6b00360 | |||
23346507 | 88322 | None | 0 | Human | Functional | pEC50 | = | 4.2 | 4.2 | -30 | 2 | ChEMBL | 255 | 6 | 2 | 2 | 3.3 | O=C(O)CCc1ccc(NCc2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL234834 | 88322 | None | 0 | Human | Functional | pEC50 | = | 4.2 | 4.2 | -30 | 2 | ChEMBL | 255 | 6 | 2 | 2 | 3.3 | O=C(O)CCc1ccc(NCc2ccccc2)cc1 | 10.1021/jm300215x | |||
10223146 | 2155 | None | 46 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -30 | 5 | ChEMBL | 407 | 4 | 3 | 6 | 4.3 | O=C(Nc1cc(Cl)nc(c1)Cl)NNc1cc(C(C)C)c2c(n1)n(C)nc2C | 10.6019/CHEMBL5442687 | |||
2917 | 2155 | None | 46 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -30 | 5 | ChEMBL | 407 | 4 | 3 | 6 | 4.3 | O=C(Nc1cc(Cl)nc(c1)Cl)NNc1cc(C(C)C)c2c(n1)n(C)nc2C | 10.6019/CHEMBL5442687 | |||
CHEMBL1368758 | 2155 | None | 46 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -30 | 5 | ChEMBL | 407 | 4 | 3 | 6 | 4.3 | O=C(Nc1cc(Cl)nc(c1)Cl)NNc1cc(C(C)C)c2c(n1)n(C)nc2C | 10.6019/CHEMBL5442687 | |||
57521810 | 76292 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 350 | 7 | 1 | 2 | 5.1 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(F)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058521 | 76292 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 350 | 7 | 1 | 2 | 5.1 | O=C(O)CCc1ccc(OCc2ccccc2-c2ccc(F)cc2)cc1 | 10.1021/jm300215x | |||
24825484 | 88025 | None | 0 | Human | Functional | pEC50 | = | 4.2 | 4.2 | -208 | 2 | ChEMBL | 331 | 7 | 2 | 2 | 5.0 | O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 | 10.1021/jm300215x | |||
CHEMBL234269 | 88025 | None | 0 | Human | Functional | pEC50 | = | 4.2 | 4.2 | -208 | 2 | ChEMBL | 331 | 7 | 2 | 2 | 5.0 | O=C(O)CCc1ccc(NCc2ccc(-c3ccccc3)cc2)cc1 | 10.1021/jm300215x | |||
73777111 | 149798 | None | 0 | Mouse | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 373 | 3 | 1 | 2 | 5.1 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3947837 | 149798 | None | 0 | Mouse | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 373 | 3 | 1 | 2 | 5.1 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
137642184 | 158594 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 386 | 8 | 2 | 4 | 4.4 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c(CO)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4091118 | 158594 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 386 | 8 | 2 | 4 | 4.4 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c(CO)c1 | 10.1016/j.bmcl.2017.01.034 | |||
134156727 | 153723 | None | 0 | Mouse | Functional | pEC50 | = | 8.2 | 8.2 | 4 | 2 | ChEMBL | 419 | 7 | 1 | 5 | 4.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)n2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3980898 | 153723 | None | 0 | Mouse | Functional | pEC50 | = | 8.2 | 8.2 | 4 | 2 | ChEMBL | 419 | 7 | 1 | 5 | 4.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)n2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
137637576 | 156154 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 63 | 2 | ChEMBL | 298 | 6 | 1 | 2 | 4.2 | Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4062640 | 156154 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 63 | 2 | ChEMBL | 298 | 6 | 1 | 2 | 4.2 | Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
137658634 | 159497 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 342 | 8 | 1 | 3 | 4.7 | Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(OC(C)C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4100773 | 159497 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 342 | 8 | 1 | 3 | 4.7 | Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(OC(C)C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
137643146 | 158156 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 455 | 8 | 1 | 4 | 5.8 | CCc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4086174 | 158156 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 455 | 8 | 1 | 4 | 5.8 | CCc1ccc(-c2noc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
134144214 | 150446 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -2 | 3 | ChEMBL | 384 | 8 | 1 | 3 | 5.7 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3953203 | 150446 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -2 | 3 | ChEMBL | 384 | 8 | 1 | 3 | 5.7 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccc(F)c3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
59455552 | 156132 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 384 | 7 | 1 | 4 | 4.7 | Cc1c(CCC(=O)O)ccc(OCc2ccnn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4062462 | 156132 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 384 | 7 | 1 | 4 | 4.7 | Cc1c(CCC(=O)O)ccc(OCc2ccnn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
134134229 | 143342 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -1 | 3 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3896657 | 143342 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -1 | 3 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1021/acsmedchemlett.6b00360 | |||
134134229 | 143342 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -1 | 3 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3896657 | 143342 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -1 | 3 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
137637576 | 156154 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 63 | 2 | ChEMBL | 298 | 6 | 1 | 2 | 4.2 | Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4062640 | 156154 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 63 | 2 | ChEMBL | 298 | 6 | 1 | 2 | 4.2 | Cc1cc(C)cc(COc2ccc(CCC(=O)O)cc2C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
137658634 | 159497 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 342 | 8 | 1 | 3 | 4.7 | Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(OC(C)C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4100773 | 159497 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 342 | 8 | 1 | 3 | 4.7 | Cc1cc(COc2ccc(CCC(=O)O)cc2C)cc(OC(C)C)c1 | 10.1016/j.bmcl.2017.01.034 | |||
57522038 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmc.2017.10.040 | |||
6490 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmc.2017.10.040 | |||
CHEMBL2058533 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmc.2017.10.040 | |||
137638911 | 156821 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 32 | 2 | ChEMBL | 384 | 7 | 1 | 3 | 5.5 | Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4070298 | 156821 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 32 | 2 | ChEMBL | 384 | 7 | 1 | 3 | 5.5 | Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
137656526 | 159847 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 2 | 2 | ChEMBL | 356 | 7 | 1 | 3 | 4.9 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4105013 | 159847 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 2 | 2 | ChEMBL | 356 | 7 | 1 | 3 | 4.9 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
743974 | 113090 | None | 54 | Mouse | Functional | pEC50 | = | 6.2 | 6.2 | -3 | 3 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311308 | 113090 | None | 54 | Mouse | Functional | pEC50 | = | 6.2 | 6.2 | -3 | 3 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
46941175 | 61832 | None | 27 | Human | Functional | pEC50 | = | 5.2 | 5.2 | -331 | 3 | ChEMBL | 345 | 7 | 2 | 2 | 5.3 | Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm3002026 | |||
CHEMBL1773261 | 61832 | None | 27 | Human | Functional | pEC50 | = | 5.2 | 5.2 | -331 | 3 | ChEMBL | 345 | 7 | 2 | 2 | 5.3 | Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm3002026 | |||
46941175 | 61832 | None | 27 | Human | Functional | pEC50 | = | 5.2 | 5.2 | -331 | 3 | ChEMBL | 345 | 7 | 2 | 2 | 5.3 | Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm300215x | |||
CHEMBL1773261 | 61832 | None | 27 | Human | Functional | pEC50 | = | 5.2 | 5.2 | -331 | 3 | ChEMBL | 345 | 7 | 2 | 2 | 5.3 | Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm300215x | |||
3518281 | 113095 | None | 8 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 293 | 3 | 1 | 2 | 3.6 | Cc1cc(C)c(NS(=O)(=O)c2ccc(F)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311317 | 113095 | None | 8 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 293 | 3 | 1 | 2 | 3.6 | Cc1cc(C)c(NS(=O)(=O)c2ccc(F)cc2)c(C)c1 | 10.1016/j.bmcl.2014.05.012 | |||
137642184 | 158594 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 386 | 8 | 2 | 4 | 4.4 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c(CO)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4091118 | 158594 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | ChEMBL | 386 | 8 | 2 | 4 | 4.4 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)c(CO)c1 | 10.1016/j.bmcl.2017.01.034 | |||
145985122 | 166003 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 17 | 2 | ChEMBL | 456 | 11 | 1 | 4 | 5.5 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4250132 | 166003 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 17 | 2 | ChEMBL | 456 | 11 | 1 | 4 | 5.5 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
134147174 | 149791 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 2 | 2 | ChEMBL | 370 | 6 | 1 | 3 | 5.7 | O=C(O)CCc1cc2cc(-c3cc(Cl)cc(OC4CCC4)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3947787 | 149791 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 2 | 2 | ChEMBL | 370 | 6 | 1 | 3 | 5.7 | O=C(O)CCc1cc2cc(-c3cc(Cl)cc(OC4CCC4)c3)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
134145412 | 149359 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -2 | 2 | ChEMBL | 330 | 8 | 1 | 3 | 4.3 | O=C(O)CCCOc1ccc(-c2cc(OC3CC3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3944507 | 149359 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -2 | 2 | ChEMBL | 330 | 8 | 1 | 3 | 4.3 | O=C(O)CCCOc1ccc(-c2cc(OC3CC3)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
73777156 | 152804 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 1 | 3 | ChEMBL | 396 | 4 | 1 | 4 | 4.7 | N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3973034 | 152804 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 1 | 3 | ChEMBL | 396 | 4 | 1 | 4 | 4.7 | N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
134143163 | 145832 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 2 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.7 | Cc1ccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3916564 | 145832 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 2 | 2 | ChEMBL | 362 | 8 | 1 | 3 | 5.7 | Cc1ccc(Oc2cccc(-c3ccc(OCCCC(=O)O)cc3)c2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137638911 | 156821 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 32 | 2 | ChEMBL | 384 | 7 | 1 | 3 | 5.5 | Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4070298 | 156821 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 32 | 2 | ChEMBL | 384 | 7 | 1 | 3 | 5.5 | Cc1cc(CCC(=O)O)cc(C)c1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
134134149 | 143462 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 2 | 3 | ChEMBL | 348 | 8 | 1 | 3 | 5.4 | O=C(O)CCCOc1ccc(-c2cccc(Oc3ccccc3)c2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3897776 | 143462 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 2 | 3 | ChEMBL | 348 | 8 | 1 | 3 | 5.4 | O=C(O)CCCOc1ccc(-c2cccc(Oc3ccccc3)c2)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137640328 | 157076 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 461 | 7 | 1 | 4 | 5.9 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)c1F | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4073078 | 157076 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 461 | 7 | 1 | 4 | 5.9 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)c1F | 10.1016/j.bmcl.2017.06.028 | |||
117886639 | 148538 | None | 0 | Mouse | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 391 | 3 | 1 | 3 | 5.3 | CC1(C)Cc2cc(Cl)cc(N3CCC4(CCC(CC(=O)O)CC4)CC3)c2O1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3937916 | 148538 | None | 0 | Mouse | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 391 | 3 | 1 | 3 | 5.3 | CC1(C)Cc2cc(Cl)cc(N3CCC4(CCC(CC(=O)O)CC4)CC3)c2O1 | 10.1021/acsmedchemlett.6b00360 | |||
118184919 | 162968 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 468 | 7 | 1 | 5 | 5.6 | N#Cc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4173280 | 162968 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 468 | 7 | 1 | 5 | 5.6 | N#Cc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
54586984 | 61827 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | -34 | 2 | ChEMBL | 323 | 6 | 2 | 2 | 4.3 | O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 | 10.1021/jm300215x | |||
CHEMBL1773256 | 61827 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | -34 | 2 | ChEMBL | 323 | 6 | 2 | 2 | 4.3 | O=C(O)CCc1ccc(NCc2cccc(C(F)(F)F)c2)cc1 | 10.1021/jm300215x | |||
134139171 | 146351 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -2 | 3 | ChEMBL | 350 | 6 | 1 | 3 | 5.4 | Cc1cc(OC2CCC2)cc(-c2ccc3oc(CCC(=O)O)cc3c2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3920591 | 146351 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | -2 | 3 | ChEMBL | 350 | 6 | 1 | 3 | 5.4 | Cc1cc(OC2CCC2)cc(-c2ccc3oc(CCC(=O)O)cc3c2)c1 | 10.1016/j.bmcl.2016.10.054 | |||
137661886 | 159421 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 453 | 7 | 1 | 4 | 6.2 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4099943 | 159421 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 453 | 7 | 1 | 4 | 6.2 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c1C | 10.1016/j.bmcl.2017.06.028 | |||
90418886 | 163015 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 423 | 9 | 1 | 4 | 6.1 | CCc1ccc(-c2nsc(CC)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4174122 | 163015 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 423 | 9 | 1 | 4 | 6.1 | CCc1ccc(-c2nsc(CC)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
137656526 | 159847 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 2 | 2 | ChEMBL | 356 | 7 | 1 | 3 | 4.9 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4105013 | 159847 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 2 | 2 | ChEMBL | 356 | 7 | 1 | 3 | 4.9 | O=C(O)CCc1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
145985686 | 165525 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 354 | 2 | ChEMBL | 358 | 7 | 1 | 3 | 4.2 | COc1cc(F)c(F)c(-c2cc(F)c(OCCCC(=O)O)c(F)c2)c1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4238809 | 165525 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 354 | 2 | ChEMBL | 358 | 7 | 1 | 3 | 4.2 | COc1cc(F)c(F)c(-c2cc(F)c(OCCCC(=O)O)c(F)c2)c1 | 10.1016/j.bmcl.2018.06.047 | |||
137648785 | 157702 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 427 | 7 | 1 | 4 | 5.2 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccccc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4080995 | 157702 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 427 | 7 | 1 | 4 | 5.2 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccccc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
134153986 | 152595 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 396 | 4 | 1 | 3 | 4.8 | O=C(O)[C@@H]1C[C@H]1[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3971308 | 152595 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 396 | 4 | 1 | 3 | 4.8 | O=C(O)[C@@H]1C[C@H]1[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
134153562 | 152812 | None | 0 | Mouse | Functional | pEC50 | = | 8.2 | 8.2 | 2 | 3 | ChEMBL | 394 | 7 | 1 | 3 | 4.9 | O=C(O)CCCOc1c(F)cc(-c2cc(OC(F)(F)F)ccc2F)cc1F | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3973101 | 152812 | None | 0 | Mouse | Functional | pEC50 | = | 8.2 | 8.2 | 2 | 3 | ChEMBL | 394 | 7 | 1 | 3 | 4.9 | O=C(O)CCCOc1c(F)cc(-c2cc(OC(F)(F)F)ccc2F)cc1F | 10.1016/j.bmcl.2016.10.054 | |||
134140073 | 146409 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 1 | 2 | ChEMBL | 382 | 5 | 1 | 3 | 5.4 | CC(Cc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1)C(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3921062 | 146409 | None | 0 | Mouse | Functional | pEC50 | = | 7.2 | 7.2 | 1 | 2 | ChEMBL | 382 | 5 | 1 | 3 | 5.4 | CC(Cc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1)C(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
134135468 | 144563 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 389 | 4 | 1 | 3 | 4.8 | O=C(O)C1CCC(C2CCN(c3cc(OC(F)(F)F)ccc3F)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3906716 | 144563 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | 1 | 2 | ChEMBL | 389 | 4 | 1 | 3 | 4.8 | O=C(O)C1CCC(C2CCN(c3cc(OC(F)(F)F)ccc3F)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
57521702 | 76289 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | -11 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccccc1-c1ccccc1COc1ccc(CCC(=O)O)cc1 | 10.1021/jm300215x | |||
CHEMBL2058518 | 76289 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | -11 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccccc1-c1ccccc1COc1ccc(CCC(=O)O)cc1 | 10.1021/jm300215x | |||
137636575 | 155991 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 479 | 7 | 1 | 4 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(F)cc3Cl)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4060663 | 155991 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 479 | 7 | 1 | 4 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(F)cc3Cl)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
137635671 | 156082 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 461 | 7 | 1 | 4 | 5.9 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4061699 | 156082 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 461 | 7 | 1 | 4 | 5.9 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)noc2C(F)(F)F)c(F)c1 | 10.1016/j.bmcl.2017.06.028 | |||
85471695 | 158761 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 394 | 8 | 1 | 3 | 6.2 | CCc1ccc(-c2cscc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4092882 | 158761 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | ChEMBL | 394 | 8 | 1 | 3 | 6.2 | CCc1ccc(-c2cscc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
85470884 | 164099 | None | 3 | Rat | Functional | pEC50 | = | 6.2 | 6.2 | -7 | 5 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4208325 | 164099 | None | 3 | Rat | Functional | pEC50 | = | 6.2 | 6.2 | -7 | 5 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
134155847 | 151191 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | 63 | 2 | ChEMBL | 418 | 5 | 1 | 3 | 5.6 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)cc(Cl)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3959144 | 151191 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | 63 | 2 | ChEMBL | 418 | 5 | 1 | 3 | 5.6 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)cc(Cl)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
134132711 | 145026 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | -1 | 2 | ChEMBL | 372 | 3 | 0 | 4 | 4.2 | O=S1(=O)c2ccccc2CN1c1cc(Cl)cc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3910333 | 145026 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | -1 | 2 | ChEMBL | 372 | 3 | 0 | 4 | 4.2 | O=S1(=O)c2ccccc2CN1c1cc(Cl)cc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
137636167 | 156078 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | 2 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.2 | Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4061630 | 156078 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | 2 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.2 | Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O | 10.1016/j.bmcl.2017.01.034 | |||
134142450 | 145534 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 10 | 2 | ChEMBL | 382 | 5 | 1 | 3 | 5.7 | CC(CC(=O)O)c1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3914253 | 145534 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 10 | 2 | ChEMBL | 382 | 5 | 1 | 3 | 5.7 | CC(CC(=O)O)c1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
137660302 | 159532 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 413 | 8 | 1 | 4 | 5.8 | CCc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4101135 | 159532 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 413 | 8 | 1 | 4 | 5.8 | CCc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
90418333 | 162750 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 473 | 8 | 1 | 5 | 5.7 | COc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4169851 | 162750 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 473 | 8 | 1 | 5 | 5.7 | COc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
57522038 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmc.2017.10.040 | |||
6490 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmc.2017.10.040 | |||
CHEMBL2058533 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmc.2017.10.040 | |||
57839754 | 157908 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 270 | 6 | 1 | 2 | 3.6 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4083325 | 157908 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 270 | 6 | 1 | 2 | 3.6 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1 | 10.1016/j.bmcl.2017.01.034 | |||
90407037 | 157380 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 377 | 8 | 1 | 3 | 5.3 | CCc1ccc(-n2cccc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4076902 | 157380 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 377 | 8 | 1 | 3 | 5.3 | CCc1ccc(-n2cccc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
3893 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -10 | 4 | ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
4642 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -10 | 4 | ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
5534 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -10 | 4 | ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
CHEMBL108766 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -10 | 4 | ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
DB03017 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -10 | 4 | ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | |||
59455555 | 158808 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 399 | 7 | 1 | 4 | 5.5 | Cc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4093383 | 158808 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 399 | 7 | 1 | 4 | 5.5 | Cc1onc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
134149615 | 148664 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -1 | 3 | ChEMBL | 370 | 5 | 1 | 3 | 4.6 | O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3939004 | 148664 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -1 | 3 | ChEMBL | 370 | 5 | 1 | 3 | 4.6 | O=C(O)CCC1Cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1016/j.bmcl.2016.10.054 | |||
90418278 | 162473 | None | 16 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | -1 | 2 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3F)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4165366 | 162473 | None | 16 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | -1 | 2 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3F)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
134155277 | 151414 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 3 | 2 | ChEMBL | 388 | 7 | 1 | 3 | 5.5 | Cc1cc(OCCCC(=O)O)ccc1-c1cc(OC(F)(F)F)ccc1Cl | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3961009 | 151414 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 3 | 2 | ChEMBL | 388 | 7 | 1 | 3 | 5.5 | Cc1cc(OCCCC(=O)O)ccc1-c1cc(OC(F)(F)F)ccc1Cl | 10.1016/j.bmcl.2016.10.054 | |||
134133992 | 143826 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cnc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3900705 | 143826 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cnc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
134133297 | 143866 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 3 | 3 | ChEMBL | 372 | 7 | 1 | 3 | 4.9 | Cc1cc(-c2cc(OC(F)(F)F)ccc2F)ccc1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3900990 | 143866 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 3 | 3 | ChEMBL | 372 | 7 | 1 | 3 | 4.9 | Cc1cc(-c2cc(OC(F)(F)F)ccc2F)ccc1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
977153 | 51435 | None | 11 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 339 | 4 | 1 | 3 | 4.1 | COc1cc(S(=O)(=O)Nc2c(C)cc(C)cc2C)ccc1Cl | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL1581959 | 51435 | None | 11 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 339 | 4 | 1 | 3 | 4.1 | COc1cc(S(=O)(=O)Nc2c(C)cc(C)cc2C)ccc1Cl | 10.1016/j.bmcl.2014.05.012 | |||
137636167 | 156078 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | 2 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.2 | Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4061630 | 156078 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | 2 | 2 | ChEMBL | 370 | 7 | 1 | 3 | 5.2 | Cc1cc(OCc2ccccc2SC(F)(F)F)ccc1CCC(=O)O | 10.1016/j.bmcl.2017.01.034 | |||
57839754 | 157908 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 270 | 6 | 1 | 2 | 3.6 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4083325 | 157908 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 270 | 6 | 1 | 2 | 3.6 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1 | 10.1016/j.bmcl.2017.01.034 | |||
743974 | 113090 | None | 54 | Rat | Functional | pEC50 | = | 6.1 | 6.1 | -1 | 3 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311308 | 113090 | None | 54 | Rat | Functional | pEC50 | = | 6.1 | 6.1 | -1 | 3 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
8190702 | 113094 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 317 | 4 | 1 | 3 | 3.6 | CC(=O)c1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311316 | 113094 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | - | 1 | ChEMBL | 317 | 4 | 1 | 3 | 3.6 | CC(=O)c1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
85470884 | 164099 | None | 3 | Human | Functional | pEC50 | = | 7.1 | 7.1 | 2 | 5 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4208325 | 164099 | None | 3 | Human | Functional | pEC50 | = | 7.1 | 7.1 | 2 | 5 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
137634829 | 156163 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2scnc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4062742 | 156163 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2scnc2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
134154417 | 152793 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 2 | 2 | ChEMBL | 374 | 7 | 1 | 3 | 4.6 | O=C(O)CCCOc1ccc(-c2cc(-[n+]3ccsc3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3972973 | 152793 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 2 | 2 | ChEMBL | 374 | 7 | 1 | 3 | 4.6 | O=C(O)CCCOc1ccc(-c2cc(-[n+]3ccsc3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137631865 | 156425 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 399 | 7 | 1 | 4 | 5.5 | Cc1noc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4065769 | 156425 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 399 | 7 | 1 | 4 | 5.5 | Cc1noc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1016/j.bmcl.2017.06.028 | |||
134145750 | 149233 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -3 | 2 | ChEMBL | 324 | 6 | 1 | 2 | 4.6 | O=C(O)CCCOc1ccc(-c2ccccc2C(F)(F)F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3943430 | 149233 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -3 | 2 | ChEMBL | 324 | 6 | 1 | 2 | 4.6 | O=C(O)CCCOc1ccc(-c2ccccc2C(F)(F)F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
134142450 | 145534 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | -10 | 2 | ChEMBL | 382 | 5 | 1 | 3 | 5.7 | CC(CC(=O)O)c1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3914253 | 145534 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | -10 | 2 | ChEMBL | 382 | 5 | 1 | 3 | 5.7 | CC(CC(=O)O)c1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
134140073 | 146409 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -1 | 2 | ChEMBL | 382 | 5 | 1 | 3 | 5.4 | CC(Cc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1)C(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3921062 | 146409 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -1 | 2 | ChEMBL | 382 | 5 | 1 | 3 | 5.4 | CC(Cc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1)C(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
46892131 | 144759 | None | 3 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 3 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3908362 | 144759 | None | 3 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 3 | 2 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
51350138 | 58866 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -660 | 2 | ChEMBL | 378 | 7 | 1 | 2 | 5.7 | Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/jm3002026 | |||
CHEMBL1688473 | 58866 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -660 | 2 | ChEMBL | 378 | 7 | 1 | 2 | 5.7 | Cc1cccc(C)c1-c1cccc(COc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/jm3002026 | |||
86343792 | 164776 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 475 | 7 | 1 | 3 | 6.3 | O=C(O)CCc1ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4216937 | 164776 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 475 | 7 | 1 | 3 | 6.3 | O=C(O)CCc1ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2018.02.013 | |||
60195038 | 81823 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -912 | 2 | ChEMBL | 363 | 7 | 2 | 2 | 5.4 | Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/jm3002026 | |||
CHEMBL2164239 | 81823 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -912 | 2 | ChEMBL | 363 | 7 | 2 | 2 | 5.4 | Cc1ccccc1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/jm3002026 | |||
85472487 | 162572 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 477 | 7 | 1 | 4 | 6.4 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4167097 | 162572 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 477 | 7 | 1 | 4 | 6.4 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
51350272 | 58858 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -107 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm300215x | |||
CHEMBL1688465 | 58858 | None | 0 | Human | Functional | pEC50 | = | 5.1 | 5.1 | -107 | 2 | ChEMBL | 346 | 7 | 1 | 2 | 5.3 | Cc1ccccc1-c1cccc(COc2ccc(CCC(=O)O)cc2)c1 | 10.1021/jm300215x | |||
145985219 | 165559 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 420 | 9 | 1 | 4 | 5.0 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(C)c(OCCCC(=O)O)c(C)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4239630 | 165559 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 420 | 9 | 1 | 4 | 5.0 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(C)c(OCCCC(=O)O)c(C)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
90406893 | 164530 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 454 | 8 | 1 | 4 | 5.3 | CCc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cn1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4213710 | 164530 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 454 | 8 | 1 | 4 | 5.3 | CCc1ccc(-n2ccc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cn1 | 10.1016/j.bmcl.2018.02.013 | |||
134148736 | 148642 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -2 | 2 | ChEMBL | 383 | 8 | 1 | 4 | 5.4 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccnc3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3938783 | 148642 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | -2 | 2 | ChEMBL | 383 | 8 | 1 | 4 | 5.4 | O=C(O)CCCOc1ccc(-c2cc(Oc3cccnc3)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
86281121 | 164107 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 451 | 7 | 1 | 3 | 6.4 | Cc1c(CCC(=O)O)ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4208442 | 164107 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | - | 1 | ChEMBL | 451 | 7 | 1 | 3 | 6.4 | Cc1c(CCC(=O)O)ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2018.02.013 | |||
134138802 | 148007 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 4 | 2 | ChEMBL | 383 | 4 | 1 | 3 | 4.7 | O=C(O)C1CCN(c2ccc(-c3cc(OC(F)(F)F)ccc3F)cc2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3933619 | 148007 | None | 0 | Mouse | Functional | pEC50 | = | 7.1 | 7.1 | 4 | 2 | ChEMBL | 383 | 4 | 1 | 3 | 4.7 | O=C(O)C1CCN(c2ccc(-c3cc(OC(F)(F)F)ccc3F)cc2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
137649416 | 157611 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 338 | 6 | 1 | 2 | 4.6 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4079893 | 157611 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 338 | 6 | 1 | 2 | 4.6 | Cc1cc(CCC(=O)O)ccc1OCc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2017.01.034 | |||
134150245 | 152334 | None | 0 | Mouse | Functional | pEC50 | = | 8.1 | 8.1 | 6 | 3 | ChEMBL | 374 | 7 | 1 | 3 | 5.1 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3968947 | 152334 | None | 0 | Mouse | Functional | pEC50 | = | 8.1 | 8.1 | 6 | 3 | ChEMBL | 374 | 7 | 1 | 3 | 5.1 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2Cl)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
137657968 | 159686 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 394 | 8 | 1 | 3 | 6.2 | CCc1ccc(-c2ccsc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4103081 | 159686 | None | 0 | Human | Functional | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 394 | 8 | 1 | 3 | 6.2 | CCc1ccc(-c2ccsc2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1016/j.bmcl.2017.06.028 | |||
90407263 | 163694 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1F | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4203559 | 163694 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1F | 10.1016/j.bmcl.2018.02.013 | |||
57521917 | 76302 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -8 | 2 | ChEMBL | 366 | 7 | 1 | 2 | 5.6 | O=C(O)CCc1ccc(OCc2ccc(Cl)cc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
CHEMBL2058530 | 76302 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -8 | 2 | ChEMBL | 366 | 7 | 1 | 2 | 5.6 | O=C(O)CCc1ccc(OCc2ccc(Cl)cc2-c2ccccc2)cc1 | 10.1021/jm300215x | |||
90418067 | 162425 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 425 | 9 | 1 | 5 | 5.6 | CCc1ccc(-c2nsc(OC)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4164722 | 162425 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 425 | 9 | 1 | 5 | 5.6 | CCc1ccc(-c2nsc(OC)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
86343790 | 164034 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 441 | 7 | 1 | 3 | 5.9 | O=C(O)CCc1ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)cc1Cl | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4207603 | 164034 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 441 | 7 | 1 | 3 | 5.9 | O=C(O)CCc1ccc(OCc2c(C(F)(F)F)ccn2-c2ccc(F)cc2)cc1Cl | 10.1016/j.bmcl.2018.02.013 | |||
145984796 | 165837 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 428 | 9 | 1 | 4 | 4.7 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
CHEMBL4246396 | 165837 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 428 | 9 | 1 | 4 | 4.7 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3cc(F)c(OCCCC(=O)O)c(F)c3)c2)C1 | 10.1016/j.bmcl.2018.06.047 | |||
90405989 | 156051 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 383 | 7 | 1 | 3 | 5.3 | Cc1c(CCC(=O)O)ccc(OCc2cccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
CHEMBL4061340 | 156051 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | ChEMBL | 383 | 7 | 1 | 3 | 5.3 | Cc1c(CCC(=O)O)ccc(OCc2cccn2-c2ccc(Cl)cc2)c1C | 10.1016/j.bmcl.2017.06.028 | |||
60195040 | 81825 | None | 0 | Human | Functional | pEC50 | = | 4.0 | 4.0 | -5248 | 2 | ChEMBL | 377 | 7 | 2 | 2 | 5.7 | Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/jm3002026 | |||
CHEMBL2164241 | 81825 | None | 0 | Human | Functional | pEC50 | = | 4.0 | 4.0 | -5248 | 2 | ChEMBL | 377 | 7 | 2 | 2 | 5.7 | Cc1cccc(C)c1-c1cccc(CNc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/jm3002026 | |||
134132142 | 144957 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -13 | 2 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3909872 | 144957 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -13 | 2 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1021/acsmedchemlett.6b00360 | |||
134132142 | 144957 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -13 | 2 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3909872 | 144957 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -13 | 2 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1016/j.bmcl.2016.10.054 | |||
145971522 | 163211 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 469 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)ccc(OCc2c(C(F)(F)F)nsc2-c2ccc(Cl)cc2)c1C | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4177287 | 163211 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | ChEMBL | 469 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)ccc(OCc2c(C(F)(F)F)nsc2-c2ccc(Cl)cc2)c1C | 10.1021/acsmedchemlett.7b00233 | |||
1599 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -501 | 32 | ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
3955 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -501 | 32 | ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
3955.0 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -501 | 32 | ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
7215 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -501 | 32 | ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
CHEMBL841 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -501 | 32 | ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
DB00836 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -501 | 32 | ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | |||
134142866 | 145730 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -2 | 3 | ChEMBL | 358 | 7 | 1 | 3 | 4.6 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3915765 | 145730 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -2 | 3 | ChEMBL | 358 | 7 | 1 | 3 | 4.6 | O=C(O)CCCOc1ccc(-c2cc(OC(F)(F)F)ccc2F)cc1 | 10.1016/j.bmcl.2016.10.054 | |||
57522038 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
6490 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
CHEMBL2058533 | 3887 | None | 48 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -13 | 3 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1021/jm300215x | |||
137634844 | 156207 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | ChEMBL | 412 | 9 | 1 | 3 | 6.1 | CC(C)Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4063239 | 156207 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | ChEMBL | 412 | 9 | 1 | 3 | 6.1 | CC(C)Cc1cc(CCC(=O)O)ccc1OCc1ccccc1SC(F)(F)F | 10.1016/j.bmcl.2017.01.034 | |||
23136363 | 58850 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -14 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.1 | O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL1688458 | 58850 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -14 | 2 | ChEMBL | 348 | 8 | 1 | 3 | 5.1 | O=C(O)CCc1ccc(OCc2cccc(Oc3ccccc3)c2)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
134141029 | 147255 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -4 | 2 | ChEMBL | 352 | 6 | 1 | 3 | 4.8 | O=C(O)CCc1cc2cc(-c3cc(C(=O)C4CC4)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
CHEMBL3927879 | 147255 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -4 | 2 | ChEMBL | 352 | 6 | 1 | 3 | 4.8 | O=C(O)CCc1cc2cc(-c3cc(C(=O)C4CC4)ccc3F)ccc2o1 | 10.1016/j.bmcl.2016.10.054 | |||
82051616 | 159551 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 12 | 2 | ChEMBL | 304 | 6 | 1 | 2 | 4.2 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4101323 | 159551 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 12 | 2 | ChEMBL | 304 | 6 | 1 | 2 | 4.2 | Cc1cc(CCC(=O)O)ccc1OCc1ccccc1Cl | 10.1016/j.bmcl.2017.01.034 | |||
73777063 | 1154 | None | 36 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
8418 | 1154 | None | 36 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3919973 | 1154 | None | 36 | Human | Functional | pEC50 | = | 7.0 | 7.0 | -4 | 2 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
85472618 | 162404 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 491 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4164509 | 162404 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | ChEMBL | 491 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
137640323 | 157070 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 358 | 7 | 1 | 4 | 4.3 | O=C(O)COc1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4073013 | 157070 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | ChEMBL | 358 | 7 | 1 | 4 | 4.3 | O=C(O)COc1ccc(OCc2ccccc2SC(F)(F)F)cc1 | 10.1016/j.bmcl.2017.01.034 | |||
1692 | 2154 | None | 25 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -338 | 18 | ChEMBL | 411 | 6 | 2 | 4 | 5.5 | CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C | 10.6019/CHEMBL5442687 | |||
5311340 | 2154 | None | 25 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -338 | 18 | ChEMBL | 411 | 6 | 2 | 4 | 5.5 | CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C | 10.6019/CHEMBL5442687 | |||
CHEMBL140979 | 2154 | None | 25 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -338 | 18 | ChEMBL | 411 | 6 | 2 | 4 | 5.5 | CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C | 10.6019/CHEMBL5442687 | |||
233085 | 113086 | None | 38 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -43 | 3 | ChEMBL | 351 | 3 | 1 | 3 | 4.2 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | 10.6019/CHEMBL5442687 | |||
CHEMBL3311302 | 113086 | None | 38 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -43 | 3 | ChEMBL | 351 | 3 | 1 | 3 | 4.2 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | 10.6019/CHEMBL5442687 | |||
28 | 3496 | None | 35 | Human | Functional | pIC50 | = | 5.5 | 5.5 | 1 | 15 | ChEMBL | 486 | 9 | 1 | 7 | 5.2 | COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C | 10.6019/CHEMBL5442687 | |||
3292447 | 3496 | None | 35 | Human | Functional | pIC50 | = | 5.5 | 5.5 | 1 | 15 | ChEMBL | 486 | 9 | 1 | 7 | 5.2 | COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C | 10.6019/CHEMBL5442687 | |||
CHEMBL20963 | 3496 | None | 35 | Human | Functional | pIC50 | = | 5.5 | 5.5 | 1 | 15 | ChEMBL | 486 | 9 | 1 | 7 | 5.2 | COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C | 10.6019/CHEMBL5442687 | |||
5588 | 1861 | None | 0 | Human | Functional | pA2 | = | 5.0 | 5.0 | - | 1 | Guide to Pharmacology | 372 | 9 | 3 | 3 | 6.1 | C/C(=C\Cc1c(O)cc(c(c1O)C(=O)O)C)/CC/C=C(/CCC=C(C)C)\C | 19471906 | |||
9976563 | 1861 | None | 0 | Human | Functional | pA2 | = | 5.0 | 5.0 | - | 1 | Guide to Pharmacology | 372 | 9 | 3 | 3 | 6.1 | C/C(=C\Cc1c(O)cc(c(c1O)C(=O)O)C)/CC/C=C(/CCC=C(C)C)\C | 19471906 | |||
CHEMBL513978 | 1861 | None | 0 | Human | Functional | pA2 | = | 5.0 | 5.0 | - | 1 | Guide to Pharmacology | 372 | 9 | 3 | 3 | 6.1 | C/C(=C\Cc1c(O)cc(c(c1O)C(=O)O)C)/CC/C=C(/CCC=C(C)C)\C | 19471906 | |||
11531145 | 1862 | None | 0 | Human | Functional | pA2 | = | 5.0 | 5.0 | - | 1 | Guide to Pharmacology | 386 | 10 | 2 | 3 | 6.4 | COc1cc(C)c(c(c1C/C=C(/CC/C=C(/CCC=C(C)C)\C)\C)O)C(=O)O | 19471906 | |||
11531145 | 1862 | None | 0 | Human | Functional | pA2 | = | 5.0 | 5.0 | - | 1 | Guide to Pharmacology | 386 | 10 | 2 | 3 | 6.4 | COc1cc(C)c(c(c1C/C=C(/CC/C=C(/CCC=C(C)C)\C)\C)O)C(=O)O | 20685848 | |||
5589 | 1862 | None | 0 | Human | Functional | pA2 | = | 5.0 | 5.0 | - | 1 | Guide to Pharmacology | 386 | 10 | 2 | 3 | 6.4 | COc1cc(C)c(c(c1C/C=C(/CC/C=C(/CCC=C(C)C)\C)\C)O)C(=O)O | 19471906 | |||
5589 | 1862 | None | 0 | Human | Functional | pA2 | = | 5.0 | 5.0 | - | 1 | Guide to Pharmacology | 386 | 10 | 2 | 3 | 6.4 | COc1cc(C)c(c(c1C/C=C(/CC/C=C(/CCC=C(C)C)\C)\C)O)C(=O)O | 20685848 | |||
1054 | 2917 | None | 55 | Human | Functional | pEC50 | = | 8.3 | 8.3 | -1 | 5 | Drug Central | 282 | 15 | 1 | 1 | 6.1 | CCCCCCCC/C=C\CCCCCCCC(=O)O | None | |||
3400 | 2917 | None | 55 | Human | Functional | pEC50 | = | 8.3 | 8.3 | -1 | 5 | Drug Central | 282 | 15 | 1 | 1 | 6.1 | CCCCCCCC/C=C\CCCCCCCC(=O)O | None | |||
445639 | 2917 | None | 55 | Human | Functional | pEC50 | = | 8.3 | 8.3 | -1 | 5 | Drug Central | 282 | 15 | 1 | 1 | 6.1 | CCCCCCCC/C=C\CCCCCCCC(=O)O | None | |||
CHEMBL8659 | 2917 | None | 55 | Human | Functional | pEC50 | = | 8.3 | 8.3 | -1 | 5 | Drug Central | 282 | 15 | 1 | 1 | 6.1 | CCCCCCCC/C=C\CCCCCCCC(=O)O | None | |||
1052 | 2321 | None | 51 | Human | Functional | pEC50 | = | 8.2 | 8.2 | 3 | 4 | Drug Central | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | None | |||
3323 | 2321 | None | 51 | Human | Functional | pEC50 | = | 8.2 | 8.2 | 3 | 4 | Drug Central | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | None | |||
5280450 | 2321 | None | 51 | Human | Functional | pEC50 | = | 8.2 | 8.2 | 3 | 4 | Drug Central | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | None | |||
CHEMBL267476 | 2321 | None | 51 | Human | Functional | pEC50 | = | 8.2 | 8.2 | 3 | 4 | Drug Central | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | None | |||
DB14104 | 2321 | None | 51 | Human | Functional | pEC50 | = | 8.2 | 8.2 | 3 | 4 | Drug Central | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | None | |||
11195 | 3882 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 1 | 2 | Guide to Pharmacology | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 27570890 | |||
86280676 | 3882 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 1 | 2 | Guide to Pharmacology | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 27570890 | |||
CHEMBL3941880 | 3882 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | 1 | 2 | Guide to Pharmacology | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 27570890 | |||
11195 | 3882 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 2 | Guide to Pharmacology | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 27570890 | |||
86280676 | 3882 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 2 | Guide to Pharmacology | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 27570890 | |||
CHEMBL3941880 | 3882 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | -1 | 2 | Guide to Pharmacology | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 27570890 | |||
73777063 | 1154 | None | 36 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -4 | 2 | Guide to Pharmacology | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 24997608 | |||
8418 | 1154 | None | 36 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -4 | 2 | Guide to Pharmacology | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 24997608 | |||
CHEMBL3919973 | 1154 | None | 36 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -4 | 2 | Guide to Pharmacology | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 24997608 | |||
1054 | 2917 | None | 55 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -1 | 5 | Guide to Pharmacology | 282 | 15 | 1 | 1 | 6.1 | CCCCCCCC/C=C\CCCCCCCC(=O)O | 22282525 | |||
3400 | 2917 | None | 55 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -1 | 5 | Guide to Pharmacology | 282 | 15 | 1 | 1 | 6.1 | CCCCCCCC/C=C\CCCCCCCC(=O)O | 22282525 | |||
445639 | 2917 | None | 55 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -1 | 5 | Guide to Pharmacology | 282 | 15 | 1 | 1 | 6.1 | CCCCCCCC/C=C\CCCCCCCC(=O)O | 22282525 | |||
CHEMBL8659 | 2917 | None | 55 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -1 | 5 | Guide to Pharmacology | 282 | 15 | 1 | 1 | 6.1 | CCCCCCCC/C=C\CCCCCCCC(=O)O | 22282525 | |||
1049 | 363 | None | 48 | Rat | Functional | pEC50 | = | 5.1 | 5.1 | -4 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 18320172 | |||
4618 | 363 | None | 48 | Rat | Functional | pEC50 | = | 5.1 | 5.1 | -4 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 18320172 | |||
5280934 | 363 | None | 48 | Rat | Functional | pEC50 | = | 5.1 | 5.1 | -4 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 18320172 | |||
CHEMBL8739 | 363 | None | 48 | Rat | Functional | pEC50 | = | 5.1 | 5.1 | -4 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 18320172 | |||
DB00132 | 363 | None | 48 | Rat | Functional | pEC50 | = | 5.1 | 5.1 | -4 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 18320172 | |||
11005 | 2694 | None | 67 | Human | Functional | pEC50 | = | 5.2 | 5.2 | 1 | 3 | Guide to Pharmacology | 228 | 12 | 1 | 1 | 4.8 | CCCCCCCCCCCCCC(=O)O | 22282525 | |||
2806 | 2694 | None | 67 | Human | Functional | pEC50 | = | 5.2 | 5.2 | 1 | 3 | Guide to Pharmacology | 228 | 12 | 1 | 1 | 4.8 | CCCCCCCCCCCCCC(=O)O | 22282525 | |||
CHEMBL111077 | 2694 | None | 67 | Human | Functional | pEC50 | = | 5.2 | 5.2 | 1 | 3 | Guide to Pharmacology | 228 | 12 | 1 | 1 | 4.8 | CCCCCCCCCCCCCC(=O)O | 22282525 | |||
DB08231 | 2694 | None | 67 | Human | Functional | pEC50 | = | 5.2 | 5.2 | 1 | 3 | Guide to Pharmacology | 228 | 12 | 1 | 1 | 4.8 | CCCCCCCCCCCCCC(=O)O | 22282525 | |||
1050 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | Guide to Pharmacology | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 16702987 | |||
1050 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | Guide to Pharmacology | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 18827341 | |||
11595431 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | Guide to Pharmacology | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 16702987 | |||
11595431 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | Guide to Pharmacology | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 18827341 | |||
CHEMBL207881 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | Guide to Pharmacology | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 16702987 | |||
CHEMBL207881 | 1902 | None | 58 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -26 | 3 | Guide to Pharmacology | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 18827341 | |||
1049 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 22519963 | |||
4618 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 22519963 | |||
5280934 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 22519963 | |||
CHEMBL8739 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 22519963 | |||
DB00132 | 363 | None | 48 | Human | Functional | pEC50 | = | 5.5 | 5.5 | -1 | 3 | Guide to Pharmacology | 278 | 13 | 1 | 1 | 5.7 | CC/C=C\C/C=C\C/C=C\CCCCCCCC(=O)O | 22519963 | |||
1052 | 2321 | None | 51 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 3 | 4 | Guide to Pharmacology | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 16702987 | |||
3323 | 2321 | None | 51 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 3 | 4 | Guide to Pharmacology | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 16702987 | |||
5280450 | 2321 | None | 51 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 3 | 4 | Guide to Pharmacology | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 16702987 | |||
CHEMBL267476 | 2321 | None | 51 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 3 | 4 | Guide to Pharmacology | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 16702987 | |||
DB14104 | 2321 | None | 51 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 3 | 4 | Guide to Pharmacology | 280 | 14 | 1 | 1 | 5.9 | CCCCC/C=C\C/C=C\CCCCCCCC(=O)O | 16702987 | |||
25098573 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 8 | 2 | Guide to Pharmacology | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 19007110 | |||
5587 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 8 | 2 | Guide to Pharmacology | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 19007110 | |||
CHEMBL463785 | 2747 | None | 10 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 8 | 2 | Guide to Pharmacology | 376 | 10 | 1 | 4 | 4.7 | OC(=O)CCCc1ccc(cc1)OCCN(c1ccccn1)c1ccccc1 | 19007110 |
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name |
GPCRdb ID |
Reference ligand |
Vendors |
Species |
Assay Type |
Activity Type |
Activity Relation |
Activity Value |
p-value (-log) |
Fold selectivity |
Tested GPCRs |
Assay Description |
Source |
Mol weight |
Rot Bonds |
H don |
H acc |
LogP |
Smiles |
DOI |
|
134154473 | 152463 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 370 | 6 | 1 | 3 | 5.0 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3970238 | 152463 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | ChEMBL | 370 | 6 | 1 | 3 | 5.0 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
73776979 | 143446 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 419 | 5 | 1 | 3 | 5.9 | O=C(O)CCC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3897637 | 143446 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 419 | 5 | 1 | 3 | 5.9 | O=C(O)CCC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
137638318 | 156826 | None | 0 | Mouse | Binding | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 402 | 4 | 1 | 5 | 4.4 | Cc1ccc(-n2nc(C)c3cnc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4F)cc32)nc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4070359 | 156826 | None | 0 | Mouse | Binding | pEC50 | = | 6 | 6.0 | - | 1 | ChEMBL | 402 | 4 | 1 | 5 | 4.4 | Cc1ccc(-n2nc(C)c3cnc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4F)cc32)nc1 | 10.1021/acs.jmedchem.7b00210 | |||
171351623 | 193594 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 484 | 10 | 2 | 8 | 3.7 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(OC(F)F)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5266523 | 193594 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 484 | 10 | 2 | 8 | 3.7 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(OC(F)F)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
171342834 | 193713 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.1 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(C(F)(F)F)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5269688 | 193713 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.1 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(C(F)(F)F)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
171354496 | 194105 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.1 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3C(F)(F)F)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5278791 | 194105 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.1 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3C(F)(F)F)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
171348900 | 194335 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 466 | 8 | 2 | 7 | 4.3 | Cc1cc(OCc2nc(N)nc(NCC(C)c3cccc(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5283726 | 194335 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | ChEMBL | 466 | 8 | 2 | 7 | 4.3 | Cc1cc(OCc2nc(N)nc(NCC(C)c3cccc(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
127031569 | 139271 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 264 | 4 | 1 | 1 | 3.3 | O=C(O)CCc1ccc(C#CCc2ccccc2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3787580 | 139271 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 264 | 4 | 1 | 1 | 3.3 | O=C(O)CCc1ccc(C#CCc2ccccc2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
145971522 | 163211 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 469 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)ccc(OCc2c(C(F)(F)F)nsc2-c2ccc(Cl)cc2)c1C | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4177287 | 163211 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 469 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)ccc(OCc2c(C(F)(F)F)nsc2-c2ccc(Cl)cc2)c1C | 10.1021/acsmedchemlett.7b00233 | |||
134129938 | 142527 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 414 | 6 | 1 | 4 | 5.0 | COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3890089 | 142527 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | ChEMBL | 414 | 6 | 1 | 4 | 5.0 | COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
156011529 | 177502 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 420 | 7 | 1 | 3 | 6.2 | CCc1cc2cc(C(F)(F)F)cc(COc3ccc(CCC(=O)O)c(C)c3C)c2o1 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4638249 | 177502 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 420 | 7 | 1 | 3 | 6.2 | CCc1cc2cc(C(F)(F)F)cc(COc3ccc(CCC(=O)O)c(C)c3C)c2o1 | 10.1016/j.bmc.2019.115263 | |||
134132142 | 144957 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3909872 | 144957 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1021/acsmedchemlett.6b00360 | |||
73777175 | 143996 | None | 0 | Mouse | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 357 | 3 | 1 | 2 | 4.9 | O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3901994 | 143996 | None | 0 | Mouse | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | ChEMBL | 357 | 3 | 1 | 2 | 4.9 | O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
85472621 | 162898 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4172392 | 162898 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
66562488 | 90405 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 336 | 4 | 1 | 1 | 4.3 | O=C(O)CCc1ccc(C#Cc2cc(F)ccc2C(F)F)cc1F | 10.1021/ml4000673 | |||
CHEMBL2386364 | 90405 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 336 | 4 | 1 | 1 | 4.3 | O=C(O)CCc1ccc(C#Cc2cc(F)ccc2C(F)F)cc1F | 10.1021/ml4000673 | |||
171352188 | 193918 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 492 | 6 | 2 | 7 | 4.9 | Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3C(F)(F)F)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5274344 | 193918 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 492 | 6 | 2 | 7 | 4.9 | Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3C(F)(F)F)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
164888199 | 194467 | None | 2 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 362 | 3 | 0 | 4 | 3.6 | C#Cc1cc(Oc2cccnc2)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL5286838 | 194467 | None | 2 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 362 | 3 | 0 | 4 | 3.6 | C#Cc1cc(Oc2cccnc2)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.0c01002 | |||
73777153 | 142910 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 355 | 3 | 1 | 2 | 5.2 | O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3893026 | 142910 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 355 | 3 | 1 | 2 | 5.2 | O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
171353999 | 194022 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 417 | 6 | 2 | 8 | 4.3 | Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(C(C)C)cc4)n3)ccc12 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5276740 | 194022 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 417 | 6 | 2 | 8 | 4.3 | Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(C(C)C)cc4)n3)ccc12 | 10.1021/acsmedchemlett.2c00160 | |||
171355332 | 194219 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 442 | 6 | 2 | 7 | 4.0 | Cc1ccc(Nc2nc(N)nc(COc3cc(F)cc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5281423 | 194219 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 442 | 6 | 2 | 7 | 4.0 | Cc1ccc(Nc2nc(N)nc(COc3cc(F)cc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
171349936 | 194525 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 482 | 9 | 2 | 8 | 3.9 | COC(CNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1)c1cccc(Cl)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5288340 | 194525 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 482 | 9 | 2 | 8 | 3.9 | COC(CNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1)c1cccc(Cl)c1 | 10.1021/acsmedchemlett.2c00160 | |||
137640163 | 156940 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 372 | 5 | 1 | 5 | 4.4 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(C(C)CC(=O)O)cc3)ncc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4071523 | 156940 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 372 | 5 | 1 | 5 | 4.4 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(C(C)CC(=O)O)cc3)ncc12 | 10.1021/acs.jmedchem.7b00210 | |||
7614387 | 194382 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 389 | 5 | 2 | 8 | 3.5 | Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5284985 | 194382 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 389 | 5 | 2 | 8 | 3.5 | Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1 | 10.1021/acsmedchemlett.2c00160 | |||
11195 | 3882 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
86280676 | 3882 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3941880 | 3882 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
171354782 | 193990 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 462 | 7 | 1 | 3 | 6.9 | OCCCc1c(F)cc(OCc2c(-c3ccc(Cl)cc3)csc2C(F)(F)F)cc1F | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL5275980 | 193990 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 462 | 7 | 1 | 3 | 6.9 | OCCCc1c(F)cc(OCc2c(-c3ccc(Cl)cc3)csc2C(F)(F)F)cc1F | 10.1021/acs.jmedchem.0c01002 | |||
134153222 | 152614 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccncc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3971461 | 152614 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccncc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
171348041 | 194458 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 457 | 5 | 2 | 8 | 4.8 | Cc1c(Cl)cc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5286544 | 194458 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 457 | 5 | 2 | 8 | 4.8 | Cc1c(Cl)cc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
11195 | 3882 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
86280676 | 3882 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3941880 | 3882 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
145955668 | 162520 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 415 | 7 | 1 | 4 | 6.0 | Cc1snc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4166208 | 162520 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 415 | 7 | 1 | 4 | 6.0 | Cc1snc(-c2ccc(Cl)cc2)c1COc1ccc(CCC(=O)O)c(C)c1C | 10.1021/acsmedchemlett.7b00233 | |||
162644046 | 181916 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 361 | 4 | 2 | 5 | 3.0 | Nc1ccc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4778107 | 181916 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 361 | 4 | 2 | 5 | 3.0 | Nc1ccc(NS(=O)(=O)c2ccc([N+](=O)[O-])cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
134146720 | 149219 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 443 | 7 | 1 | 6 | 5.6 | COc1cc(Oc2ncc(C)s2)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3943315 | 149219 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 443 | 7 | 1 | 6 | 5.6 | COc1cc(Oc2ncc(C)s2)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134146958 | 149697 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 388 | 6 | 1 | 3 | 5.1 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cc(F)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3947070 | 149697 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | ChEMBL | 388 | 6 | 1 | 3 | 5.1 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cc(F)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
134147601 | 150116 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 396 | 4 | 1 | 3 | 4.8 | O=C(O)[C@H]1C[C@@H]1[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3950444 | 150116 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 396 | 4 | 1 | 3 | 4.8 | O=C(O)[C@H]1C[C@@H]1[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
90418139 | 162676 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 443 | 7 | 1 | 4 | 5.7 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccccc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4168786 | 162676 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 443 | 7 | 1 | 4 | 5.7 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccccc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
8357996 | 193835 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 403 | 6 | 2 | 8 | 3.8 | CCc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(C)cc4)n3)ccc12 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5272492 | 193835 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 403 | 6 | 2 | 8 | 3.8 | CCc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(C)cc4)n3)ccc12 | 10.1021/acsmedchemlett.2c00160 | |||
90418650 | 157447 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2csnc2-c2ccc(Cl)cc2)c1C | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4077787 | 157447 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 401 | 7 | 1 | 4 | 5.7 | Cc1c(CCC(=O)O)ccc(OCc2csnc2-c2ccc(Cl)cc2)c1C | 10.1021/acsmedchemlett.7b00233 | |||
134132711 | 145026 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 372 | 3 | 0 | 4 | 4.2 | O=S1(=O)c2ccccc2CN1c1cc(Cl)cc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3910333 | 145026 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 372 | 3 | 0 | 4 | 4.2 | O=S1(=O)c2ccccc2CN1c1cc(Cl)cc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
73345869 | 90396 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 321 | 5 | 1 | 2 | 3.7 | N#CCCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
CHEMBL2386355 | 90396 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 321 | 5 | 1 | 2 | 3.7 | N#CCCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
171354164 | 194204 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 442 | 6 | 2 | 7 | 4.0 | Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3F)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5281020 | 194204 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 442 | 6 | 2 | 7 | 4.0 | Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3F)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
134133992 | 143826 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cnc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3900705 | 143826 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cnc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
73777135 | 150458 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 412 | 4 | 1 | 4 | 5.4 | N#Cc1cc(SC(F)(F)F)cc(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3953289 | 150458 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 412 | 4 | 1 | 4 | 5.4 | N#Cc1cc(SC(F)(F)F)cc(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
73777175 | 143996 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 357 | 3 | 1 | 2 | 4.9 | O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3901994 | 143996 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | ChEMBL | 357 | 3 | 1 | 2 | 4.9 | O=C(O)CC1CCC2(CC1)CCN(c1cc(F)cc(Cl)c1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
171348401 | 194489 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 448 | 9 | 2 | 8 | 3.1 | COc1ccccc1CCNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5287358 | 194489 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 448 | 9 | 2 | 8 | 3.1 | COc1ccccc1CCNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1 | 10.1021/acsmedchemlett.2c00160 | |||
171351236 | 194531 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 448 | 9 | 2 | 8 | 3.1 | COc1cccc(CCNc2nc(N)nc(COc3cc(C)cc(N4CCCC4=O)c3)n2)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5288405 | 194531 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | ChEMBL | 448 | 9 | 2 | 8 | 3.1 | COc1cccc(CCNc2nc(N)nc(COc3cc(C)cc(N4CCCC4=O)c3)n2)c1 | 10.1021/acsmedchemlett.2c00160 | |||
90418653 | 137600 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 469 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c1C | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL3754160 | 137600 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | ChEMBL | 469 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c1C | 10.1021/acsmedchemlett.7b00233 | |||
90418278 | 162473 | None | 16 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3F)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4165366 | 162473 | None | 16 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3F)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
171357993 | 194299 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 449 | 6 | 2 | 8 | 3.7 | Cc1ccc(Nc2nc(N)nc(COc3cc(C#N)cc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5283217 | 194299 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 449 | 6 | 2 | 8 | 3.7 | Cc1ccc(Nc2nc(N)nc(COc3cc(C#N)cc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
171352664 | 194070 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 438 | 6 | 2 | 7 | 4.2 | Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCC4=O)c3C)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5277986 | 194070 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 438 | 6 | 2 | 7 | 4.2 | Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCC4=O)c3C)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
25150014 | 3885 | None | 44 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 264 | 3 | 1 | 1 | 3.4 | OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C | 10.1021/ml4000673 | |||
3952 | 3885 | None | 44 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 264 | 3 | 1 | 1 | 3.4 | OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C | 10.1021/ml4000673 | |||
CHEMBL449588 | 3885 | None | 44 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | ChEMBL | 264 | 3 | 1 | 1 | 3.4 | OC(=O)CCc1ccc(cc1)C#Cc1ccccc1C | 10.1021/ml4000673 | |||
171349259 | 193609 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 458 | 6 | 2 | 7 | 4.5 | Cc1ccc(Nc2nc(N)nc(COc3cc(Cl)cc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5266881 | 193609 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 458 | 6 | 2 | 7 | 4.5 | Cc1ccc(Nc2nc(N)nc(COc3cc(Cl)cc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
171358500 | 194625 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 423 | 5 | 2 | 8 | 4.2 | Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5290885 | 194625 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 423 | 5 | 2 | 8 | 4.2 | Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
134151903 | 153445 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 438 | 6 | 1 | 6 | 4.2 | COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3978465 | 153445 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 438 | 6 | 1 | 6 | 4.2 | COc1cc(OC(F)(F)F)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134133797 | 143655 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 338 | 3 | 0 | 4 | 3.6 | O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3899190 | 143655 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 338 | 3 | 0 | 4 | 3.6 | O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
162674347 | 183227 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | Cc1ccc(-c2ccc(F)cc2OCc2ccc(CCC(=O)O)cc2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4794951 | 183227 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | Cc1ccc(-c2ccc(F)cc2OCc2ccc(CCC(=O)O)cc2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
90418651 | 162508 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 469 | 8 | 1 | 4 | 6.6 | CCc1cc(CCC(=O)O)ccc1OCc1c(-c2ccc(Cl)cc2)nsc1C(F)(F)F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4166012 | 162508 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 469 | 8 | 1 | 4 | 6.6 | CCc1cc(CCC(=O)O)ccc1OCc1c(-c2ccc(Cl)cc2)nsc1C(F)(F)F | 10.1021/acsmedchemlett.7b00233 | |||
171349824 | 194568 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 425 | 6 | 2 | 8 | 4.1 | Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C(F)F)cc(=O)oc4c3)n2)cc1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5289099 | 194568 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 425 | 6 | 2 | 8 | 4.1 | Cc1ccc(Nc2nc(N)nc(COc3ccc4c(C(F)F)cc(=O)oc4c3)n2)cc1 | 10.1021/acsmedchemlett.2c00160 | |||
57522038 | 3887 | None | 48 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmcl.2020.127650 | |||
6490 | 3887 | None | 48 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL2058533 | 3887 | None | 48 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 364 | 7 | 1 | 2 | 5.4 | OC(=O)CCc1ccc(cc1)OCc1cc(F)ccc1c1ccc(cc1)C | 10.1016/j.bmcl.2020.127650 | |||
66562385 | 90402 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 282 | 3 | 1 | 1 | 3.6 | Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
CHEMBL2386361 | 90402 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 282 | 3 | 1 | 1 | 3.6 | Cc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
134134229 | 143342 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3896657 | 143342 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1021/acsmedchemlett.6b00360 | |||
134138802 | 148007 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 383 | 4 | 1 | 3 | 4.7 | O=C(O)C1CCN(c2ccc(-c3cc(OC(F)(F)F)ccc3F)cc2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3933619 | 148007 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 383 | 4 | 1 | 3 | 4.7 | O=C(O)C1CCN(c2ccc(-c3cc(OC(F)(F)F)ccc3F)cc2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
134145071 | 150255 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 380 | 3 | 0 | 4 | 4.2 | N#Cc1ccccc1Oc1cc(F)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3951664 | 150255 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 380 | 3 | 0 | 4 | 4.2 | N#Cc1ccccc1Oc1cc(F)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.6b00685 | |||
171354782 | 193990 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 462 | 7 | 1 | 3 | 6.9 | OCCCc1c(F)cc(OCc2c(-c3ccc(Cl)cc3)csc2C(F)(F)F)cc1F | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL5275980 | 193990 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 462 | 7 | 1 | 3 | 6.9 | OCCCc1c(F)cc(OCc2c(-c3ccc(Cl)cc3)csc2C(F)(F)F)cc1F | 10.1021/acs.jmedchem.0c01002 | |||
171357390 | 194099 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 438 | 6 | 2 | 7 | 4.3 | Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5278703 | 194099 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 438 | 6 | 2 | 7 | 4.3 | Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
134152545 | 153566 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 380 | 3 | 0 | 4 | 4.2 | N#Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3979588 | 153566 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | ChEMBL | 380 | 3 | 0 | 4 | 4.2 | N#Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
134154975 | 151489 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 362 | 5 | 1 | 4 | 4.0 | O=S(=O)(Nc1cc(F)cc(Oc2cccnc2)c1)c1ccc(F)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3961620 | 151489 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 362 | 5 | 1 | 4 | 4.0 | O=S(=O)(Nc1cc(F)cc(Oc2cccnc2)c1)c1ccc(F)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
90418513 | 162718 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 429 | 8 | 1 | 4 | 6.2 | CCc1ccc(-c2snc(Cl)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4169436 | 162718 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 429 | 8 | 1 | 4 | 6.2 | CCc1ccc(-c2snc(Cl)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
134155950 | 151179 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 430 | 6 | 1 | 4 | 4.6 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H]([C@@H]3C[C@H]3C(=O)O)O4)c2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3959068 | 151179 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 430 | 6 | 1 | 4 | 4.6 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H]([C@@H]3C[C@H]3C(=O)O)O4)c2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
134155847 | 151191 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 418 | 5 | 1 | 3 | 5.6 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)cc(Cl)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3959144 | 151191 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 418 | 5 | 1 | 3 | 5.6 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)cc(Cl)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
134155480 | 151340 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 384 | 5 | 1 | 3 | 5.0 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3960231 | 151340 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 384 | 5 | 1 | 3 | 5.0 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
137654131 | 159106 | None | 0 | Mouse | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 416 | 5 | 1 | 4 | 5.3 | COc1nn(-c2ccc(C)cc2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)cc(F)c12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4096579 | 159106 | None | 0 | Mouse | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | ChEMBL | 416 | 5 | 1 | 4 | 5.3 | COc1nn(-c2ccc(C)cc2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)cc(F)c12 | 10.1021/acs.jmedchem.7b00210 | |||
134143370 | 145891 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 442 | 7 | 1 | 6 | 4.0 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCc3nnn[nH]3)O4)c2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3916986 | 145891 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 442 | 7 | 1 | 6 | 4.0 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCc3nnn[nH]3)O4)c2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
171358383 | 194614 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 432 | 8 | 2 | 7 | 3.4 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3C)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5290651 | 194614 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 432 | 8 | 2 | 7 | 3.4 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3C)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
127031003 | 139231 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 232 | 3 | 1 | 1 | 2.8 | C/C=C\C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3787072 | 139231 | None | 0 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 232 | 3 | 1 | 1 | 2.8 | C/C=C\C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/acs.jmedchem.5b01962 | |||
8452407 | 180492 | None | 3 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 293 | 4 | 2 | 5 | 2.0 | Nc1ccc(NS(=O)(=O)c2ccccc2)cc1[N+](=O)[O-] | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4751828 | 180492 | None | 3 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | ChEMBL | 293 | 4 | 2 | 5 | 2.0 | Nc1ccc(NS(=O)(=O)c2ccccc2)cc1[N+](=O)[O-] | 10.1016/j.bmcl.2020.127650 | |||
78426052 | 178197 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 489 | 7 | 1 | 4 | 6.4 | Cc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CC(C)C(=O)O)cc2F)c(F)c1 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4647832 | 178197 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | ChEMBL | 489 | 7 | 1 | 4 | 6.4 | Cc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CC(C)C(=O)O)cc2F)c(F)c1 | 10.1016/j.bmc.2019.115263 | |||
171346217 | 194474 | None | 0 | Human | Binding | pEC50 | = | 4.7 | 4.7 | - | 0 | ChEMBL | 438 | 6 | 2 | 7 | 4.2 | Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3C)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5286962 | 194474 | None | 0 | Human | Binding | pEC50 | = | 4.7 | 4.7 | - | 0 | ChEMBL | 438 | 6 | 2 | 7 | 4.2 | Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)ccc3C)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
90418782 | 163178 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 513 | 7 | 1 | 4 | 6.6 | O=C(O)CCc1c(F)c(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4176642 | 163178 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 513 | 7 | 1 | 4 | 6.6 | O=C(O)CCc1c(F)c(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
73777153 | 142910 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 355 | 3 | 1 | 2 | 5.2 | O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3893026 | 142910 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 355 | 3 | 1 | 2 | 5.2 | O=C(O)CC1CCC2(CC1)CCN(c1cc(Cl)cc(Cl)c1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
66562288 | 139096 | None | 0 | Human | Binding | pEC50 | = | 4.7 | 4.7 | - | 0 | ChEMBL | 246 | 3 | 1 | 1 | 3.2 | C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3785637 | 139096 | None | 0 | Human | Binding | pEC50 | = | 4.7 | 4.7 | - | 0 | ChEMBL | 246 | 3 | 1 | 1 | 3.2 | C/C=C(/C)C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/acs.jmedchem.5b01962 | |||
167312323 | 194388 | None | 1 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3cc(Cl)ccc3Cl)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5285139 | 194388 | None | 1 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3cc(Cl)ccc3Cl)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
137633489 | 156691 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 368 | 5 | 1 | 5 | 4.0 | N#Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4068825 | 156691 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 368 | 5 | 1 | 5 | 4.0 | N#Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 | 10.1021/acs.jmedchem.7b00210 | |||
134148110 | 149658 | None | 0 | Human | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3nc(OC4CCC4)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3946820 | 149658 | None | 0 | Human | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3nc(OC4CCC4)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
134134229 | 143342 | None | 0 | Mouse | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3896657 | 143342 | None | 0 | Mouse | Binding | pEC50 | = | 7.7 | 7.7 | - | 0 | ChEMBL | 368 | 5 | 1 | 3 | 5.2 | O=C(O)CCc1cc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2o1 | 10.1021/acsmedchemlett.6b00360 | |||
90418753 | 162491 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 463 | 8 | 1 | 4 | 6.6 | CCc1ccc(-c2nsc(C(F)(F)F)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4165803 | 162491 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 463 | 8 | 1 | 4 | 6.6 | CCc1ccc(-c2nsc(C(F)(F)F)c2COc2ccc(CCC(=O)O)c(C)c2C)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
73776997 | 154369 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 407 | 4 | 1 | 4 | 4.5 | O=C(O)CC1CCC2(CCN(c3cc(OC(F)(F)F)ccc3Cl)CC2)OC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3986483 | 154369 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 407 | 4 | 1 | 4 | 4.5 | O=C(O)CC1CCC2(CCN(c3cc(OC(F)(F)F)ccc3Cl)CC2)OC1 | 10.1021/acsmedchemlett.6b00360 | |||
16777240 | 179885 | None | 1 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 330 | 3 | 2 | 3 | 3.4 | Cc1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4744629 | 179885 | None | 1 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 330 | 3 | 2 | 3 | 3.4 | Cc1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
171354494 | 194104 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 508 | 7 | 2 | 8 | 4.8 | Cc1ccc(Nc2nc(N)nc(COc3cc(OC(F)(F)F)cc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5278789 | 194104 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 508 | 7 | 2 | 8 | 4.8 | Cc1ccc(Nc2nc(N)nc(COc3cc(OC(F)(F)F)cc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
156016724 | 177822 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 378 | 7 | 1 | 3 | 5.5 | O=C(O)[C@H]1C[C@@H]1CCC12CCC(c3cccc(Oc4ccccc4)c3)(CC1)O2 | 10.1016/j.ejmech.2018.04.061 | |||
CHEMBL4642294 | 177822 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 378 | 7 | 1 | 3 | 5.5 | O=C(O)[C@H]1C[C@@H]1CCC12CCC(c3cccc(Oc4ccccc4)c3)(CC1)O2 | 10.1016/j.ejmech.2018.04.061 | |||
156016724 | 177822 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 378 | 7 | 1 | 3 | 5.5 | O=C(O)[C@H]1C[C@@H]1CCC12CCC(c3cccc(Oc4ccccc4)c3)(CC1)O2 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4642294 | 177822 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | ChEMBL | 378 | 7 | 1 | 3 | 5.5 | O=C(O)[C@H]1C[C@@H]1CCC12CCC(c3cccc(Oc4ccccc4)c3)(CC1)O2 | 10.1016/j.bmc.2019.115263 | |||
73777111 | 149798 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 373 | 3 | 1 | 2 | 5.1 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3947837 | 149798 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | ChEMBL | 373 | 3 | 1 | 2 | 5.1 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
134153546 | 152670 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ncc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3971857 | 152670 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.4 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)ncc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
137633536 | 156386 | None | 0 | Rat | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4065397 | 156386 | None | 0 | Rat | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | |||
134145778 | 149435 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 355 | 3 | 0 | 3 | 4.3 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccccc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3945213 | 149435 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 355 | 3 | 0 | 3 | 4.3 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2ccccc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
134156727 | 153723 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | ChEMBL | 419 | 7 | 1 | 5 | 4.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)n2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3980898 | 153723 | None | 0 | Human | Binding | pEC50 | = | 7.6 | 7.6 | - | 0 | ChEMBL | 419 | 7 | 1 | 5 | 4.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)n2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
137650498 | 157414 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 382 | 5 | 1 | 5 | 4.3 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3C#N)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4077353 | 157414 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 382 | 5 | 1 | 5 | 4.3 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3C#N)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
134134846 | 144327 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 337 | 3 | 0 | 3 | 4.2 | O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3904654 | 144327 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 337 | 3 | 0 | 3 | 4.2 | O=S1(=O)c2ccccc2CN1c1cccc(Oc2ccccc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
137641818 | 158299 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 373 | 6 | 1 | 5 | 4.1 | COc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4087992 | 158299 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 373 | 6 | 1 | 5 | 4.1 | COc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
73777085 | 153319 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 351 | 4 | 1 | 3 | 4.6 | COc1ccc(Cl)c(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3977361 | 153319 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 351 | 4 | 1 | 3 | 4.6 | COc1ccc(Cl)c(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
171346891 | 194387 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)cc3Cl)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5285104 | 194387 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)cc3Cl)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
137651638 | 157313 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.8 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4076190 | 157313 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.8 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
137646368 | 158120 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 358 | 5 | 1 | 5 | 3.8 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ncc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4085695 | 158120 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 358 | 5 | 1 | 5 | 3.8 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ncc12 | 10.1021/acs.jmedchem.7b00210 | |||
134154953 | 151365 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3960369 | 151365 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
66562289 | 139106 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | - | 0 | ChEMBL | 246 | 3 | 1 | 1 | 3.2 | C/C=C(\C)C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3785764 | 139106 | None | 0 | Human | Binding | pEC50 | = | 4.6 | 4.6 | - | 0 | ChEMBL | 246 | 3 | 1 | 1 | 3.2 | C/C=C(\C)C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/acs.jmedchem.5b01962 | |||
134153067 | 152345 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1ccccc1Oc1cc(F)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3969073 | 152345 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1ccccc1Oc1cc(F)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.6b00685 | |||
78425909 | 177779 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 398 | 8 | 1 | 3 | 6.1 | O=C(O)CCC12CCC(OCc3cc(F)cc(Oc4ccccc4)c3)(CC1)CC2 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4641735 | 177779 | None | 0 | Human | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | ChEMBL | 398 | 8 | 1 | 3 | 6.1 | O=C(O)CCC12CCC(OCc3cc(F)cc(Oc4ccccc4)c3)(CC1)CC2 | 10.1016/j.bmc.2019.115263 | |||
117873187 | 152433 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC1CC2(CCC1CC(=O)O)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3969920 | 152433 | None | 0 | Human | Binding | pEC50 | = | 5.6 | 5.6 | - | 0 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC1CC2(CCC1CC(=O)O)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
73777156 | 152804 | None | 0 | Mouse | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 396 | 4 | 1 | 4 | 4.7 | N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3973034 | 152804 | None | 0 | Mouse | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 396 | 4 | 1 | 4 | 4.7 | N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
171350458 | 193622 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 436 | 8 | 2 | 7 | 3.3 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(F)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5267225 | 193622 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 436 | 8 | 2 | 7 | 3.3 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(F)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
837245 | 10602 | None | 37 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 315 | 3 | 1 | 2 | 3.8 | Cc1ccc(S(=O)(=O)Nc2cccc(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL1170012 | 10602 | None | 37 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 315 | 3 | 1 | 2 | 3.8 | Cc1ccc(S(=O)(=O)Nc2cccc(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
73356514 | 90409 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 404 | 8 | 1 | 4 | 2.8 | CS(=O)(=O)CCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
CHEMBL2386368 | 90409 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 404 | 8 | 1 | 4 | 2.8 | CS(=O)(=O)CCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
73345870 | 90410 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 404 | 8 | 1 | 4 | 2.8 | CS(=O)(=O)CCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
CHEMBL2386369 | 90410 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 404 | 8 | 1 | 4 | 2.8 | CS(=O)(=O)CCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
73354950 | 90412 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 418 | 9 | 1 | 4 | 3.2 | CS(=O)(=O)CCCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
CHEMBL2386370 | 90412 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 418 | 9 | 1 | 4 | 3.2 | CS(=O)(=O)CCCOCc1ccccc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
73348895 | 90413 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 418 | 9 | 1 | 4 | 3.2 | CS(=O)(=O)CCCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
CHEMBL2386371 | 90413 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 418 | 9 | 1 | 4 | 3.2 | CS(=O)(=O)CCCOCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
171343639 | 193687 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 452 | 8 | 2 | 7 | 3.8 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3Cl)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5268800 | 193687 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 452 | 8 | 2 | 7 | 3.8 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3Cl)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
73777111 | 149798 | None | 0 | Mouse | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 373 | 3 | 1 | 2 | 5.1 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3947837 | 149798 | None | 0 | Mouse | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 373 | 3 | 1 | 2 | 5.1 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
171358819 | 194593 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 458 | 6 | 2 | 7 | 4.5 | Cc1ccc(Nc2nc(N)nc(COc3ccc(Cl)c(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5289929 | 194593 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 458 | 6 | 2 | 7 | 4.5 | Cc1ccc(Nc2nc(N)nc(COc3ccc(Cl)c(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
156635006 | 179646 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 400 | 4 | 2 | 4 | 4.0 | Nc1ccc(NS(=O)(=O)c2ccc(OC(F)(F)F)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4741544 | 179646 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 400 | 4 | 2 | 4 | 4.0 | Nc1ccc(NS(=O)(=O)c2ccc(OC(F)(F)F)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
117886639 | 148538 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 391 | 3 | 1 | 3 | 5.3 | CC1(C)Cc2cc(Cl)cc(N3CCC4(CCC(CC(=O)O)CC4)CC3)c2O1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3937916 | 148538 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 391 | 3 | 1 | 3 | 5.3 | CC1(C)Cc2cc(Cl)cc(N3CCC4(CCC(CC(=O)O)CC4)CC3)c2O1 | 10.1021/acsmedchemlett.6b00360 | |||
171344695 | 193701 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 454 | 7 | 2 | 8 | 3.9 | COc1ccc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc1N1CCCC1=O | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5269158 | 193701 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 454 | 7 | 2 | 8 | 3.9 | COc1ccc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc1N1CCCC1=O | 10.1021/acsmedchemlett.2c00160 | |||
66562392 | 90406 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 336 | 3 | 1 | 1 | 4.6 | O=C(O)CCc1ccc(C#Cc2cc(Cl)cc(Cl)c2)cc1F | 10.1021/ml4000673 | |||
CHEMBL2386365 | 90406 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 336 | 3 | 1 | 1 | 4.6 | O=C(O)CCc1ccc(C#Cc2cc(Cl)cc(Cl)c2)cc1F | 10.1021/ml4000673 | |||
134138281 | 147874 | None | 0 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | ChEMBL | 410 | 7 | 1 | 6 | 3.9 | COc1cc(OC2CC2)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3932664 | 147874 | None | 0 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | ChEMBL | 410 | 7 | 1 | 6 | 3.9 | COc1cc(OC2CC2)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134138802 | 148007 | None | 0 | Mouse | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 383 | 4 | 1 | 3 | 4.7 | O=C(O)C1CCN(c2ccc(-c3cc(OC(F)(F)F)ccc3F)cc2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3933619 | 148007 | None | 0 | Mouse | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 383 | 4 | 1 | 3 | 4.7 | O=C(O)C1CCN(c2ccc(-c3cc(OC(F)(F)F)ccc3F)cc2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
134153986 | 152595 | None | 0 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | ChEMBL | 396 | 4 | 1 | 3 | 4.8 | O=C(O)[C@@H]1C[C@H]1[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3971308 | 152595 | None | 0 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | ChEMBL | 396 | 4 | 1 | 3 | 4.8 | O=C(O)[C@@H]1C[C@H]1[C@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
117886649 | 152167 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 391 | 4 | 1 | 3 | 5.4 | OCCC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3967504 | 152167 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 391 | 4 | 1 | 3 | 5.4 | OCCC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
171347514 | 194479 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 418 | 8 | 2 | 7 | 3.1 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5287009 | 194479 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 418 | 8 | 2 | 7 | 3.1 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
118184919 | 162968 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 468 | 7 | 1 | 5 | 5.6 | N#Cc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4173280 | 162968 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | ChEMBL | 468 | 7 | 1 | 5 | 5.6 | N#Cc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
127030344 | 139232 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 242 | 3 | 1 | 1 | 3.2 | O=C(O)CCc1ccc(C#CC2CCCC2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3787110 | 139232 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 242 | 3 | 1 | 1 | 3.2 | O=C(O)CCc1ccc(C#CC2CCCC2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
127031002 | 139174 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 232 | 3 | 1 | 1 | 2.8 | C/C=C/C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3786526 | 139174 | None | 0 | Human | Binding | pEC50 | = | 4.5 | 4.5 | - | 0 | ChEMBL | 232 | 3 | 1 | 1 | 2.8 | C/C=C/C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/acs.jmedchem.5b01962 | |||
134132142 | 144957 | None | 0 | Mouse | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3909872 | 144957 | None | 0 | Mouse | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | ChEMBL | 402 | 7 | 1 | 3 | 5.8 | Cc1cc(-c2cc(OC(F)(F)F)ccc2Cl)cc(C)c1OCCCC(=O)O | 10.1021/acsmedchemlett.6b00360 | |||
1050 | 1902 | None | 58 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 2 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1021/acs.jmedchem.0c01002 | |||
11595431 | 1902 | None | 58 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 2 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL207881 | 1902 | None | 58 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 2 | ChEMBL | 347 | 8 | 2 | 3 | 5.1 | OC(=O)CCc1ccc(cc1)NCc1cccc(c1)Oc1ccccc1 | 10.1021/acs.jmedchem.0c01002 | |||
674995 | 143091 | None | 9 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 343 | 5 | 1 | 3 | 4.4 | O=S(=O)(Nc1ccc(Oc2ccccc2)cc1)c1ccc(F)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3894632 | 143091 | None | 9 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 343 | 5 | 1 | 3 | 4.4 | O=S(=O)(Nc1ccc(Oc2ccccc2)cc1)c1ccc(F)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
162672256 | 182978 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 346 | 4 | 2 | 4 | 3.1 | COc1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4791789 | 182978 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | ChEMBL | 346 | 4 | 2 | 4 | 3.1 | COc1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
171355610 | 194097 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 443 | 5 | 2 | 8 | 4.5 | Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(Cl)c(Cl)c4)n3)ccc12 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5278642 | 194097 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 443 | 5 | 2 | 8 | 4.5 | Cc1cc(=O)oc2cc(OCc3nc(N)nc(Nc4ccc(Cl)c(Cl)c4)n3)ccc12 | 10.1021/acsmedchemlett.2c00160 | |||
137648938 | 157504 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 382 | 4 | 1 | 3 | 5.5 | Cc1ccc(-n2nc(C)c3ccc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4078553 | 157504 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 382 | 4 | 1 | 3 | 5.5 | Cc1ccc(-n2nc(C)c3ccc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
73777156 | 152804 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 396 | 4 | 1 | 4 | 4.7 | N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3973034 | 152804 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 396 | 4 | 1 | 4 | 4.7 | N#Cc1ccc(OC(F)(F)F)cc1N1CCC2(CCC(CC(=O)O)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
171345288 | 194304 | None | 0 | Human | Binding | pEC50 | = | 4.4 | 4.4 | - | 0 | ChEMBL | 502 | 9 | 2 | 8 | 4.0 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3OC(F)(F)F)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5283269 | 194304 | None | 0 | Human | Binding | pEC50 | = | 4.4 | 4.4 | - | 0 | ChEMBL | 502 | 9 | 2 | 8 | 4.0 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3OC(F)(F)F)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
71655293 | 90395 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 307 | 4 | 1 | 2 | 3.3 | N#CCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
CHEMBL2386354 | 90395 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 307 | 4 | 1 | 2 | 3.3 | N#CCc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
71655227 | 90403 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 282 | 3 | 1 | 1 | 3.6 | Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
CHEMBL2386362 | 90403 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 282 | 3 | 1 | 1 | 3.6 | Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
134147107 | 149964 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 417 | 3 | 1 | 3 | 5.5 | O=C(O)C1CC12CCC1(CCN(c3cc(OC(F)(F)F)ccc3Cl)CC1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3949142 | 149964 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 417 | 3 | 1 | 3 | 5.5 | O=C(O)C1CC12CCC1(CCN(c3cc(OC(F)(F)F)ccc3Cl)CC1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
156635004 | 179818 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 344 | 4 | 2 | 3 | 3.7 | CCc1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4743951 | 179818 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 344 | 4 | 2 | 3 | 3.7 | CCc1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
162674533 | 183571 | None | 0 | Human | Binding | pEC50 | = | 4.4 | 4.4 | - | 0 | ChEMBL | 372 | 3 | 2 | 3 | 4.4 | CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4799103 | 183571 | None | 0 | Human | Binding | pEC50 | = | 4.4 | 4.4 | - | 0 | ChEMBL | 372 | 3 | 2 | 3 | 4.4 | CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc(N)c(C(F)(F)F)c2)cc1 | 10.1016/j.bmcl.2020.127650 | |||
134144000 | 150297 | None | 0 | Mouse | Binding | pEC50 | = | 8.3 | 8.3 | - | 0 | ChEMBL | 431 | 8 | 1 | 6 | 4.0 | COc1cc(O[C@H]2C[C@H](OC)C2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3952043 | 150297 | None | 0 | Mouse | Binding | pEC50 | = | 8.3 | 8.3 | - | 0 | ChEMBL | 431 | 8 | 1 | 6 | 4.0 | COc1cc(O[C@H]2C[C@H](OC)C2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134132711 | 145026 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | ChEMBL | 372 | 3 | 0 | 4 | 4.2 | O=S1(=O)c2ccccc2CN1c1cc(Cl)cc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3910333 | 145026 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | ChEMBL | 372 | 3 | 0 | 4 | 4.2 | O=S1(=O)c2ccccc2CN1c1cc(Cl)cc(Oc2ccccn2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
171352518 | 193895 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 466 | 8 | 2 | 7 | 4.1 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)c(C)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5273939 | 193895 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 466 | 8 | 2 | 7 | 4.1 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)c(C)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
137660172 | 159206 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 357 | 5 | 1 | 4 | 4.4 | C[C@@H](Cc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1)C(=O)O | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4097652 | 159206 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 357 | 5 | 1 | 4 | 4.4 | C[C@@H](Cc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1)C(=O)O | 10.1021/acs.jmedchem.7b00210 | |||
117886639 | 148538 | None | 0 | Mouse | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 391 | 3 | 1 | 3 | 5.3 | CC1(C)Cc2cc(Cl)cc(N3CCC4(CCC(CC(=O)O)CC4)CC3)c2O1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3937916 | 148538 | None | 0 | Mouse | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 391 | 3 | 1 | 3 | 5.3 | CC1(C)Cc2cc(Cl)cc(N3CCC4(CCC(CC(=O)O)CC4)CC3)c2O1 | 10.1021/acsmedchemlett.6b00360 | |||
127033352 | 139107 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 272 | 8 | 1 | 1 | 4.4 | CCCCCCCC#Cc1ccc(CCC(=O)O)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3785789 | 139107 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 272 | 8 | 1 | 1 | 4.4 | CCCCCCCC#Cc1ccc(CCC(=O)O)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
137658977 | 159197 | None | 0 | Mouse | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 385 | 5 | 1 | 5 | 4.3 | COc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4097537 | 159197 | None | 0 | Mouse | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 385 | 5 | 1 | 5 | 4.3 | COc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
137649363 | 157488 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 385 | 5 | 1 | 4 | 5.0 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CC(C)(C)C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4078374 | 157488 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 385 | 5 | 1 | 4 | 5.0 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CC(C)(C)C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
134146386 | 148995 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | ChEMBL | 384 | 5 | 1 | 3 | 5.0 | O=C(O)CC[C@@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3941726 | 148995 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | ChEMBL | 384 | 5 | 1 | 3 | 5.0 | O=C(O)CC[C@@H]1CCc2cc(-c3cc(OC(F)(F)F)ccc3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
73777174 | 150542 | None | 0 | Mouse | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 356 | 3 | 1 | 3 | 4.4 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccn1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3954140 | 150542 | None | 0 | Mouse | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 356 | 3 | 1 | 3 | 4.4 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccn1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
90442039 | 163004 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 509 | 7 | 1 | 4 | 7.1 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)cc1C(F)(F)F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4173940 | 163004 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 509 | 7 | 1 | 4 | 7.1 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)cc1C(F)(F)F | 10.1021/acsmedchemlett.7b00233 | |||
134132951 | 144710 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | ChEMBL | 454 | 8 | 1 | 7 | 3.9 | COc1cc(O[C@H]2C[C@H](OC)C2)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3907996 | 144710 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | ChEMBL | 454 | 8 | 1 | 7 | 3.9 | COc1cc(O[C@H]2C[C@H](OC)C2)cc(-c2ccc3c(c2)CC[C@H](CCc2nnn[nH]2)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
137652399 | 157587 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 357 | 5 | 1 | 4 | 4.4 | C[C@H](Cc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1)C(=O)O | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4079621 | 157587 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 357 | 5 | 1 | 4 | 4.4 | C[C@H](Cc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1)C(=O)O | 10.1021/acs.jmedchem.7b00210 | |||
46892131 | 144759 | None | 3 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3908362 | 144759 | None | 3 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | O=S1(=O)c2ccccc2CN1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
134138099 | 147910 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3932897 | 147910 | None | 0 | Human | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | ChEMBL | 369 | 3 | 0 | 3 | 4.6 | Cc1ccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
7614420 | 194588 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 375 | 5 | 2 | 8 | 3.2 | Cc1ccc(Nc2nc(N)nc(COc3ccc4ccc(=O)oc4c3)n2)cc1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5289774 | 194588 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 375 | 5 | 2 | 8 | 3.2 | Cc1ccc(Nc2nc(N)nc(COc3ccc4ccc(=O)oc4c3)n2)cc1 | 10.1021/acsmedchemlett.2c00160 | |||
73507535 | 177569 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | ChEMBL | 391 | 6 | 1 | 3 | 5.5 | O=C(O)CCC1CCC2(CCN(c3cc(OC4CCC4)ccc3Cl)CC2)C1 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4639009 | 177569 | None | 0 | Human | Binding | pEC50 | = | 7.4 | 7.4 | - | 0 | ChEMBL | 391 | 6 | 1 | 3 | 5.5 | O=C(O)CCC1CCC2(CCN(c3cc(OC4CCC4)ccc3Cl)CC2)C1 | 10.1016/j.bmc.2019.115263 | |||
73777065 | 147344 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC(C(=O)O)C1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3928591 | 147344 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC(C(=O)O)C1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
137642248 | 158245 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 357 | 5 | 1 | 4 | 4.4 | Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4087308 | 158245 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 357 | 5 | 1 | 4 | 4.4 | Cc1cc(-c2ccc(CCC(=O)O)cc2)cc2c1cnn2-c1ccccn1 | 10.1021/acs.jmedchem.7b00210 | |||
137643731 | 158478 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 361 | 5 | 1 | 4 | 4.2 | O=C(O)CCc1ccc(-c2cc(F)c3cnn(-c4ccccn4)c3c2)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4089919 | 158478 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 361 | 5 | 1 | 4 | 4.2 | O=C(O)CCc1ccc(-c2cc(F)c3cnn(-c4ccccn4)c3c2)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
137658977 | 159197 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 385 | 5 | 1 | 5 | 4.3 | COc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4097537 | 159197 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 385 | 5 | 1 | 5 | 4.3 | COc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
73777069 | 142756 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 389 | 4 | 1 | 3 | 5.0 | O=C(O)CC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3891920 | 142756 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 389 | 4 | 1 | 3 | 5.0 | O=C(O)CC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
11195 | 3882 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
86280676 | 3882 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3941880 | 3882 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 356 | 3 | 0 | 4 | 3.7 | Fc1cc(Oc2ccccn2)cc(c1)N1Cc2c(S1(=O)=O)cccc2 | 10.1021/acs.jmedchem.6b00685 | |||
67072752 | 86563 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 289 | 4 | 1 | 2 | 3.2 | N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 | 10.1021/jm301470a | |||
CHEMBL2315528 | 86563 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 1 | ChEMBL | 289 | 4 | 1 | 2 | 3.2 | N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 | 10.1021/jm301470a | |||
127033353 | 139238 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 278 | 5 | 1 | 1 | 3.7 | O=C(O)CCc1ccc(C#CCCc2ccccc2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3787151 | 139238 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 278 | 5 | 1 | 1 | 3.7 | O=C(O)CCc1ccc(C#CCCc2ccccc2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
73777135 | 150458 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 412 | 4 | 1 | 4 | 5.4 | N#Cc1cc(SC(F)(F)F)cc(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3953289 | 150458 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 412 | 4 | 1 | 4 | 5.4 | N#Cc1cc(SC(F)(F)F)cc(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
137632610 | 156437 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 368 | 5 | 1 | 5 | 4.0 | N#Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4065890 | 156437 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 368 | 5 | 1 | 5 | 4.0 | N#Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
743974 | 113090 | None | 54 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3311308 | 113090 | None | 54 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
162673626 | 183299 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 350 | 3 | 2 | 3 | 3.7 | Nc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4795755 | 183299 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 350 | 3 | 2 | 3 | 3.7 | Nc1ccc(NS(=O)(=O)c2ccc(Cl)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
134144000 | 150297 | None | 0 | Human | Binding | pEC50 | = | 8.3 | 8.3 | - | 0 | ChEMBL | 431 | 8 | 1 | 6 | 4.0 | COc1cc(O[C@H]2C[C@H](OC)C2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3952043 | 150297 | None | 0 | Human | Binding | pEC50 | = | 8.3 | 8.3 | - | 0 | ChEMBL | 431 | 8 | 1 | 6 | 4.0 | COc1cc(O[C@H]2C[C@H](OC)C2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
164888199 | 194467 | None | 2 | Human | Binding | pEC50 | = | 8.3 | 8.3 | - | 0 | ChEMBL | 362 | 3 | 0 | 4 | 3.6 | C#Cc1cc(Oc2cccnc2)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL5286838 | 194467 | None | 2 | Human | Binding | pEC50 | = | 8.3 | 8.3 | - | 0 | ChEMBL | 362 | 3 | 0 | 4 | 3.6 | C#Cc1cc(Oc2cccnc2)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.0c01002 | |||
134154415 | 152783 | None | 0 | Human | Binding | pEC50 | = | 8.3 | 8.3 | - | 0 | ChEMBL | 447 | 6 | 1 | 5 | 6.3 | Cc1cnc(Oc2cc(Cl)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)c2)s1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3972870 | 152783 | None | 0 | Human | Binding | pEC50 | = | 8.3 | 8.3 | - | 0 | ChEMBL | 447 | 6 | 1 | 5 | 6.3 | Cc1cnc(Oc2cc(Cl)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)c2)s1 | 10.1021/acsmedchemlett.6b00394 | |||
118679768 | 177725 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 390 | 9 | 1 | 2 | 6.4 | O=C(O)CCCc1ccc(OCC2=C(c3ccc(C4CC4)cc3)CCCC2)cc1 | 10.1016/j.ejmech.2018.04.061 | |||
CHEMBL4641038 | 177725 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 390 | 9 | 1 | 2 | 6.4 | O=C(O)CCCc1ccc(OCC2=C(c3ccc(C4CC4)cc3)CCCC2)cc1 | 10.1016/j.ejmech.2018.04.061 | |||
118679768 | 177725 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 390 | 9 | 1 | 2 | 6.4 | O=C(O)CCCc1ccc(OCC2=C(c3ccc(C4CC4)cc3)CCCC2)cc1 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4641038 | 177725 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 390 | 9 | 1 | 2 | 6.4 | O=C(O)CCCc1ccc(OCC2=C(c3ccc(C4CC4)cc3)CCCC2)cc1 | 10.1016/j.bmc.2019.115263 | |||
118679768 | 177725 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 390 | 9 | 1 | 2 | 6.4 | O=C(O)CCCc1ccc(OCC2=C(c3ccc(C4CC4)cc3)CCCC2)cc1 | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL4641038 | 177725 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 390 | 9 | 1 | 2 | 6.4 | O=C(O)CCCc1ccc(OCC2=C(c3ccc(C4CC4)cc3)CCCC2)cc1 | 10.1021/acs.jmedchem.0c01002 | |||
118679791 | 193824 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 364 | 8 | 1 | 2 | 5.8 | Cc1ccc(C2=C(COc3ccc(CCCC(=O)O)cc3)CCCC2)cc1 | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL5272316 | 193824 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 364 | 8 | 1 | 2 | 5.8 | Cc1ccc(C2=C(COc3ccc(CCCC(=O)O)cc3)CCCC2)cc1 | 10.1021/acs.jmedchem.0c01002 | |||
118679744 | 194430 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 404 | 8 | 1 | 2 | 6.4 | O=C(O)CCCc1ccc(OCC2=C(c3ccc4c(c3)CCCC4)CCCC2)cc1 | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL5285896 | 194430 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 404 | 8 | 1 | 2 | 6.4 | O=C(O)CCCc1ccc(OCC2=C(c3ccc4c(c3)CCCC4)CCCC2)cc1 | 10.1021/acs.jmedchem.0c01002 | |||
171342776 | 193659 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 454 | 8 | 2 | 7 | 3.4 | Cc1cc(OCc2nc(N)nc(NCCc3cc(F)ccc3F)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5268182 | 193659 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 454 | 8 | 2 | 7 | 3.4 | Cc1cc(OCc2nc(N)nc(NCCc3cc(F)ccc3F)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
46908122 | 151659 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 334 | 3 | 0 | 4 | 3.8 | O=C1c2ccccc2C(=O)N1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3963275 | 151659 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 334 | 3 | 0 | 4 | 3.8 | O=C1c2ccccc2C(=O)N1c1cc(F)cc(Oc2cccnc2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
162676836 | 183609 | None | 0 | Human | Binding | pEC50 | = | 4.3 | 4.3 | - | 0 | ChEMBL | 332 | 3 | 3 | 4 | 2.8 | Nc1ccc(NS(=O)(=O)c2ccc(O)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4799668 | 183609 | None | 0 | Human | Binding | pEC50 | = | 4.3 | 4.3 | - | 0 | ChEMBL | 332 | 3 | 3 | 4 | 2.8 | Nc1ccc(NS(=O)(=O)c2ccc(O)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
90418476 | 162881 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 511 | 7 | 1 | 4 | 6.7 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C(F)(F)F)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4172136 | 162881 | None | 0 | Human | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | ChEMBL | 511 | 7 | 1 | 4 | 6.7 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(C(F)(F)F)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
137645249 | 157703 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 403 | 5 | 1 | 5 | 4.4 | COc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)cc(F)c12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4080998 | 157703 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 403 | 5 | 1 | 5 | 4.4 | COc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)cc(F)c12 | 10.1021/acs.jmedchem.7b00210 | |||
137648938 | 157504 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 382 | 4 | 1 | 3 | 5.5 | Cc1ccc(-n2nc(C)c3ccc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4078553 | 157504 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 382 | 4 | 1 | 3 | 5.5 | Cc1ccc(-n2nc(C)c3ccc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
156635003 | 181042 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 394 | 3 | 2 | 3 | 3.9 | Nc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4758125 | 181042 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 394 | 3 | 2 | 3 | 3.9 | Nc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
137657813 | 159868 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 400 | 4 | 1 | 3 | 5.6 | Cc1ccc(-n2nc(C)c3c(F)cc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4105241 | 159868 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 400 | 4 | 1 | 3 | 5.6 | Cc1ccc(-n2nc(C)c3c(F)cc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
134147328 | 150137 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 394 | 4 | 0 | 4 | 4.4 | N#CCc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3950610 | 150137 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 394 | 4 | 0 | 4 | 4.4 | N#CCc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
162649435 | 180146 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 288 | 6 | 1 | 2 | 3.7 | Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4747554 | 180146 | None | 0 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 288 | 6 | 1 | 2 | 3.7 | Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 | 10.1016/j.bmcl.2020.127650 | |||
73777085 | 153319 | None | 0 | Mouse | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 351 | 4 | 1 | 3 | 4.6 | COc1ccc(Cl)c(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3977361 | 153319 | None | 0 | Mouse | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 351 | 4 | 1 | 3 | 4.6 | COc1ccc(Cl)c(N2CCC3(CCC(CC(=O)O)CC3)CC2)c1 | 10.1021/acsmedchemlett.6b00360 | |||
171347136 | 194333 | None | 0 | Human | Binding | pEC50 | = | 4.3 | 4.3 | - | 0 | ChEMBL | 482 | 9 | 2 | 8 | 3.8 | COc1ccc(Cl)cc1CCNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5283683 | 194333 | None | 0 | Human | Binding | pEC50 | = | 4.3 | 4.3 | - | 0 | ChEMBL | 482 | 9 | 2 | 8 | 3.8 | COc1ccc(Cl)cc1CCNc1nc(N)nc(COc2cc(C)cc(N3CCCC3=O)c2)n1 | 10.1021/acsmedchemlett.2c00160 | |||
2843133 | 147735 | None | 42 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 307 | 6 | 1 | 2 | 4.0 | CCCCc1ccc(NS(=O)(=O)c2ccc(F)cc2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3931570 | 147735 | None | 42 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | ChEMBL | 307 | 6 | 1 | 2 | 4.0 | CCCCc1ccc(NS(=O)(=O)c2ccc(F)cc2)cc1 | 10.1021/acs.jmedchem.6b00685 | |||
73777063 | 1154 | None | 36 | Mouse | Binding | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
8418 | 1154 | None | 36 | Mouse | Binding | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3919973 | 1154 | None | 36 | Mouse | Binding | pEC50 | = | 7.3 | 7.3 | - | 1 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
137657813 | 159868 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 400 | 4 | 1 | 3 | 5.6 | Cc1ccc(-n2nc(C)c3c(F)cc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4105241 | 159868 | None | 0 | Mouse | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 400 | 4 | 1 | 3 | 5.6 | Cc1ccc(-n2nc(C)c3c(F)cc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
171354473 | 194088 | None | 0 | Human | Binding | pEC50 | = | 4.3 | 4.3 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)c(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5278391 | 194088 | None | 0 | Human | Binding | pEC50 | = | 4.3 | 4.3 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(Cl)c(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
171346828 | 193862 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 437 | 6 | 2 | 8 | 4.4 | CCc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5273250 | 193862 | None | 0 | Human | Binding | pEC50 | = | 6.3 | 6.3 | - | 0 | ChEMBL | 437 | 6 | 2 | 8 | 4.4 | CCc1ccc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
134141650 | 146787 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 380 | 3 | 0 | 4 | 4.2 | N#Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
CHEMBL3923955 | 146787 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 380 | 3 | 0 | 4 | 4.2 | N#Cc1cccc(Oc2cc(F)cc(N3Cc4ccccc4S3(=O)=O)c2)c1 | 10.1021/acs.jmedchem.6b00685 | |||
66562390 | 90399 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 268 | 3 | 1 | 1 | 3.2 | O=C(O)CCc1ccc(C#Cc2ccccc2)c(F)c1 | 10.1021/ml4000673 | |||
CHEMBL2386358 | 90399 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 268 | 3 | 1 | 1 | 3.2 | O=C(O)CCc1ccc(C#Cc2ccccc2)c(F)c1 | 10.1021/ml4000673 | |||
162645828 | 179769 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 352 | 6 | 1 | 2 | 4.2 | O=C(O)CCc1ccc(COc2cc(F)ccc2Br)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4743323 | 179769 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 352 | 6 | 1 | 2 | 4.2 | O=C(O)CCc1ccc(COc2cc(F)ccc2Br)cc1 | 10.1016/j.bmcl.2020.127650 | |||
73776995 | 148830 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC1CC(CC(=O)O)CCC12CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3940359 | 148830 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 419 | 4 | 1 | 3 | 5.7 | CC1CC(CC(=O)O)CCC12CCN(c1cc(OC(F)(F)F)ccc1Cl)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
171357825 | 194101 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 424 | 6 | 2 | 7 | 3.9 | Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5278718 | 194101 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 424 | 6 | 2 | 7 | 3.9 | Cc1ccc(Nc2nc(N)nc(COc3cccc(N4CCCC4=O)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
90118275 | 177485 | None | 0 | Human | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | ChEMBL | 377 | 9 | 1 | 4 | 4.8 | O=C(O)CCc1ccc(OCc2cccc(SCC3CC3)n2)c(Cl)c1 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4637969 | 177485 | None | 0 | Human | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | ChEMBL | 377 | 9 | 1 | 4 | 4.8 | O=C(O)CCc1ccc(OCc2cccc(SCC3CC3)n2)c(Cl)c1 | 10.1016/j.bmc.2019.115263 | |||
156021563 | 178130 | None | 0 | Human | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | ChEMBL | 534 | 12 | 1 | 6 | 6.2 | COc1ccc(F)c(-c2ncc(COc3ccc([C@@H](CC(=O)O)C4CC4)cc3)nc2OCCC(F)(F)F)c1 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4646784 | 178130 | None | 0 | Human | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | ChEMBL | 534 | 12 | 1 | 6 | 6.2 | COc1ccc(F)c(-c2ncc(COc3ccc([C@@H](CC(=O)O)C4CC4)cc3)nc2OCCC(F)(F)F)c1 | 10.1016/j.bmc.2019.115263 | |||
134155067 | 151395 | None | 0 | Human | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | ChEMBL | 401 | 7 | 1 | 5 | 4.4 | COc1cc(OC2CCC2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3960738 | 151395 | None | 0 | Human | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | ChEMBL | 401 | 7 | 1 | 5 | 4.4 | COc1cc(OC2CCC2)nc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134156727 | 153723 | None | 0 | Mouse | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | ChEMBL | 419 | 7 | 1 | 5 | 4.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)n2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3980898 | 153723 | None | 0 | Mouse | Binding | pEC50 | = | 8.2 | 8.2 | - | 0 | ChEMBL | 419 | 7 | 1 | 5 | 4.1 | CO[C@H]1C[C@H](Oc2cc(F)c(F)c(-c3ccc4c(c3)CC[C@H](CCC(=O)O)O4)n2)C1 | 10.1021/acsmedchemlett.6b00394 | |||
164888199 | 194467 | None | 2 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 362 | 3 | 0 | 4 | 3.6 | C#Cc1cc(Oc2cccnc2)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.0c01002 | |||
CHEMBL5286838 | 194467 | None | 2 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 362 | 3 | 0 | 4 | 3.6 | C#Cc1cc(Oc2cccnc2)cc(N2Cc3ccccc3S2(=O)=O)c1 | 10.1021/acs.jmedchem.0c01002 | |||
171342623 | 193668 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 438 | 6 | 2 | 7 | 4.2 | Cc1cc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5268316 | 193668 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 438 | 6 | 2 | 7 | 4.2 | Cc1cc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
171342052 | 193672 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 423 | 5 | 2 | 8 | 4.2 | Cc1cc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)ccc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5268389 | 193672 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 423 | 5 | 2 | 8 | 4.2 | Cc1cc(Nc2nc(N)nc(COc3ccc4c(C)cc(=O)oc4c3)n2)ccc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
171346998 | 194496 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 454 | 7 | 2 | 8 | 3.9 | COc1cc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5287642 | 194496 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 454 | 7 | 2 | 8 | 3.9 | COc1cc(OCc2nc(N)nc(Nc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
137651358 | 157235 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 375 | 5 | 1 | 4 | 4.6 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3F)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4075162 | 157235 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 375 | 5 | 1 | 4 | 4.6 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3F)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
171355983 | 194108 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 452 | 8 | 2 | 7 | 3.8 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5278836 | 194108 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 452 | 8 | 2 | 7 | 3.8 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
162656082 | 180808 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 299 | 6 | 1 | 3 | 3.3 | N#Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4755578 | 180808 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 299 | 6 | 1 | 3 | 3.3 | N#Cc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 | 10.1016/j.bmcl.2020.127650 | |||
90405673 | 178115 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 489 | 7 | 1 | 3 | 6.0 | OCCCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Br)cc2)c(F)c1 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4646553 | 178115 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 489 | 7 | 1 | 3 | 6.0 | OCCCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Br)cc2)c(F)c1 | 10.1016/j.bmc.2019.115263 | |||
90417978 | 162078 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 477 | 7 | 1 | 4 | 6.4 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4159180 | 162078 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 477 | 7 | 1 | 4 | 6.4 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
137645249 | 157703 | None | 0 | Mouse | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 403 | 5 | 1 | 5 | 4.4 | COc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)cc(F)c12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4080998 | 157703 | None | 0 | Mouse | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 403 | 5 | 1 | 5 | 4.4 | COc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)cc(F)c12 | 10.1021/acs.jmedchem.7b00210 | |||
743974 | 113090 | None | 54 | Mouse | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311308 | 113090 | None | 54 | Mouse | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 305 | 4 | 1 | 3 | 3.4 | COc1ccc(S(=O)(=O)Nc2c(C)cc(C)cc2C)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
81762207 | 182853 | None | 1 | Human | Binding | pEC50 | = | 4.2 | 4.2 | - | 0 | ChEMBL | 266 | 3 | 2 | 3 | 2.2 | Nc1ccc(NS(=O)(=O)c2ccccc2)cc1F | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4790052 | 182853 | None | 1 | Human | Binding | pEC50 | = | 4.2 | 4.2 | - | 0 | ChEMBL | 266 | 3 | 2 | 3 | 2.2 | Nc1ccc(NS(=O)(=O)c2ccccc2)cc1F | 10.1016/j.bmcl.2020.127650 | |||
171350799 | 193579 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 480 | 6 | 2 | 7 | 5.2 | Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)cc(C(C)(C)C)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5266170 | 193579 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 480 | 6 | 2 | 7 | 5.2 | Cc1ccc(Nc2nc(N)nc(COc3cc(N4CCCC4=O)cc(C(C)(C)C)c3)n2)cc1Cl | 10.1021/acsmedchemlett.2c00160 | |||
137649555 | 157422 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 357 | 5 | 1 | 4 | 4.4 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4077507 | 157422 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 357 | 5 | 1 | 4 | 4.4 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
137656733 | 159678 | None | 0 | Mouse | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 383 | 4 | 1 | 4 | 4.9 | Cc1ccc(-n2nc(C)c3cnc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4102951 | 159678 | None | 0 | Mouse | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 383 | 4 | 1 | 4 | 4.9 | Cc1ccc(-n2nc(C)c3cnc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
66562388 | 90408 | None | 0 | Human | Binding | pEC50 | = | 4.2 | 4.2 | - | 0 | ChEMBL | 360 | 5 | 1 | 3 | 2.8 | CS(=O)(=O)Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
CHEMBL2386367 | 90408 | None | 0 | Human | Binding | pEC50 | = | 4.2 | 4.2 | - | 0 | ChEMBL | 360 | 5 | 1 | 3 | 2.8 | CS(=O)(=O)Cc1cccc(C#Cc2ccc(CCC(=O)O)c(F)c2)c1 | 10.1021/ml4000673 | |||
73777063 | 1154 | None | 36 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
8418 | 1154 | None | 36 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3919973 | 1154 | None | 36 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 1 | ChEMBL | 405 | 4 | 1 | 3 | 5.5 | OC(=O)CC1CCC2(CC1)CCN(CC2)c1cc(ccc1Cl)OC(F)(F)F | 10.1021/acsmedchemlett.6b00360 | |||
85470884 | 164099 | None | 3 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
CHEMBL4208325 | 164099 | None | 3 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 459 | 7 | 1 | 3 | 6.0 | O=C(O)CCc1cc(F)c(OCc2c(C(F)(F)F)ccn2-c2ccc(Cl)cc2)c(F)c1 | 10.1016/j.bmcl.2018.02.013 | |||
137637713 | 155946 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 369 | 4 | 1 | 4 | 4.6 | Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4060171 | 155946 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 369 | 4 | 1 | 4 | 4.6 | Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
134133355 | 143623 | None | 0 | Human | Binding | pEC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 413 | 6 | 1 | 5 | 4.2 | COc1cc(OC2CCC2)nc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3898962 | 143623 | None | 0 | Human | Binding | pEC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 413 | 6 | 1 | 5 | 4.2 | COc1cc(OC2CCC2)nc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
137633536 | 156386 | None | 0 | Mouse | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | |||
CHEMBL4065397 | 156386 | None | 0 | Mouse | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 368 | 7 | 1 | 3 | 4.6 | COc1ccc(C(F)(F)F)cc1COc1ccc(CCC(=O)O)cc1C | 10.1016/j.bmcl.2017.01.034 | |||
73777069 | 142756 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 389 | 4 | 1 | 3 | 5.0 | O=C(O)CC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3891920 | 142756 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 389 | 4 | 1 | 3 | 5.0 | O=C(O)CC1CCC2(CC1)CCN(c1cc(OC(F)(F)F)ccc1F)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
171349741 | 193599 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3cc(Cl)cc(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5266730 | 193599 | None | 0 | Human | Binding | pEC50 | = | 5.2 | 5.2 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3cc(Cl)cc(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
85472618 | 162404 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 491 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4164509 | 162404 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 491 | 7 | 1 | 4 | 6.7 | Cc1c(CCC(=O)O)cc(F)c(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
156016929 | 177830 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 540 | 7 | 1 | 7 | 5.3 | COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)C4CC(=O)O)cc3)C(C)C2)c(Cl)cn1 | 10.1016/j.bmc.2019.115263 | |||
CHEMBL4642324 | 177830 | None | 0 | Human | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | ChEMBL | 540 | 7 | 1 | 7 | 5.3 | COc1cc(N2CCC(Oc3ccc(N4N=C(C(F)(F)F)[C@@H](C)C4CC(=O)O)cc3)C(C)C2)c(Cl)cn1 | 10.1016/j.bmc.2019.115263 | |||
137659366 | 159525 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 391 | 5 | 1 | 4 | 5.1 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3Cl)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4101071 | 159525 | None | 0 | Human | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | ChEMBL | 391 | 5 | 1 | 4 | 5.1 | Cc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3Cl)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
137638317 | 156814 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 387 | 6 | 1 | 5 | 4.4 | COc1cc(CCC(=O)O)ccc1-c1ccc2c(C)nn(-c3ccccn3)c2c1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4070273 | 156814 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 387 | 6 | 1 | 5 | 4.4 | COc1cc(CCC(=O)O)ccc1-c1ccc2c(C)nn(-c3ccccn3)c2c1 | 10.1021/acs.jmedchem.7b00210 | |||
171351058 | 193644 | None | 0 | Human | Binding | pEC50 | = | 4.1 | 4.1 | - | 0 | ChEMBL | 446 | 8 | 2 | 7 | 3.7 | Cc1cc(OCc2nc(N)nc(NCCc3c(C)cccc3C)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5267671 | 193644 | None | 0 | Human | Binding | pEC50 | = | 4.1 | 4.1 | - | 0 | ChEMBL | 446 | 8 | 2 | 7 | 3.7 | Cc1cc(OCc2nc(N)nc(NCCc3c(C)cccc3C)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
137638318 | 156826 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 402 | 4 | 1 | 5 | 4.4 | Cc1ccc(-n2nc(C)c3cnc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4F)cc32)nc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4070359 | 156826 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 402 | 4 | 1 | 5 | 4.4 | Cc1ccc(-n2nc(C)c3cnc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4F)cc32)nc1 | 10.1021/acs.jmedchem.7b00210 | |||
127031001 | 139220 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 242 | 3 | 1 | 1 | 3.4 | CC(C)=C(C)C#Cc1ccc(CCC(=O)O)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3786972 | 139220 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 242 | 3 | 1 | 1 | 3.4 | CC(C)=C(C)C#Cc1ccc(CCC(=O)O)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
137651153 | 157296 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.7 | CCc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4076004 | 157296 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 371 | 6 | 1 | 4 | 4.7 | CCc1nn(-c2ccccn2)c2cc(-c3ccc(CCC(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
67072752 | 86563 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 289 | 4 | 1 | 2 | 3.2 | N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 | 10.1021/ml4000673 | |||
CHEMBL2315528 | 86563 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 1 | ChEMBL | 289 | 4 | 1 | 2 | 3.2 | N#CCc1ccccc1C#Cc1ccc(CCC(=O)O)cc1 | 10.1021/ml4000673 | |||
137654131 | 159106 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 416 | 5 | 1 | 4 | 5.3 | COc1nn(-c2ccc(C)cc2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)cc(F)c12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4096579 | 159106 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 416 | 5 | 1 | 4 | 5.3 | COc1nn(-c2ccc(C)cc2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)cc(F)c12 | 10.1021/acs.jmedchem.7b00210 | |||
134131620 | 142519 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 442 | 7 | 1 | 5 | 4.5 | COc1cc(O[C@H]2C[C@H](OC)C2)cc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3890035 | 142519 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 442 | 7 | 1 | 5 | 4.5 | COc1cc(O[C@H]2C[C@H](OC)C2)cc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
66562286 | 90400 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 268 | 3 | 1 | 1 | 3.2 | O=C(O)CCc1ccc(C#Cc2ccccc2)cc1F | 10.1021/ml4000673 | |||
CHEMBL2386359 | 90400 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 268 | 3 | 1 | 1 | 3.2 | O=C(O)CCc1ccc(C#Cc2ccccc2)cc1F | 10.1021/ml4000673 | |||
134153298 | 152455 | None | 0 | Human | Binding | pEC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 412 | 6 | 1 | 4 | 4.8 | COc1cc(OC2CCC2)cc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3970166 | 152455 | None | 0 | Human | Binding | pEC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 412 | 6 | 1 | 4 | 4.8 | COc1cc(OC2CCC2)cc(-c2ccc3c(c2)CC[C@H]([C@@H]2C[C@H]2C(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
134131874 | 144945 | None | 0 | Human | Binding | pEC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 404 | 6 | 1 | 3 | 5.6 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cc(Cl)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3909773 | 144945 | None | 0 | Human | Binding | pEC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 404 | 6 | 1 | 3 | 5.6 | O=C(O)CC[C@H]1CCc2cc(-c3cc(OC4CCC4)cc(Cl)c3F)ccc2O1 | 10.1021/acsmedchemlett.6b00394 | |||
171349686 | 194572 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 466 | 8 | 2 | 7 | 4.1 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5289306 | 194572 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 466 | 8 | 2 | 7 | 4.1 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(C)c(Cl)c3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
171350316 | 193632 | None | 0 | Human | Binding | pEC50 | = | 4.1 | 4.1 | - | 0 | ChEMBL | 503 | 9 | 2 | 9 | 3.0 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3N3CCOCC3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5267354 | 193632 | None | 0 | Human | Binding | pEC50 | = | 4.1 | 4.1 | - | 0 | ChEMBL | 503 | 9 | 2 | 9 | 3.0 | Cc1cc(OCc2nc(N)nc(NCCc3ccccc3N3CCOCC3)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
85472227 | 162282 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 519 | 7 | 1 | 4 | 6.8 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(Br)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4162566 | 162282 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 519 | 7 | 1 | 4 | 6.8 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(Br)c1 | 10.1021/acsmedchemlett.7b00233 | |||
66562389 | 90401 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 286 | 3 | 1 | 1 | 3.4 | O=C(O)CCc1c(F)cc(C#Cc2ccccc2)cc1F | 10.1021/ml4000673 | |||
CHEMBL2386360 | 90401 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 286 | 3 | 1 | 1 | 3.4 | O=C(O)CCc1c(F)cc(C#Cc2ccccc2)cc1F | 10.1021/ml4000673 | |||
134156455 | 154410 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 394 | 6 | 1 | 5 | 4.3 | Fc1ccc(OC2CCC2)cc1-c1ccc2c(c1)CC[C@H](CCc1nnn[nH]1)O2 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3986721 | 154410 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 394 | 6 | 1 | 5 | 4.3 | Fc1ccc(OC2CCC2)cc1-c1ccc2c(c1)CC[C@H](CCc1nnn[nH]1)O2 | 10.1021/acsmedchemlett.6b00394 | |||
137637713 | 155946 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 369 | 4 | 1 | 4 | 4.6 | Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4060171 | 155946 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 369 | 4 | 1 | 4 | 4.6 | Cc1nn(-c2ccccn2)c2cc(-c3ccc([C@H]4C[C@@H]4C(=O)O)cc3)ccc12 | 10.1021/acs.jmedchem.7b00210 | |||
25149901 | 186792 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 250 | 3 | 1 | 1 | 3.1 | O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 | 10.1021/ml4000673 | |||
CHEMBL488384 | 186792 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 250 | 3 | 1 | 1 | 3.1 | O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 | 10.1021/ml4000673 | |||
25149901 | 186792 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 250 | 3 | 1 | 1 | 3.1 | O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL488384 | 186792 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 250 | 3 | 1 | 1 | 3.1 | O=C(O)CCc1ccc(C#Cc2ccccc2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
85472225 | 162856 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4171724 | 162856 | None | 0 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 495 | 7 | 1 | 4 | 6.5 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(Cl)c(F)c3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
16775835 | 180269 | None | 1 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 316 | 3 | 2 | 3 | 3.1 | Nc1ccc(NS(=O)(=O)c2ccccc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4748982 | 180269 | None | 1 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 316 | 3 | 2 | 3 | 3.1 | Nc1ccc(NS(=O)(=O)c2ccccc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
134152336 | 153545 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 408 | 5 | 1 | 5 | 4.2 | Fc1ccc(OC(F)(F)F)cc1-c1ccc2c(c1)CC[C@H](CCc1nnn[nH]1)O2 | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3979448 | 153545 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 408 | 5 | 1 | 5 | 4.2 | Fc1ccc(OC(F)(F)F)cc1-c1ccc2c(c1)CC[C@H](CCc1nnn[nH]1)O2 | 10.1021/acsmedchemlett.6b00394 | |||
16770747 | 182277 | None | 1 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 334 | 3 | 2 | 3 | 3.2 | Nc1ccc(NS(=O)(=O)c2ccc(F)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4782622 | 182277 | None | 1 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 334 | 3 | 2 | 3 | 3.2 | Nc1ccc(NS(=O)(=O)c2ccc(F)cc2)cc1C(F)(F)F | 10.1016/j.bmcl.2020.127650 | |||
134145700 | 148839 | None | 0 | Human | Binding | pEC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 400 | 7 | 1 | 4 | 5.0 | COc1cc(OC2CCC2)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
CHEMBL3940429 | 148839 | None | 0 | Human | Binding | pEC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 400 | 7 | 1 | 4 | 5.0 | COc1cc(OC2CCC2)cc(-c2ccc3c(c2)CC[C@H](CCC(=O)O)O3)c1F | 10.1021/acsmedchemlett.6b00394 | |||
137656733 | 159678 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 383 | 4 | 1 | 4 | 4.9 | Cc1ccc(-n2nc(C)c3cnc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4102951 | 159678 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | - | 0 | ChEMBL | 383 | 4 | 1 | 4 | 4.9 | Cc1ccc(-n2nc(C)c3cnc(-c4ccc([C@H]5C[C@@H]5C(=O)O)cc4)cc32)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
171352230 | 193970 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 454 | 8 | 2 | 7 | 3.4 | Cc1cc(OCc2nc(N)nc(NCCc3c(F)cccc3F)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5275546 | 193970 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 454 | 8 | 2 | 7 | 3.4 | Cc1cc(OCc2nc(N)nc(NCCc3c(F)cccc3F)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
171356095 | 194253 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(Cl)c3Cl)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5282108 | 194253 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | ChEMBL | 486 | 8 | 2 | 7 | 4.4 | Cc1cc(OCc2nc(N)nc(NCCc3cccc(Cl)c3Cl)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
90418333 | 162750 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 473 | 8 | 1 | 5 | 5.7 | COc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4169851 | 162750 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 473 | 8 | 1 | 5 | 5.7 | COc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
71655226 | 90398 | None | 0 | Human | Binding | pEC50 | = | 4.0 | 4.0 | - | 0 | ChEMBL | 251 | 3 | 1 | 2 | 2.5 | O=C(O)CCc1ccc(C#Cc2ccccc2)nc1 | 10.1021/ml4000673 | |||
CHEMBL2386357 | 90398 | None | 0 | Human | Binding | pEC50 | = | 4.0 | 4.0 | - | 0 | ChEMBL | 251 | 3 | 1 | 2 | 2.5 | O=C(O)CCc1ccc(C#Cc2ccccc2)nc1 | 10.1021/ml4000673 | |||
73777174 | 150542 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 356 | 3 | 1 | 3 | 4.4 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccn1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3954140 | 150542 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 356 | 3 | 1 | 3 | 4.4 | O=C(O)CC1CCC2(CC1)CCN(c1cc(C(F)(F)F)ccn1)CC2 | 10.1021/acsmedchemlett.6b00360 | |||
171346166 | 194419 | None | 0 | Human | Binding | pEC50 | = | 4.0 | 4.0 | - | 0 | ChEMBL | 446 | 8 | 2 | 7 | 3.7 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(C)cc3C)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
CHEMBL5285725 | 194419 | None | 0 | Human | Binding | pEC50 | = | 4.0 | 4.0 | - | 0 | ChEMBL | 446 | 8 | 2 | 7 | 3.7 | Cc1cc(OCc2nc(N)nc(NCCc3ccc(C)cc3C)n2)cc(N2CCCC2=O)c1 | 10.1021/acsmedchemlett.2c00160 | |||
6483 | 3886 | None | 39 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 2 | ChEMBL | 307 | 4 | 1 | 2 | 3.3 | N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O | 10.1021/ml4000673 | |||
66553168 | 3886 | None | 39 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 2 | ChEMBL | 307 | 4 | 1 | 2 | 3.3 | N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O | 10.1021/ml4000673 | |||
CHEMBL2386353 | 3886 | None | 39 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 2 | ChEMBL | 307 | 4 | 1 | 2 | 3.3 | N#CCc1ccccc1C#Cc1ccc(c(c1)F)CCC(=O)O | 10.1021/ml4000673 | |||
66562386 | 90404 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 307 | 3 | 1 | 2 | 3.4 | Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
CHEMBL2386363 | 90404 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 307 | 3 | 1 | 2 | 3.4 | Cc1ccc(C#N)cc1C#Cc1ccc(CCC(=O)O)c(F)c1 | 10.1021/ml4000673 | |||
127033020 | 139163 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 256 | 3 | 1 | 1 | 3.6 | O=C(O)CCc1ccc(C#CC2CCCCC2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
CHEMBL3786418 | 139163 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 256 | 3 | 1 | 1 | 3.6 | O=C(O)CCc1ccc(C#CC2CCCCC2)cc1 | 10.1021/acs.jmedchem.5b01962 | |||
162652317 | 180427 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 304 | 7 | 1 | 3 | 3.4 | COc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4751137 | 180427 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 304 | 7 | 1 | 3 | 3.4 | COc1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 | 10.1016/j.bmcl.2020.127650 | |||
162672935 | 183308 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 332 | 7 | 1 | 4 | 3.2 | COC(=O)c1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 | 10.1016/j.bmcl.2020.127650 | |||
CHEMBL4795858 | 183308 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | ChEMBL | 332 | 7 | 1 | 4 | 3.2 | COC(=O)c1ccc(F)cc1OCc1ccc(CCC(=O)O)cc1 | 10.1016/j.bmcl.2020.127650 | |||
85472359 | 162223 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 471 | 8 | 1 | 4 | 6.3 | CCc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4161536 | 162223 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 471 | 8 | 1 | 4 | 6.3 | CCc1ccc(-c2nsc(C(F)(F)F)c2COc2c(F)cc(CCC(=O)O)cc2F)cc1 | 10.1021/acsmedchemlett.7b00233 | |||
85472487 | 162572 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 477 | 7 | 1 | 4 | 6.4 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4167097 | 162572 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | ChEMBL | 477 | 7 | 1 | 4 | 6.4 | O=C(O)CCc1ccc(OCc2c(-c3ccc(Cl)cc3)nsc2C(F)(F)F)c(F)c1F | 10.1021/acsmedchemlett.7b00233 | |||
145960576 | 162246 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 527 | 8 | 1 | 5 | 6.6 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(OC(F)(F)F)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
CHEMBL4161929 | 162246 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | ChEMBL | 527 | 8 | 1 | 5 | 6.6 | O=C(O)CCc1cc(F)c(OCc2c(-c3ccc(OC(F)(F)F)cc3)nsc2C(F)(F)F)c(F)c1 | 10.1021/acsmedchemlett.7b00233 | |||
137637243 | 155979 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 343 | 5 | 1 | 4 | 4.1 | O=C(O)CCc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
CHEMBL4060517 | 155979 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 343 | 5 | 1 | 4 | 4.1 | O=C(O)CCc1ccc(-c2ccc3cnn(-c4ccccn4)c3c2)cc1 | 10.1021/acs.jmedchem.7b00210 | |||
134135468 | 144563 | None | 0 | Mouse | Binding | pEC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 389 | 4 | 1 | 3 | 4.8 | O=C(O)C1CCC(C2CCN(c3cc(OC(F)(F)F)ccc3F)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
CHEMBL3906716 | 144563 | None | 0 | Mouse | Binding | pEC50 | = | 6 | 6.0 | - | 0 | ChEMBL | 389 | 4 | 1 | 3 | 4.8 | O=C(O)C1CCC(C2CCN(c3cc(OC(F)(F)F)ccc3F)CC2)CC1 | 10.1021/acsmedchemlett.6b00360 | |||
233085 | 113086 | None | 38 | Mouse | Binding | pIC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 351 | 3 | 1 | 3 | 4.2 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311302 | 113086 | None | 38 | Mouse | Binding | pIC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 351 | 3 | 1 | 3 | 4.2 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
233085 | 113086 | None | 38 | Rat | Binding | pIC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 351 | 3 | 1 | 3 | 4.2 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311302 | 113086 | None | 38 | Rat | Binding | pIC50 | = | 8.1 | 8.1 | - | 0 | ChEMBL | 351 | 3 | 1 | 3 | 4.2 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
233085 | 113086 | None | 38 | Human | Binding | pIC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 351 | 3 | 1 | 3 | 4.2 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | 10.1016/j.bmcl.2014.05.012 | |||
CHEMBL3311302 | 113086 | None | 38 | Human | Binding | pIC50 | = | 7.1 | 7.1 | - | 0 | ChEMBL | 351 | 3 | 1 | 3 | 4.2 | Cc1ccc(S(=O)(=O)NC2c3ccccc3Oc3ccccc32)cc1 | 10.1016/j.bmcl.2014.05.012 |