Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

145971909 164700 0 None 11 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 411 11 2 6 4.8 CCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4217198 164700 0 None 11 3 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 411 11 2 6 4.8 CCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
66978356 163708 0 None 10 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4204996 163708 0 None 10 3 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
127027876 139476 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 4.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3794302 139476 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 4.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
145978309 163752 0 None 27 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 429 12 2 6 4.8 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCCCF 10.1016/j.bmc.2017.11.035
CHEMBL4205480 163752 0 None 27 3 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 429 12 2 6 4.8 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCCCF 10.1016/j.bmc.2017.11.035
127029692 139404 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 423 5 2 6 4.1 Cc1cc(OC[C@H]2[C@@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793515 139404 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 423 5 2 6 4.1 Cc1cc(OC[C@H]2[C@@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
11855868 152544 0 None 24 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 152544 0 None 24 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855865 153277 0 None 35 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 153277 0 None 35 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
127026955 139450 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 5 2 6 4.4 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794016 139450 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 5 2 6 4.4 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl 10.1016/j.bmcl.2016.03.110
1883 3082 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
1916 3082 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
5280360 3082 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
913 3082 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
CHEMBL548 3082 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
DB00917 3082 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
18376258 195902 0 None - 1 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 465 9 1 3 5.4 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559065 195902 0 None - 1 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 465 9 1 3 5.4 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
127026956 139426 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cc(Cl)c(Cl)cc3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793862 139426 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cc(Cl)c(Cl)cc3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
126495400 139321 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3792632 139321 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
1929 1605 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
9890801 1605 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
CHEMBL563646 1605 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
DB12022 1605 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
67082748 164363 0 None 9 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 451 10 2 6 5.0 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCC(F)(F)F 10.1016/j.bmc.2017.11.035
CHEMBL4212770 164363 0 None 9 3 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 451 10 2 6 5.0 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CCC(F)(F)F 10.1016/j.bmc.2017.11.035
15979081 163840 0 None 5 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCCC(C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4206444 163840 0 None 5 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCCC(C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
127051063 140322 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806284 140322 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 10.1021/acsmedchemlett.5b00455
127027877 139419 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 443 5 2 6 4.4 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793802 139419 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 443 5 2 6 4.4 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3)O2)n1 10.1016/j.bmcl.2016.03.110
16725337 149601 0 None 4 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 149601 0 None 4 4 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11294085 137252 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmc.2017.11.035
CHEMBL3751951 137252 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmc.2017.11.035
127028169 139490 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 6 2 6 4.4 CCc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794466 139490 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 6 2 6 4.4 CCc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
118352160 139429 0 None 7079 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 423 5 2 6 4.1 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793892 139429 0 None 7079 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 423 5 2 6 4.1 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
127027874 139363 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793045 139363 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
127027874 139363 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3793045 139363 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
127051656 140294 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(OC(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805981 140294 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(OC(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
89443871 151445 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 8 2 4 5.5 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(C)ccc(OCC(=O)O)c1C nan
CHEMBL3961932 151445 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 8 2 4 5.5 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(C)ccc(OCC(=O)O)c1C nan
89443827 144113 0 None - 1 Human 9.0 pEC50 = 9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 395 7 3 4 4.9 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(O)cc(-c2cccc(F)c2)c1 nan
CHEMBL3903635 144113 0 None - 1 Human 9.0 pEC50 = 9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 395 7 3 4 4.9 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(O)cc(-c2cccc(F)c2)c1 nan
18376082 194923 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 472 9 1 5 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2nccs2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL541517 194923 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 472 9 1 5 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2nccs2)cc1 10.1016/j.bmcl.2009.01.059
145977227 164007 0 None -1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4208379 164007 0 None -1 4 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
10315 2926 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
44230575 2926 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
CHEMBL3707245 2926 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
126495463 140307 0 None 69 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 6 2 6 3.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806130 140307 0 None 69 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 6 2 6 3.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
11502897 142793 0 None 43 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 142793 0 None 43 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855870 146280 0 None 467 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 146280 0 None 467 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855868 152544 0 None 24 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 152544 0 None 24 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855865 153277 0 None 35 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 153277 0 None 35 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
44230722 171729 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 489 10 2 7 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4467099 171729 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 489 10 2 7 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
11855868 152544 0 None 24 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 152544 0 None 24 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
127026953 139499 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 439 6 2 7 3.8 COc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794585 139499 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 439 6 2 7 3.8 COc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
1883 3082 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
1916 3082 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
5280360 3082 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
913 3082 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
CHEMBL548 3082 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
DB00917 3082 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
126495398 140211 0 None 416 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 403 7 2 6 3.9 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805044 140211 0 None 416 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 403 7 2 6 3.9 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
89443586 145685 0 None - 1 Human 8.0 pEC50 = 8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3916133 145685 0 None - 1 Human 8.0 pEC50 = 8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
118517489 143691 0 None -18 3 Human 8.0 pEC50 = 8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 143691 0 None -18 3 Human 8.0 pEC50 = 8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
92135977 152896 0 None -141 4 Human 8.0 pEC50 = 8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 152896 0 None -141 4 Human 8.0 pEC50 = 8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
8541 2944 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
9824353 2944 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL292964 2944 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
59465571 146285 0 None -1 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920796 146285 0 None -1 2 Human 6.0 pEC50 = 6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
118517361 153370 0 None -107 3 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 153370 0 None -107 3 Human 6.0 pEC50 = 6.0 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
11955384 147538 0 None 33 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 360 8 2 3 4.4 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3930718 147538 0 None 33 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 360 8 2 3 4.4 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
45268715 195976 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccccc2CCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559760 195976 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccccc2CCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
16750455 151272 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 342 7 1 2 5.2 CC(C)(C)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3960352 151272 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 342 7 1 2 5.2 CC(C)(C)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
53259980 176369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1cccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)c1 10.1021/acs.jmedchem.8b00808
CHEMBL4566584 176369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1cccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)c1 10.1021/acs.jmedchem.8b00808
CHEMBL4595789 176369 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1cccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)c1 10.1021/acs.jmedchem.8b00808
126495507 139379 0 None 154 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 425 5 1 5 5.1 Cc1cc(OC[C@H]2[C@@H](F)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793167 139379 0 None 154 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 425 5 1 5 5.1 Cc1cc(OC[C@H]2[C@@H](F)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
71515776 154356 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.5 CC(Nc1c(F)ccc(OCC(=O)O)c1F)c1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3986985 154356 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.5 CC(Nc1c(F)ccc(OCC(=O)O)c1F)c1cc(-c2cccc(F)c2)ccc1F nan
44304164 203234 0 None - 1 Mouse 8.0 pEC50 = 8.0 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 378 11 3 4 3.6 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64483 203234 0 None - 1 Mouse 8.0 pEC50 = 8.0 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 378 11 3 4 3.6 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
118517485 142750 0 None -3 4 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
CHEMBL3892492 142750 0 None -3 4 Human 8.0 pEC50 = 8.0 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
71515515 151004 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 369 7 2 3 4.7 O=C(O)COc1cccc(NCc2cc(-c3cccc(F)c3)ccc2F)c1 nan
CHEMBL3958411 151004 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 369 7 2 3 4.7 O=C(O)COc1cccc(NCc2cc(-c3cccc(F)c3)ccc2F)c1 nan
126495427 139466 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 422 5 2 5 4.7 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4csc(C(=O)O)c4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794185 139466 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 422 5 2 5 4.7 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4csc(C(=O)O)c4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
11955193 143584 0 None 10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 378 7 2 2 5.3 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3899346 143584 0 None 10 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 378 7 2 2 5.3 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
155550016 176682 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 13 2 6 3.6 O=C(O)CNc1cccc(CN(CCCCCc2ccccc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4539881 176682 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 13 2 6 3.6 O=C(O)CNc1cccc(CN(CCCCCc2ccccc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4598324 176682 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 13 2 6 3.6 O=C(O)CNc1cccc(CN(CCCCCc2ccccc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
53260150 176532 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 9 2 6 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(C(F)(F)F)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4451786 176532 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 9 2 6 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(C(F)(F)F)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4597091 176532 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 9 2 6 3.4 O=C(O)CNc1cccc(CN(Cc2ccc(C(F)(F)F)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
11855590 144374 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3905811 144374 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855591 144436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 144436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
11855591 144436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 144436 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
118517360 143975 0 None -61 3 Human 6.9 pEC50 = 6.9 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
CHEMBL3902700 143975 0 None -61 3 Human 6.9 pEC50 = 6.9 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
118517489 143691 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 143691 0 None -18 3 Human 6.9 pEC50 = 6.9 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
11955257 153886 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 410 9 3 3 5.3 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3983069 153886 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 410 9 3 3 5.3 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
118352211 139385 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 375 5 2 6 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793209 139385 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 375 5 2 6 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3)O2)n1 10.1016/j.bmcl.2016.03.110
118352211 139385 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 375 5 2 6 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3793209 139385 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 375 5 2 6 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
126495491 140225 0 None 28 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 429 8 2 6 4.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805169 140225 0 None 28 4 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 429 8 2 6 4.5 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
127050452 140244 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(C(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805408 140244 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(C(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
53260293 176213 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 11 2 6 4.2 CCC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CCC1 10.1021/acs.jmedchem.8b00808
CHEMBL4594090 176213 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 11 2 6 4.2 CCC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CCC1 10.1021/acs.jmedchem.8b00808
89443700 152586 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1F nan
CHEMBL3971868 152586 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1F nan
89444072 148944 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1c(-c2cccc(F)c2)ccc(F)c1CNc1c(F)ccc(OCC(=O)O)c1F nan
CHEMBL3941975 148944 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1c(-c2cccc(F)c2)ccc(F)c1CNc1c(F)ccc(OCC(=O)O)c1F nan
44303952 100886 0 None - 1 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293697 100886 0 None - 1 Mouse 6.9 pEC50 = 6.9 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10270893 94228 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 376 12 2 4 3.1 CCCCCC(O)CCCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249954 94228 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 376 12 2 4 3.1 CCCCCC(O)CCCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
9885481 195383 0 None 14 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL551951 195383 0 None 14 2 Rat 6.9 pEC50 = 6.9 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
11855325 144691 0 None 19 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 144691 0 None 19 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855325 144691 0 None 19 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 144691 0 None 19 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
127050451 140221 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(OC(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805122 140221 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(OC(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
89443781 149278 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 7 2 3 5.1 O=C(O)COc1ccc(F)c(NCc2cc(-c3ccc(F)c(F)c3)ccc2F)c1F nan
CHEMBL3944601 149278 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 7 2 3 5.1 O=C(O)COc1ccc(F)c(NCc2cc(-c3ccc(F)c(F)c3)ccc2F)c1F nan
10481859 75167 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
CHEMBL2036321 75167 0 None -67 2 Rat 5.9 pEC50 = 5.9 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
44303627 203205 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 364 11 3 3 4.5 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64358 203205 0 None - 1 Mouse 5.9 pEC50 = 5.9 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 364 11 3 3 4.5 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
134146425 149203 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 12 2 2 6.4 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3943966 149203 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 12 2 2 6.4 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
11855591 144436 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 144436 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
10291963 84708 0 None -32 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL222715 84708 0 None -32 4 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
127029402 139358 0 None 524 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 407 5 2 6 3.6 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)co4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793009 139358 0 None 524 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 407 5 2 6 3.6 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)co4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
24760052 151185 0 None 24 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3959769 151185 0 None 24 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
17751059 148268 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3936540 148268 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
89444124 143431 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1cc(-c2ccccc2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
CHEMBL3898152 143431 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1cc(-c2ccccc2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
156014791 177584 0 None -309 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 439 11 2 4 5.0 CCCCCC(O)CCc1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4640635 177584 0 None -309 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 439 11 2 4 5.0 CCCCCC(O)CCc1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
57464006 75168 0 None -288 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036322 75168 0 None -288 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
10269242 155575 0 None -54 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL404413 155575 0 None -54 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
59465577 143189 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 13 2 2 6.8 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3896183 143189 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 13 2 2 6.8 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
59465570 143259 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 392 13 2 2 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3896693 143259 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 392 13 2 2 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)O)cc1 nan
134143292 145228 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 12 1 3 6.5 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3912658 145228 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 12 1 3 6.5 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465574 145945 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
CHEMBL3918084 145945 0 None 1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
59465601 149894 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.4 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3949271 149894 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.4 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
58681356 150371 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 434 7 3 4 3.9 O=C(O)COCC#CCC1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3953307 150371 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 434 7 3 4 3.9 O=C(O)COCC#CCC1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
44442327 94459 0 None -891 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251294 94459 0 None -891 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
11855870 146280 0 None 467 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 146280 0 None 467 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855870 146280 0 None 467 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 146280 0 None 467 3 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
71515516 148306 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 387 7 2 3 4.8 O=C(O)COc1ccc(F)c(NCc2cccc(-c3cccc(F)c3)c2)c1F nan
CHEMBL3936868 148306 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 387 7 2 3 4.8 O=C(O)COc1ccc(F)c(NCc2cccc(-c3cccc(F)c3)c2)c1F nan
71516448 152560 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 3 4 4.7 O=C(O)COc1ccc(F)c(NCc2cc(O)cc(-c3cccc(F)c3)c2F)c1F nan
CHEMBL3971730 152560 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 3 4 4.7 O=C(O)COc1ccc(F)c(NCc2cc(O)cc(-c3cccc(F)c3)c2F)c1F nan
57893848 75169 0 None -724 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036323 75169 0 None -724 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
118517488 153711 0 None -14 3 Human 6.8 pEC50 = 6.8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 153711 0 None -14 3 Human 6.8 pEC50 = 6.8 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
58708286 154344 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 398 9 2 3 5.6 O=C(O)CCC/C=C\C[C@H]1C(=O)CC[C@@H]1c1ccc([C@H](O)C2CCCCC2)cc1 nan
CHEMBL3986874 154344 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 398 9 2 3 5.6 O=C(O)CCC/C=C\C[C@H]1C(=O)CC[C@@H]1c1ccc([C@H](O)C2CCCCC2)cc1 nan
1929 1605 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
9890801 1605 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
CHEMBL563646 1605 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
DB12022 1605 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
89444254 142780 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 7 2 3 5.1 O=C(O)COc1ccc(F)c(NCc2c(F)ccc(-c3cccc(F)c3)c2F)c1F nan
CHEMBL3892751 142780 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 423 7 2 3 5.1 O=C(O)COc1ccc(F)c(NCc2c(F)ccc(-c3cccc(F)c3)c2F)c1F nan
89443784 142906 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 431 8 2 4 5.2 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
CHEMBL3893770 142906 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 431 8 2 4 5.2 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
89444126 147388 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 403 7 3 4 4.6 O=C(O)COc1ccc(F)c(NCc2cc(O)cc(-c3cccc(F)c3)c2)c1F nan
CHEMBL3929662 147388 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 403 7 3 4 4.6 O=C(O)COc1ccc(F)c(NCc2cc(O)cc(-c3cccc(F)c3)c2)c1F nan
11955383 142533 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 358 7 2 3 4.2 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3890808 142533 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 358 7 2 3 4.2 CC(C)(C)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
53260155 171404 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 11 2 6 4.1 CC(C)C1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4462507 171404 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 11 2 6 4.1 CC(C)C1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
117703250 143639 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.5 C[C@@H](Nc1c(F)ccc(OCC(=O)O)c1F)c1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3899837 143639 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.5 C[C@@H](Nc1c(F)ccc(OCC(=O)O)c1F)c1cc(-c2cccc(F)c2)ccc1F nan
89444132 143866 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 417 8 2 4 4.9 COc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
CHEMBL3901709 143866 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 417 8 2 4 4.9 COc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
89443635 151904 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(OCC(=O)O)c(C)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
CHEMBL3965998 151904 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(OCC(=O)O)c(C)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
57394893 71306 0 None -223 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957435 71306 0 None -223 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
10291963 84708 0 None -3801 4 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmc.2012.02.018
CHEMBL222715 84708 0 None -3801 4 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmc.2012.02.018
57394893 71306 0 None -223 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957435 71306 0 None -223 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
11855867 145983 0 None 10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 145983 0 None 10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855867 145983 0 None 10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 145983 0 None 10 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
44455115 95562 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL257658 95562 0 None -6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
1883 3082 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
1916 3082 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
5280360 3082 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
913 3082 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
CHEMBL548 3082 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
DB00917 3082 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
53259985 176477 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 497 10 2 6 4.3 COc1ccc(S(=O)(=O)N(Cc2ccc(C(C)(C)C)cc2)Cc2cccc(NCC(=O)O)n2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4548451 176477 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 497 10 2 6 4.3 COc1ccc(S(=O)(=O)N(Cc2ccc(C(C)(C)C)cc2)Cc2cccc(NCC(=O)O)n2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596602 176477 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 497 10 2 6 4.3 COc1ccc(S(=O)(=O)N(Cc2ccc(C(C)(C)C)cc2)Cc2cccc(NCC(=O)O)n2)cc1 10.1021/acs.jmedchem.8b00808
44442332 94527 0 None -97 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251709 94527 0 None -97 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
127026952 139361 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 451 6 2 6 4.9 CC(C)c1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3793020 139361 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 451 6 2 6 4.9 CC(C)c1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
59465581 144112 0 None 22 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3903611 144112 0 None 22 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
145966519 164399 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4213312 164399 0 None 15 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 437 10 2 6 5.2 C[C@](O)(C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1)CC1CCCC1 10.1016/j.bmc.2017.11.035
44230429 176328 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 488 10 2 6 4.0 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4471378 176328 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 488 10 2 6 4.0 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4595426 176328 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 488 10 2 6 4.0 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccccc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
89443841 145895 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 407 7 2 3 5.8 Cc1cc(-c2cccc(F)c2)cc(CNc2c(C)ccc(OCC(=O)O)c2C)c1C nan
CHEMBL3917749 145895 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 407 7 2 3 5.8 Cc1cc(-c2cccc(F)c2)cc(CNc2c(C)ccc(OCC(=O)O)c2C)c1C nan
89444231 146113 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
CHEMBL3919482 146113 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
89443843 148797 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 433 7 2 3 5.6 Cc1cc(-c2ccc(F)c(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
CHEMBL3940781 148797 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 433 7 2 3 5.6 Cc1cc(-c2ccc(F)c(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
89443583 150478 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2C)c1F nan
CHEMBL3954347 150478 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2C)c1F nan
66857988 164122 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 428 12 2 7 4.0 CCCCCC(C)(O)C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4209929 164122 0 None 1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 428 12 2 7 4.0 CCCCCC(C)(O)C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
5283086 203310 24 None -10 4 Mouse 8.7 pEC50 = 8.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
CHEMBL64804 203310 24 None -10 4 Mouse 8.7 pEC50 = 8.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
118352285 139469 0 None 2398 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 406 5 2 5 4.2 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4ccc(C(=O)O)o4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794226 139469 0 None 2398 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 406 5 2 5 4.2 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4ccc(C(=O)O)o4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
18376196 194922 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 466 9 1 4 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccn2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL541516 194922 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 466 9 1 4 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccn2)cc1 10.1016/j.bmcl.2009.01.059
70815687 176546 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 466 10 2 6 3.4 CC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4515583 176546 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 466 10 2 6 3.4 CC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4597208 176546 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 466 10 2 6 3.4 CC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
138 3081 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
1882 3081 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
5280723 3081 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
CHEMBL495 3081 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
DB00770 3081 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
53260134 176262 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4466224 176262 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4594970 176262 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(F)cc2)cc1 10.1021/acs.jmedchem.8b00808
53259986 176520 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccn2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4442505 176520 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccn2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596979 176520 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccn2)cc1 10.1021/acs.jmedchem.8b00808
53259987 176498 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4591201 176498 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596748 176498 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 6 3.7 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
9807448 203172 0 None 1 2 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64246 203172 0 None 1 2 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
118352215 139417 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 403 5 2 6 3.8 Cc1ccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc1C 10.1016/j.bmcl.2016.03.110
CHEMBL3793797 139417 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 403 5 2 6 3.8 Cc1ccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc1C 10.1016/j.bmcl.2016.03.110
11855865 153277 0 None 35 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 153277 0 None 35 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
10126807 195098 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 405 8 1 4 3.4 CC(C)(C)c1ccc(CN(Cc2cccc(OCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549869 195098 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 405 8 1 4 3.4 CC(C)(C)c1ccc(CN(Cc2cccc(OCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11955273 152787 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 438 10 3 4 4.6 O=C(O)COCCCC[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3973644 152787 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 438 10 3 4 4.6 O=C(O)COCCCC[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
138107701 187464 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
5311181 187464 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
CHEMBL494 187464 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
59465583 143274 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 398 9 2 3 5.6 O=C(O)CCC/C=C\C[C@H]1C(=O)CC[C@@H]1c1ccc(C(O)C2CCCCC2)cc1 nan
CHEMBL3896863 143274 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 398 9 2 3 5.6 O=C(O)CCC/C=C\C[C@H]1C(=O)CC[C@@H]1c1ccc(C(O)C2CCCCC2)cc1 nan
11855594 152980 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 152980 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855594 152980 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 152980 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855871 146408 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 146408 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855871 146408 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 146408 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
54013831 146460 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3922151 146460 0 None 1 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
10363130 101035 1 None - 1 Mouse 6.7 pEC50 = 6.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL294585 101035 1 None - 1 Mouse 6.7 pEC50 = 6.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
9975502 94489 0 None -14 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251504 94489 0 None -14 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
24760052 151185 0 None 24 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3959769 151185 0 None 24 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
70667255 151474 0 None 24 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3962183 151474 0 None 24 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
72950089 150591 0 None -4365 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL3955128 150591 0 None -4365 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
11955180 151660 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2ccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)cc2)CCC1 nan
CHEMBL3963968 151660 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2ccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)cc2)CCC1 nan
10089562 154422 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL398948 154422 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
118352177 139412 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 6 1 6 4.8 CO[C@H]1C[C@@H]2O[C@@H](c3nc(C(=O)O)cs3)CC[C@@H]2[C@H]1COc1ccc(Cl)c(C)c1 10.1016/j.bmcl.2016.03.110
CHEMBL3793724 139412 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 437 6 1 6 4.8 CO[C@H]1C[C@@H]2O[C@@H](c3nc(C(=O)O)cs3)CC[C@@H]2[C@H]1COc1ccc(Cl)c(C)c1 10.1016/j.bmcl.2016.03.110
127051064 140299 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3F)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806060 140299 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3F)O2)n1 10.1021/acsmedchemlett.5b00455
89443417 151592 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2Cl)c1F nan
CHEMBL3963438 151592 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2Cl)c1F nan
44455046 95727 0 None -8317 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL258332 95727 0 None -8317 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
56839536 143169 0 None -141 7 Human 5.6 pEC50 = 5.6 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 604 15 2 7 5.1 CCCCCCCCNC(=O)c1coc([C@@H]2CCCN2Cc2cc(F)ccc2CCC(=O)NS(=O)(=O)C(F)(F)F)n1 nan
CHEMBL3896035 143169 0 None -141 7 Human 5.6 pEC50 = 5.6 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 604 15 2 7 5.1 CCCCCCCCNC(=O)c1coc([C@@H]2CCCN2Cc2cc(F)ccc2CCC(=O)NS(=O)(=O)C(F)(F)F)n1 nan
57529188 147195 0 None 19 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 147195 0 None 19 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
89443813 151738 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3964577 151738 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
118517359 144396 0 None -79 4 Human 7.6 pEC50 = 7.6 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 144396 0 None -79 4 Human 7.6 pEC50 = 7.6 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
57384034 71307 0 None -9 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957436 71307 0 None -9 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
57384034 71307 0 None -9 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957436 71307 0 None -9 2 Rat 6.6 pEC50 = 6.6 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
11955194 151003 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 380 8 2 2 5.5 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3958410 151003 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 380 8 2 2 5.5 CC(C)(C)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
58708282 153124 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 412 11 2 3 6.0 CCCC1([C@@H](O)c2cccc([C@H]3CCC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3976452 153124 0 None 1 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 412 11 2 3 6.0 CCCC1([C@@H](O)c2cccc([C@H]3CCC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
58681352 154339 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 486 10 3 4 5.5 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3Cc3cccc(OCC(=O)O)c3)c2)CCC1 nan
CHEMBL3986829 154339 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 486 10 3 4 5.5 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3Cc3cccc(OCC(=O)O)c3)c2)CCC1 nan
126495360 140234 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 5 2 6 3.4 Cc1ccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc1 10.1021/acsmedchemlett.5b00455
CHEMBL3805316 140234 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 5 2 6 3.4 Cc1ccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc1 10.1021/acsmedchemlett.5b00455
11855866 144602 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 144602 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
89443595 144961 5 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 412 7 2 4 4.7 N#Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
CHEMBL3910551 144961 5 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 412 7 2 4 4.7 N#Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
57894053 75170 0 None -208 2 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036324 75170 0 None -208 2 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
118517359 144396 0 None -79 4 Human 6.6 pEC50 = 6.6 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 144396 0 None -79 4 Human 6.6 pEC50 = 6.6 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
126495420 140249 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 9 2 6 4.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805455 140249 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 9 2 6 4.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3CCCCCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
11855324 142605 0 None 14 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 142605 0 None 14 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
71515514 147626 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 405 7 2 3 5.0 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
CHEMBL3931335 147626 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 405 7 2 3 5.0 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
11955198 147243 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 436 10 3 3 5.8 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3928466 147243 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 436 10 3 3 5.8 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
155541719 176382 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 9 1 6 3.7 CN(CC(=O)O)c1cccc(CN(Cc2ccc(C(C)(C)C)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4519118 176382 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 9 1 6 3.7 CN(CC(=O)O)c1cccc(CN(Cc2ccc(C(C)(C)C)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4595870 176382 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 9 1 6 3.7 CN(CC(=O)O)c1cccc(CN(Cc2ccc(C(C)(C)C)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
132836 59695 23 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL1722929 59695 23 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
155532079 171689 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 10 2 6 4.4 O=C(O)CNc1cccc(CN(Cc2ccc(C3CCCCC3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4466523 171689 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 494 10 2 6 4.4 O=C(O)CNc1cccc(CN(Cc2ccc(C3CCCCC3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
44455084 97867 0 None -10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
CHEMBL272277 97867 0 None -10 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
59465581 144112 0 None 22 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3903611 144112 0 None 22 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
89443767 145712 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 409 8 2 4 5.2 COc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
CHEMBL3916293 145712 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 409 8 2 4 5.2 COc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
89443716 147026 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
CHEMBL3926711 147026 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 397 7 2 3 5.3 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
89443671 147838 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1c(F)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
CHEMBL3932999 147838 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1c(F)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
89445501 152276 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(-c2cccc(F)c2)cc(F)c1C nan
CHEMBL3969269 152276 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1ccc(OCC(=O)O)c(C)c1NCc1cc(-c2cccc(F)c2)cc(F)c1C nan
89443873 153940 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)c(F)c(-c2cccc(F)c2)c1 nan
CHEMBL3983500 153940 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)c(F)c(-c2cccc(F)c2)c1 nan
127051062 140274 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3Cl)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805767 140274 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3Cl)O2)n1 10.1021/acsmedchemlett.5b00455
46931421 176263 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 7 3.6 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3s2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4476670 176263 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 7 3.6 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3s2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4594971 176263 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 2 7 3.6 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3s2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
126495424 140255 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 5 2 6 3.4 Cc1cccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)c1 10.1021/acsmedchemlett.5b00455
CHEMBL3805554 140255 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 389 5 2 6 3.4 Cc1cccc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)c1 10.1021/acsmedchemlett.5b00455
127052615 140270 0 None 181 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 401 6 2 6 3.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805693 140270 0 None 181 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 401 6 2 6 3.7 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
127027875 139416 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)cc3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793786 139416 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)cc3)O2)n1 10.1016/j.bmcl.2016.03.110
127026954 139420 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 457 5 2 6 4.5 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.110
CHEMBL3793809 139420 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 457 5 2 6 4.5 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)ccc1C(F)(F)F 10.1016/j.bmcl.2016.03.110
127027875 139416 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3793786 139416 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
127052614 140226 0 None 40 6 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 415 7 2 6 4.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805176 140226 0 None 40 6 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 415 7 2 6 4.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/CCOc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
118517490 153155 0 None -12 4 Human 7.5 pEC50 = 7.5 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
CHEMBL3976710 153155 0 None -12 4 Human 7.5 pEC50 = 7.5 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
44230723 176505 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 490 10 2 8 2.8 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccnnc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4473407 176505 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 490 10 2 8 2.8 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccnnc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4596867 176505 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 490 10 2 8 2.8 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccnnc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
134155748 151169 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959653 151169 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
145965248 164230 0 None -9 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 439 10 2 6 5.4 CC(C)(C)CC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4211120 164230 0 None -9 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 439 10 2 6 5.4 CC(C)(C)CC[C@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
11855867 145983 0 None 10 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 145983 0 None 10 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
58681361 144681 0 None -33 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 318 8 2 3 3.5 Cc1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3908432 144681 0 None -33 3 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 318 8 2 3 3.5 Cc1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
44304181 203273 0 None -1 2 Mouse 7.5 pEC50 = 7.5 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 394 13 3 4 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64663 203273 0 None -1 2 Mouse 7.5 pEC50 = 7.5 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 394 13 3 4 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
58932683 75287 0 None -1995 2 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037289 75287 0 None -1995 2 Rat 5.5 pEC50 = 5.5 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
11955178 153787 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3982222 153787 0 None 1 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 448 11 3 3 6.0 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
44303980 168074 0 None 1 2 Mouse 7.5 pEC50 = 7.5 Functional
Effective concentration which increases intracellular c-AMP production in mouse EP2- receptorEffective concentration which increases intracellular c-AMP production in mouse EP2- receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL432522 168074 0 None 1 2 Mouse 7.5 pEC50 = 7.5 Functional
Effective concentration which increases intracellular c-AMP production in mouse EP2- receptorEffective concentration which increases intracellular c-AMP production in mouse EP2- receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/s0960-894x(01)00359-6
1883 3082 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
1916 3082 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
5280360 3082 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
913 3082 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL548 3082 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
DB00917 3082 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
17757350 152754 0 None 870 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
CHEMBL3973347 152754 0 None 870 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
89444121 147432 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1Cl nan
CHEMBL3929987 147432 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1Cl nan
45271237 195099 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.0 CCCCc1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549870 195099 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.0 CCCCc1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
66858036 163891 0 None -93 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 468 10 2 7 4.8 C[C@@H]1OC(=O)N(CCSc2nc(C(=O)O)cs2)[C@H]1/C=C/CC(C)(O)CC1CCCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4207054 163891 0 None -93 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 468 10 2 7 4.8 C[C@@H]1OC(=O)N(CCSc2nc(C(=O)O)cs2)[C@H]1/C=C/CC(C)(O)CC1CCCCC1 10.1016/j.bmc.2017.11.035
59465599 146561 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 12 2 3 6.2 CCCC1(C(O)c2cccc([C@H]3CCC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
CHEMBL3922856 146561 0 None 1 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 12 2 3 6.2 CCCC1(C(O)c2cccc([C@H]3CCC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
59465600 151698 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.3 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3964261 151698 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.3 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
58681358 150659 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 420 10 2 2 6.3 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(CC3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3955642 150659 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 420 10 2 2 6.3 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(CC3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
44442331 94490 0 None -346 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251505 94490 0 None -346 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulationAgonist activity at EP2 receptor expressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
44230430 176370 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 506 10 2 6 4.2 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(F)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4449902 176370 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 506 10 2 6 4.2 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(F)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4595790 176370 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 506 10 2 6 4.2 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(F)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
71515518 142806 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
CHEMBL3892911 142806 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
89443584 145177 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2C)c(F)c(-c2cccc(F)c2)c1 nan
CHEMBL3912323 145177 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2C)c(F)c(-c2cccc(F)c2)c1 nan
118517361 153370 0 None -107 3 Human 7.5 pEC50 = 7.5 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 153370 0 None -107 3 Human 7.5 pEC50 = 7.5 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
155542681 176600 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 7 3.7 CC(C)(C)c1ccc(CN(Cc2csc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4521659 176600 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 7 3.7 CC(C)(C)c1ccc(CN(Cc2csc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4597685 176600 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 7 3.7 CC(C)(C)c1ccc(CN(Cc2csc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
11955156 148454 1 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 3 4 4.9 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3937945 148454 1 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 3 4 4.9 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
118689427 151852 0 None -8 2 Human 7.4 pEC50 = 7.4 Functional
cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
CHEMBL3965497 151852 0 None -8 2 Human 7.4 pEC50 = 7.4 Functional
cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.cAMP Assay: EP4 receptors couple to Gs and mediate elevations in cAMP concentration, although they do participate in other pathways as well. There are some redundancies in function between EP2 and EP4 receptors. For example, both receptors induce PGE2-mediated RANKL through cAMP.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
57893982 75164 0 None -25 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036318 75164 0 None -25 2 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
11955259 146759 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 436 9 3 4 4.4 O=C(O)COC/C=C\C[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3924405 146759 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 436 9 3 4 4.4 O=C(O)COC/C=C\C[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
57529188 147195 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 147195 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
57529188 147195 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 147195 0 None 19 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
44303626 168182 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL433249 168182 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
56839344 152051 0 None -12882 8 Human 5.4 pEC50 = 5.4 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 656 13 2 9 5.1 O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F nan
CHEMBL3967284 152051 0 None -12882 8 Human 5.4 pEC50 = 5.4 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 656 13 2 9 5.1 O=C(CCc1cc2c(cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC3CCCCC3)co1)OCO2)NS(=O)(=O)C(F)(F)F nan
11955196 144422 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 434 9 3 3 5.6 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3906280 144422 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 434 9 3 3 5.6 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C(O)C3CCCCC3)cc2)[C@H](O)C[C@H]1Cl nan
44444722 94256 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 402 11 2 4 3.5 CCCC1(C(O)CCCN2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.09.074
CHEMBL250153 94256 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 402 11 2 4 3.5 CCCC1(C(O)CCCN2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.09.074
17751059 148268 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3936540 148268 0 None 3 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
17757350 152754 0 None 870 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
CHEMBL3973347 152754 0 None 870 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
89444221 144280 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 430 8 3 4 3.9 NC(=O)c1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
CHEMBL3904996 144280 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 430 8 3 4 3.9 NC(=O)c1cc(CNc2c(F)ccc(OCC(=O)O)c2F)cc(-c2cccc(F)c2)c1 nan
53259981 176350 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 467 9 2 5 4.3 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4456588 176350 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 467 9 2 5 4.3 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4595646 176350 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 467 9 2 5 4.3 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2)cc1 10.1021/acs.jmedchem.8b00808
53259984 176535 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4447271 176535 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4597100 176535 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.8b00808
53260154 171131 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 11 2 6 3.8 CCC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4458330 171131 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 480 11 2 6 3.8 CCC1(c2ccc(CN(Cc3cccc(NCC(=O)O)n3)S(=O)(=O)c3cccnc3)cc2)CC1 10.1021/acs.jmedchem.8b00808
11955276 150751 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 358 7 3 4 2.9 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc2c(c1)CCC2O nan
CHEMBL3956391 150751 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 358 7 3 4 2.9 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc2c(c1)CCC2O nan
22246893 195952 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 371 13 1 4 2.7 CCCCc1ccc(CN(CCCCOCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559561 195952 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 371 13 1 4 2.7 CCCCc1ccc(CN(CCCCOCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11855588 147357 0 None 12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 147357 0 None 12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
11855588 147357 0 None 12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 147357 0 None 12 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
22246765 195198 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 3.7 CCCCc1ccc(CN(CCc2ccc(CC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL550619 195198 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 3.7 CCCCc1ccc(CN(CCc2ccc(CC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
22246895 195564 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 399 14 2 4 3.7 CCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL554823 195564 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 399 14 2 4 3.7 CCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11855866 144602 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 144602 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855866 144602 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 144602 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
57564500 151210 0 None 2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959926 151210 0 None 2 3 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
44230997 170537 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 479 10 2 9 1.9 O=C(O)CNc1cccc(CN(Cc2ccc(-n3cncn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4449855 170537 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 479 10 2 9 1.9 O=C(O)CNc1cccc(CN(Cc2ccc(-n3cncn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
44304199 100817 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2C/C=C/CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293242 100817 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2C/C=C/CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
9821171 97866 0 None -14454 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL272276 97866 0 None -14454 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
10223499 196341 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 413 15 2 4 4.1 CCCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562411 196341 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 413 15 2 4 4.1 CCCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11855324 142605 0 None 14 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 142605 0 None 14 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855324 142605 0 None 14 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 142605 0 None 14 2 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
53259982 176435 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2F)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4561017 176435 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2F)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596258 176435 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2ccccc2F)cc1 10.1021/acs.jmedchem.8b00808
89443872 145841 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 437 7 2 3 6.0 O=C(O)COc1ccc(Cl)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1Cl nan
CHEMBL3917219 145841 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 437 7 2 3 6.0 O=C(O)COc1ccc(Cl)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1Cl nan
44304124 102623 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 12 3 4 4.3 CC(C)CC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL304225 102623 0 None - 1 Mouse 7.4 pEC50 = 7.4 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 12 3 4 4.3 CC(C)CC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
11955297 149887 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 416 10 3 4 4.8 O=C(O)CCCCCC[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc(C(O)C2CCCCC2)cc1 nan
CHEMBL3949225 149887 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 416 10 3 4 4.8 O=C(O)CCCCCC[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc(C(O)C2CCCCC2)cc1 nan
22246983 195862 0 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 389 11 1 3 4.2 CS(=O)(=O)N(CCCCCCC(=O)O)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL558671 195862 0 None - 1 Rat 6.3 pEC50 = 6.3 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 389 11 1 3 4.2 CS(=O)(=O)N(CCCCCCC(=O)O)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
23729077 78218 31 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 520 11 0 8 4.0 CC(C)OC(=O)COc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)c1 nan
CHEMBL2105692 78218 31 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 520 11 0 8 4.0 CC(C)OC(=O)COc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)c1 nan
57894063 75165 0 None -301 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036319 75165 0 None -301 2 Rat 5.3 pEC50 = 5.3 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
156010583 177078 0 None -162 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 451 10 2 4 5.4 CCCCCC(C)(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
CHEMBL4633041 177078 0 None -162 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assayAgonist activity at human EP2 receptor expressed in HEK293 cells by calcium-5 dye based FLIPR assay
ChEMBL 451 10 2 4 5.4 CCCCCC(C)(O)/C=C/c1c(Cl)cc(Cl)c(=O)n1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2020.127104
45271238 195641 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 8 1 3 4.0 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL556333 195641 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 8 1 3 4.0 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
59465587 145190 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 372 13 2 2 6.5 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)O)cc1 nan
CHEMBL3912391 145190 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 372 13 2 2 6.5 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)O)cc1 nan
11955315 143791 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 9 3 3 4.6 CC(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3901088 143791 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 9 3 3 4.6 CC(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
11955256 143316 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 424 9 2 4 5.4 COC(=O)CCCCCC[C@@H]1[C@@H](c2ccc(C(O)C(C)(C)C)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3897181 143316 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 424 9 2 4 5.4 COC(=O)CCCCCC[C@@H]1[C@@H](c2ccc(C(O)C(C)(C)C)cc2)[C@H](O)C[C@H]1Cl nan
16725337 149601 0 None 4 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 149601 0 None 4 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
16725337 149601 0 None 4 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 149601 0 None 4 4 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
89443809 148145 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 427 8 2 4 5.3 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1C nan
CHEMBL3935521 148145 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 427 8 2 4 5.3 COc1c(C)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1C nan
89443631 148665 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1c(F)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1C nan
CHEMBL3939716 148665 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 415 7 2 3 5.5 Cc1c(F)cc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1C nan
127050450 140300 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806076 140300 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
57395059 69474 0 None -11 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL1933725 69474 0 None -11 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1021/acsmedchemlett.5b00455
44229605 176654 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 452 9 2 7 3.1 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3o2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4470479 176654 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 452 9 2 7 3.1 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3o2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4598070 176654 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 452 9 2 7 3.1 O=C(O)CNc1cccc(CN(Cc2cc3ccccc3o2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
89443989 148668 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(OCC(=O)O)c(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
CHEMBL3939740 148668 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(OCC(=O)O)c(F)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
44444714 94138 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 362 10 2 4 2.6 CCCC(C)C(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249341 94138 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 362 10 2 4 2.6 CCCC(C)C(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
59465588 143526 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 422 13 1 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3898887 143526 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 422 13 1 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465575 145067 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)c1 nan
CHEMBL3911438 145067 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)c1 nan
59465595 145423 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)c1 nan
CHEMBL3914108 145423 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)c1 nan
59465592 149702 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)OC)cc1 nan
CHEMBL3947785 149702 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 386 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)OC)cc1 nan
59465590 150945 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 406 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3957958 150945 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 406 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465584 151430 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 13 2 2 6.7 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCCO)cc1 nan
CHEMBL3961847 151430 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 13 2 2 6.7 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCCO)cc1 nan
11855325 144691 0 None 19 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 144691 0 None 19 3 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11955233 145593 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 392 8 3 3 4.3 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C3(O)CCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3915426 145593 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 392 8 3 3 4.3 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C3(O)CCC3)cc2)[C@H](O)C[C@H]1Cl nan
11855593 146834 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 425 11 2 4 4.7 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2cccc(C(=O)O)c2)cc1 nan
CHEMBL3924987 146834 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 425 11 2 4 4.7 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2cccc(C(=O)O)c2)cc1 nan
89444078 146074 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 405 7 2 3 5.0 O=C(O)COc1ccc(F)c(NCc2cc(F)cc(-c3cccc(F)c3)c2)c1F nan
CHEMBL3919144 146074 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 405 7 2 3 5.0 O=C(O)COc1ccc(F)c(NCc2cc(F)cc(-c3cccc(F)c3)c2)c1F nan
11955406 146104 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 376 10 3 4 3.4 CC(C)(CO)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3919393 146104 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 376 10 3 4 3.4 CC(C)(CO)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
11955294 144768 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 380 8 3 3 4.2 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
CHEMBL3909111 144768 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 380 8 3 3 4.2 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
44303889 203217 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 414 10 3 4 4.2 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64423 203217 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 414 10 3 4 4.2 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/s0960-894x(01)00359-6
11955179 146482 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 450 12 3 3 6.2 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
CHEMBL3922332 146482 0 None 5 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 450 12 3 3 6.2 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
11855588 147357 0 None 12 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 147357 0 None 12 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
126495432 139324 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 406 5 2 5 4.2 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4coc(C(=O)O)c4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3792668 139324 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay
ChEMBL 406 5 2 5 4.2 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4coc(C(=O)O)c4)CC[C@@H]32)ccc1Cl 10.1016/j.bmcl.2016.03.110
71515517 148082 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)c(F)c(-c2cccc(F)c2)c1 nan
CHEMBL3934986 148082 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 419 7 2 3 5.3 Cc1cc(CNc2c(F)ccc(OCC(=O)O)c2F)c(F)c(-c2cccc(F)c2)c1 nan
56839343 144279 0 None -147 6 Human 5.3 pEC50 = 5.3 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 642 14 2 8 5.4 COc1ccc(CCC(=O)NS(=O)(=O)C(F)(F)F)c(CN2CCC[C@H]2c2nc(C(=O)NCCCCC3CCCCC3)co2)c1 nan
CHEMBL3904989 144279 0 None -147 6 Human 5.3 pEC50 = 5.3 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 642 14 2 8 5.4 COc1ccc(CCC(=O)NS(=O)(=O)C(F)(F)F)c(CN2CCC[C@H]2c2nc(C(=O)NCCCCC3CCCCC3)co2)c1 nan
45266955 195645 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 485 10 1 6 3.7 Cn1ccnc1CS(=O)(=O)N(Cc1ccc(C(C)(C)C)cc1)Cc1cccc(OCC(=O)O)c1 10.1016/j.bmcl.2009.01.059
CHEMBL556416 195645 0 None - 1 Rat 7.2 pEC50 = 7.2 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 485 10 1 6 3.7 Cn1ccnc1CS(=O)(=O)N(Cc1ccc(C(C)(C)C)cc1)Cc1cccc(OCC(=O)O)c1 10.1016/j.bmcl.2009.01.059
57564500 151210 0 None 2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959926 151210 0 None 2 3 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
44303723 202935 0 None - 1 Mouse 6.2 pEC50 = 6.2 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 12 3 4 4.4 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCC1 10.1016/s0960-894x(01)00359-6
CHEMBL62885 202935 0 None - 1 Mouse 6.2 pEC50 = 6.2 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 12 3 4 4.4 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCC1 10.1016/s0960-894x(01)00359-6
45269576 195983 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccc(CCCC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559820 195983 0 None - 1 Rat 6.2 pEC50 = 6.2 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccc(CCCC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
9863804 94098 0 None -120 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249136 94098 0 None -120 2 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human prostaglandin EP2 receptorAgonist activity at human prostaglandin EP2 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
89444271 151908 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2C)c1C nan
CHEMBL3966050 151908 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 411 7 2 3 5.6 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2C)c1C nan
53259983 176301 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(F)c2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4587628 176301 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(F)c2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4595199 176301 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 485 9 2 5 4.4 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(F)c2)cc1 10.1021/acs.jmedchem.8b00808
2720 3854 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
5820 3854 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
6918140 3854 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
CHEMBL1237119 3854 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
DB00374 3854 59 None -10 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 10.1016/j.ejmech.2022.114154
127052577 140260 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(Cl)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805596 140260 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(Cl)c3)O2)n1 10.1021/acsmedchemlett.5b00455
67082722 164628 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCC[C@@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
CHEMBL4216182 164628 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 425 12 2 6 5.2 CCCCC[C@@](C)(O)C/C=C/[C@H]1CCC(=O)[C@@H]1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2017.11.035
8541 2944 2 None -66069 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
9824353 2944 2 None -66069 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL292964 2944 2 None -66069 4 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
155527947 176534 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4460294 176534 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4597099 176534 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 501 9 2 5 4.9 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.8b00808
11955157 152643 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 430 12 3 4 5.1 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
CHEMBL3972401 152643 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 430 12 3 4 5.1 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3CCCCCCC(=O)O)c2)CCC1 nan
56649302 152666 0 None -169 6 Human 5.2 pEC50 = 5.2 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 630 13 2 7 5.5 O=C(CCc1ccc(F)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
CHEMBL3972583 152666 0 None -169 6 Human 5.2 pEC50 = 5.2 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 630 13 2 7 5.5 O=C(CCc1ccc(F)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
155539238 176481 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 6 4.0 CC(C)(C)C1CCC(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4514124 176481 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 6 4.0 CC(C)(C)C1CCC(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)CC1 10.1021/acs.jmedchem.8b00808
CHEMBL4596631 176481 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 474 9 2 6 4.0 CC(C)(C)C1CCC(CN(Cc2cccc(NCC(=O)O)n2)S(=O)(=O)c2cccnc2)CC1 10.1021/acs.jmedchem.8b00808
71516449 149436 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1ccc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
CHEMBL3945923 149436 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1ccc(-c2cccc(F)c2)cc1CNc1c(F)ccc(OCC(=O)O)c1F nan
127050766 140213 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805075 140213 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 393 5 2 6 3.3 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
89443614 150589 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 393 7 2 3 5.5 Cc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
CHEMBL3955120 150589 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 393 7 2 3 5.5 Cc1cc(CNc2c(C)ccc(OCC(=O)O)c2C)cc(-c2cccc(F)c2)c1 nan
127052613 140206 0 None -10 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 7 3 7 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/[C@@H](O)COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3804978 140206 0 None -10 6 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 431 7 3 7 3.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3/C=C/[C@@H](O)COc3ccccc3)O2)n1 10.1021/acsmedchemlett.5b00455
11955236 146456 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 396 10 3 3 4.5 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3922121 146456 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 396 10 3 3 4.5 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
44303711 102352 0 None - 1 Mouse 7.2 pEC50 = 7.2 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL303763 102352 0 None - 1 Mouse 7.2 pEC50 = 7.2 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
67245477 144883 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 13 1 4 7.0 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)s1 nan
CHEMBL3909989 144883 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 13 1 4 7.0 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)s1 nan
24760055 143888 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3901873 143888 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
24760055 143888 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3901873 143888 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
89443736 151354 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(Cl)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
CHEMBL3961188 151354 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 421 7 2 3 5.5 O=C(O)COc1ccc(Cl)c(NCc2cc(-c3cccc(F)c3)ccc2F)c1F nan
12521 2197 0 None -23988 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
72722131 2197 0 None -23988 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
CHEMBL3918816 2197 0 None -23988 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
11955234 152217 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 9 3 3 4.6 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(C3(O)CCC3)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3968751 152217 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 394 9 3 3 4.6 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc(C3(O)CCC3)cc2)[C@H](O)C[C@H]1Cl nan
44230431 176653 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 522 10 2 6 4.7 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(Cl)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4531171 176653 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 522 10 2 6 4.7 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(Cl)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4598069 176653 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 522 10 2 6 4.7 O=C(O)CNc1cccc(CN(Cc2ccc(-c3ccc(Cl)cc3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
118517483 144271 0 None -22 3 Human 7.1 pEC50 = 7.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 144271 0 None -22 3 Human 7.1 pEC50 = 7.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
11855590 144374 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3905811 144374 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855590 144374 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3905811 144374 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
134147021 150024 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 13 2 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)s1 nan
CHEMBL3950412 150024 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 414 13 2 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)s1 nan
11955255 146257 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 8 3 3 5.0 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920560 146257 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 408 8 3 3 5.0 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
92135977 152896 0 None -141 4 Human 7.1 pEC50 = 7.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 152896 0 None -141 4 Human 7.1 pEC50 = 7.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
5819 1012 29 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at EP2 receptor (unknown origin) by cAMP assayAgonist activity at EP2 receptor (unknown origin) by cAMP assay
ChEMBL 333 4 1 5 4.0 CCOC(=O)c1c(sc2c1CCCCC2)NC(=O)c1ccco1 10.1021/jm401431x
673766 1012 29 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at EP2 receptor (unknown origin) by cAMP assayAgonist activity at EP2 receptor (unknown origin) by cAMP assay
ChEMBL 333 4 1 5 4.0 CCOC(=O)c1c(sc2c1CCCCC2)NC(=O)c1ccco1 10.1021/jm401431x
CHEMBL1578948 1012 29 None 1 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at EP2 receptor (unknown origin) by cAMP assayAgonist activity at EP2 receptor (unknown origin) by cAMP assay
ChEMBL 333 4 1 5 4.0 CCOC(=O)c1c(sc2c1CCCCC2)NC(=O)c1ccco1 10.1021/jm401431x
11855871 146408 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 146408 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855594 152980 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 152980 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11502897 142793 0 None 43 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 142793 0 None 43 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11502897 142793 0 None 43 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 142793 0 None 43 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assayAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of calcium mobilization after 45 mins by fluo-4AM dye-based FLIPR assay
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
89443779 148739 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 399 7 3 4 4.7 Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(O)cc(-c2cccc(F)c2)c1 nan
CHEMBL3940318 148739 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 399 7 3 4 4.7 Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(O)cc(-c2cccc(F)c2)c1 nan
89443711 150979 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 433 7 2 3 5.6 Cc1cc(-c2cc(F)cc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
CHEMBL3958279 150979 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 433 7 2 3 5.6 Cc1cc(-c2cc(F)cc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1C nan
118517483 144271 0 None -22 3 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 144271 0 None -22 3 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
118517359 144396 0 None -79 4 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 144396 0 None -79 4 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
118517488 153711 0 None -14 3 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 153711 0 None -14 3 Human 8.1 pEC50 = 8.1 Functional
cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.cAMP Assay: A 384-well drug plate was prepared to contain test compounds, PGE2 and cAMP in 16 serial dilutions in triplicate, using a Biomek station. HEK-EBNA cells expressing a target PG receptor subtype (EP2 or EP4) were suspended in a stimulation buffer (HBSS, 0.1% BSA, 0.5 mM IBMX and 5 mM HEPES, pH 7.4) in a density of 104 cells/5 μl. The reaction was initiated by mixing 5 μL drug dilutions with 5 μl of HEK-EBNA cells in a well, carried out for 30 min at room temperature, and followed by the addition of 5 μl anti-cAMP acceptor beads in the control buffer with Tween-20 (25 mM NaCl, 0.03% Tween-20, 5 mM HEPES, pH7.4). After 30 min in the dark at room temperature, the mixtures were incubated with 15 μl biotinylated-cAMP/strpavidin donor beads in Lysis/Detection buffer (0.1% BSA, 0.3% Tween-20 and 5 mM HEPES, pH7.4) for 45 min at the room temperature. Fluorescence changes were read using a Fusion-alpha HT microplate reader.
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
44442327 94459 0 None -891 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL251294 94459 0 None -891 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human EP2 receptor by cAMP assayAgonist activity at human EP2 receptor by cAMP assay
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
11955358 153082 0 None -11 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 364 8 2 2 4.7 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
CHEMBL3976116 153082 0 None -11 3 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 364 8 2 2 4.7 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
155521507 176449 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 10 2 6 4.1 CC(C)(C)c1ccc(CN(Cc2cccc(NCCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4451941 176449 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 10 2 6 4.1 CC(C)(C)c1ccc(CN(Cc2cccc(NCCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4596396 176449 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 482 10 2 6 4.1 CC(C)(C)c1ccc(CN(Cc2cccc(NCCC(=O)O)n2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
56839342 149007 0 None -83 7 Human 6.1 pEC50 = 6.1 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 646 13 2 7 6.0 O=C(CCc1ccc(Cl)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
CHEMBL3942394 149007 0 None -83 7 Human 6.1 pEC50 = 6.1 Functional
Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.Cell Based Assay: Ca2+ signaling studies were performed using a FLIPR TETRA system (Molecular Devices, Sunnyvale, Calif., USA) in the 384-format. This is a high-throughput instrument for cell-based assays to monitor Ca2+ signaling associated with GPCRs and ion channels. Cells were seeded at a density of 5×104 cells/well in BioCoat poly-D-lysine coated, black wall, clear bottom 384-well plates (BD Biosciences, Franklin lakes, NJ, USA) and allowed to attach overnight in an incubator at 37° C. The cells were then washed twice with HBSS-HEPES buffer (Hanks' balanced salt solution without bicarbonate and phenol red, 20 mM HEPES, pH 7.4) using an ELx405 Select CW Microplate Washer (BioTek, Winooski, Vt., USA). After 60 min of dye-loading in the dark using the Ca2+-sensitive dye Fluo-4AM (Invitrogen, Carlsbad, Calif., USA), at a final concentration of 2×10^−6M, the plates were washed 4 times with HBSS-HEPES buffer to remove excess dye and leaving 50 μl of buffer in each well. The plates were then placed in the FLIPR TETRA instrument and allowed to equilibrate at 37° C. AGN-211377 was added in a 25 μl volume to each well to give final concentrations of 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, and 30 μM; or 0.067 μM, 0.1 μM, 0.2 μM, 0.3 μM, 0.67 μM, and 1 μM for cells over-expressing TP receptors. After 4.5 minutes, a 7-point serial dilution of the standard agonist for the corresponding receptor, in a 25 μl volume was injected at the final concentrations from 10^−11M to 10^−5M in 10-fold serial dilution increments for cells expressing human recombinant DP1, EP1, EP2, EP3, EP4, FP, and IP receptors. The dose range for the standard agonist for human recombinant TP receptors was from 10^−12M to 10^−6M. HBSS-HEPES buffer was used as the negative control for the standard agonists. Cells were excited with LED (light emitting diode) excitation at 470-495 nm and emission was measured through an emission filter at 515-575 nm. Assay plates were read for 3.5 minutes using the FLIPRTETRA.
ChEMBL 646 13 2 7 6.0 O=C(CCc1ccc(Cl)cc1CN1CCC[C@H]1c1nc(C(=O)NCCCCC2CCCCC2)co1)NS(=O)(=O)C(F)(F)F nan
58932678 75288 0 None -301 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
CHEMBL2037290 75288 0 None -301 2 Rat 5.1 pEC50 = 5.1 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
22246956 196319 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 411 15 1 4 4.2 CCCCCC(=O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562291 196319 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 411 15 1 4 4.2 CCCCCC(=O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
69753740 140222 0 None -2454 5 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 390 9 3 5 2.8 O=C(O)CCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.5b00455
CHEMBL3805134 140222 0 None -2454 5 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 390 9 3 5 2.8 O=C(O)CCC[C@H]1CC[C@H]2[C@H](C[C@@H](O)[C@@H]2/C=C/[C@@H](O)COc2ccccc2)O1 10.1021/acsmedchemlett.5b00455
134155748 151169 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959653 151169 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assayAgonist activity at human recombinant EP2 receptor expressed in HEK-EBNA cells incubated for 30 mins by cAMP accumulation assay
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
89443669 147212 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 417 7 3 4 4.9 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1O nan
CHEMBL3928263 147212 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 417 7 3 4 4.9 Cc1cc(-c2cccc(F)c2)cc(CNc2c(F)ccc(OCC(=O)O)c2F)c1O nan
89443662 152888 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 412 7 2 4 4.7 N#Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3974557 152888 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 412 7 2 4 4.7 N#Cc1c(OCC(=O)O)ccc(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
1883 3082 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
1916 3082 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
5280360 3082 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
913 3082 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL548 3082 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
DB00917 3082 75 None -6 12 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assayAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
56835070 69471 0 None -112 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933722 69471 0 None -112 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
56835070 69471 0 None -112 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
CHEMBL1933722 69471 0 None -112 2 Rat 7.1 pEC50 = 7.1 Functional
Agonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassayAgonist activity at rat EP2 receptor expressed in CHO cells assessed as cAMP production after 10 mins by radioimmunoassay
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
51036042 176341 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 405 8 2 5 2.8 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(C)(=O)=O)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4554216 176341 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 405 8 2 5 2.8 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(C)(=O)=O)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4595541 176341 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 405 8 2 5 2.8 CC(C)(C)c1ccc(CN(Cc2cccc(NCC(=O)O)n2)S(C)(=O)=O)cc1 10.1021/acs.jmedchem.8b00808
66857975 164488 0 None -10 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 454 10 2 7 4.4 CC(O)(C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1)CC1CCCCC1 10.1016/j.bmc.2017.11.035
CHEMBL4214346 164488 0 None -10 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIAAgonist activity at recombinant human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level by EIA
ChEMBL 454 10 2 7 4.4 CC(O)(C/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1)CC1CCCCC1 10.1016/j.bmc.2017.11.035
11955133 145649 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 374 8 1 4 4.5 COC(=O)CCCCCC[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc(C(C)(C)C)cc1 nan
CHEMBL3915820 145649 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 374 8 1 4 4.5 COC(=O)CCCCCC[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc(C(C)(C)C)cc1 nan
9820676 195045 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 369 13 1 3 3.8 CCCCc1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549461 195045 0 None - 1 Rat 7.0 pEC50 = 7.0 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 369 13 1 3 3.8 CCCCc1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
89444029 149094 0 None - 1 Human 7.0 pEC50 = 7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1ccc(OCC(=O)O)c(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
CHEMBL3943109 149094 0 None - 1 Human 7.0 pEC50 = 7 Functional
Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.Cellular Functional Assay: Human CHO cells expressing the recombinant human prostanoid EP2 receptor were suspended in assay medium (HBSS buffer (Invitrogen) containing 20 mM HEPES (pH7.4) and 500 μM isobutyl-methylxanthine IBMX) and plated out to yield approximately 1×104 cells/well in a 96-well. Following this, cells were incubated with agonists for 30 min in the presence of the test compounds. For stimulated control measurements, separate assay wells contain 10 μM PGE2 (control specific agonist). All incubations were carried out at 37° C. in a 5% CO2 atmosphere. Following incubation, the amount of cAMP in each well was determined by HTRF method. The cells are lysed and the fluorescence acceptor (D2-labeled cAMP) and fluorescence donor (anti-cAMP antibody labeled with europium cryptate) are added.
ChEMBL 401 7 2 3 5.2 Cc1ccc(OCC(=O)O)c(F)c1NCc1cc(-c2cccc(F)c2)ccc1F nan
122180297 121647 0 None 4466 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586362 121647 0 None 4466 2 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
122180261 121613 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(C#N)c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586324 121613 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(C#N)c1)C2 10.1021/acs.jmedchem.5b00567
122180274 121623 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 385 4 0 5 4.4 COc1cc(-n2ccc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586337 121623 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 385 4 0 5 4.4 COc1cc(-n2ccc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180288 121638 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 386 3 0 4 5.7 Cc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586352 121638 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 386 3 0 4 5.7 Cc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180250 121602 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 432 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1OC)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586313 121602 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 432 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1OC)C2 10.1021/acs.jmedchem.5b00567
122180267 121617 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 360 4 0 4 4.5 COc1cc(-c2cccc(C)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586330 121617 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 360 4 0 4 4.5 COc1cc(-c2cccc(C)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180251 121603 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 432 5 0 6 5.4 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cn1 10.1021/acs.jmedchem.5b00567
CHEMBL3586314 121603 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 432 5 0 6 5.4 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cn1 10.1021/acs.jmedchem.5b00567
122180273 121622 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 386 4 0 6 3.8 COc1cc(-n2cnc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586336 121622 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 386 4 0 6 3.8 COc1cc(-n2cnc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
1987175 3794 31 None 1 5 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assayAntagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assay
ChEMBL 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 10.1021/ml400112h
9283 3794 31 None 1 5 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assayAntagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assay
ChEMBL 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 10.1021/ml400112h
CHEMBL1372836 3794 31 None 1 5 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assayAntagonist activity at human EP2 receptor overexpressed in rat C6 cells assessed as inhibition of PGE2-induced cAMP accumulation incubated for 10 mins prior to PGE2 addition measured after 40 mins by TR-FRET assay
ChEMBL 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 10.1021/ml400112h
122180270 121619 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 380 4 0 4 4.8 COc1cc(-c2cccc(Cl)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586333 121619 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 380 4 0 4 4.8 COc1cc(-c2cccc(Cl)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180282 121631 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 410 4 0 6 4.3 COc1cc(-n2ccc3cc(C#N)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586345 121631 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 410 4 0 6 4.3 COc1cc(-n2ccc3cc(C#N)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180295 121644 0 None 281 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586359 121644 0 None 281 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180296 121646 0 None 758 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586361 121646 0 None 758 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
122180265 121616 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 396 4 0 4 5.3 COc1cc(-c2cccc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586328 121616 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 396 4 0 4 5.3 COc1cc(-c2cccc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180276 121625 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 399 4 0 5 4.6 COc1cc(-c2cn(C)c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586339 121625 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 399 4 0 5 4.6 COc1cc(-c2cn(C)c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180289 121639 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586353 121639 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
56927669 121645 0 None -2 4 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 121645 0 None -2 4 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
30897313 121598 0 None -2 5 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 121598 0 None -2 5 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at rat EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
42484632 121599 5 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccn1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586310 121599 5 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccn1)C2 10.1021/acs.jmedchem.5b00567
122180275 121624 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 385 4 1 4 4.6 COc1cc(-c2c[nH]c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586338 121624 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 385 4 1 4 4.6 COc1cc(-c2c[nH]c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180278 121627 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3c(Cl)cccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586341 121627 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3c(Cl)cccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180286 121635 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 388 3 1 5 5.1 Oc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586349 121635 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 388 3 1 5 5.1 Oc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
56927669 121645 0 None 2 4 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 121645 0 None 2 4 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180283 121632 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 5 4.6 COc1cc(-n2ccc3cc(F)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586346 121632 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 5 4.6 COc1cc(-n2ccc3cc(F)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180280 121629 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3ccc(Cl)cc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586343 121629 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3ccc(Cl)cc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180263 121614 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2cc3ccccc3s2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586326 121614 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2cc3ccccc3s2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
56927669 121645 0 None -3 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 121645 0 None -3 4 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180252 121604 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 418 4 1 5 4.7 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(=O)[nH]c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586315 121604 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 418 4 1 5 4.7 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(=O)[nH]c1)C2 10.1021/acs.jmedchem.5b00567
122180284 121633 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 421 4 0 5 4.8 COc1cc(N2CCc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586347 121633 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 421 4 0 5 4.8 COc1cc(N2CCc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
30897313 121598 0 None 2 5 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 121598 0 None 2 5 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at mouse EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
30897313 121598 0 None -2 5 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 121598 0 None -2 5 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180272 121621 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 6 4.8 COc1cc(-c2nsc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586335 121621 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 6 4.8 COc1cc(-c2nsc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180279 121628 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586342 121628 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180249 121601 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 6 4.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cncnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586312 121601 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 403 4 0 6 4.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cncnc1)C2 10.1021/acs.jmedchem.5b00567
30956824 121600 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccncc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586311 121600 4 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccncc1)C2 10.1021/acs.jmedchem.5b00567
122180277 121626 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2cc(Cl)c3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586340 121626 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP productionAntagonist activity at human EP2 receptor overexpressed in human ECV304 cells assessed as inhibition of prostaglandin E2-induced cAMP production
ChEMBL 419 4 0 5 5.1 COc1cc(-n2cc(Cl)c3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
44365207 40696 0 None - 0 Human 6.6 pKd = 6.6 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 489 5 2 6 3.8 O=C(CCS(=O)(=O)Cc1ccco1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
CHEMBL148449 40696 0 None - 0 Human 6.6 pKd = 6.6 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 489 5 2 6 3.8 O=C(CCS(=O)(=O)Cc1ccco1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
38191 9913 16 None - 0 Human 6.2 pKd = 6.2 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 407 4 2 3 4.6 O=C(CCCCCl)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
CHEMBL114395 9913 16 None - 0 Human 6.2 pKd = 6.2 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 407 4 2 3 4.6 O=C(CCCCCl)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
44365227 121986 0 None - 0 Human 6.2 pKd = 6.2 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 473 5 2 5 4.1 O=C(CC[S+]([O-])Cc1ccco1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
CHEMBL359231 121986 0 None - 0 Human 6.2 pKd = 6.2 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 473 5 2 5 4.1 O=C(CC[S+]([O-])Cc1ccco1)NNC(=O)N1Cc2ccccc2Oc2ccc(Cl)cc21 10.1016/0960-894X(94)80027-8
1924 3542 39 None - 0 Human 8.1 pKd = 8.1 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10.1016/0960-894X(94)80027-8
9933831 3542 39 None - 0 Human 8.1 pKd = 8.1 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10.1016/0960-894X(94)80027-8
CHEMBL358653 3542 39 None - 0 Human 8.1 pKd = 8.1 Functional
Compound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uMCompound was tested for antagonism of Prostaglandin E2 receptor activity in guinea pig ileum assay based on the dose ratio at 3 uM
ChEMBL 457 5 2 5 5.1 O=C(NNC(=O)N1Cc2ccccc2Oc2c1cc(Cl)cc2)CCSCc1ccco1 10.1016/0960-894X(94)80027-8
119461 320 72 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at EP2 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP2 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
1896 320 72 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at EP2 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP2 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
CHEMBL1317823 320 72 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at EP2 receptor (unknown origin) by functional cAMP assayAntagonist activity at EP2 receptor (unknown origin) by functional cAMP assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
9817405 165403 5 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/s0960-894x(01)00056-7
CHEMBL423815 165403 5 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/s0960-894x(01)00056-7
10402929 57543 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(01)00056-7
CHEMBL166351 57543 0 None - 0 Human 4.9 pKi = 4.9 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(01)00056-7
44377464 120085 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)cc1Cl 10.1016/s0960-894x(01)00056-7
CHEMBL350832 120085 0 None - 0 Human 5.4 pKi = 5.4 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 306 4 1 1 4.7 O=C(O)/C=C/c1ccccc1Cc1ccc(Cl)cc1Cl 10.1016/s0960-894x(01)00056-7
9817292 57227 0 None - 0 Human 4.4 pKi = 4.4 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 284 5 1 2 4.1 CSc1ccc(Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/s0960-894x(01)00056-7
CHEMBL165010 57227 0 None - 0 Human 4.4 pKi = 4.4 Functional
Antagonistic activity at Prostanoid EP2 receptor in human was determinedAntagonistic activity at Prostanoid EP2 receptor in human was determined
ChEMBL 284 5 1 2 4.1 CSc1ccc(Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/s0960-894x(01)00056-7
10483360 199228 28 None - 4 Human 4.4 pKi = 4.4 Functional
Inhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP productionInhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production
ChEMBL 580 12 3 6 5.8 CCCCNC(=O)c1ccc(Oc2ccc(CC(=O)O)cc2OC)c(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2009.09.052
CHEMBL589973 199228 28 None - 4 Human 4.4 pKi = 4.4 Functional
Inhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP productionInhibition of EP2 expressed in HEK293 cells assessed as inhibition of PGE2-induced cAMP production
ChEMBL 580 12 3 6 5.8 CCCCNC(=O)c1ccc(Oc2ccc(CC(=O)O)cc2OC)c(NS(=O)(=O)c2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2009.09.052
138 3081 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 3081 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 3081 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 3081 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 3081 88 None -4 10 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
44230999 167446 26 None - 1 Human 8.1 pEC50 = 8.1 Functional
activity measured for the active metabolite (omidenepag)activity measured for the active metabolite (omidenepag)
Drug Central 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 None
CHEMBL4297666 167446 26 None - 1 Human 8.1 pEC50 = 8.1 Functional
activity measured for the active metabolite (omidenepag)activity measured for the active metabolite (omidenepag)
Drug Central 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 None
1929 1605 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
9890801 1605 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
CHEMBL563646 1605 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
DB12022 1605 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
1883 3082 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1916 3082 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5280360 3082 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
913 3082 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
CHEMBL548 3082 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
DB00917 3082 75 None -2 12 Rat 8.1 pIC50 = 8.1 Functional
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1929 1605 55 None 2 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
9890801 1605 55 None 2 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
CHEMBL563646 1605 55 None 2 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
DB12022 1605 55 None 2 2 Rat 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 19250823
18376177 3753 50 None -1 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
5816 3753 50 None -1 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
CHEMBL2107783 3753 50 None -1 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
DB12623 3753 50 None -1 2 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
18376177 3753 50 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
5816 3753 50 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
CHEMBL2107783 3753 50 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
DB12623 3753 50 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 21376717
12520 3796 0 None - 1 Human 7.9 pKB = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 5 3 2 3.8 CC1=C(CCNC(=O)C2=CC=C(C=C2)C3=CNC=N3)C4=C(N1)C=CC=C4 35187419
12520 3796 0 None - 1 Human 7.9 pKB = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 5 3 2 3.8 CC1=C(CCNC(=O)C2=CC=C(C=C2)C3=CNC=N3)C4=C(N1)C=CC=C4 36654746
155128767 3796 0 None - 1 Human 7.9 pKB = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 5 3 2 3.8 CC1=C(CCNC(=O)C2=CC=C(C=C2)C3=CNC=N3)C4=C(N1)C=CC=C4 35187419
155128767 3796 0 None - 1 Human 7.9 pKB = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 344 5 3 2 3.8 CC1=C(CCNC(=O)C2=CC=C(C=C2)C3=CNC=N3)C4=C(N1)C=CC=C4 36654746
10603 3792 0 None 537 3 Human 8.0 pKB = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
145996528 3792 0 None 537 3 Human 8.0 pKB = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
CHEMBL4552900 3792 0 None 537 3 Human 8.0 pKB = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 400 6 3 5 4.0 Cc1cc(Nc2ncc(cn2)C(=O)NCCc2c(C)[nH]c3c2cccc3)nc(c1)C 31904232
1987175 3794 31 None 1 5 Human 8.1 pKB = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286
9283 3794 31 None 1 5 Human 8.1 pKB = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286
CHEMBL1372836 3794 31 None 1 5 Human 8.1 pKB = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 3 7 3.6 CCc1nnc(s1)NS(=O)(=O)c1ccc(cc1)NC(=S)NC(=O)/C=C/c1ccc(cc1)F 23914286
25114442 3061 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 21595651
25114442 3061 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
5817 3061 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 21595651
5817 3061 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
CHEMBL3286797 3061 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 21595651
CHEMBL3286797 3061 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
DB12024 3061 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 21595651
DB12024 3061 56 None -1 3 Human 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
25114442 3061 56 None 1 3 Mouse 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
5817 3061 56 None 1 3 Mouse 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
CHEMBL3286797 3061 56 None 1 3 Mouse 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
DB12024 3061 56 None 1 3 Mouse 8.3 pKB = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 22747912
46213069 3063 0 None - 1 Human 8.5 pKB = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 23786281
8538 3063 0 None - 1 Human 8.5 pKB = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 23786281
CHEMBL5285583 3063 0 None - 1 Human 8.5 pKB = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 23786281
8546 3795 0 None - 1 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 377 9 1 3 4.5 CCN(c1ccc(cc1)CC(=O)NCCCn1c(C)cc2c1cccc2)CC 24937185
91827368 3795 0 None - 1 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 377 9 1 3 4.5 CCN(c1ccc(cc1)CC(=O)NCCCn1c(C)cc2c1cccc2)CC 24937185
5818 3793 47 None 1096 2 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 22323596
5886965 3793 47 None 1096 2 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 22323596
CHEMBL1368005 3793 47 None 1096 2 Human 8.6 pKB = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 394 8 1 5 3.8 COc1cc(/C=C/C(=O)NCCn2c(C)cc3c2cccc3)cc(c1OC)OC 22323596




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

11855868 152544 0 None - 1 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 152544 0 None - 1 Human 9.8 pEC50 = 9.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
127037150 137560 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 426 12 2 6 4.1 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3754586 137560 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 426 12 2 6 4.1 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
16725337 149601 0 None - 1 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 149601 0 None - 1 Human 9.2 pEC50 = 9.2 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
59554827 137293 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 426 11 2 6 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3752377 137293 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 426 11 2 6 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
11502897 142793 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 142793 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855865 153277 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 153277 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855870 146280 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 146280 0 None - 1 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
1932 2942 5 None 1 6 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
5311228 2942 5 None 1 6 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
CHEMBL3286796 2942 5 None 1 6 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
90054482 143917 0 None - 0 Human 6.0 pEC50 = 6 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 463 10 2 4 4.4 C[C@@H](Cc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3902065 143917 0 None - 0 Human 6.0 pEC50 = 6 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 463 10 2 4 4.4 C[C@@H](Cc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
90054490 152190 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3968443 152190 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
127051063 140322 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3806284 140322 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 10.1021/acsmedchemlett.5b00455
11855590 144374 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3905811 144374 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 387 8 2 5 3.4 CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
90054450 143776 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 493 13 2 4 5.4 C[C@@H](CCCc1ccccc1)[C@H](O)CC[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3900979 143776 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 493 13 2 4 5.4 C[C@@H](CCCc1ccccc1)[C@H](O)CC[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
11855591 144436 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 144436 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
72948479 153033 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3975743 153033 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
70667255 151474 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3962183 151474 0 None - 1 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
90054430 149364 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 505 13 2 4 5.6 C[C@@H](CCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3945327 149364 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 505 13 2 4 5.6 C[C@@H](CCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
5283056 202860 34 None - 0 Human 7.8 pEC50 = 7.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O nan
CHEMBL62570 202860 34 None - 0 Human 7.8 pEC50 = 7.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O nan
66858111 137451 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 488 11 2 7 4.5 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCc3ccccc3)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3753622 137451 0 None - 1 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 488 11 2 7 4.5 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCc3ccccc3)CCC2)n1 10.1016/j.bmcl.2015.12.039
72950425 143050 0 None - 1 Human 5.8 pEC50 = 5.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3895047 143050 0 None - 1 Human 5.8 pEC50 = 5.8 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 419 8 2 3 3.5 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
11328569 137468 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 456 12 2 8 3.3 COCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753788 137468 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 456 12 2 8 3.3 COCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
11855324 142605 0 None - 1 Human 6.7 pEC50 = 6.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 142605 0 None - 1 Human 6.7 pEC50 = 6.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
72950929 146582 0 None - 1 Human 5.7 pEC50 = 5.7 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
CHEMBL3923027 146582 0 None - 1 Human 5.7 pEC50 = 5.7 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 395 10 2 3 3.7 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 nan
1883 3082 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
1916 3082 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
5280360 3082 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
913 3082 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
CHEMBL548 3082 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
DB00917 3082 75 None -6 24 Human 8.7 pEC50 = 8.7 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
126495400 139321 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3792632 139321 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
127026955 139450 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 437 5 2 6 4.4 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl 10.1016/j.bmcl.2016.03.110
CHEMBL3794016 139450 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 437 5 2 6 4.4 Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl 10.1016/j.bmcl.2016.03.110
18376177 3753 50 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
5816 3753 50 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
CHEMBL2107783 3753 50 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
DB12623 3753 50 None - 1 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
11294085 137252 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3751951 137252 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 458 12 2 7 4.0 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCCCF)CCC2)n1 10.1016/j.bmcl.2015.12.039
59554822 137394 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 440 11 2 7 4.0 CCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753221 137394 0 None - 1 Human 8.5 pEC50 = 8.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 440 11 2 7 4.0 CCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
127051062 140274 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3Cl)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805767 140274 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 409 5 2 6 3.8 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3Cl)O2)n1 10.1021/acsmedchemlett.5b00455
72950089 150591 0 None -1621 3 Human 6.7 pEC50 = 6.7 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
CHEMBL3955128 150591 0 None -1621 3 Human 6.7 pEC50 = 6.7 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O nan
66857670 137401 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 436 9 2 7 3.3 CC#CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753268 137401 0 None - 1 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 436 9 2 7 3.3 CC#CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
57529188 147195 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 147195 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855866 144602 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 144602 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855325 144691 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 144691 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855324 142605 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 142605 0 None - 1 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
127026652 137482 0 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 456 12 2 8 3.3 CCOCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3753898 137482 0 None - 1 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 456 12 2 8 3.3 CCOCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
127026956 139426 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cc(Cl)c(Cl)cc3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793862 139426 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 477 5 2 6 5.1 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cc(Cl)c(Cl)cc3Cl)O2)n1 10.1016/j.bmcl.2016.03.110
9807448 203172 0 None 1 4 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1021/jm401431x
CHEMBL64246 203172 0 None 1 4 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1021/jm401431x
11855867 145983 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 145983 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
1892 747 20 None -2 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
25886893 747 20 None -2 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
CHEMBL1628262 747 20 None -2 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
72948663 145734 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3916499 145734 0 None - 1 Human 6.5 pEC50 = 6.5 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 415 11 2 4 4.1 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
5311035 97803 29 None -4 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1021/jm401431x
CHEMBL271896 97803 29 None -4 9 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1021/jm401431x
1883 3082 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
1916 3082 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
5280360 3082 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
913 3082 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
CHEMBL548 3082 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
DB00917 3082 75 None -6 24 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
66857738 137300 0 None - 1 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 468 10 2 7 4.7 CC(C)(C)CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
CHEMBL3752435 137300 0 None - 1 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 468 10 2 7 4.7 CC(C)(C)CCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 10.1016/j.bmcl.2015.12.039
127050451 140221 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(OC(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805122 140221 0 None - 0 Human 5.4 pEC50 = 5.4 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(OC(F)(F)F)cc3)O2)n1 10.1021/acsmedchemlett.5b00455
1929 1605 55 None -11 2 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
9890801 1605 55 None -11 2 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
CHEMBL563646 1605 55 None -11 2 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
DB12022 1605 55 None -11 2 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
11362836 137296 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 446 12 2 7 3.8 CC(C)(CCCCF)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3752406 137296 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 446 12 2 7 3.8 CC(C)(CCCCF)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
11855325 144691 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 144691 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855593 146834 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 425 11 2 4 4.7 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2cccc(C(=O)O)c2)cc1 nan
CHEMBL3924987 146834 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 425 11 2 4 4.7 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2cccc(C(=O)O)c2)cc1 nan
11855588 147357 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3929446 147357 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 345 8 1 2 4.9 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2CCCCCCC(=O)O)cc1 nan
5283086 203310 24 None - 5 Human 7.2 pEC50 = 7.2 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O nan
CHEMBL64804 203310 24 None - 5 Human 7.2 pEC50 = 7.2 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O nan
11156167 137520 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 494 11 2 7 5.2 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCC3CCCCC3)CCC2)n1 10.1016/j.bmcl.2015.12.039
CHEMBL3754197 137520 0 None - 1 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 494 11 2 7 5.2 O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCC3CCCCC3)CCC2)n1 10.1016/j.bmcl.2015.12.039
90054537 148403 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3937596 148403 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 491 12 2 4 5.2 C[C@@H](CCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
127051656 140294 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(OC(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3805981 140294 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 459 6 2 7 4.0 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(OC(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
59554824 137475 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 428 11 2 7 3.9 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
CHEMBL3753853 137475 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor
ChEMBL 428 11 2 7 3.9 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1COC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2015.12.039
90054519 151986 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 477 11 2 4 4.8 C[C@@H](CCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3966743 151986 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 477 11 2 4 4.8 C[C@@H](CCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
72948294 149957 0 None - 1 Human 6.1 pEC50 = 6.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3949856 149957 0 None - 1 Human 6.1 pEC50 = 6.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 439 9 2 4 4.0 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
90054392 142918 0 None - 0 Human 4.1 pEC50 = 4.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
CHEMBL3893847 142918 0 None - 0 Human 4.1 pEC50 = 4.1 Binding
SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.
ChEMBL 519 14 2 4 6.0 C[C@@H](CCCCCc1ccccc1)[C@@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 nan
11855871 146408 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 146408 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855594 152980 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 152980 0 None - 1 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
127027874 139363 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
CHEMBL3793045 139363 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1021/acsmedchemlett.5b00455
127027874 139363 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
CHEMBL3793045 139363 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assayAgonist activity at human EP2 receptor expressed in HEK293 cells after 24 hrs beta-arrestin recruitment assay
ChEMBL 443 5 2 6 4.2 O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3cccc(C(F)(F)F)c3)O2)n1 10.1016/j.bmcl.2016.03.110
10339756 143085 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
CHEMBL3895324 143085 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
118689427 151852 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10N HCl is added to achieve a pH of 7.4). The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 °C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10N HCl is added to achieve a pH of 7.4). The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 °C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
CHEMBL3965497 151852 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10N HCl is added to achieve a pH of 7.4). The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 °C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10N HCl is added to achieve a pH of 7.4). The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 °C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H−] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations were for 60 min at 25 °C. and were terminated by the addition of 4 ml of ice-cold 50 mM TRIS-HCl, followed by rapid filtration through Whatman GF/B filters and three additional 4 ml washes in a cell harvester (Brandel). Competition studies were performed using a final concentration of 5 nM [3H]-PGE2, or 5 nM [3H] 17-phenyl PGF2a and non-specific binding determined with 10^−5M of unlabeled PGE2, or 17-phenyl PGF2a, according to receptor subtype studied.
ChEMBL 519 10 2 6 3.8 O=C(O)c1ccc(CCCN2[C@@H](/C=C/C(O)Cc3cccc(OC(F)(F)F)c3)CCS2(=O)=O)s1 nan
56927669 121645 0 None - 0 Mouse 8.0 pIC50 = 8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 121645 0 None - 0 Mouse 8.0 pIC50 = 8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
56927669 121645 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 121645 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
10315 2926 28 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
44230575 2926 28 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
CHEMBL3707245 2926 28 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
122180251 121603 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 432 5 0 6 5.4 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cn1 10.1021/acs.jmedchem.5b00567
CHEMBL3586314 121603 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 432 5 0 6 5.4 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cn1 10.1021/acs.jmedchem.5b00567
122180259 121611 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 479 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586322 121611 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 479 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1021/acs.jmedchem.5b00567
122180261 121613 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(C#N)c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586324 121613 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(C#N)c1)C2 10.1021/acs.jmedchem.5b00567
122180282 121631 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 410 4 0 6 4.3 COc1cc(-n2ccc3cc(C#N)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586345 121631 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 410 4 0 6 4.3 COc1cc(-n2ccc3cc(C#N)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
30897313 121598 0 None - 0 Mouse 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 121598 0 None - 0 Mouse 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from mouse EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
30897313 121598 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 121598 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from rat EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180253 121605 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 401 4 0 4 6.0 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586316 121605 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 401 4 0 4 6.0 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccc1)C2 10.1021/acs.jmedchem.5b00567
122180271 121620 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2ccc(Cl)cc2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586334 121620 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2ccc(Cl)cc2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
44564990 192650 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL521777 192650 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 538 6 1 5 5.7 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(F)c3)cccc21 10.1016/j.bmcl.2008.12.112
122180276 121625 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 399 4 0 5 4.6 COc1cc(-c2cn(C)c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586339 121625 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 399 4 0 5 4.6 COc1cc(-c2cn(C)c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180285 121634 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 372 3 0 4 5.4 c1cncc(CN2CCOc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586348 121634 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 372 3 0 4 5.4 c1cncc(CN2CCOc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
44409693 166098 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 429 11 2 4 4.3 CCc1ccc(CC(O)CC[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)cc1 10.1016/j.bmcl.2006.01.018
CHEMBL425950 166098 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 429 11 2 4 4.3 CCc1ccc(CC(O)CC[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)cc1 10.1016/j.bmcl.2006.01.018
122180269 121618 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2ccccc2Cl)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586332 121618 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2ccccc2Cl)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
44409907 77050 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2ccc(F)cc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL207237 77050 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2ccc(F)cc2)s1 10.1016/j.bmcl.2006.01.018
44570000 178650 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL467632 178650 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 544 7 2 5 6.2 O=C(COc1cccc2[nH]cc(Cc3ccc4ccccc4c3)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
44409739 139660 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2-c2ccccc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL379785 139660 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2-c2ccccc2)s1 10.1016/j.bmcl.2006.01.018
44157014 192617 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL521609 192617 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 518 6 1 5 5.9 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc4ccccc4c3)cccc21 10.1016/j.bmcl.2008.12.112
58905349 156278 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 400 6 2 4 4.3 O=C(O)c1ccc(CNC(=O)c2cc(Cl)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4065183 156278 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 400 6 2 4 4.3 O=C(O)c1ccc(CNC(=O)c2cc(Cl)cnc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4552554 214001 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000342a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000342a PTGER2
ChEMBL None None None O=C(c1ccc(F)cc1)N1CC(COc2ccc(Br)cc2)(C(=O)O)C1 10.6019/CHEMBL5210307
10047541 132510 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 416 13 4 6 3.8 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccs1 10.1021/jm990542v
CHEMBL369797 132510 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 416 13 4 6 3.8 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccs1 10.1021/jm990542v
122180293 121643 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 416 4 0 5 4.9 COc1cc(-c2csc3ccccc23)cc2c1OCC(=O)N(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586357 121643 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 416 4 0 5 4.9 COc1cc(-c2csc3ccccc23)cc2c1OCC(=O)N(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
11955294 144768 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 380 8 3 3 4.2 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
CHEMBL3909111 144768 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 380 8 3 3 4.2 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3O)[C@H](O)C[C@H]1Cl nan
11955240 147990 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 352 8 3 3 3.5 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(CO)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3934202 147990 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 352 8 3 3 3.5 O=C(O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(CO)cc2)[C@H](O)C[C@H]1Cl nan
44409910 140909 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(-c3ccccc3)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL382197 140909 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 477 11 2 4 5.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(-c3ccccc3)c2)s1 10.1016/j.bmcl.2006.01.018
25195248 182935 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity to human EP2 receptor by radioligand binding assayBinding affinity to human EP2 receptor by radioligand binding assay
ChEMBL 540 6 1 4 4.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479263 182935 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity to human EP2 receptor by radioligand binding assayBinding affinity to human EP2 receptor by radioligand binding assay
ChEMBL 540 6 1 4 4.6 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3cc(F)c(F)cc3F)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
118756024 121637 4 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 416 5 0 5 5.8 CCOc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586350 121637 4 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 416 5 0 5 5.8 CCOc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180286 121635 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 388 3 1 5 5.1 Oc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586349 121635 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 388 3 1 5 5.1 Oc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
10339756 143085 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
CHEMBL3895324 143085 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.Radioligand Binding: HEK-293 cells stably expressing the human or feline FP receptor, or EP1, EP2, EP3, or EP4 receptors were washed with TME buffer, scraped from the bottom of the flasks, and homogenized for 30 sec using a Brinkman PT 10/35 polytron. TME buffer was added to achieve a final 40 ml volume in the centrifuge tubes (the composition of TME is 100 mM TRIS base, 20 mM MgCl2, 2M EDTA; 10 N HCl is added to achieve a pH of 7.4).The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4 C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2 (5 nM) were performed in a 100 ul volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell.
ChEMBL 380 12 3 4 3.9 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C(C)(C)C(=O)[C@@H]1C/C=C\CCCC(=O)O nan
122180264 121615 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 346 4 0 4 4.2 COc1cc(-c2ccccc2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586327 121615 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 346 4 0 4 4.2 COc1cc(-c2ccccc2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180267 121617 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 360 4 0 4 4.5 COc1cc(-c2cccc(C)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586330 121617 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 360 4 0 4 4.5 COc1cc(-c2cccc(C)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
11955255 146257 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 8 3 3 5.0 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920560 146257 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 8 3 3 5.0 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
11495634 14905 13 None - 4 Human 5.8 pIC50 = 5.8 Binding
Inhibition of EP2 receptorInhibition of EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
CHEMBL1207972 14905 13 None - 4 Human 5.8 pIC50 = 5.8 Binding
Inhibition of EP2 receptorInhibition of EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
CHEMBL467114 14905 13 None - 4 Human 5.8 pIC50 = 5.8 Binding
Inhibition of EP2 receptorInhibition of EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2009.02.112
9820676 195045 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 369 13 1 3 3.8 CCCCc1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549461 195045 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 369 13 1 3 3.8 CCCCc1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
122180290 121640 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 370 3 0 3 5.9 c1cncc(CN2CCCc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586354 121640 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 370 3 0 3 5.9 c1cncc(CN2CCCc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
11575201 157422 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4078648 157422 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 C[C@H](NC(=O)c1cc(Cl)ccc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
72695027 106266 0 None -28 2 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3115074 106266 0 None -28 2 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3138992 106266 0 None -28 2 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
122180256 121608 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 431 5 0 5 6.0 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cc1 10.1021/acs.jmedchem.5b00567
CHEMBL3586319 121608 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 431 5 0 5 6.0 COc1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cc1 10.1021/acs.jmedchem.5b00567
11955406 146104 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 376 10 3 4 3.4 CC(C)(CO)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3919393 146104 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 376 10 3 4 3.4 CC(C)(CO)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
44409738 139606 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL379746 139606 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmcl.2006.01.018
11577792 159318 19 None -1819 5 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 159318 19 None -1819 5 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
46879894 6181 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human EP2 receptor by radioligand displacement assayBinding affinity to human EP2 receptor by radioligand displacement assay
ChEMBL 565 6 1 5 7.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
CHEMBL1081186 6181 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Binding affinity to human EP2 receptor by radioligand displacement assayBinding affinity to human EP2 receptor by radioligand displacement assay
ChEMBL 565 6 1 5 7.2 Cc1cn(Cc2ccc(Cl)cc2Cl)c2c(-c3cc(NS(=O)(=O)c4ccc(F)c(F)c4)no3)cc(F)cc12 10.1016/j.bmcl.2009.09.084
122180297 121647 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586362 121647 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 437 3 1 4 4.9 C[C@@H]1COc2c(Cl)cc(-n3ccc4cc(F)ccc43)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
1883 3082 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
1916 3082 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
5280360 3082 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
913 3082 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
CHEMBL548 3082 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
DB00917 3082 75 None -6 24 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human EP2 receptor (unknown origin) by radioligand displacement assayBinding affinity to human EP2 receptor (unknown origin) by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2013.03.016
1883 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
1916 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
5280360 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
913 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
CHEMBL548 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
DB00917 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.11.014
1883 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
1916 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
5280360 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
913 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
CHEMBL548 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
DB00917 3082 75 None -6 24 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2016.03.006
122180249 121601 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 6 4.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cncnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586312 121601 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 6 4.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cncnc1)C2 10.1021/acs.jmedchem.5b00567
122180295 121644 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586359 121644 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 422 3 1 4 5.3 O=c1cc(CN2CCOc3c(Cl)cc(-c4csc5ccccc45)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
30956824 121600 4 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccncc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586311 121600 4 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccncc1)C2 10.1021/acs.jmedchem.5b00567
122180250 121602 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 432 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1OC)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586313 121602 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 432 5 0 6 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1OC)C2 10.1021/acs.jmedchem.5b00567
122180252 121604 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 418 4 1 5 4.7 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(=O)[nH]c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586315 121604 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 418 4 1 5 4.7 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(=O)[nH]c1)C2 10.1021/acs.jmedchem.5b00567
122180288 121638 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 386 3 0 4 5.7 Cc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586352 121638 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 386 3 0 4 5.7 Cc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
9885481 195383 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL551951 195383 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 365 16 2 4 3.0 CCCCCC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
11955276 150751 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 358 7 3 4 2.9 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc2c(c1)CCC2O nan
CHEMBL3956391 150751 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 358 7 3 4 2.9 O=C(O)CCC/C=C\C[C@H]1C(=O)C[C@@H](O)[C@@H]1c1ccc2c(c1)CCC2O nan
44570666 183270 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human EP2 receptor by radioligand binding assayBinding affinity to human EP2 receptor by radioligand binding assay
ChEMBL 522 6 1 4 4.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
CHEMBL479664 183270 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity to human EP2 receptor by radioligand binding assayBinding affinity to human EP2 receptor by radioligand binding assay
ChEMBL 522 6 1 4 4.5 CC12CCCC(/C=C/C(=O)NS(=O)(=O)c3ccc(F)c(F)c3)=C1N(Cc1ccc(F)c(F)c1)C(=O)C2 10.1016/j.bmcl.2008.12.027
58905388 158666 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 383 6 2 3 4.4 O=C(O)c1ccc(CNC(=O)c2cc(F)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4092846 158666 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 383 6 2 3 4.4 O=C(O)c1ccc(CNC(=O)c2cc(F)ccc2Oc2ccc(F)cc2)cc1 10.1016/j.bmcl.2017.01.067
10670992 60056 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 444 13 4 5 4.4 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccc(Cl)c1 10.1021/jm990542v
CHEMBL173680 60056 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 444 13 4 5 4.4 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CCC(O)CSc1cccc(Cl)c1 10.1021/jm990542v
15486806 100487 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 392 13 4 4 3.5 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCc1ccccc1 10.1021/jm990542v
CHEMBL290969 100487 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 392 13 4 4 3.5 O=C(O)CCCCCC[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCc1ccccc1 10.1021/jm990542v
45270403 195117 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 351 14 2 4 2.5 CC(C)CC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL550015 195117 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 351 14 2 4 2.5 CC(C)CC(O)CCCN(CCCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
10180 3592 58 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 402 3 1 3 4.2 Fc1ccc2c(c1)c1CN(CCc1n2CC(=O)O)C(=O)c1cccc2c1cccc2 10.1021/jm400122f
49843471 3592 58 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 402 3 1 3 4.2 Fc1ccc2c(c1)c1CN(CCc1n2CC(=O)O)C(=O)c1cccc2c1cccc2 10.1021/jm400122f
CHEMBL2386081 3592 58 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 402 3 1 3 4.2 Fc1ccc2c(c1)c1CN(CCc1n2CC(=O)O)C(=O)c1cccc2c1cccc2 10.1021/jm400122f
DB12562 3592 58 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 402 3 1 3 4.2 Fc1ccc2c(c1)c1CN(CCc1n2CC(=O)O)C(=O)c1cccc2c1cccc2 10.1021/jm400122f
45271237 195099 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.0 CCCCc1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549870 195099 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.0 CCCCc1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
122180275 121624 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 4 1 4 4.6 COc1cc(-c2c[nH]c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586338 121624 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 4 1 4 4.6 COc1cc(-c2c[nH]c3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
71733910 90335 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 436 3 1 3 4.9 O=C(O)Cn1c2c(c3cc(F)cc(Cl)c31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
CHEMBL2385900 90335 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 436 3 1 3 4.9 O=C(O)Cn1c2c(c3cc(F)cc(Cl)c31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
18376258 195902 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 465 9 1 3 5.4 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559065 195902 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 465 9 1 3 5.4 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
122180263 121614 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2cc3ccccc3s2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586326 121614 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2cc3ccccc3s2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
22246983 195862 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 389 11 1 3 4.2 CS(=O)(=O)N(CCCCCCC(=O)O)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL558671 195862 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 389 11 1 3 4.2 CS(=O)(=O)N(CCCCCCC(=O)O)Cc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2009.01.059
1883 3082 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
1916 3082 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
5280360 3082 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
913 3082 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
CHEMBL548 3082 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
DB00917 3082 75 None -6 24 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
122180284 121633 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 421 4 0 5 4.8 COc1cc(N2CCc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586347 121633 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 421 4 0 5 4.8 COc1cc(N2CCc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180265 121616 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 396 4 0 4 5.3 COc1cc(-c2cccc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586328 121616 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 396 4 0 4 5.3 COc1cc(-c2cccc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180274 121623 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 4 0 5 4.4 COc1cc(-n2ccc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586337 121623 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 4 0 5 4.4 COc1cc(-n2ccc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180254 121606 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 435 4 0 4 6.6 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(Cl)cc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586317 121606 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 435 4 0 4 6.6 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(Cl)cc1)C2 10.1021/acs.jmedchem.5b00567
122180255 121607 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 415 4 0 4 6.3 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(C)cc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586318 121607 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 415 4 0 4 6.3 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(C)cc1)C2 10.1021/acs.jmedchem.5b00567
122180260 121612 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 435 4 0 4 6.6 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(Cl)c1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586323 121612 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 435 4 0 4 6.6 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccc(Cl)c1)C2 10.1021/acs.jmedchem.5b00567
45269575 196405 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 12 1 4 4.0 CCCCc1ccc(CN(CCCOc2cccc(C(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562825 196405 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 12 1 4 4.0 CCCCc1ccc(CN(CCCOc2cccc(C(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
45271234 195083 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 405 11 1 4 3.5 CCCCc1ccc(CN(Cc2ccccc2OCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549663 195083 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 405 11 1 4 3.5 CCCCc1ccc(CN(Cc2ccccc2OCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
45268716 195998 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 389 10 1 3 4.0 CCCCc1ccc(CN(c2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559955 195998 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 389 10 1 3 4.0 CCCCc1ccc(CN(c2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
16664733 154827 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of human recombinant EP2 receptor expressed in 293EBNA cellsInhibition of human recombinant EP2 receptor expressed in 293EBNA cells
ChEMBL 483 9 3 5 4.3 CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)N[C@@H](Cc3ccccc3)C(=O)O)cc2)c1 10.1016/j.bmcl.2006.12.025
CHEMBL400404 154827 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of human recombinant EP2 receptor expressed in 293EBNA cellsInhibition of human recombinant EP2 receptor expressed in 293EBNA cells
ChEMBL 483 9 3 5 4.3 CC(=O)Nc1cccc(-c2ccc(Cc3ocnc3C(=O)N[C@@H](Cc3ccccc3)C(=O)O)cc2)c1 10.1016/j.bmcl.2006.12.025
45266955 195645 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 485 10 1 6 3.7 Cn1ccnc1CS(=O)(=O)N(Cc1ccc(C(C)(C)C)cc1)Cc1cccc(OCC(=O)O)c1 10.1016/j.bmcl.2009.01.059
CHEMBL556416 195645 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 485 10 1 6 3.7 Cn1ccnc1CS(=O)(=O)N(Cc1ccc(C(C)(C)C)cc1)Cc1cccc(OCC(=O)O)c1 10.1016/j.bmcl.2009.01.059
44627515 196837 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
CHEMBL565799 196837 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 572 6 1 5 7.2 Cc1cn(Cc2ccc3ccccc3c2)c2c(/C=C/C(=O)NS(=O)(=O)c3cc(Cl)c(Cl)s3)cc(F)cc12 10.1021/jm9005912
11618662 158822 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 421 6 2 5 4.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C#N)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4094572 158822 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 421 6 2 5 4.6 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(C#N)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
11955257 153886 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 410 9 3 3 5.3 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3983069 153886 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 410 9 3 3 5.3 CC(C)(C)C(O)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
1883 3082 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
1916 3082 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
5280360 3082 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
913 3082 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
CHEMBL548 3082 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
DB00917 3082 75 None -6 24 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm9018756
1894 957 41 None - 5 Human 5.4 pIC50 = 5.4 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
5311053 957 41 None - 5 Human 5.4 pIC50 = 5.4 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
CHEMBL37853 957 41 None - 5 Human 5.4 pIC50 = 5.4 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
DB11507 957 41 None - 5 Human 5.4 pIC50 = 5.4 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 424 11 4 5 3.2 OC(=O)CCC/C=C\C[C@H]1[C@@H](O)C[C@H]([C@@H]1/C=C/[C@H](COc1cccc(c1)Cl)O)O 10.1021/jm990542v
118175009 136685 0 None -812 2 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3740325 136685 0 None -812 2 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
45271238 195641 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 8 1 3 4.0 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL556333 195641 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 8 1 3 4.0 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
1883 3082 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
1916 3082 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
5280360 3082 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
913 3082 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
CHEMBL548 3082 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
DB00917 3082 75 None -6 24 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.8b00808
122180272 121621 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 6 4.8 COc1cc(-c2nsc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586335 121621 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 6 4.8 COc1cc(-c2nsc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180278 121627 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3c(Cl)cccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586341 121627 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3c(Cl)cccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180292 121642 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 3 0 4 5.4 CN1CCN(Cc2cccnc2)Cc2cc(-c3csc4ccccc34)ccc21 10.1021/acs.jmedchem.5b00567
CHEMBL3586356 121642 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 385 3 0 4 5.4 CN1CCN(Cc2cccnc2)Cc2cc(-c3csc4ccccc34)ccc21 10.1021/acs.jmedchem.5b00567
11296282 1409 32 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
5822 1409 32 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
CHEMBL565591 1409 32 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 590 6 1 5 7.3 Clc1ccc(c(c1)Cl)Cn1cc(c2c1c(/C=C/C(=O)NS(=O)(=O)c1sc(c(c1)Cl)Cl)cc(c2)F)C 10.1021/jm9005912
44230999 167446 26 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
CHEMBL4297666 167446 26 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 520 11 1 9 3.4 CC(C)OC(=O)CNc1cccc(CN(Cc2ccc(-n3cccn3)cc2)S(=O)(=O)c2cccnc2)n1 10.1021/acs.jmedchem.8b00808
11955235 152751 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 9 3 3 4.2 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3973312 152751 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 9 3 3 4.2 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
44564571 186815 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL489310 186815 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
11683088 158978 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4096216 158978 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1ccc(F)cc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
162671048 182807 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from full-length recombinant human EP2 receptor expressed in HEK293 cell membranes measured after 120 mins by scintillation counting methodDisplacement of [3H]prostaglandin E2 from full-length recombinant human EP2 receptor expressed in HEK293 cell membranes measured after 120 mins by scintillation counting method
ChEMBL 451 5 1 4 5.4 Cc1c(-c2cccs2)nc2ccc(Br)cc2c1C(=O)NCCc1cccnc1 10.1021/acs.jmedchem.0c00834
CHEMBL4790821 182807 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]prostaglandin E2 from full-length recombinant human EP2 receptor expressed in HEK293 cell membranes measured after 120 mins by scintillation counting methodDisplacement of [3H]prostaglandin E2 from full-length recombinant human EP2 receptor expressed in HEK293 cell membranes measured after 120 mins by scintillation counting method
ChEMBL 451 5 1 4 5.4 Cc1c(-c2cccs2)nc2ccc(Br)cc2c1C(=O)NCCc1cccnc1 10.1021/acs.jmedchem.0c00834
9934368 138921 11 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to rat EP2 receptorBinding affinity to rat EP2 receptor
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1021/jm9018756
CHEMBL378376 138921 11 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to rat EP2 receptorBinding affinity to rat EP2 receptor
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1021/jm9018756
9934368 138921 11 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL378376 138921 11 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 469 10 2 4 4.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CC[C@@H](O)Cc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2006.01.018
44627395 196872 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
CHEMBL565992 196872 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
ChEMBL 563 7 1 7 5.6 O=C(COc1cccc2ncn(Cc3ccc(Cl)cc3Cl)c12)NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/jm9005912
11955410 152529 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 9 2 4 4.3 COC(=O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C(C)(C)CO)cc2)[C@H](O)C[C@H]1Cl nan
CHEMBL3971493 152529 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 9 2 4 4.3 COC(=O)CCC/C=C\C[C@@H]1[C@@H](c2ccc(C(C)(C)CO)cc2)[C@H](O)C[C@H]1Cl nan
5311239 130618 31 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 358 14 4 4 3.5 CCCCC[C@H](O)CC[C@H]1[C@H](O)C[C@H](O)[C@@H]1CCCCCCC(=O)O 10.1021/jm990542v
CHEMBL36817 130618 31 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 358 14 4 4 3.5 CCCCC[C@H](O)CC[C@H]1[C@H](O)C[C@H](O)[C@@H]1CCCCCCC(=O)O 10.1021/jm990542v
45268715 195976 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccccc2CCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559760 195976 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccccc2CCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
25114442 3061 56 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210307
5817 3061 56 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210307
CHEMBL3286797 3061 56 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210307
DB12024 3061 56 None - 1 Human 8.3 pIC50 = 8.3 Binding
Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2Affinity Biochemical interaction (Enzymatic inhibition assay) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210307
1883 3082 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
1916 3082 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
5280360 3082 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
913 3082 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
CHEMBL548 3082 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
DB00917 3082 75 None -7 24 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
1929 1605 55 None - 2 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
9890801 1605 55 None - 2 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
CHEMBL563646 1605 55 None - 2 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
DB12022 1605 55 None - 2 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
22246895 195564 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 399 14 2 4 3.7 CCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL554823 195564 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 399 14 2 4 3.7 CCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
18376196 194922 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 466 9 1 4 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccn2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL541516 194922 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 466 9 1 4 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2ccccn2)cc1 10.1016/j.bmcl.2009.01.059
58681352 154339 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 486 10 3 4 5.5 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3Cc3cccc(OCC(=O)O)c3)c2)CCC1 nan
CHEMBL3986829 154339 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 486 10 3 4 5.5 CCCC1(C(O)c2cccc([C@H]3[C@H](O)C[C@@H](Cl)[C@@H]3Cc3cccc(OCC(=O)O)c3)c2)CCC1 nan
122180281 121630 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cccc(Cl)c32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586344 121630 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cccc(Cl)c32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
16048029 195504 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 369 10 1 3 3.8 CC(C)(C)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL553468 195504 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 369 10 1 3 3.8 CC(C)(C)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
122180277 121626 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2cc(Cl)c3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586340 121626 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2cc(Cl)c3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180257 121609 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 459 5 0 6 5.8 COC(=O)c1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cc1 10.1021/acs.jmedchem.5b00567
CHEMBL3586320 121609 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 459 5 0 6 5.8 COC(=O)c1ccc(CN2CCOc3c(cc(-c4csc5ccccc45)cc3OC)C2)cc1 10.1021/acs.jmedchem.5b00567
122180258 121610 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(C#N)cc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586321 121610 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 426 4 0 5 5.8 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccc(C#N)cc1)C2 10.1021/acs.jmedchem.5b00567
122180291 121641 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 371 3 1 4 5.4 c1cncc(CN2CCNc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586355 121641 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 371 3 1 4 5.4 c1cncc(CN2CCNc3ccc(-c4csc5ccccc45)cc3C2)c1 10.1021/acs.jmedchem.5b00567
11955358 153082 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 364 8 2 2 4.7 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
CHEMBL3976116 153082 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 364 8 2 2 4.7 O=C(O)CCCCCC[C@@H]1[C@@H](c2ccc3c(c2)CCC3)[C@H](O)C[C@H]1Cl nan
18376082 194923 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 472 9 1 5 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2nccs2)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL541517 194923 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 472 9 1 5 4.8 CC(C)(C)c1ccc(CN(Cc2cccc(CCC(=O)O)c2)S(=O)(=O)c2nccs2)cc1 10.1016/j.bmcl.2009.01.059
22246956 196319 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 411 15 1 4 4.2 CCCCCC(=O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562291 196319 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 411 15 1 4 4.2 CCCCCC(=O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
44409917 139250 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(F)c2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL378968 139250 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 419 10 2 4 3.9 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2cccc(F)c2)s1 10.1016/j.bmcl.2006.01.018
122180273 121622 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 386 4 0 6 3.8 COc1cc(-n2cnc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586336 121622 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 386 4 0 6 3.8 COc1cc(-n2cnc3ccccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
11539410 90339 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 438 5 1 3 5.2 CCc1ccc(-c2ccc(C(=O)N3CCc4c(c5ccccc5n4CC(=O)O)C3)cc2)cc1 10.1021/jm400122f
CHEMBL2385904 90339 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 438 5 1 3 5.2 CCc1ccc(-c2ccc(C(=O)N3CCc4c(c5ccccc5n4CC(=O)O)C3)cc2)cc1 10.1021/jm400122f
45269576 195983 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccc(CCCC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559820 195983 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 4.4 CCCCc1ccc(CN(c2ccc(CCCC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11653874 90359 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 384 3 1 3 4.1 O=C(O)Cn1c2c(c3ccccc31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
CHEMBL2386079 90359 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 384 3 1 3 4.1 O=C(O)Cn1c2c(c3ccccc31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
1955 16 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 428 13 4 5 3.6 O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O 10.1021/jm990542v
5311240 16 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 428 13 4 5 3.6 O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O 10.1021/jm990542v
CHEMBL36041 16 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for Prostanoid EP2 receptor expressed in CHO cellsAffinity for Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 428 13 4 5 3.6 O[C@@H](COc1cccc(c1)Cl)CC[C@H]1[C@H](O)C[C@@H]([C@@H]1CCCCCCC(=O)O)O 10.1021/jm990542v
44409733 140884 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 401 10 2 4 3.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL382029 140884 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 401 10 2 4 3.8 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccccc2)s1 10.1016/j.bmcl.2006.01.018
30897313 121598 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586309 121598 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
42484632 121599 5 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccn1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586310 121599 5 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 402 4 0 5 5.4 COc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1ccccn1)C2 10.1021/acs.jmedchem.5b00567
122180270 121619 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2cccc(Cl)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586333 121619 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 380 4 0 4 4.8 COc1cc(-c2cccc(Cl)c2)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
22246893 195952 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 371 13 1 4 2.7 CCCCc1ccc(CN(CCCCOCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL559561 195952 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 371 13 1 4 2.7 CCCCc1ccc(CN(CCCCOCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
11524454 946 55 None - 1 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
5857 946 55 None - 1 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
CHEMBL591666 946 55 None - 1 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 413 6 2 3 5.5 Clc1ccc(c(c1)C(=O)N[C@H](c1ccc(cc1)C(=O)O)C)Oc1ccc(cc1)F 10.1016/j.bmcl.2017.01.067
68505327 90360 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 418 3 1 3 4.7 O=C(O)Cn1c2c(c3cc(Cl)ccc31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
CHEMBL2386080 90360 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 418 3 1 3 4.7 O=C(O)Cn1c2c(c3cc(Cl)ccc31)CN(C(=O)c1cccc3ccccc13)CC2 10.1021/jm400122f
44564892 180522 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475348 180522 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)c(Cl)c3)cccc21 10.1016/j.bmcl.2008.12.112
10126807 195098 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 405 8 1 4 3.4 CC(C)(C)c1ccc(CN(Cc2cccc(OCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL549869 195098 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 405 8 1 4 3.4 CC(C)(C)c1ccc(CN(Cc2cccc(OCC(=O)O)c2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
56927669 121645 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
CHEMBL3586360 121645 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 423 3 1 4 4.5 O=c1cc(CN2CCOc3c(Cl)cc(-n4ccc5cc(F)ccc54)cc3C2)cc[nH]1 10.1021/acs.jmedchem.5b00567
122180296 121646 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
CHEMBL3586361 121646 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 436 3 1 4 5.7 C[C@@H]1COc2c(Cl)cc(-c3csc4ccccc34)cc2CN1Cc1cc[nH]c(=O)c1 10.1021/acs.jmedchem.5b00567
122180279 121628 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586342 121628 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3cc(Cl)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180289 121639 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586353 121639 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 406 3 0 4 6.0 Clc1cc(-c2csc3ccccc23)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
122180280 121629 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3ccc(Cl)cc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586343 121629 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 419 4 0 5 5.1 COc1cc(-n2ccc3ccc(Cl)cc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
22246765 195198 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 3.7 CCCCc1ccc(CN(CCc2ccc(CC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL550619 195198 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 403 11 1 3 3.7 CCCCc1ccc(CN(CCc2ccc(CC(=O)O)cc2)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
44409918 165973 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc(Cl)cc2)s1 10.1016/j.bmcl.2006.01.018
CHEMBL425243 165973 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity to rat EP2 receptor expressed in HEK293 cellsBinding affinity to rat EP2 receptor expressed in HEK293 cells
ChEMBL 435 10 2 4 4.4 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2CCC(O)Cc2ccc(Cl)cc2)s1 10.1016/j.bmcl.2006.01.018
11955236 146456 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 396 10 3 3 4.5 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3922121 146456 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 396 10 3 3 4.5 CC(C)(CO)c1ccc([C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
122180283 121632 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 5 4.6 COc1cc(-n2ccc3cc(F)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
CHEMBL3586346 121632 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assayDisplacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL 403 4 0 5 4.6 COc1cc(-n2ccc3cc(F)ccc32)cc2c1OCCN(Cc1cccnc1)C2 10.1021/acs.jmedchem.5b00567
45268713 195951 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 351 15 2 4 2.6 CCCCCC(O)CCCN(CCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
CHEMBL559560 195951 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 351 15 2 4 2.6 CCCCCC(O)CCCN(CCCCCC(=O)O)S(C)(=O)=O 10.1016/j.bmcl.2009.01.059
10223499 196341 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 413 15 2 4 4.1 CCCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
CHEMBL562411 196341 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of rat EP2 receptor expressed in HEK293 cellsInhibition of rat EP2 receptor expressed in HEK293 cells
ChEMBL 413 15 2 4 4.1 CCCCCC(O)c1ccc(CN(CCCCCCC(=O)O)S(C)(=O)=O)cc1 10.1016/j.bmcl.2009.01.059
44564893 180523 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL475349 180523 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 554 6 1 5 6.2 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2cc(F)c(F)cc2F)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
71733912 90338 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 430 5 1 3 4.5 O=C(O)Cn1c2c(c3cc(F)ccc31)CN(C(=O)CCc1cccc3ccccc13)CC2 10.1021/jm400122f
CHEMBL2385903 90338 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assayInhibition of beta-arrestin binding to recombinant human prostanoid EP2 receptor expressed in HEK293 cell membranes by beta-lactamase complementation assay
ChEMBL 430 5 1 3 4.5 O=C(O)Cn1c2c(c3cc(F)ccc31)CN(C(=O)CCc1cccc3ccccc13)CC2 10.1021/jm400122f
44564804 176700 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
CHEMBL459885 176700 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of radioligand from EP2 receptorDisplacement of radioligand from EP2 receptor
ChEMBL 536 6 1 5 6.1 Cn1cc(/C=C/C(=O)NS(=O)(=O)c2ccc(F)c(F)c2)c2c(Oc3ccc(Cl)cc3Cl)cccc21 10.1016/j.bmcl.2008.12.112
25114442 3061 56 None - 1 Human 8.7 pKd = 8.7 Binding
Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210121
5817 3061 56 None - 1 Human 8.7 pKd = 8.7 Binding
Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210121
CHEMBL3286797 3061 56 None - 1 Human 8.7 pKd = 8.7 Binding
Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210121
DB12024 3061 56 None - 1 Human 8.7 pKd = 8.7 Binding
Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2Affinity On-target Cellular interaction (Functional reporter assay (prostaglandin E2 (PGE2)-induced increase in cAMP in CHO cells expressing EP2 receptors)) EUB0000351a PTGER2
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.6019/CHEMBL5210121
CHEMBL5281349 194110 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assayBinding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assay
ChEMBL 1581 31 10 14 8.1 CC(C)C[C@H]1CN(CC(=O)NCCC(=O)N[C@@H](CCCCNC(=S)Nc2ccccc2)C(N)=O)C(=O)CCSCc2ccc(cc2)C(=O)N[C@@H](CC(C)C)CN(C(=O)CC2CC2)CC(=O)N[C@@H](CCCCN)CN(C(=O)CCc2ccccc2)CC(=O)N[C@@H](Cc2ccccc2)CN(C(=O)CCC2CCCCC2)CC(=O)N1 10.1016/j.bmcl.2023.129255
CHEMBL5279002 194009 0 None - 1 Human 7.8 pKd = 7.8 Binding
Binding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assayBinding affinity to human recombinant PTGER2 assessed as dissociation constant by high throughput fluorescence polarization assay
ChEMBL 1921 33 12 18 12.0 CC(C)C[C@H]1CN(CC(=O)NCCC(=O)N[C@@H](CCCCNC(=S)Nc2ccc(-c3c4ccc(=O)cc-4oc4cc(O)ccc34)c(C(=O)O)c2)C(N)=O)C(=O)CCSCc2ccc(cc2)C(=O)N[C@@H](CCCCN)CN(C(=O)CCc2ccccc2)CC(=O)N[C@@H](CC(C)C)CN(C(=O)CCC2CCCCC2)CC(=O)N[C@@H](Cc2ccccc2)CN(C(=O)Cc2ccc3ccccc3c2)CC(=O)N1 10.1016/j.bmcl.2023.129255
46213069 3063 0 None 1905 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP2 receptor in human mast cell assessed as inhibition constantBinding affinity to EP2 receptor in human mast cell assessed as inhibition constant
ChEMBL 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 10.1021/acs.jmedchem.1c00816
8538 3063 0 None 1905 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP2 receptor in human mast cell assessed as inhibition constantBinding affinity to EP2 receptor in human mast cell assessed as inhibition constant
ChEMBL 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 10.1021/acs.jmedchem.1c00816
CHEMBL5285583 3063 0 None 1905 3 Human 9.2 pKi = 9.2 Binding
Binding affinity to EP2 receptor in human mast cell assessed as inhibition constantBinding affinity to EP2 receptor in human mast cell assessed as inhibition constant
ChEMBL 456 7 1 5 4.2 COc1ccc(cc1)C(=O)N1CCC(C1)(COc1ccc(cc1)c1ccc(cc1)C#N)C(=O)O 10.1021/acs.jmedchem.1c00816
9807448 203172 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Compound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorCompound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64246 203172 0 None 1 4 Human 9.1 pKi = 9.1 Binding
Compound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorCompound was evaluated for its competitive binding affinity towards human Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
1883 3082 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
1916 3082 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
5280360 3082 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
913 3082 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL548 3082 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
DB00917 3082 75 None -6 24 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
51039069 129203 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 419 6 4 4 4.1 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(F)cc2)cc1 nan
CHEMBL3670659 129203 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 419 6 4 4 4.1 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(F)cc2)cc1 nan
51039071 129207 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 419 6 4 4 4.1 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccccc3)cc2-c2ccc(F)cc2)o1 nan
CHEMBL3670663 129207 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 419 6 4 4 4.1 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccccc3)cc2-c2ccc(F)cc2)o1 nan
10481859 75167 0 None -4 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
CHEMBL2036321 75167 0 None -4 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1C 10.1016/j.bmc.2012.04.008
1932 2942 5 None 1 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
5311228 2942 5 None 1 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
CHEMBL3286796 2942 5 None 1 6 Human 8.8 pKi = 8.8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10.1021/jm401431x
1883 3082 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
1916 3082 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
5280360 3082 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
913 3082 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
CHEMBL548 3082 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
DB00917 3082 75 None -6 24 Human 8.8 pKi = 8.8 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.ejmech.2013.01.044
57384034 71307 0 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957436 71307 0 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.02.018
57384034 71307 0 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957436 71307 0 None -2 3 Mouse 8.8 pKi = 8.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 528 10 2 6 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc(Cl)cc3)c2)n1 10.1016/j.bmc.2012.04.008
67078793 129197 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 287 3 2 2 4.2 O=C(O)c1[nH]c(-c2cccs2)cc1-c1ccc(F)cc1 nan
CHEMBL3670653 129197 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 287 3 2 2 4.2 O=C(O)c1[nH]c(-c2cccs2)cc1-c1ccc(F)cc1 nan
18376177 3753 50 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
5816 3753 50 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
CHEMBL2107783 3753 50 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
DB12623 3753 50 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 478 10 1 7 3.1 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/jm401431x
11855865 153277 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 153277 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
10116114 125886 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL364841 125886 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
13231966 100951 0 None -141 5 Mouse 7.0 pKi = 7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL294108 100951 0 None -141 5 Mouse 7.0 pKi = 7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
13231966 100951 0 None -141 5 Mouse 7.0 pKi = 7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL294108 100951 0 None -141 5 Mouse 7.0 pKi = 7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 372 13 3 5 3.2 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
44455046 95727 0 None -50118 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL258332 95727 0 None -50118 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 413 8 2 3 3.7 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.11.020
44304057 203259 0 None -288 4 Mouse 6.0 pKi = 6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.6 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64598 203259 0 None -288 4 Mouse 6.0 pKi = 6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.6 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
10181606 206351 0 None -645 7 Human 5.0 pKi = 5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
CHEMBL87371 206351 0 None -645 7 Human 5.0 pKi = 5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
118517483 144271 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 144271 0 None -93 2 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
71455094 81881 0 None -407 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 623 12 1 8 6.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
CHEMBL2164609 81881 0 None -407 4 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 623 12 1 8 6.4 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
44303627 203205 0 None 467 2 Mouse 8.0 pKi = 8.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 364 11 3 3 4.5 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64358 203205 0 None 467 2 Mouse 8.0 pKi = 8.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 364 11 3 3 4.5 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
5311035 97803 29 None -4 9 Human 7.0 pKi = 7.0 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/j.bmcl.2007.09.074
CHEMBL271896 97803 29 None -4 9 Human 7.0 pKi = 7.0 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/j.bmcl.2007.09.074
52941778 16542 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 712 14 2 4 11.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1Oc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237304 16542 0 None -1 3 Human 7.0 pKi = 7.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 712 14 2 4 11.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1Oc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1Oc1ccccc1 10.1016/j.bmcl.2004.11.051
5311035 97803 29 None -4 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/j.bmcl.2007.11.020
CHEMBL271896 97803 29 None -4 9 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/j.bmcl.2007.11.020
44390782 64603 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 402 10 1 3 5.5 COc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL181691 64603 0 None -57 3 Human 6.0 pKi = 6.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 402 10 1 3 5.5 COc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44303907 202741 0 None - 1 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 390 10 3 4 3.5 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CC#CCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL61925 202741 0 None - 1 Mouse 6.0 pKi = 6.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 390 10 3 4 3.5 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CC#CCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10431288 69366 0 None -1318 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 403 12 2 3 4.5 CCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929546 69366 0 None -1318 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 403 12 2 3 4.5 CCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
46201043 200582 0 None -5011 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL599154 200582 0 None -5011 3 Mouse 6.0 pKi = 6.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
9939791 161918 0 None -912 8 Human 5.0 pKi = 5.0 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
CHEMBL415310 161918 0 None -912 8 Human 5.0 pKi = 5.0 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
9873528 206930 0 None -72 4 Human 5.0 pKi = 5.0 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 602 7 1 5 6.9 O=C(NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)OCc1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL91063 206930 0 None -72 4 Human 5.0 pKi = 5.0 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 602 7 1 5 6.9 O=C(NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)OCc1ccccc1 10.1016/s0960-894x(99)00465-5
134155748 151169 0 None 25 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959653 151169 0 None 25 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 400 12 2 4 4.7 CCCCCC(=O)c1ccc([C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
11502897 142793 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 142793 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11502897 142793 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3892847 142793 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 431 11 2 5 4.8 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
119461 320 72 None -3 10 Human 5.9 pKi = 5.9 Binding
Inhibition of EP2 receptor (unknown origin) by competitive binding assayInhibition of EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
1896 320 72 None -3 10 Human 5.9 pKi = 5.9 Binding
Inhibition of EP2 receptor (unknown origin) by competitive binding assayInhibition of EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
CHEMBL1317823 320 72 None -3 10 Human 5.9 pKi = 5.9 Binding
Inhibition of EP2 receptor (unknown origin) by competitive binding assayInhibition of EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10.1021/jm401431x
118517359 144396 0 None -114 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 144396 0 None -114 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
24952927 201231 0 None -851 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
CHEMBL603690 201231 0 None -851 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(C(F)(F)F)cc1 10.1021/jm901771h
44304404 100581 0 None -23 4 Mouse 7.9 pKi = 7.9 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 12 3 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL291630 100581 0 None -23 4 Mouse 7.9 pKi = 7.9 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 12 3 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
10291963 84708 0 None -74 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL222715 84708 0 None -74 6 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
44520989 199764 0 None -2 3 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 396 6 2 4 5.0 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1ccccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
CHEMBL593764 199764 0 None -2 3 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 396 6 2 4 5.0 Cc1c(C)c2c(c(C)c1O)CCC(C)(CCOc1ccccc1/C=C/C(=O)O)O2 10.1016/j.bmc.2009.08.007
23016719 201220 0 None -1 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(OCc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL603625 201220 0 None -1 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(OCc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
44304055 102723 0 None -371 4 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCSCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL304887 102723 0 None -371 4 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCSCCC(=O)O 10.1016/s0960-894x(01)00364-x
44304034 200594 0 None -165 3 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
CHEMBL59921 200594 0 None -165 3 Mouse 5.9 pKi = 5.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
9817405 165403 5 None -165 6 Human 4.9 pKi = 4.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2006.08.025
CHEMBL423815 165403 5 None -165 6 Human 4.9 pKi = 4.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 288 4 1 1 4.5 O=C(O)/C=C/c1ccccc1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2006.08.025
72695027 106266 0 None -28 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3115074 106266 0 None -28 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
CHEMBL3138992 106266 0 None -28 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor by liquid scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2015.05.091
72706947 174664 20 None -5128 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 363 11 2 3 3.4 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL4558749 174664 20 None -5128 3 Human 4.9 pKi = 4.9 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 363 11 2 3 3.4 CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
118517488 153711 0 None -56 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 153711 0 None -56 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
44442327 94459 0 None -147 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251294 94459 0 None -147 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
17757350 152754 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
CHEMBL3973347 152754 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 413 12 3 4 5.1 CCCCCC(O)c1ccc([C@@H]2[C@@H](C/C=C\CCCC(=O)O)[C@H](C#N)C[C@H]2O)cc1 nan
10112412 69468 0 None -208 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933719 69468 0 None -208 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
10112412 69468 0 None -208 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933719 69468 0 None -208 3 Mouse 6.9 pKi = 6.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 9 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
118517489 143691 0 None -44 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 143691 0 None -44 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
51039070 129204 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 433 6 5 5 4.2 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(O)cc2)cc1 nan
CHEMBL3670660 129204 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 433 6 5 5 4.2 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(O)cc2)cc1 nan
44303626 168182 0 None - 1 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL433249 168182 0 None - 1 Mouse 7.9 pKi = 7.9 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
57400249 69477 0 None 3 3 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 410 9 2 6 3.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CC2CCCC2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933728 69477 0 None 3 3 Mouse 7.9 pKi = 7.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 410 9 2 6 3.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CC2CCCC2)n1 10.1016/j.bmcl.2011.10.109
10291963 84708 0 None -74 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
CHEMBL222715 84708 0 None -74 6 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
11315933 123294 4 None -707 5 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 413 7 1 4 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL361457 123294 4 None -707 5 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 413 7 1 4 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
44394432 127326 0 None -10 5 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 457 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@H]2COc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365908 127326 0 None -10 5 Mouse 5.9 pKi = 5.9 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 457 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@H]2COc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
23017109 200074 0 None -6 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 416 10 1 5 4.3 O=C(O)COCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595830 200074 0 None -6 2 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 416 10 1 5 4.3 O=C(O)COCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
15907747 207023 0 None -257 4 Human 4.9 pKi = 4.9 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
CHEMBL91537 207023 0 None -257 4 Human 4.9 pKi = 4.9 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 684 8 1 5 7.2 CO[C@@](C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)(c1ccccc1)C(F)(F)F 10.1016/s0960-894x(99)00465-5
118517361 153370 0 None -218 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 153370 0 None -218 2 Human 5.9 pKi = 5.9 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
9975502 94489 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251504 94489 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
3356 2280 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
4326 2280 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
9867642 2280 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
CHEMBL426559 2280 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
DB11629 2280 73 None -53 8 Human 6.9 pKi = 6.9 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F 10.1021/jm0603668
70667255 151474 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3962183 151474 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 nan
24760052 151185 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3959769 151185 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 427 10 2 4 5.4 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2/C=C/Cc2ccc(C(=O)O)s2)cc1 nan
44304436 203320 0 None -35 5 Mouse 7.9 pKi = 7.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 400 14 3 5 3.8 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64854 203320 0 None -35 5 Mouse 7.9 pKi = 7.9 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 400 14 3 5 3.8 CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCCCC(=O)O 10.1016/s0960-894x(01)00364-x
44320373 206250 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 376 9 1 2 5.8 O=C(O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1 10.1016/s0960-894x(02)00518-8
CHEMBL86799 206250 0 None 5 4 Human 6.9 pKi = 6.9 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 376 9 1 2 5.8 O=C(O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1 10.1016/s0960-894x(02)00518-8
52947851 16545 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237315 16545 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2004.11.051
52947851 16545 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237315 16545 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 528 10 2 2 8.1 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
9813912 137882 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 264 5 1 1 4.0 O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL376282 137882 0 None -14 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 264 5 1 1 4.0 O=C(O)/C=C/c1ccccc1C/C=C/c1ccccc1 10.1016/j.bmcl.2006.08.025
57394140 69371 0 None -707 3 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 419 13 2 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929550 69371 0 None -707 3 Mouse 5.9 pKi = 5.9 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 419 13 2 4 4.1 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
134146425 149203 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 12 2 2 6.4 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3943966 149203 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 12 2 2 6.4 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
11519006 102486 0 None -229 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]PGE-2 binding to Prostanoid EP2 receptorInhibition of [3H]PGE-2 binding to Prostanoid EP2 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
CHEMBL2373410 102486 0 None -229 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]PGE-2 binding to Prostanoid EP2 receptorInhibition of [3H]PGE-2 binding to Prostanoid EP2 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
CHEMBL3040272 102486 0 None -229 6 Human 5.9 pKi = 5.9 Binding
Inhibition of [3H]PGE-2 binding to Prostanoid EP2 receptorInhibition of [3H]PGE-2 binding to Prostanoid EP2 receptor
ChEMBL 481 8 1 5 6.1 O=C(O)COc1cccc(C[C@@H]2CCC[C@H]3O[C@]23c2nc(-c3ccccc3)c(-c3ccccc3)o2)c1 10.1016/j.bmcl.2005.04.076
9808508 111560 0 None -245 3 Human 4.9 pKi = 4.9 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 586 7 1 4 6.3 O=C(Cc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL328067 111560 0 None -245 3 Human 4.9 pKi = 4.9 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 586 7 1 4 6.3 O=C(Cc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
44455115 95562 0 None -15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL257658 95562 0 None -15 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 387 10 2 3 4.1 CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
118517359 144396 0 None -114 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 144396 0 None -114 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
44289922 163524 0 None -954 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL42027 163524 0 None -954 5 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
11855868 152544 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 152544 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
57393340 69475 0 None -10 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 530 12 2 7 4.2 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(COCC(F)(F)F)c2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933726 69475 0 None -10 4 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 530 12 2 7 4.2 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(COCC(F)(F)F)c2)n1 10.1016/j.bmcl.2011.10.109
11855868 152544 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3971632 152544 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 429 11 2 4 5.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
57894053 75170 0 None -79 3 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036324 75170 0 None -79 3 Mouse 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 551 10 2 8 5.4 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
155516303 170077 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 7 1 5 5.2 CC(C)(C)c1ccc(CN(Cc2cccc3oc(C(=O)O)cc23)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4443289 170077 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 7 1 5 5.2 CC(C)(C)c1ccc(CN(Cc2cccc3oc(C(=O)O)cc23)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
18973764 16647 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 346 8 1 2 5.1 O=C(O)c1ccc(CCCc2ccccc2OCc2ccccc2)cc1 10.1016/s0960-894x(03)00794-7
CHEMBL124199 16647 0 None 1 4 Human 6.8 pKi = 6.8 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 346 8 1 2 5.1 O=C(O)c1ccc(CCCc2ccccc2OCc2ccccc2)cc1 10.1016/s0960-894x(03)00794-7
44304058 203177 0 None -66 5 Mouse 6.8 pKi = 6.8 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 374 13 3 6 2.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCOCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64254 203177 0 None -66 5 Mouse 6.8 pKi = 6.8 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 374 13 3 6 2.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCOCC(=O)O 10.1016/s0960-894x(01)00364-x
23017216 199159 0 None -1380 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL589411 199159 0 None -1380 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 439 9 2 3 5.4 O=C(O)CCc1ccc(COc2ccccc2)cc1C(=O)NCc1cccc2ccccc12 10.1016/j.bmc.2009.11.023
44304051 102760 0 None -213 4 Mouse 5.8 pKi = 5.8 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
CHEMBL305126 102760 0 None -213 4 Mouse 5.8 pKi = 5.8 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)cc1 10.1016/s0960-894x(01)00364-x
134143292 145228 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 12 1 3 6.5 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3912658 145228 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 12 1 3 6.5 CCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465595 145423 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)c1 nan
CHEMBL3914108 145423 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)c1 nan
59465574 145945 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
CHEMBL3918084 145945 0 None 1 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 400 12 1 4 5.7 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)OC)cc1 nan
118517490 153155 0 None -125 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
CHEMBL3976710 153155 0 None -125 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
72695027 106266 0 None -28 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3115074 106266 0 None -28 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
CHEMBL3138992 106266 0 None -28 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysisDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cell membranes after 90 mins by topcount scintillation counting analysis
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 10.1021/ml5000367
72695027 106266 0 None -28 2 Human 5.8 pKi = 5.8 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3115074 106266 0 None -28 2 Human 5.8 pKi = 5.8 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 nan
CHEMBL3138992 106266 0 None -28 2 Human 5.8 pKi = 5.8 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 396 8 2 4 3.5 C[C@H](NC(=O)[C@H]1CCCCN1CCOc1ccccc1)c1ccc(C(=O)O)cc1 nan
24952577 200561 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 399 6 2 3 5.2 C[C@H](NC(=O)c1cscc1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL599051 200561 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 399 6 2 3 5.2 C[C@H](NC(=O)c1cscc1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
1929 1605 55 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
9890801 1605 55 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
CHEMBL563646 1605 55 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
DB12022 1605 55 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
44349503 168390 0 None -100 4 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 553 10 1 5 7.1 O=C(CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
CHEMBL434637 168390 0 None -100 4 Human 5.8 pKi = 5.8 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 553 10 1 5 7.1 O=C(CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(03)00794-7
44419351 84143 0 None -28 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 533 12 1 5 6.2 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL220821 84143 0 None -28 4 Human 5.8 pKi = 5.8 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 533 12 1 5 6.2 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
44324368 96518 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 587 6 2 4 6.8 O=C(Nc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL262690 96518 0 None -3 4 Human 4.8 pKi = 4.8 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 587 6 2 4 6.8 O=C(Nc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10144273 205834 0 None -131 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 558 8 1 5 7.2 O=C(CCc1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL83450 205834 0 None -131 4 Human 4.8 pKi = 4.8 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 558 8 1 5 7.2 O=C(CCc1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
11855871 146408 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 146408 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855871 146408 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3921784 146408 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 429 11 1 5 4.9 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855866 144602 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 144602 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855866 144602 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3907809 144602 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 403 9 2 5 4.0 CCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
53494965 64813 0 None -5 3 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 7 2 5 4.5 Cc1ccc(CC(=O)O)cc1NC(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1C 10.1016/j.bmc.2011.08.007
CHEMBL1819611 64813 0 None -5 3 Mouse 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 7 2 5 4.5 Cc1ccc(CC(=O)O)cc1NC(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1C 10.1016/j.bmc.2011.08.007
52947847 16538 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1.Cc1cccc(C/C=C\c2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237300 16538 0 None 1 3 Human 5.8 pKi = 5.8 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1.Cc1cccc(C/C=C\c2ccc(/C=C/C(=O)O)cc2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
11314979 66109 0 None -11 4 Mouse 5.8 pKi = 5.8 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 379 7 1 4 4.8 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(C)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL183933 66109 0 None -11 4 Mouse 5.8 pKi = 5.8 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 379 7 1 4 4.8 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(C)ccc32)cc1 10.1016/j.bmcl.2004.06.006
11234840 125055 0 None -4 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 395 8 1 5 4.5 CCCCOc1cccc(C(=O)n2c(C)c(CC(=O)O)c3cc(OC)ccc32)c1 10.1016/j.bmcl.2004.06.006
CHEMBL364421 125055 0 None -4 2 Mouse 5.8 pKi = 5.8 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 395 8 1 5 4.5 CCCCOc1cccc(C(=O)n2c(C)c(CC(=O)O)c3cc(OC)ccc32)c1 10.1016/j.bmcl.2004.06.006
56949973 69372 0 None -3388 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 407 11 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929551 69372 0 None -3388 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 407 11 2 4 3.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
57894092 75158 0 None -8511 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 12 2 6 4.5 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036312 75158 0 None -8511 3 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 12 2 6 4.5 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
10157810 63787 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 400 9 1 3 5.6 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1021/ml300191g
CHEMBL180191 63787 0 None 3 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 400 9 1 3 5.6 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1021/ml300191g
44442334 94528 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 327 7 1 2 3.8 CC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251710 94528 0 None -7 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 327 7 1 2 3.8 CC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
11495634 14905 13 None -218 4 Mouse 5.8 pKi = 5.8 Binding
Antagonist activity at mouse EP2 receptorAntagonist activity at mouse EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
CHEMBL1207972 14905 13 None -218 4 Mouse 5.8 pKi = 5.8 Binding
Antagonist activity at mouse EP2 receptorAntagonist activity at mouse EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
CHEMBL467114 14905 13 None -218 4 Mouse 5.8 pKi = 5.8 Binding
Antagonist activity at mouse EP2 receptorAntagonist activity at mouse EP2 receptor
ChEMBL 405 6 1 3 5.4 O=C(O)c1cccc(Cc2cc(Cl)ccc2OCc2ccc(Cl)cc2F)n1 10.1016/j.bmcl.2012.11.046
92135977 152896 0 None -275 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 152896 0 None -275 2 Human 5.8 pKi = 5.8 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
52945421 16536 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(OCc2ccccc2)c1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.11.051
CHEMBL1237298 16536 0 None 2 4 Human 7.8 pKi = 7.8 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(OCc2ccccc2)c1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(OCc2ccccc2)c1 10.1016/j.bmcl.2004.11.051
21362912 171175 0 None -8 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 535 12 1 5 6.7 O=C(CCCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL445895 171175 0 None -8 4 Human 5.8 pKi = 5.8 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 535 12 1 5 6.7 O=C(CCCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
23017362 199978 0 None -45 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 10 1 4 5.1 O=C(O)CCCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595157 199978 0 None -45 4 Mouse 5.8 pKi = 5.8 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 10 1 4 5.1 O=C(O)CCCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
11577792 159318 19 None -1819 5 Human 5.7 pKi = 5.7 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
CHEMBL4099851 159318 19 None -1819 5 Human 5.7 pKi = 5.7 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 414 6 2 4 4.9 C[C@H](NC(=O)c1cc(Cl)cnc1Oc1cccc(F)c1)c1ccc(C(=O)O)cc1 10.1016/j.bmcl.2017.01.067
10448293 154421 0 None -41 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 313 6 1 2 3.4 CC(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL398947 154421 0 None -41 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 313 6 1 2 3.4 CC(C)=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
11855324 142605 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 142605 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
57395059 69474 0 None -12 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmcl.2011.10.109
CHEMBL1933725 69474 0 None -12 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmcl.2011.10.109
57395059 69474 0 None -12 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1933725 69474 0 None -12 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 418 9 2 6 3.1 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)n1 10.1016/j.bmc.2012.02.018
11855865 153277 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3977724 153277 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 445 12 2 5 5.2 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
57403612 71305 0 None -239 3 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 9 2 4 4.2 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmc.2012.02.018
CHEMBL1957434 71305 0 None -239 3 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 9 2 4 4.2 O=C(O)c1ccc(CCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)s1 10.1016/j.bmc.2012.02.018
15948325 2526 45 None -1548 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
5856 2526 45 None -1548 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
CHEMBL402162 2526 45 None -1548 6 Human 5.7 pKi = 5.7 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 603 11 1 8 4.7 CCOc1c2CN(C(=O)c2c(c2c1nccc2)OCC)c1ccc(cc1C)CS(=O)(=O)NC(=O)Cc1ccccc1OC 10.1016/j.bmcl.2008.01.103
59465577 143189 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 13 2 2 6.8 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3896183 143189 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 408 13 2 2 6.8 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)cc1 nan
57893982 75164 0 None -4 3 Mouse 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036318 75164 0 None -4 3 Mouse 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 508 10 2 6 5.1 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
57464006 75168 0 None -17 4 Mouse 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036322 75168 0 None -17 4 Mouse 8.7 pKi = 8.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 534 10 2 7 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3cc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
9807448 203172 0 None -1 4 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64246 203172 0 None -1 4 Mouse 8.7 pKi = 8.7 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
67078538 129198 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 269 3 3 3 3.3 O=C(O)c1[nH]c(-c2ccoc2)cc1-c1ccc(O)cc1 nan
CHEMBL3670654 129198 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 269 3 3 3 3.3 O=C(O)c1[nH]c(-c2ccoc2)cc1-c1ccc(O)cc1 nan
44303952 100886 0 None 41 4 Mouse 7.7 pKi = 7.7 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293697 100886 0 None 41 4 Mouse 7.7 pKi = 7.7 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 420 14 3 4 4.8 CCCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10361472 65208 0 None -199 3 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)cc3c(CC(=O)O)cccc32)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL182555 65208 0 None -199 3 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)cc3c(CC(=O)O)cccc32)cc1 10.1016/j.bmcl.2004.07.039
10118889 206273 0 None -74 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1cccc(CSCCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL86933 206273 0 None -74 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1cccc(CSCCc2ccccc2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
11187675 65214 0 None -61 4 Mouse 5.7 pKi = 5.7 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL182572 65214 0 None -61 4 Mouse 5.7 pKi = 5.7 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
12002527 75160 0 None -19952 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 493 12 2 5 5.1 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2cc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036314 75160 0 None -19952 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 493 12 2 5 5.1 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2cc3ccccc3o2)c1 10.1016/j.bmc.2012.04.008
24953628 200603 0 None -63 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(Cl)cc1 10.1021/jm901771h
CHEMBL599262 200603 0 None -63 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1ccc(Cl)cc1 10.1021/jm901771h
57529188 147195 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 147195 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
57529188 147195 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3928130 147195 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 415 11 2 5 4.3 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
44444721 154406 0 None -77 2 Human 5.7 pKi = 5.7 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 508 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(I)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL398827 154406 0 None -77 2 Human 5.7 pKi = 5.7 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 508 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(I)c2)cc1 10.1016/j.bmcl.2007.09.074
44455084 97867 0 None -10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
CHEMBL272277 97867 0 None -10 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 399 10 2 3 4.2 CCCCC1([C@@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.11.020
58932681 75172 0 None -100 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2036326 75172 0 None -100 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
10116116 64411 0 None -26 5 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813115 64411 0 None -26 5 Mouse 6.7 pKi = 6.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
10206535 66572 0 None -398 4 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 488 6 1 6 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccc(F)cc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL185251 66572 0 None -398 4 Mouse 5.7 pKi = 5.7 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 488 6 1 6 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccc(F)cc3O2)cc1 10.1016/j.bmcl.2004.07.039
44320126 206412 0 None -17 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 537 11 1 7 6.2 Cc1cccc(OCCCOc2ccc(-c3ccccc3COC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87816 206412 0 None -17 4 Human 5.7 pKi = 5.7 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 537 11 1 7 6.2 Cc1cccc(OCCCOc2ccc(-c3ccccc3COC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
22009011 64073 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(/C=C/C(O)c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL180742 64073 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(/C=C/C(O)c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
11187675 65214 0 None -61 4 Mouse 5.7 pKi = 5.7 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL182572 65214 0 None -61 4 Mouse 5.7 pKi = 5.7 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 365 7 1 4 4.4 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)cc1 10.1016/j.bmcl.2004.06.006
44419380 83079 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218178 83079 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
44419384 83080 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218179 83080 0 None -208 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 529 10 1 5 6.4 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2006.08.025
57894081 75154 0 None -3467 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 503 12 2 4 5.6 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036308 75154 0 None -3467 2 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 503 12 2 4 5.6 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3ccccc3c2)c1 10.1016/j.bmc.2012.04.008
23017746 199849 0 None -13 3 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 8 1 3 6.2 O=C(O)/C=C/c1ccc(Cc2cccs2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL594365 199849 0 None -13 3 Mouse 5.7 pKi = 5.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 414 8 1 3 6.2 O=C(O)/C=C/c1ccc(Cc2cccs2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
9846782 100905 7 None -676 3 Mouse 5.7 pKi = 5.7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 454 13 3 7 2.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL293856 100905 7 None -676 3 Mouse 5.7 pKi = 5.7 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 454 13 3 7 2.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
15907748 111464 0 None -147 4 Human 4.7 pKi = 4.7 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 615 7 2 4 7.0 C[C@H](NC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL327597 111464 0 None -147 4 Human 4.7 pKi = 4.7 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 615 7 2 4 7.0 C[C@H](NC(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
138 3081 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
1882 3081 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
5280723 3081 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
CHEMBL495 3081 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
DB00770 3081 88 None -19 18 Mouse 7.7 pKi = 7.7 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
1883 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
1916 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
5280360 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
913 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
CHEMBL548 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
DB00917 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2011.10.109
1883 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
1916 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
5280360 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
913 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
CHEMBL548 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
DB00917 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
57396660 71308 0 None -1819 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957437 71308 0 None -1819 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.02.018
57396660 71308 0 None -1819 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957437 71308 0 None -1819 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 544 10 2 6 5.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccc4ccccc4c3)c2)n1 10.1016/j.bmc.2012.04.008
10348321 75171 0 None -87 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 585 10 2 8 6.0 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036325 75171 0 None -87 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 585 10 2 8 6.0 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4s3)c2)n1 10.1016/j.bmc.2012.04.008
58932678 75288 0 None -104 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
CHEMBL2037290 75288 0 None -104 3 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1cccc2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc12 10.1016/j.bmc.2012.04.008
56672020 64825 0 None -1 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 7 2 5 4.6 CN1C[C@@H](COc2ccc(C(=O)Nc3cc(CC(=O)O)ccc3F)c(Cl)c2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819623 64825 0 None -1 2 Mouse 7.7 pKi = 7.7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 7 2 5 4.6 CN1C[C@@H](COc2ccc(C(=O)Nc3cc(CC(=O)O)ccc3F)c(Cl)c2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
11337782 84943 0 None -12 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 373 10 2 3 3.6 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2CC[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
CHEMBL223744 84943 0 None -12 3 Human 6.7 pKi = 6.7 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 373 10 2 3 3.6 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2CC[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
9863804 94098 0 None -8 2 Human 5.7 pKi = 5.7 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249136 94098 0 None -8 2 Human 5.7 pKi = 5.7 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 362 11 2 4 2.7 CCCCCC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
9938669 168058 0 None -154 4 Human 4.7 pKi = 4.7 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 602 8 1 5 6.2 O=C(COc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL432380 168058 0 None -154 4 Human 4.7 pKi = 4.7 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 602 8 1 5 6.2 O=C(COc1ccccc1)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10113454 177501 0 None -1380 3 Human 4.7 pKi = 4.7 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 429 12 2 3 4.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL46395 177501 0 None -1380 3 Human 4.7 pKi = 4.7 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 429 12 2 3 4.4 O=C(O)CCCCCCN1C(=O)CC[C@@H]1CC[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
118517483 144271 0 None -93 2 Human 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
CHEMBL3904946 144271 0 None -93 2 Human 5.7 pKi = 5.7 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccccc2F)cc1 nan
11488860 19291 0 None -5370 8 Human 5.6 pKi = 5.6 Binding
Binding affinity to prostanoid receptor EP2 receptorBinding affinity to prostanoid receptor EP2 receptor
ChEMBL 497 5 1 4 5.7 C[C@@H](c1ccc(C(F)(F)F)cc1)n1c2c(c3cc(F)cc(S(C)(=O)=O)c31)CCC[C@@H]2CC(=O)O 10.1016/j.bmcl.2010.10.018
CHEMBL1290413 19291 0 None -5370 8 Human 5.6 pKi = 5.6 Binding
Binding affinity to prostanoid receptor EP2 receptorBinding affinity to prostanoid receptor EP2 receptor
ChEMBL 497 5 1 4 5.7 C[C@@H](c1ccc(C(F)(F)F)cc1)n1c2c(c3cc(F)cc(S(C)(=O)=O)c31)CCC[C@@H]2CC(=O)O 10.1016/j.bmcl.2010.10.018
24760055 143888 0 None -2 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3901873 143888 0 None -2 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
24760055 143888 0 None -2 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
CHEMBL3901873 143888 0 None -2 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 411 10 2 4 4.6 CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COc2ccc(C(=O)O)cc2)cc1 nan
11855591 144436 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 144436 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
11855591 144436 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
CHEMBL3906402 144436 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 435 9 2 5 4.0 O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 nan
10414412 75166 0 None -6 3 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)c(C)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036320 75166 0 None -6 3 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 522 10 2 6 5.4 Cc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)c(C)c1 10.1016/j.bmc.2012.04.008
11408533 141327 0 None -89 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 459 6 1 5 4.5 CC(=O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1016/j.bmcl.2006.02.062
CHEMBL383484 141327 0 None -89 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 459 6 1 5 4.5 CC(=O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1016/j.bmcl.2006.02.062
11408533 141327 0 None -89 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 459 6 1 5 4.5 CC(=O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
CHEMBL383484 141327 0 None -89 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 459 6 1 5 4.5 CC(=O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
11743212 17164 0 None -758 7 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 426 7 1 3 6.8 O=C(O)C1CC1c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125588 17164 0 None -758 7 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 426 7 1 3 6.8 O=C(O)C1CC1c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
56658143 64805 0 None -16 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 468 8 2 6 3.4 CN1C[C@@H](COc2ccc(S(=O)(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819604 64805 0 None -16 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 468 8 2 6 3.4 CN1C[C@@H](COc2ccc(S(=O)(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
9809136 106889 0 None -2290 8 Human 4.6 pKi = 4.6 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 614 7 1 4 7.1 CC(C)(C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
CHEMBL314533 106889 0 None -2290 8 Human 4.6 pKi = 4.6 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 614 7 1 4 7.1 CC(C)(C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1)c1ccccc1 10.1016/s0960-894x(99)00465-5
9874010 207190 0 None -1348 8 Human 4.6 pKi = 4.6 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 629 8 1 4 6.9 CN(CCc1ccccc1)C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
CHEMBL92539 207190 0 None -1348 8 Human 4.6 pKi = 4.6 Binding
Affinity at human EP2 receptor.Affinity at human EP2 receptor.
ChEMBL 629 8 1 4 6.9 CN(CCc1ccccc1)C(=O)NS(=O)(=O)c1ccccc1-c1ccc(CN2C(=O)c3ccccc3CCc3ccccc32)cc1 10.1016/s0960-894x(99)00465-5
10229201 155576 0 None -87 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 508 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(I)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL404414 155576 0 None -87 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 508 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(I)c2)cc1 10.1016/j.bmcl.2007.09.074
10076580 75289 0 None -158 3 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 563 10 2 8 5.5 Cc1cc(C)c2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037291 75289 0 None -158 3 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 563 10 2 8 5.5 Cc1cc(C)c2oc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)nc2c1 10.1016/j.bmc.2012.04.008
132836 59695 23 None 1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 10.1021/jm401431x
CHEMBL1722929 59695 23 None 1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 10.1021/jm401431x
57403799 69469 0 None -6 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 9 2 5 2.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)co2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933720 69469 0 None -6 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 9 2 5 2.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)co2)c1 10.1016/j.bmcl.2011.10.109
57403799 69469 0 None -6 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 9 2 5 2.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)co2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933720 69469 0 None -6 2 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 9 2 5 2.8 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)co2)c1 10.1016/j.bmc.2012.02.018
5311035 97803 29 None -4 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1021/jm401431x
CHEMBL271896 97803 29 None -4 9 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1021/jm401431x
44303980 168074 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 408 13 2 5 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL432522 168074 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 408 13 2 5 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 10.1016/s0960-894x(01)00359-6
22009004 141751 0 None -2884 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1021/ml300191g
CHEMBL385955 141751 0 None -2884 4 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1021/ml300191g
10270893 94228 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 376 12 2 4 3.1 CCCCCC(O)CCCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249954 94228 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 376 12 2 4 3.1 CCCCCC(O)CCCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
44303889 203217 0 None - 1 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 414 10 3 4 4.2 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64423 203217 0 None - 1 Mouse 7.6 pKi = 7.6 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 414 10 3 4 4.2 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/s0960-894x(01)00359-6
17751059 148268 0 None 56 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3936540 148268 0 None 56 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
21974328 66270 0 None -26 5 Mouse 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 443 6 1 6 4.4 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Oc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL184684 66270 0 None -26 5 Mouse 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 443 6 1 6 4.4 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Oc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
10228100 64414 0 None -43 5 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 6 1 6 4.7 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813118 64414 0 None -43 5 Mouse 6.6 pKi = 6.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 488 6 1 6 4.7 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
44349551 16814 0 None -47 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 415 8 2 4 6.2 O=C(O)CNc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124675 16814 0 None -47 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 415 8 2 4 6.2 O=C(O)CNc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
10158725 16828 0 None -109 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124738 16828 0 None -109 4 Human 5.6 pKi = 5.6 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
44320405 106165 0 None -5 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.2 O=C(NS(=O)(=O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL313700 106165 0 None -5 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.2 O=C(NS(=O)(=O)CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)c1cccs1 10.1016/s0960-894x(02)00518-8
52944194 16543 0 None -194 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 936 18 4 6 12.8 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(CO)c1OCc1c(Cl)cccc1Cl.O=C(O)/C=C/c1ccccc1C/C=C/c1cccc(CO)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL1237305 16543 0 None -194 4 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 936 18 4 6 12.8 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(CO)c1OCc1c(Cl)cccc1Cl.O=C(O)/C=C/c1ccccc1C/C=C/c1cccc(CO)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
52947852 16546 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237316 16546 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2004.11.051
52947852 16546 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237316 16546 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 588 12 2 4 8.1 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1.COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
44419388 83415 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 294 6 1 2 4.0 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL219590 83415 0 None -37 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 294 6 1 2 4.0 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)O)cc1 10.1016/j.bmcl.2006.08.025
11339240 84728 0 None -3548 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 423 10 2 4 3.2 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
CHEMBL222834 84728 0 None -3548 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 423 10 2 4 3.2 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
9885106 84773 0 None -1258 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmcl.2011.10.109
CHEMBL223151 84773 0 None -1258 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmcl.2011.10.109
9885106 84773 0 None -1258 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmc.2012.02.018
CHEMBL223151 84773 0 None -1258 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1016/j.bmc.2012.02.018
44304258 102356 0 None -114 3 Mouse 5.6 pKi = 5.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL303787 102356 0 None -114 3 Mouse 5.6 pKi = 5.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
44455158 97721 0 None -933 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 331 8 2 3 2.6 CCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL271488 97721 0 None -933 2 Human 4.6 pKi = 4.6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 331 8 2 3 2.6 CCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
9821171 97866 0 None -51286 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL272276 97866 0 None -51286 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 379 8 2 3 3.1 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.11.020
44304011 202808 0 None -83 3 Mouse 5.6 pKi = 5.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL62305 202808 0 None -83 3 Mouse 5.6 pKi = 5.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 440 12 3 7 2.4 COc1ccccc1C[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
44290263 101329 0 None -3235 2 Human 4.6 pKi = 4.6 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 453 12 3 4 5.2 Cc1cc(O)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
CHEMBL296715 101329 0 None -3235 2 Human 4.6 pKi = 4.6 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 453 12 3 4 5.2 Cc1cc(O)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCCCCCC(=O)O)c1 10.1016/j.bmcl.2004.01.063
77050677 128584 0 None -588 2 Human 6.6 pKi = 6.6 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 385 10 2 4 3.7 CC(C)[C@@H](OCCOc1ccccc1)C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 nan
CHEMBL3667607 128584 0 None -588 2 Human 6.6 pKi = 6.6 Binding
In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing the human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498).Kd values for [3]H-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series.
ChEMBL 385 10 2 4 3.7 CC(C)[C@@H](OCCOc1ccccc1)C(=O)N[C@@H](C)c1ccc(C(=O)O)cc1 nan
11855325 144691 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 144691 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells at pH 6 after 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
21362900 205840 0 None -58 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL83518 205840 0 None -58 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
11418818 66662 0 None -14 4 Mouse 5.6 pKi = 5.6 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 423 10 1 5 5.2 CCCCOc1ccc(C(=O)n2c(C)c(CCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL185369 66662 0 None -14 4 Mouse 5.6 pKi = 5.6 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 423 10 1 5 5.2 CCCCOc1ccc(C(=O)n2c(C)c(CCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
53358921 64441 0 None -562 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 482 7 1 5 5.4 CCN1c2ccccc2C[C@@H]1COc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)c(C)c1 10.1016/j.bmc.2011.06.014
CHEMBL1813287 64441 0 None -562 6 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 482 7 1 5 5.4 CCN1c2ccccc2C[C@@H]1COc1ccc(C(=O)n2c(C)c(CC(=O)O)c3ccccc32)c(C)c1 10.1016/j.bmc.2011.06.014
10181606 206351 0 None -645 7 Human 4.6 pKi = 4.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL87371 206351 0 None -645 7 Human 4.6 pKi = 4.6 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 437 5 1 4 5.2 O=C(/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
118517360 143975 0 None -1380 2 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
CHEMBL3902700 143975 0 None -1380 2 Human 5.6 pKi = 5.6 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 412 8 2 3 4.7 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Cl)c2)cc1 nan
44444714 94138 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 362 10 2 4 2.6 CCCC(C)C(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249341 94138 0 None 2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 362 10 2 4 2.6 CCCC(C)C(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
57893848 75169 0 None -234 2 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2036323 75169 0 None -234 2 Mouse 7.6 pKi = 7.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 535 10 2 8 4.9 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4ccccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
21974362 122044 0 None -1 4 Mouse 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 455 6 1 5 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2COc3ccccc3C2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL359564 122044 0 None -1 4 Mouse 6.6 pKi = 6.6 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 455 6 1 5 4.9 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2COc3ccccc3C2)cc1 10.1016/j.bmcl.2004.07.039
9886718 203163 0 None -398 4 Mouse 6.6 pKi = 6.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
CHEMBL64217 203163 0 None -398 4 Mouse 6.6 pKi = 6.6 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 390 13 3 6 2.7 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O 10.1016/s0960-894x(01)00364-x
118175009 136685 0 None -812 2 Human 5.6 pKi = 5.6 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
CHEMBL3740325 136685 0 None -812 2 Human 5.6 pKi = 5.6 Binding
Antagonist activity at human EP2 receptorAntagonist activity at human EP2 receptor
ChEMBL 429 4 2 2 6.7 Cc1ccc(C(=O)O)c(C)c1NC(=O)c1cc(-c2cccc(Cl)c2)cc2ccccc12 10.1016/j.bmcl.2015.11.023
10157813 201616 0 None -177 4 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL605833 201616 0 None -177 4 Mouse 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 400 9 1 4 4.7 O=C(O)CCc1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
59465587 145190 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 372 13 2 2 6.5 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)O)cc1 nan
CHEMBL3912391 145190 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 372 13 2 2 6.5 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)O)cc1 nan
10205205 94168 0 None -47 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 466 10 2 5 3.3 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249539 94168 0 None -47 2 Human 5.6 pKi = 5.6 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 466 10 2 5 3.3 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(OC(F)(F)F)c2)cc1 10.1016/j.bmcl.2007.09.074
10089562 154422 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL398948 154422 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
44304335 202978 0 None -37 4 Mouse 6.5 pKi = 6.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 422 10 4 4 4.0 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
CHEMBL63061 202978 0 None -37 4 Mouse 6.5 pKi = 6.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 422 10 4 4 4.0 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C/CCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
21362879 16568 0 None -107 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1cc(-c2ccccc2OCc2ccccc2)cs1 10.1016/s0960-894x(03)00794-7
CHEMBL123855 16568 0 None -107 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1cc(-c2ccccc2OCc2ccccc2)cs1 10.1016/s0960-894x(03)00794-7
21362853 18532 0 None -32 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2COc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL127482 18532 0 None -32 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2COc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
12112239 106560 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 549 12 1 6 6.3 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL314200 106560 0 None -8 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 549 12 1 6 6.3 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
21362893 206327 0 None -54 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 535 12 1 6 6.0 Cc1cccc(OCCCOc2ccc(-c3ccccc3CCC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87263 206327 0 None -54 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 535 12 1 6 6.0 Cc1cccc(OCCCOc2ccc(-c3ccccc3CCC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
44320321 206434 0 None -6 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 563 12 1 6 6.6 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87975 206434 0 None -6 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 563 12 1 6 6.6 Cc1cccc(OCCCOc2ccc(-c3ccccc3CC(C)(C)C(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
52941777 16540 0 None 1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 744 16 2 4 10.9 Cc1cccc(/C=C/Cc2ccccc2CC(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2CC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237302 16540 0 None 1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 744 16 2 4 10.9 Cc1cccc(/C=C/Cc2ccccc2CC(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2CC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44393681 66861 0 None -1 3 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 409 9 1 5 5.2 CCCCOc1ccc(C(=O)n2c(CCC)c(C(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL186244 66861 0 None -1 3 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 409 9 1 5 5.2 CCCCOc1ccc(C(=O)n2c(CCC)c(C(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
10202765 172687 0 None -18197 3 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 427 11 2 3 4.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL45008 172687 0 None -18197 3 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 427 11 2 3 4.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
71458758 120862 0 None -21 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
CHEMBL2164612 120862 0 None -21 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
CHEMBL3558858 120862 0 None -21 4 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 615 14 1 4 7.8 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCC[n+]1c(C)cc(/C=C/C=C/c2ccc(N(C)C)cc2)cc1C 10.1021/ml300191g
57396825 69473 0 None -6 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2011.10.109
CHEMBL1933724 69473 0 None -6 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmcl.2011.10.109
57396825 69473 0 None -6 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2012.02.018
CHEMBL1933724 69473 0 None -6 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 398 11 2 6 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 10.1016/j.bmc.2012.02.018
57394893 71306 0 None -3 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
CHEMBL1957435 71306 0 None -3 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.02.018
57394893 71306 0 None -3 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL1957435 71306 0 None -3 4 Mouse 8.5 pKi = 8.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 10 2 6 4.8 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3ccccc3)c2)n1 10.1016/j.bmc.2012.04.008
51039072 129206 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 4 5 4.3 COc1ccc(-c2cc(-c3ccccc3)[nH]c2C(=O)Nc2ccc(C(=O)NO)o2)cc1 nan
CHEMBL3670662 129206 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 4 5 4.3 COc1ccc(-c2cc(-c3ccccc3)[nH]c2C(=O)Nc2ccc(C(=O)NO)o2)cc1 nan
9807448 203172 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1021/jm401431x
CHEMBL64246 203172 0 None 1 4 Human 8.5 pKi = 8.5 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 398 11 3 3 4.7 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1021/jm401431x
10315 2926 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to EP2 (unknown origin) assessed as inhibition constantBinding affinity to EP2 (unknown origin) assessed as inhibition constant
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1016/j.ejmech.2021.113842
44230575 2926 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to EP2 (unknown origin) assessed as inhibition constantBinding affinity to EP2 (unknown origin) assessed as inhibition constant
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1016/j.ejmech.2021.113842
CHEMBL3707245 2926 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to EP2 (unknown origin) assessed as inhibition constantBinding affinity to EP2 (unknown origin) assessed as inhibition constant
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1016/j.ejmech.2021.113842
67078580 129200 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 435 6 2 5 4.7 COC(=O)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(F)cc2)nc1 nan
CHEMBL3670656 129200 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 435 6 2 5 4.7 COC(=O)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(F)cc2)nc1 nan
51039068 129202 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 436 6 4 5 4.0 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(F)cc2)nc1 nan
CHEMBL3670658 129202 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 436 6 4 5 4.0 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3cccs3)cc2-c2ccc(F)cc2)nc1 nan
44304164 203234 0 None - 1 Mouse 7.5 pKi = 7.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 378 11 3 4 3.6 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64483 203234 0 None - 1 Mouse 7.5 pKi = 7.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 378 11 3 4 3.6 CCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
15947857 155513 7 None -269 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 767 12 1 9 6.3 COc1cccc(OC)c1C1(C(=O)NS(=O)(=O)Cc2ccc(N3Cc4c(c(OCC(F)(F)F)c5cccnc5c4OCC(F)(F)F)C3=O)c(C)c2)CC1 10.1016/j.bmcl.2008.01.103
CHEMBL404199 155513 7 None -269 7 Human 6.5 pKi = 6.5 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 767 12 1 9 6.3 COc1cccc(OC)c1C1(C(=O)NS(=O)(=O)Cc2ccc(N3Cc4c(c(OCC(F)(F)F)c5cccnc5c4OCC(F)(F)F)C3=O)c(C)c2)CC1 10.1016/j.bmcl.2008.01.103
44320294 106007 0 None -4 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 557 12 1 6 5.7 O=S(=O)(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL313266 106007 0 None -4 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 557 12 1 6 5.7 O=S(=O)(CCc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
230826 93431 32 None -19 3 Human 5.5 pKi = 5.5 Binding
Binding affinity at prostanoid EP2 receptorBinding affinity at prostanoid EP2 receptor
ChEMBL 268 4 1 2 3.9 O=C(O)COc1ccc(Cl)cc1C1CCCCC1 10.1016/j.bmcl.2007.05.019
CHEMBL245908 93431 32 None -19 3 Human 5.5 pKi = 5.5 Binding
Binding affinity at prostanoid EP2 receptorBinding affinity at prostanoid EP2 receptor
ChEMBL 268 4 1 2 3.9 O=C(O)COc1ccc(Cl)cc1C1CCCCC1 10.1016/j.bmcl.2007.05.019
44269516 43633 30 None -87 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CCC1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL15096 43633 30 None -87 3 Human 5.5 pKi = 5.5 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CCC1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
10413147 9080 0 None -13182 3 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 486 10 3 3 7.2 Cc1cc(C)cc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1099047 9080 0 None -13182 3 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 486 10 3 3 7.2 Cc1cc(C)cc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
44444720 94227 0 None -239 2 Human 5.5 pKi = 5.5 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249953 94227 0 None -239 2 Human 5.5 pKi = 5.5 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
11855870 146280 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 146280 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11855870 146280 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3920756 146280 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 427 11 1 4 5.7 CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
11269563 141610 0 None -281 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 399 5 1 3 5.2 CC(=O)c1cc(F)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
CHEMBL385126 141610 0 None -281 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 399 5 1 3 5.2 CC(=O)c1cc(F)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
10185382 64415 0 None -30 5 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 1 7 4.6 COc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813119 64415 0 None -30 5 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 1 7 4.6 COc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
9867899 203124 0 None -97 3 Mouse 5.5 pKi = 5.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 440 13 3 5 3.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2CCSCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL64072 203124 0 None -97 3 Mouse 5.5 pKi = 5.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 440 13 3 5 3.6 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2CCSCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44303590 202911 0 None -363 3 Mouse 5.5 pKi = 5.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 468 14 3 7 2.6 COCCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL62779 202911 0 None -363 3 Mouse 5.5 pKi = 5.5 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 468 14 3 7 2.6 COCCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
21362867 107102 0 None -128 4 Human 4.5 pKi = 4.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 417 7 1 5 4.6 CSc1cccc(-c2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL315974 107102 0 None -128 4 Human 4.5 pKi = 4.5 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 417 7 1 5 4.6 CSc1cccc(-c2ccccc2CCC(=O)NS(=O)(=O)c2cccs2)c1 10.1016/s0960-894x(02)00518-8
44269544 35252 0 None -7762 3 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 359 11 2 3 3.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1ccccc1 10.1016/j.bmcl.2004.01.063
CHEMBL14359 35252 0 None -7762 3 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 359 11 2 3 3.2 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)Cc1ccccc1 10.1016/j.bmcl.2004.01.063
118517488 153711 0 None -56 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
CHEMBL3981554 153711 0 None -56 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2F)cc1 nan
118517361 153370 0 None -218 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
CHEMBL3978590 153370 0 None -218 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 446 8 2 3 5.1 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(C(F)(F)F)c2)cc1 nan
57393339 69472 0 None -57 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ncc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933723 69472 0 None -57 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ncc(C(=O)O)s2)c1 10.1016/j.bmcl.2011.10.109
57393339 69472 0 None -57 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ncc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933723 69472 0 None -57 2 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ncc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
44290312 178920 0 None -87 2 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 421 11 2 3 5.0 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL47018 178920 0 None -87 2 Human 4.5 pKi = 4.5 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 421 11 2 3 5.0 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.063
72950089 150591 0 None -1621 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
CHEMBL3955128 150591 0 None -1621 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 375 13 2 3 3.8 CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCCCCC(=O)O 10.1021/acs.jmedchem.9b00336
21974331 126546 0 None -5 4 Mouse 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 399 6 1 4 4.8 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365243 126546 0 None -5 4 Mouse 6.5 pKi = 6.5 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 399 6 1 4 4.8 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
10363130 101035 1 None 3 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL294585 101035 1 None 3 2 Mouse 6.5 pKi = 6.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
10185612 64413 0 None -11 4 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 504 6 1 6 5.2 Cc1c(CC(=O)O)c2cc(Cl)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813117 64413 0 None -11 4 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 504 6 1 6 5.2 Cc1c(CC(=O)O)c2cc(Cl)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
11338015 66118 0 None -1 2 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 381 7 2 5 4.2 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(O)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL183983 66118 0 None -1 2 Mouse 5.5 pKi = 5.5 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 381 7 2 5 4.2 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(O)ccc32)cc1 10.1016/j.bmcl.2004.06.006
44303967 202958 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 420 12 3 4 4.8 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCCC1 10.1016/s0960-894x(01)00359-6
CHEMBL62987 202958 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 420 12 3 4 4.8 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCCC1 10.1016/s0960-894x(01)00359-6
10294290 200053 0 None -275 4 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL595632 200053 0 None -275 4 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 398 8 1 4 4.8 O=C(O)/C=C/c1ccc(Cn2cccn2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
50898361 56873 0 None -2630 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 549 7 2 5 5.4 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
CHEMBL1644003 56873 0 None -2630 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 549 7 2 5 5.4 Cc1ccc(S(=O)(=O)NC(=O)NCCc2ccc(-c3c(C(=O)N(C)C)sc4c(C)cc(C)cc34)cc2)cc1 10.1016/j.bmcl.2010.11.118
44304474 202931 0 None -91 5 Mouse 6.5 pKi = 6.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCSCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL62868 202931 0 None -91 5 Mouse 6.5 pKi = 6.5 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCSCCC(=O)O 10.1016/s0960-894x(01)00365-1
10277744 64412 0 None -12 7 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL1813116 64412 0 None -12 7 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1ccc2c(c1)c(CC(=O)O)c(C)n2C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
10291963 84708 0 None -199 6 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.10.109
CHEMBL222715 84708 0 None -199 6 Mouse 6.5 pKi = 6.5 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 359 10 2 3 3.4 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2011.10.109
11476788 161274 0 None -23 6 Human 5.5 pKi = 5.5 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 463 5 1 5 4.4 CS(=O)(=O)c1cc(F)cc2c1c(C(=O)c1ccc(Cl)cc1)c1n2CCC[C@@H]1CC(=O)O 10.1016/j.bmcl.2008.03.015
CHEMBL412070 161274 0 None -23 6 Human 5.5 pKi = 5.5 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 463 5 1 5 4.4 CS(=O)(=O)c1cc(F)cc2c1c(C(=O)c1ccc(Cl)cc1)c1n2CCC[C@@H]1CC(=O)O 10.1016/j.bmcl.2008.03.015
92135977 152896 0 None -275 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
CHEMBL3974652 152896 0 None -275 2 Human 5.5 pKi = 5.5 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(F)c2)cc1 nan
11405770 137908 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 361 11 2 3 3.6 CCCCC[C@H](O)CC[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
CHEMBL376347 137908 0 None -2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 361 11 2 3 3.6 CCCCC[C@H](O)CC[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1021/jm049290a
21362910 16925 0 None -5 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 9 1 2 7.0 O=C(O)CCCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125269 16925 0 None -5 4 Human 5.5 pKi = 5.5 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 9 1 2 7.0 O=C(O)CCCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
57893867 75157 0 None -12302 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 492 12 3 4 4.9 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3[nH]ccc3c2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036311 75157 0 None -12302 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 492 12 3 4 4.9 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccc3[nH]ccc3c2)c1 10.1016/j.bmc.2012.04.008
56658144 64806 0 None 1 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 7 2 5 3.8 CN1C[C@@H](COc2ccc(NC(=O)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819605 64806 0 None 1 2 Mouse 5.5 pKi = 5.5 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 7 2 5 3.8 CN1C[C@@H](COc2ccc(NC(=O)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
44349531 16565 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 394 7 1 2 6.2 O=C(O)Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL123844 16565 0 None -3 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 394 7 1 2 6.2 O=C(O)Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
21362849 168328 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 8 1 2 6.9 CC(Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
CHEMBL434247 168328 0 None -4 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 422 8 1 2 6.9 CC(Cc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
44269464 34477 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL14286 34477 0 None -3 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
118517489 143691 0 None -44 2 Human 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
CHEMBL3900245 143691 0 None -44 2 Human 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cc(F)ccc2F)cc1 nan
44304417 202110 0 None -138 4 Mouse 6.4 pKi = 6.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 438 13 3 4 4.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL60894 202110 0 None -138 4 Mouse 6.4 pKi = 6.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 438 13 3 4 4.3 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44303723 202935 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 12 3 4 4.4 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCC1 10.1016/s0960-894x(01)00359-6
CHEMBL62885 202935 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 12 3 4 4.4 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCCC1 10.1016/s0960-894x(01)00359-6
53358922 64430 0 None -70 6 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 522 6 1 6 5.3 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
CHEMBL1813276 64430 0 None -70 6 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 522 6 1 6 5.3 Cc1c(CC(=O)O)c2cc(F)ccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
21362851 116904 0 None -67 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL338388 116904 0 None -67 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 408 8 1 2 6.6 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
10109445 85143 0 None -537 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 365 10 2 4 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)s1 10.1021/jm049290a
CHEMBL224970 85143 0 None -537 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 365 10 2 4 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)s1 10.1021/jm049290a
1883 3082 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
1916 3082 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
5280360 3082 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
913 3082 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
CHEMBL548 3082 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
DB00917 3082 75 None -6 24 Human 7.4 pKi = 7.4 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/jm401431x
5283086 203310 24 None -269 5 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
CHEMBL64804 203310 24 None -269 5 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
10271490 165893 0 None -29 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 386 9 1 2 5.8 Cc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL424975 165893 0 None -29 3 Human 6.4 pKi = 6.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 386 9 1 2 5.8 Cc1cccc(CCCc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44320433 167943 0 None -45 4 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccccc1CSCCc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL431612 167943 0 None -45 4 Human 5.4 pKi = 5.4 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 521 11 1 5 6.3 O=C(CCc1ccccc1-c1ccccc1CSCCc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
24953283 199448 0 None -426 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 467 6 2 3 6.5 C[C@@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL591431 199448 0 None -426 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 467 6 2 3 6.5 C[C@@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
11855594 152980 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 152980 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855594 152980 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3975238 152980 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 417 10 2 5 4.4 CCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11294166 77045 0 None -213 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 461 6 2 5 4.3 CC(O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1016/j.bmcl.2006.02.062
CHEMBL207203 77045 0 None -213 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 461 6 2 5 4.3 CC(O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1016/j.bmcl.2006.02.062
11294166 77045 0 None -213 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 461 6 2 5 4.3 CC(O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
CHEMBL207203 77045 0 None -213 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 461 6 2 5 4.3 CC(O)c1cc(S(C)(=O)=O)cc2c3c(n(Cc4ccc(Cl)cc4)c12)[C@@H](CC(=O)O)CC3 10.1021/jm0603668
22009003 122616 0 None -436 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(C(O)/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL360290 122616 0 None -436 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 468 8 2 3 6.7 Cc1cccc(C(O)/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
44304008 203242 0 None -549 4 Mouse 5.4 pKi = 5.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 410 11 3 6 2.4 O=C(O)CSCCCS[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/s0960-894x(01)00364-x
CHEMBL64542 203242 0 None -549 4 Mouse 5.4 pKi = 5.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 410 11 3 6 2.4 O=C(O)CSCCCS[C@H]1C(=O)C[C@@H](O)[C@@H]1/C=C/[C@@H](O)Cc1ccccc1 10.1016/s0960-894x(01)00364-x
44138108 184285 0 None -12302 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
CHEMBL483991 184285 0 None -12302 6 Human 5.4 pKi = 5.4 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
51039064 129201 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 5 5 3.7 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(O)cc2)cc1 nan
CHEMBL3670657 129201 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 5 5 3.7 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(O)cc2)cc1 nan
1883 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
1916 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
5280360 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
913 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
CHEMBL548 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
DB00917 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.09.074
1883 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
1916 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
5280360 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
913 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
CHEMBL548 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
DB00917 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.11.020
1883 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
1916 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
5280360 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
913 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
CHEMBL548 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
DB00917 3082 75 None -6 24 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2007.05.025
44304124 102623 0 None - 1 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 12 3 4 4.3 CC(C)CC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL304225 102623 0 None - 1 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 12 3 4 4.3 CC(C)CC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
11855324 142605 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 142605 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
11855324 142605 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
CHEMBL3891401 142605 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 371 6 1 4 4.0 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 nan
44269486 166842 0 None -144 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL428524 166842 0 None -144 3 Human 5.4 pKi = 5.4 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 341 14 2 3 3.7 CCCCCC(O)CC[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
138 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
1882 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
5280723 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
CHEMBL495 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
DB00770 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
138 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
1882 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
5280723 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
CHEMBL495 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
DB00770 3081 88 None -19 18 Mouse 7.4 pKi = 7.4 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00364-x
10183680 127166 0 None -2 3 Mouse 6.4 pKi = 6.4 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365696 127166 0 None -2 3 Mouse 6.4 pKi = 6.4 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
11597294 166176 4 None -489 8 Human 6.4 pKi = 6.4 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 4 1 2 5.7 O=C(O)C[C@H]1CCc2c1n(Cc1ccc(Cl)cc1)c1c(Br)cc(F)cc21 10.1021/jm0603668
CHEMBL426387 166176 4 None -489 8 Human 6.4 pKi = 6.4 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
ChEMBL 435 4 1 2 5.7 O=C(O)C[C@H]1CCc2c1n(Cc1ccc(Cl)cc1)c1c(Br)cc(F)cc21 10.1021/jm0603668
57391585 69467 0 None -457 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 393 8 2 3 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933718 69467 0 None -457 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 393 8 2 3 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmcl.2011.10.109
57391585 69467 0 None -457 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 393 8 2 3 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933718 69467 0 None -457 2 Mouse 6.4 pKi = 6.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 393 8 2 3 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1016/j.bmc.2012.02.018
10112486 16901 0 None -7 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1ccc(-c2ccccc2OCc2ccccc2)s1 10.1016/s0960-894x(03)00794-7
CHEMBL125110 16901 0 None -7 4 Human 5.4 pKi = 5.4 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 414 8 1 3 6.7 O=C(O)CCc1ccccc1-c1ccc(-c2ccccc2OCc2ccccc2)s1 10.1016/s0960-894x(03)00794-7
44390831 63637 0 None -575 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 402 8 1 2 6.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccc(F)cc1 10.1016/j.bmcl.2004.11.051
CHEMBL180089 63637 0 None -575 4 Human 5.4 pKi = 5.4 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 402 8 1 2 6.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccc(F)cc1 10.1016/j.bmcl.2004.11.051
44289969 101378 0 None -17 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 345 10 2 3 3.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccccc1 10.1016/j.bmcl.2004.01.063
CHEMBL297139 101378 0 None -17 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 345 10 2 3 3.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccccc1 10.1016/j.bmcl.2004.01.063
57398586 69476 0 None -53 3 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 422 9 2 7 3.0 Cc1ccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)o1 10.1016/j.bmcl.2011.10.109
CHEMBL1933727 69476 0 None -53 3 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 422 9 2 7 3.0 Cc1ccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)o1 10.1016/j.bmcl.2011.10.109
44290262 178519 0 None -10 2 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL46671 178519 0 None -10 2 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccc(Cl)cc2)c1 10.1016/j.bmcl.2004.01.063
44290272 101443 0 None -6760 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2Cl)c1 10.1016/j.bmcl.2004.01.063
CHEMBL297578 101443 0 None -6760 2 Human 4.4 pKi = 4.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2ccccc2Cl)c1 10.1016/j.bmcl.2004.01.063
44442327 94459 0 None -147 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL251294 94459 0 None -147 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 345 9 2 3 3.0 CCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
71462285 81880 0 None -239 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 478 10 1 5 6.0 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
CHEMBL2164608 81880 0 None -239 4 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta countingDisplacement of [3H]PGE2 from human EP2R expressed in chem1 cells after 2hrs by beta counting
ChEMBL 478 10 1 5 6.0 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCCn1cc2ccccc2c1C#N 10.1021/ml300191g
44303711 102352 0 None 18 3 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL303763 102352 0 None 18 3 Mouse 7.4 pKi = 7.4 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 406 13 3 4 4.4 CCCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
24953285 200869 0 None -53 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 453 6 2 3 5.9 O=C(O)c1ccc(CNC(=O)c2c(Cl)sc(Cl)c2Cc2cccc(Cl)c2)cc1 10.1021/jm901771h
CHEMBL601299 200869 0 None -53 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 453 6 2 3 5.9 O=C(O)c1ccc(CNC(=O)c2c(Cl)sc(Cl)c2Cc2cccc(Cl)c2)cc1 10.1021/jm901771h
155520370 170476 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 7 1 5 5.2 CC(C)(C)c1ccc(CN(Cc2ccc3cc(C(=O)O)oc3c2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
CHEMBL4448995 170476 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation countingDisplacement of [3H]prostaglandin E2 from human EP2 receptor expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting
ChEMBL 478 7 1 5 5.2 CC(C)(C)c1ccc(CN(Cc2ccc3cc(C(=O)O)oc3c2)S(=O)(=O)c2cccnc2)cc1 10.1021/acs.jmedchem.8b00808
56665068 64824 0 None -3 4 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 2 5 5.1 CN1C[C@@H](COc2ccc(C(=O)Nc3cc(CC(=O)O)ccc3Cl)c(Cl)c2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819622 64824 0 None -3 4 Mouse 7.4 pKi = 7.4 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 500 7 2 5 5.1 CN1C[C@@H](COc2ccc(C(=O)Nc3cc(CC(=O)O)ccc3Cl)c(Cl)c2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
10269242 155575 0 None -2 2 Human 5.4 pKi = 5.4 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL404413 155575 0 None -2 2 Human 5.4 pKi = 5.4 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 348 9 2 4 2.2 CC(C)CC(O)CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.09.074
21974528 124450 0 None -22 5 Mouse 6.4 pKi = 6.4 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 441 6 1 5 4.6 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Cc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL363984 124450 0 None -22 5 Mouse 6.4 pKi = 6.4 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 441 6 1 5 4.6 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2Cc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
44289922 163524 0 None -954 5 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmcl.2004.01.063
CHEMBL42027 163524 0 None -954 5 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 339 13 2 3 3.5 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/j.bmcl.2004.01.063
10227492 16898 0 None -218 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 476 8 1 2 7.9 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2c(Cl)cccc2Cl)c1 10.1016/s0960-894x(03)00794-7
CHEMBL125087 16898 0 None -218 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 476 8 1 2 7.9 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2OCc2c(Cl)cccc2Cl)c1 10.1016/s0960-894x(03)00794-7
44349528 113801 0 None -131 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 7.2 CC(CC(=O)O)c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL332446 113801 0 None -131 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 7.2 CC(CC(=O)O)c1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
59465601 149894 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.4 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3949271 149894 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.4 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
24953286 201384 0 None -151 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(Cl)c1 10.1021/jm901771h
CHEMBL604546 201384 0 None -151 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 427 6 2 3 5.8 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(Cl)c1 10.1021/jm901771h
54013831 146460 0 None 3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3922151 146460 0 None 3 2 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)cc1 nan
9845064 69348 0 None -194 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 420 13 2 5 3.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)[C@@H]2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929528 69348 0 None -194 3 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 420 13 2 5 3.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)[C@@H]2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
11395329 123847 0 None -17 2 Mouse 5.3 pKi = 5.3 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 395 8 1 5 4.5 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL362541 123847 0 None -17 2 Mouse 5.3 pKi = 5.3 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 395 8 1 5 4.5 CCCCOc1ccc(C(=O)n2c(C)c(CC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
9885106 84773 0 None -2344 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1021/jm049290a
CHEMBL223151 84773 0 None -2344 6 Human 5.3 pKi = 5.3 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 357 13 2 4 3.1 CCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSCCCC(=O)O 10.1021/jm049290a
44304389 203153 0 None -40 4 Mouse 7.3 pKi = 7.3 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCSCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL64188 203153 0 None -40 4 Mouse 7.3 pKi = 7.3 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCSCC(=O)O 10.1016/s0960-894x(01)00365-1
10168694 206349 0 None -309 4 Human 5.3 pKi = 5.3 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 671 17 1 7 8.2 O=C(CCc1ccccc1-c1ccc(OCCCOc2cccc(CSCCc3ccccc3)c2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL87366 206349 0 None -309 4 Human 5.3 pKi = 5.3 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 671 17 1 7 8.2 O=C(CCc1ccccc1-c1ccc(OCCCOc2cccc(CSCCc3ccccc3)c2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
12521 2197 0 None -20892 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
72722131 2197 0 None -20892 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
CHEMBL3918816 2197 0 None -20892 4 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting methodDisplacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
ChEMBL 399 11 2 3 3.6 FC1(C(N([C@H](C1)/C=C/[C@H]([C@H](CC#CCC)C)O)CCCCCCC(=O)O)=O)F 10.1021/acs.jmedchem.9b00336
1929 1605 55 None -11 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
9890801 1605 55 None -11 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
CHEMBL563646 1605 55 None -11 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
DB12022 1605 55 None -11 2 Human 7.3 pKi = 7.3 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/jm401431x
10299717 64417 0 None -144 6 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1cc(OC[C@@H]2CN(C)c3ccccc3O2)ccc1C(=O)n1c(C)c(CC(=O)O)c2ccccc21 10.1016/j.bmc.2011.06.014
CHEMBL1813120 64417 0 None -144 6 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 484 6 1 6 4.9 Cc1cc(OC[C@@H]2CN(C)c3ccccc3O2)ccc1C(=O)n1c(C)c(CC(=O)O)c2ccccc21 10.1016/j.bmc.2011.06.014
59465588 143526 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 422 13 1 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3898887 143526 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 422 13 1 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465575 145067 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)c1 nan
CHEMBL3911438 145067 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 402 13 1 4 5.9 CCCCCC(O)c1cccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)OC)c1 nan
59465592 149702 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 386 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)OC)cc1 nan
CHEMBL3947785 149702 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 386 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CCC=C2CCCCCCC(=O)OC)cc1 nan
59465590 150945 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 406 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)OC)cc1 nan
CHEMBL3957958 150945 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 406 13 1 3 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)OC)cc1 nan
59465584 151430 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 13 2 2 6.7 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCCO)cc1 nan
CHEMBL3961847 151430 0 None - 1 Human 4.3 pKi = 4.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 394 13 2 2 6.7 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCCO)cc1 nan
11855325 144691 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 144691 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855325 144691 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3908484 144691 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 387 6 1 4 4.5 CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
57564500 151210 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3959926 151210 0 None 4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 440 12 2 2 6.8 CCCCCC(O)c1ccc([C@H]2[C@@H](Cl)C[C@@H](Cl)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
12137443 84703 0 None -5495 4 Human 5.3 pKi = 5.3 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 491 9 2 3 6.1 Cc1cc(Cl)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
CHEMBL222677 84703 0 None -5495 4 Human 5.3 pKi = 5.3 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 491 9 2 3 6.1 Cc1cc(Cl)ccc1-c1cccc([C@H](O)CC[C@H]2CCC(=O)N2CCc2ccc(C(=O)O)cc2)c1 10.1021/jm049290a
11224239 64804 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 7 2 5 3.8 CN1C[C@@H](COc2ccc(C(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819603 64804 0 None -1 4 Mouse 6.3 pKi = 6.3 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 7 2 5 3.8 CN1C[C@@H](COc2ccc(C(=O)Nc3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
11282034 66630 0 None -13 3 Mouse 5.3 pKi = 5.3 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 437 11 1 5 5.6 CCCCOc1ccc(C(=O)n2c(C)c(CCCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL185277 66630 0 None -13 3 Mouse 5.3 pKi = 5.3 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 437 11 1 5 5.6 CCCCOc1ccc(C(=O)n2c(C)c(CCCCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
46887240 8754 0 None -13489 3 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 472 10 3 3 6.9 Cc1cccc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
CHEMBL1096382 8754 0 None -13489 3 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 472 10 3 3 6.9 Cc1cccc(Nc2ccc(CCC(=O)O)c(C(=O)N[C@H](CC(C)C)c3cc(C)cc(C)c3)c2)c1 10.1016/j.bmc.2010.03.028
52945419 16534 0 None -478 4 Human 5.3 pKi = 5.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 772 16 4 6 10.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(O)c1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237296 16534 0 None -478 4 Human 5.3 pKi = 5.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 772 16 4 6 10.7 O=C(O)/C=C/c1ccccc1/C=C/Cc1cccc(O)c1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1cccc(O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
56672018 64807 0 None -6 3 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 446 7 1 5 3.9 CN1C[C@@H](COc2ccc(C(=O)N(C)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
CHEMBL1819606 64807 0 None -6 3 Mouse 5.3 pKi = 5.3 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 446 7 1 5 3.9 CN1C[C@@H](COc2ccc(C(=O)N(C)c3cccc(CC(=O)O)c3)cc2)Oc2ccccc21 10.1016/j.bmc.2011.08.007
44303709 203200 0 None -870 3 Mouse 5.3 pKi = 5.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 470 13 3 7 3.3 CSCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL64338 203200 0 None -870 3 Mouse 5.3 pKi = 5.3 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 470 13 3 7 3.3 CSCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
59465581 144112 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3903611 144112 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 428 11 2 4 6.1 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
44455236 95475 0 None -53 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 373 11 2 3 3.8 CCCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
CHEMBL257217 95475 0 None -53 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from human EP2 receptorDisplacement of [3H]PGE2 from human EP2 receptor
ChEMBL 373 11 2 3 3.8 CCCCCC[C@H](O)/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.11.020
21974448 66963 0 None -53 4 Mouse 6.3 pKi = 6.3 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 429 8 1 5 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCOc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL186735 66963 0 None -53 4 Mouse 6.3 pKi = 6.3 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 429 8 1 5 4.7 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCCOc2ccccc2)cc1 10.1016/j.bmcl.2004.07.039
11155228 66106 0 None -1778 4 Human 5.3 pKi = 5.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 452 8 1 2 7.2 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
CHEMBL183919 66106 0 None -1778 4 Human 5.3 pKi = 5.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 452 8 1 2 7.2 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1c(Cl)cccc1Cl 10.1016/j.bmcl.2004.11.051
44419347 82775 0 None -1778 4 Human 5.3 pKi = 5.3 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 452 8 1 2 7.2 Cc1ccc(OCc2c(Cl)cccc2Cl)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL217988 82775 0 None -1778 4 Human 5.3 pKi = 5.3 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 452 8 1 2 7.2 Cc1ccc(OCc2c(Cl)cccc2Cl)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
10298293 94167 0 None -426 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249538 94167 0 None -426 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 460 9 2 4 3.1 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Br)c2)cc1 10.1016/j.bmcl.2007.09.074
52944193 16533 0 None -63 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237295 16533 0 None -63 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
21362905 171307 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 6.9 CC(Cc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
CHEMBL446098 171307 0 None -8 4 Human 5.3 pKi = 5.3 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 428 8 1 3 6.9 CC(Cc1ccccc1-c1csc(-c2ccccc2OCc2ccccc2)c1)C(=O)O 10.1016/s0960-894x(03)00794-7
58932683 75287 0 None -354 3 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
CHEMBL2037289 75287 0 None -354 3 Mouse 7.3 pKi = 7.3 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 549 10 2 8 5.2 Cc1ccc2nc(-c3cccc(C[C@H](O)/C=C/[C@H]4CCC(=O)N4CCSc4nc(C(=O)O)cs4)c3)oc2c1 10.1016/j.bmc.2012.04.008
44444716 154837 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 484 12 1 3 5.4 CC(CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1)Cc1cccc(CCc2ccccc2)c1 10.1016/j.bmcl.2007.09.074
CHEMBL400447 154837 0 None -12 2 Human 6.3 pKi = 6.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 484 12 1 3 5.4 CC(CCN1CCC(=O)N1CCc1ccc(C(=O)O)cc1)Cc1cccc(CCc2ccccc2)c1 10.1016/j.bmcl.2007.09.074
10295421 94197 0 None -316 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 416 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249744 94197 0 None -316 2 Human 5.3 pKi = 5.3 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 416 9 2 4 3.0 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(Cl)c2)cc1 10.1016/j.bmcl.2007.09.074
44234032 147925 0 None -81 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 415 8 1 4 5.0 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2cccc(F)c2)CC1 10.1021/acs.jmedchem.6b00871
CHEMBL3933704 147925 0 None -81 6 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 415 8 1 4 5.0 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2cccc(F)c2)CC1 10.1021/acs.jmedchem.6b00871
11165749 165959 0 None -20 3 Mouse 5.2 pKi = 5.2 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 409 9 1 5 4.8 CCCCOc1ccc(C(=O)n2c(C)c(CCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL425167 165959 0 None -20 3 Mouse 5.2 pKi = 5.2 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 409 9 1 5 4.8 CCCCOc1ccc(C(=O)n2c(C)c(CCC(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
44520990 199853 0 None -6 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 410 6 2 4 5.3 Cc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
CHEMBL594423 199853 0 None -6 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 410 6 2 4 5.3 Cc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
11855867 145983 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 145983 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
11855867 145983 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3918349 145983 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 389 8 2 5 3.6 CCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 nan
44304403 169097 0 None -16 4 Mouse 7.2 pKi = 7.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 420 12 3 4 3.8 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
CHEMBL439934 169097 0 None -16 4 Mouse 7.2 pKi = 7.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 420 12 3 4 3.8 COCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)C[C@@H](F)[C@@H]2C/C=C/CCCC(=O)O)c1 10.1016/s0960-894x(01)00365-1
44290314 173974 0 None -5754 3 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 403 10 2 4 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccc(C(F)(F)F)o1 10.1016/j.bmcl.2004.01.063
CHEMBL45418 173974 0 None -5754 3 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 403 10 2 4 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1ccc(C(F)(F)F)o1 10.1016/j.bmcl.2004.01.063
44320272 206262 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 507 10 1 5 5.9 O=C(Cc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL86886 206262 0 None -1 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 507 10 1 5 5.9 O=C(Cc1ccccc1-c1ccc(CSCCc2ccccc2)cc1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
24952929 2554 42 None -9332 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
4041 2554 42 None -9332 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
CHEMBL597997 2554 42 None -9332 5 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
10295336 201446 0 None -53 4 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 415 8 1 3 4.7 O=C(O)/C=C/c1ccc(CN2CCCC2=O)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL604897 201446 0 None -53 4 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 415 8 1 3 4.7 O=C(O)/C=C/c1ccc(CN2CCCC2=O)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
44290266 161708 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 353 12 3 4 2.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)N1C/C=C/CCCC(=O)O 10.1016/j.bmcl.2004.01.063
CHEMBL413509 161708 0 None -8 4 Human 8.2 pKi = 8.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 353 12 3 4 2.3 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)N1C/C=C/CCCC(=O)O 10.1016/j.bmcl.2004.01.063
44394380 125429 0 None -6 4 Mouse 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 457 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2COc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL364593 125429 0 None -6 4 Mouse 7.2 pKi = 7.2 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 457 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2COc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
44442337 94007 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 381 8 1 2 5.0 C/C(=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)CC1CCCC1 10.1016/j.bmcl.2007.05.025
CHEMBL248678 94007 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 381 8 1 2 5.0 C/C(=C/C=C/[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)CC1CCCC1 10.1016/j.bmcl.2007.05.025
44442331 94490 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251505 94490 0 None -15 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C(C)=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
10278907 64418 0 None -138 3 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 504 6 1 6 5.2 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
CHEMBL1813121 64418 0 None -138 3 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 504 6 1 6 5.2 Cc1c(CC(=O)O)c2ccccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1Cl 10.1016/j.bmc.2011.06.014
59465570 143259 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 392 13 2 2 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3896693 143259 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 392 13 2 2 6.6 CCCCCC(O)c1ccc([C@H]2CC[C@@H](F)[C@@H]2CCCCCCC(=O)O)cc1 nan
134147021 150024 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 414 13 2 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)s1 nan
CHEMBL3950412 150024 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 414 13 2 3 6.9 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)O)s1 nan
10204257 94169 0 None -104 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 450 9 2 4 3.4 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249540 94169 0 None -104 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 450 9 2 4 3.4 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2007.09.074
44219292 112582 38 None -204 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 431 8 1 4 5.5 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00871
CHEMBL3301604 112582 38 None -204 7 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hrDisplacement of [3H]-PGE2 from recombinant human EP2 receptor expressed in HEK293 cell membranes incubated for 1 hr
ChEMBL 431 8 1 4 5.5 O=C(O)COC[C@H]1CC[C@H](COC(=O)N(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1021/acs.jmedchem.6b00871
57400087 71302 0 None -2 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 8 2 3 4.0 O=C(O)CCc1cccc(N2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1957431 71302 0 None -2 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 413 8 2 3 4.0 O=C(O)CCc1cccc(N2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(Cl)c2)c1 10.1016/j.bmc.2012.02.018
57893916 75155 0 None -1288 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 454 12 2 5 3.8 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccn2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036309 75155 0 None -1288 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 454 12 2 5 3.8 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2ccccn2)c1 10.1016/j.bmc.2012.04.008
56672019 64814 0 None -7 4 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 7 2 5 4.5 Cc1cc(CC(=O)O)cc(NC(=O)c2ccc(OC[C@@H]3CN(C)c4ccccc4O3)cc2C)c1 10.1016/j.bmc.2011.08.007
CHEMBL1819612 64814 0 None -7 4 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 460 7 2 5 4.5 Cc1cc(CC(=O)O)cc(NC(=O)c2ccc(OC[C@@H]3CN(C)c4ccccc4O3)cc2C)c1 10.1016/j.bmc.2011.08.007
8541 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
9824353 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
CHEMBL292964 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/s0960-894x(01)00365-1
8541 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse EP2 receptor by competitive binding assayBinding affinity to mouse EP2 receptor by competitive binding assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/jm9018756
9824353 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse EP2 receptor by competitive binding assayBinding affinity to mouse EP2 receptor by competitive binding assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/jm9018756
CHEMBL292964 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Binding affinity to mouse EP2 receptor by competitive binding assayBinding affinity to mouse EP2 receptor by competitive binding assay
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/jm9018756
8541 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
9824353 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
CHEMBL292964 2944 2 None -1548 4 Mouse 6.2 pKi = 6.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1016/j.bmc.2011.12.009
10221497 94139 0 None -91 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 382 9 2 4 2.4 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249342 94139 0 None -91 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 382 9 2 4 2.4 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.09.074
10272306 154836 0 None -173 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 400 9 2 4 2.5 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(F)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL400446 154836 0 None -173 2 Human 5.2 pKi = 5.2 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 400 9 2 4 2.5 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(F)c2)cc1 10.1016/j.bmcl.2007.09.074
71452690 78625 0 None 15 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 400 9 1 4 5.1 c1ccc(CCSCc2ccc(-c3ccccc3CCc3nnn[nH]3)cc2)cc1 10.1016/s0960-894x(02)00518-8
CHEMBL2112332 78625 0 None 15 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 400 9 1 4 5.1 c1ccc(CCSCc2ccc(-c3ccccc3CCc3nnn[nH]3)cc2)cc1 10.1016/s0960-894x(02)00518-8
52950151 16537 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1.Cc1cccc(C/C=C/c2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237299 16537 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1.Cc1cccc(C/C=C/c2cccc(/C=C/C(=O)O)c2)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
22008967 83149 0 None -2691 4 Human 5.2 pKi = 5.2 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL218228 83149 0 None -2691 4 Human 5.2 pKi = 5.2 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
22008966 83150 0 None -2691 4 Human 5.2 pKi = 5.2 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
CHEMBL218229 83150 0 None -2691 4 Human 5.2 pKi = 5.2 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 439 8 1 5 4.5 COc1ccc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)cc1 10.1016/j.bmcl.2006.08.025
13230981 35067 0 None -1122 3 Human 5.2 pKi = 5.2 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 339 13 2 3 3.5 CCCCCC(O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
CHEMBL14334 35067 0 None -1122 3 Human 5.2 pKi = 5.2 Binding
Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAsBinding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly expressing the corresponding human prostanoid cDNAs
ChEMBL 339 13 2 3 3.5 CCCCCC(O)/C=C/[C@H]1CCC(=O)N1CCCCCCC(=O)O 10.1016/s0960-894x(03)00042-8
10348006 75290 0 None -338 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 569 10 2 8 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
CHEMBL2037292 75290 0 None -338 3 Mouse 7.2 pKi = 7.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 569 10 2 8 5.5 O=C(O)c1csc(SCCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)Cc2cccc(-c3nc4cc(Cl)ccc4o3)c2)n1 10.1016/j.bmc.2012.04.008
52943000 16535 0 None -26 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237297 16535 0 None -26 4 Human 6.2 pKi = 6.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 740 16 2 4 11.2 O=C(O)/C=C/c1ccccc1/C=C/Cc1ccccc1OCc1ccccc1.O=C(O)/C=C/c1ccccc1C/C=C\c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
10319835 69367 0 None -16982 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 417 13 2 3 4.9 CCCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929547 69367 0 None -16982 3 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 417 13 2 3 4.9 CCCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=S)N2CCCCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
44520991 199702 0 None -7 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 426 7 2 5 5.0 COc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
CHEMBL593260 199702 0 None -7 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 426 7 2 5 5.0 COc1ccc(/C=C/C(=O)O)c(OCCC2(C)CCc3c(C)c(O)c(C)c(C)c3O2)c1 10.1016/j.bmc.2009.08.007
44289977 162759 0 None -478 2 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 413 10 2 3 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
CHEMBL417171 162759 0 None -478 2 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 413 10 2 3 4.3 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.063
12003887 71299 0 None -776 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 411 11 2 4 3.4 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(Cl)c1 10.1016/j.bmc.2012.02.018
CHEMBL1957308 71299 0 None -776 2 Mouse 5.2 pKi = 5.2 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 411 11 2 4 3.4 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(Cl)c1 10.1016/j.bmc.2012.02.018
67078970 129199 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 416 6 3 5 4.4 COC(=O)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(O)cc2)cc1 nan
CHEMBL3670655 129199 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 416 6 3 5 4.4 COC(=O)c1ccc(CNC(=O)c2[nH]c(-c3ccoc3)cc2-c2ccc(O)cc2)cc1 nan
25114442 3061 56 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.1021/acs.jmedchem.1c00816
5817 3061 56 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.1021/acs.jmedchem.1c00816
CHEMBL3286797 3061 56 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.1021/acs.jmedchem.1c00816
DB12024 3061 56 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constantBinding affinity to human EP2 receptor expressed in CHO cells assessed as inhibition constant
ChEMBL 409 6 1 4 3.6 COc1ccc2c(c1)ccc(c2)OCC1(CN(C1)C(=O)c1ccc(cc1)F)C(=O)O 10.1021/acs.jmedchem.1c00816
59465571 146285 0 None 21 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
CHEMBL3920796 146285 0 None 21 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 386 12 2 3 5.6 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2C/C=C\CCCC(=O)O)cc1 nan
59465600 151698 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.3 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL3964261 151698 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.3 CCCCC(O)Cc1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
21362845 106903 0 None -630 4 Human 4.2 pKi = 4.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 556 7 1 5 7.3 O=C(/C=C/c1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
CHEMBL314616 106903 0 None -630 4 Human 4.2 pKi = 4.2 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 556 7 1 5 7.3 O=C(/C=C/c1ccccc1-c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1)NS(=O)(=O)c1cccs1 10.1016/s0960-894x(02)00518-8
52943002 16539 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 716 14 2 4 11.1 Cc1cccc(/C=C\Cc2ccccc2C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237301 16539 0 None -2 4 Human 5.2 pKi = 5.2 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 716 14 2 4 11.1 Cc1cccc(/C=C\Cc2ccccc2C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
67245477 144883 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 428 13 1 4 7.0 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)s1 nan
CHEMBL3909989 144883 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 428 13 1 4 7.0 CCCCCC(O)c1ccc([C@H]2CC[C@@H](Cl)[C@@H]2CCCCCCC(=O)OC)s1 nan
44289921 164371 0 None -9332 3 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 365 11 2 3 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)CC1CCCCC1 10.1016/j.bmcl.2004.01.063
CHEMBL42129 164371 0 None -9332 3 Human 4.2 pKi = 4.2 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 365 11 2 3 3.9 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)CC1CCCCC1 10.1016/j.bmcl.2004.01.063
57893891 75159 0 None -1995 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 12 2 6 5.0 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3s2)c1 10.1016/j.bmc.2012.04.008
CHEMBL2036313 75159 0 None -1995 2 Mouse 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 12 2 6 5.0 O=C(O)CCCSCCN1C(=O)CC[C@@H]1/C=C/[C@@H](O)Cc1cccc(-c2nc3ccccc3s2)c1 10.1016/j.bmc.2012.04.008
24952929 2554 42 None -11481 5 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
4041 2554 42 None -11481 5 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
CHEMBL597997 2554 42 None -11481 5 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from rat EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 473 6 2 3 6.1 OC(=O)c1ccc(cc1)C1(CC1)NC(=O)c1c(C)sc(c1Cc1ccc(cc1)C(F)(F)F)C 10.1021/jm901771h
1892 747 20 None -2 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
25886893 747 20 None -2 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
CHEMBL1628262 747 20 None -2 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to EP2 receptor (unknown origin) by competitive binding assayBinding affinity to EP2 receptor (unknown origin) by competitive binding assay
ChEMBL 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1021/jm401431x
44304181 203273 0 None 12 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 394 13 3 4 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL64663 203273 0 None 12 2 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 394 13 3 4 4.3 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
9965922 63877 0 None -724 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 294 5 2 2 4.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1O 10.1016/j.bmcl.2004.11.051
CHEMBL180389 63877 0 None -724 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 294 5 2 2 4.1 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1O 10.1016/j.bmcl.2004.11.051
24765153 184529 0 None -11481 8 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
CHEMBL484778 184529 0 None -11481 8 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 434 5 1 4 6.6 CC(C)c1nccc2c1c(Sc1ccc(Cl)c(Cl)c1)c1n2CC[C@H]1CC(=O)O 10.1016/j.bmcl.2009.03.010
9910141 100875 0 None -1513 3 Mouse 5.1 pKi = 5.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 422 11 4 6 2.7 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCSCCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
CHEMBL293647 100875 0 None -1513 3 Mouse 5.1 pKi = 5.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 422 11 4 6 2.7 Cc1cc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCSCCCC(=O)O)ccc1O 10.1016/s0960-894x(01)00365-1
118517485 142750 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
CHEMBL3892492 142750 0 None -50 2 Human 6.1 pKi = 6.1 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
24952580 200562 0 None -575 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 467 6 2 3 6.5 C[C@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
CHEMBL599052 200562 0 None -575 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 467 6 2 3 6.5 C[C@H](NC(=O)c1c(Cl)sc(Cl)c1Cc1cccc(Cl)c1)c1ccc(C(=O)O)cc1 10.1021/jm901771h
10452108 94008 0 None -25 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 375 7 1 2 4.6 C/C(=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)c1ccccc1 10.1016/j.bmcl.2007.05.025
CHEMBL248679 94008 0 None -25 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 375 7 1 2 4.6 C/C(=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1)c1ccccc1 10.1016/j.bmcl.2007.05.025
44304388 203152 0 None -151 5 Mouse 7.1 pKi = 7.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL64187 203152 0 None -151 5 Mouse 7.1 pKi = 7.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O 10.1016/s0960-894x(01)00365-1
11440167 84718 0 None -75 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 371 9 2 3 3.4 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
CHEMBL222782 84718 0 None -75 3 Human 7.1 pKi = 7.1 Binding
Binding affinity to human EP2 receptorBinding affinity to human EP2 receptor
ChEMBL 371 9 2 3 3.4 O=C(O)c1ccc(CCN2C(=O)CC[C@@H]2/C=C/[C@@H](O)CCC2CCC2)cc1 10.1021/jm049290a
44444722 94256 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 402 11 2 4 3.5 CCCC1(C(O)CCCN2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.09.074
CHEMBL250153 94256 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 402 11 2 4 3.5 CCCC1(C(O)CCCN2CCC(=O)N2CCc2ccc(C(=O)O)cc2)CCC1 10.1016/j.bmcl.2007.09.074
52945294 16547 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237317 16547 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
52945294 16547 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL1237317 16547 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 800 18 2 6 11.3 COc1cc(/C=C\Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1.COc1cc(C/C=C/c2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
10111602 83228 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 400 9 1 3 5.6 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL218626 83228 0 None -95 3 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 400 9 1 3 5.6 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)O)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
22990263 16793 0 None -4 3 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 292 3 1 1 4.8 O=C(O)/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(03)00794-7
CHEMBL124574 16793 0 None -4 3 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 292 3 1 1 4.8 O=C(O)/C=C/c1ccccc1-c1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(03)00794-7
10410111 102841 0 None -398 3 Mouse 6.1 pKi = 6.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL305568 102841 0 None -398 3 Mouse 6.1 pKi = 6.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 424 11 3 6 2.7 Cc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
44304009 100736 0 None -1479 3 Mouse 5.1 pKi = 5.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 482 15 3 7 3.3 CCCOCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
CHEMBL292717 100736 0 None -1479 3 Mouse 5.1 pKi = 5.1 Binding
Evaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptorEvaluated for its competitive binding affinity towards mouse Prostanoid EP2 receptor in CHO cells expressing prostanoid receptor
ChEMBL 482 15 3 7 3.3 CCCOCc1cccc(C[C@H](O)/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2SCCCSCC(=O)O)c1 10.1016/s0960-894x(01)00364-x
11210487 64294 0 None 177 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 356 7 1 2 5.5 O=C(O)/C=C/c1ccccc1/C=C/c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL181035 64294 0 None 177 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 356 7 1 2 5.5 O=C(O)/C=C/c1ccccc1/C=C/c1ccccc1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
16725337 149601 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 149601 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 minsDisplacement of [3H]-PGE2 from human EP2 receptor expressed in HEK293 cells after 60 mins
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
16725337 149601 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
CHEMBL3947001 149601 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 443 12 2 4 6.0 CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 nan
24953625 201532 0 None -323 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(C(F)(F)F)c1 10.1021/jm901771h
CHEMBL605330 201532 0 None -323 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation countingDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293-EBNA cells by scintillation counting
ChEMBL 461 6 2 3 6.2 Cc1sc(C)c(C(=O)N[C@@H](C)c2ccc(C(=O)O)cc2)c1Cc1cccc(C(F)(F)F)c1 10.1021/jm901771h
10302378 82779 0 None -6606 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 539 9 1 5 6.6 O=C(/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL217991 82779 0 None -6606 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 539 9 1 5 6.6 O=C(/C=C/c1ccccc1Cc1ccc2cc(OCc3ccccc3)ccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
22009006 141564 0 None -1584 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1/C=C/Cc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL384878 141564 0 None -1584 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1/C=C/Cc1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
9953337 141660 0 None -1584 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1C/C=C/c1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL385396 141660 0 None -1584 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 409 7 1 4 4.5 O=C(/C=C/c1ccccc1C/C=C/c1ccccc1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
25003075 6838 18 None -28183 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from human prostanoid EP2 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP2 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 478 6 2 3 5.8 O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
CHEMBL1084009 6838 18 None -28183 7 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]PGE2 from human prostanoid EP2 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from human prostanoid EP2 receptor expressed in HEK293-EBNA cells after 60 mins by scintillation counting
ChEMBL 478 6 2 3 5.8 O=C(O)c1ccc(C2(NC(=O)c3cccc4ccn(Cc5ccc(C(F)(F)F)cc5)c34)CC2)cc1 10.1016/j.bmcl.2010.04.065
10247632 77991 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL2096894 77991 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 355 9 1 2 4.6 CCCC/C=C(C)/C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
10178073 16559 0 None -1148 4 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/s0960-894x(03)00794-7
CHEMBL123794 16559 0 None -1148 4 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/s0960-894x(03)00794-7
9944231 18035 0 None -10 4 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 302 5 1 1 5.0 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL126472 18035 0 None -10 4 Human 5.1 pKi = 5.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 302 5 1 1 5.0 O=C(O)CCc1ccccc1-c1cccc(-c2ccccc2)c1 10.1016/s0960-894x(03)00794-7
10178073 16559 0 None -1148 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL123794 16559 0 None -1148 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
12112238 118071 0 None -10 4 Human 6.1 pKi = 6.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 406 7 1 2 6.7 O=C(O)/C=C/c1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
CHEMBL340501 118071 0 None -10 4 Human 6.1 pKi = 6.1 Binding
Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.Affinity at human Prostanoid EP2 receptor in the human embryonic kidney (HEK) 293 cell line.
ChEMBL 406 7 1 2 6.7 O=C(O)/C=C/c1ccccc1-c1cccc(-c2ccccc2OCc2ccccc2)c1 10.1016/s0960-894x(03)00794-7
44444715 94198 0 None -25 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 450 12 2 4 3.7 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(CCC3CC3)c2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249745 94198 0 None -25 2 Human 5.1 pKi = 5.1 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 450 12 2 4 3.7 O=C(O)c1ccc(CCN2C(=O)CCN2CCC(O)Cc2cccc(CCC3CC3)c2)cc1 10.1016/j.bmcl.2007.09.074
57398585 69470 0 None -6 2 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 414 9 2 5 3.2 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933721 69470 0 None -6 2 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 414 9 2 5 3.2 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
57398585 69470 0 None -6 2 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 9 2 5 3.2 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933721 69470 0 None -6 2 Mouse 7.1 pKi = 7.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 414 9 2 5 3.2 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCCc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
56834112 69347 0 None -1071 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 421 13 2 5 2.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
CHEMBL1929527 69347 0 None -1071 2 Mouse 5.1 pKi = 5.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counterDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counter
ChEMBL 421 13 2 5 2.9 COCc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSCCCC(=O)O)c1 10.1016/j.bmc.2011.12.009
44290271 179048 0 None -204 2 Human 4.1 pKi = 4.1 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2004.01.063
CHEMBL47138 179048 0 None -204 2 Human 4.1 pKi = 4.1 Binding
Binding affinity was determined against prostanoid EP2 receptorBinding affinity was determined against prostanoid EP2 receptor
ChEMBL 455 11 2 3 5.6 O=C(O)CCCCCCN1C(=O)CC[C@@H]1/C=C/C(O)c1cccc(-c2cccc(Cl)c2)c1 10.1016/j.bmcl.2004.01.063
52944193 16533 0 None -63 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL1237295 16533 0 None -63 4 Human 6.1 pKi = 6.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 768 16 2 4 11.9 Cc1cccc(/C=C/Cc2ccccc2/C=C/C(=O)O)c1OCc1ccccc1.Cc1cccc(C/C=C/c2ccccc2/C=C/C(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44419374 82995 0 None -95 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL218123 82995 0 None -95 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
44419379 137863 0 None -95 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL376053 137863 0 None -95 4 Human 6.1 pKi = 6.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 384 8 1 2 5.9 Cc1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2006.08.025
44320388 206408 0 None -56 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 536 11 2 6 5.8 Cc1cccc(OCCCOc2ccc(-c3ccccc3CNC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
CHEMBL87797 206408 0 None -56 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human Prostanoid EP2 receptor.Binding affinity at human Prostanoid EP2 receptor.
ChEMBL 536 11 2 6 5.8 Cc1cccc(OCCCOc2ccc(-c3ccccc3CNC(=O)NS(=O)(=O)c3cccs3)cc2)c1 10.1016/s0960-894x(02)00518-8
9954562 84137 0 None -478 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
CHEMBL220802 84137 0 None -478 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 433 6 1 4 5.0 O=C(/C=C/c1ccccc1Cc1ccc2ccccc2c1)NS(=O)(=O)c1cccs1 10.1016/j.bmcl.2006.08.025
138 3081 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
1882 3081 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
5280723 3081 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
CHEMBL495 3081 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
DB00770 3081 88 None -19 18 Mouse 7.1 pKi = 7.1 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
52945423 16541 0 None -33 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 824 18 2 6 11.6 CC(=O)c1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1.CC(=O)c1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2004.11.051
CHEMBL1237303 16541 0 None -33 4 Human 5.1 pKi = 5.1 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 824 18 2 6 11.6 CC(=O)c1ccc(OCc2ccccc2)c(/C=C/Cc2ccccc2/C=C/C(=O)O)c1.CC(=O)c1ccc(OCc2ccccc2)c(C/C=C/c2ccccc2/C=C/C(=O)O)c1 10.1016/j.bmcl.2004.11.051
22009008 83157 0 None -5495 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL218280 83157 0 None -5495 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(/C=C/Cc2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
22009004 141751 0 None -2884 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
CHEMBL385955 141751 0 None -2884 4 Human 5.1 pKi = 5.1 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 545 11 1 6 6.1 COc1cc(C/C=C/c2ccccc2/C=C/C(=O)NS(=O)(=O)c2cccs2)ccc1OCc1ccccc1 10.1016/j.bmcl.2006.08.025
132836 59695 23 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL1722929 59695 23 None 1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 7.3 membranes incubated for 60 mins
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
44442332 94527 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
CHEMBL251709 94527 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cellsDisplacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
ChEMBL 341 9 1 2 4.2 CCCC/C=C\C=C\[C@H]1CCC(=O)N1CCc1ccc(C(=O)O)cc1 10.1016/j.bmcl.2007.05.025
44393680 66345 0 None -4 2 Mouse 5.1 pKi = 5.1 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 367 7 1 5 4.2 CCCCOc1ccc(C(=O)n2cc(C(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
CHEMBL185087 66345 0 None -4 2 Mouse 5.1 pKi = 5.1 Binding
Binding affinity for mouse Prostanoid EP2 receptorBinding affinity for mouse Prostanoid EP2 receptor
ChEMBL 367 7 1 5 4.2 CCCCOc1ccc(C(=O)n2cc(C(=O)O)c3cc(OC)ccc32)cc1 10.1016/j.bmcl.2004.06.006
84973026 129208 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 441 7 4 4 4.7 COc1ccc(-c2cc(-c3ccccc3)[nH]c2C(=O)Nc2cccc(CC(=O)NO)c2)cc1 nan
CHEMBL3670664 129208 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 441 7 4 4 4.7 COc1ccc(-c2cc(-c3ccccc3)[nH]c2C(=O)Nc2cccc(CC(=O)NO)c2)cc1 nan
57894063 75165 0 None -5 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
CHEMBL2036319 75165 0 None -5 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 11 2 7 4.8 COc1ccc(-c2cccc(C[C@H](O)/C=C/[C@H]3CCC(=O)N3CCSc3nc(C(=O)O)cs3)c2)cc1 10.1016/j.bmc.2012.04.008
56835070 69471 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
CHEMBL1933722 69471 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmcl.2011.10.109
56835070 69471 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1933722 69471 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.02.018
56835070 69471 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
CHEMBL1933722 69471 0 None -22 3 Mouse 8.0 pKi = 8.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 432 9 2 6 3.4 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2nc(C(=O)O)cs2)c1 10.1016/j.bmc.2012.04.008
84973025 129205 5 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 5 5 3.7 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccc(O)cc3)cc2-c2ccoc2)cc1 nan
CHEMBL3670661 129205 5 None - 1 Human 8.0 pKi = 8.0 Binding
Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).Binding Assay: Measurement of EP2 receptor binding affinity was carried out according to the method of Abramovitz et al. (Biochimica et Biophysica Acta, 1483, 285 (2000)). A test compound dissolved in dimethylsulfoxide and [3H]PGE2 (NET-428, available from PerkinElmer Inc.) (final concentration: 10 nM) were added to a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2, 1 mM EDTA) in which 10 μg of a membrane fraction (ES-562-M, available from Euroscreen S.A.) of HEK293 cells expressing human EP2 receptor had been suspended, followed by incubation at 30° C. for 60 minutes. The membrane fraction was recovered on glass fiber filter paper (GF/B, available from Whatman PLC) using a cell harvester (M30R, available from Brandel Inc.), and after washing with a buffer solution (10 mM MES-KOH (pH 6.0), 10 mM MgCl2), radioactivity was measured with a liquid scintillation analyzer (2000CA, available from Packard).
ChEMBL 417 6 5 5 3.7 O=C(NO)c1ccc(CNC(=O)c2[nH]c(-c3ccc(O)cc3)cc2-c2ccoc2)cc1 nan
21974374 127247 0 None -1 5 Mouse 7.1 pKi = 7.1 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 455 6 1 5 5.0 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2CCc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
CHEMBL365829 127247 0 None -1 5 Mouse 7.1 pKi = 7.1 Binding
Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2Ability to inhibit the binding of [3H]-PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP2
ChEMBL 455 6 1 5 5.0 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OCC2CCc3ccccc3O2)cc1 10.1016/j.bmcl.2004.07.039
44304334 201576 0 None -45 5 Mouse 7.0 pKi = 7.0 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
CHEMBL60555 201576 0 None -45 5 Mouse 7.0 pKi = 7.0 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
ChEMBL 372 13 3 5 3.0 CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CSCCCCC(=O)O 10.1016/s0960-894x(01)00365-1
57396659 71301 0 None -114 3 Mouse 7.0 pKi = 7.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 431 9 2 5 4.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
CHEMBL1957430 71301 0 None -114 3 Mouse 7.0 pKi = 7.0 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 431 9 2 5 4.0 Cc1cccc(C[C@H](O)/C=C/[C@H]2CCC(=O)N2CCSc2ccc(C(=O)O)s2)c1 10.1016/j.bmc.2012.02.018
44304199 100817 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2C/C=C/CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL293242 100817 0 None - 1 Mouse 7.0 pKi = 7.0 Binding
Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.Binding affinity towards mouse Prostanoid EP2 receptor expressed in CHO cells.
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/C2[C@H](O)CC(=O)[C@@H]2C/C=C/CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
44444719 94226 0 None -67 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 382 9 2 4 2.4 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.09.074
CHEMBL249952 94226 0 None -67 2 Human 5.0 pKi = 5.0 Binding
Binding affinity at human prostaglandin EP2 receptorBinding affinity at human prostaglandin EP2 receptor
ChEMBL 382 9 2 4 2.4 O=C(O)c1ccc(CCN2C(=O)CCN2CC[C@@H](O)Cc2ccccc2)cc1 10.1016/j.bmcl.2007.09.074
10273914 199672 0 None -70 3 Mouse 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(COc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
CHEMBL593041 199672 0 None -70 3 Mouse 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 424 9 1 3 6.1 O=C(O)/C=C/c1ccc(COc2ccccc2)cc1OCCc1ccc2ccccc2c1 10.1016/j.bmc.2009.08.007
46230201 200616 0 None -436 3 Mouse 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
CHEMBL599355 200616 0 None -436 3 Mouse 5.0 pKi = 5.0 Binding
Displacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation countingDisplacement of [3H]PGE2 from mouse EP2 receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 453 9 2 3 5.9 C[C@H](NC(=O)c1cc(COc2ccccc2)ccc1CCC(=O)O)c1cccc2ccccc12 10.1016/j.bmc.2009.11.023
118517485 142750 0 None -50 2 Human 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
CHEMBL3892492 142750 0 None -50 2 Human 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 396 8 2 3 4.2 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)cc2)cc1 nan
118517490 153155 0 None -125 2 Human 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
CHEMBL3976710 153155 0 None -125 2 Human 5.0 pKi = 5.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 414 8 2 3 4.4 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2ccc(F)c(F)c2)cc1 nan
9865111 63865 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 388 10 1 2 5.8 Cc1cccc(CCCc2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL180343 63865 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 388 10 1 2 5.8 Cc1cccc(CCCc2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
44419350 84142 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 388 10 1 2 5.8 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)O)c1 10.1016/j.bmcl.2006.08.025
CHEMBL220820 84142 0 None -14 4 Human 6.0 pKi = 6.0 Binding
Binding affinity to EP2 receptorBinding affinity to EP2 receptor
ChEMBL 388 10 1 2 5.8 Cc1ccc(OCc2ccccc2)c(CCCc2ccccc2CCC(=O)O)c1 10.1016/j.bmcl.2006.08.025
118517359 144396 0 None -114 2 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
CHEMBL3906016 144396 0 None -114 2 Human 6.0 pKi = 6.0 Binding
Radioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations wRadioligand Binding Assay: The cell homogenate was centrifuged at 19000 r.p.m. for 20 min at 4° C. using a Beckman Ti-60 rotor. The resultant pellet was resuspended in TME buffer to give a final 1 mg/ml protein concentration, as determined by Biorad assay. Radioligand binding competition assays vs. [3H-]17-phenyl PGF2a , (5 nM) were performed in a 100 μl volume for 60 min. Binding reactions were started by adding plasma membrane fraction. The reaction was terminated by the addition of 4 ml ice-cold TRIS-HCl buffer and rapid filtration through glass fiber GF/B filters using a Brandel cell harvester. The filters were washed 3 times with ice-cold buffer and oven dried for one hour. [3H-] PGE2 (specific activity 180 Ci mmol) was used as the radioligand for EP receptors. [3H] 17-phenyl PGF2a, was employed for FP receptor binding studies. Binding studies employing EP1, EP2, EP4 and FP receptors were performed in duplicate in at least three separate experiments. A 200 μl assay volume was used. Incubations w
ChEMBL 456 8 2 3 4.8 O=C(O)c1ccc(CC[C@H]2C(=O)CC[C@@H]2/C=C/C(O)Cc2cccc(Br)c2)cc1 nan
10116114 125886 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
CHEMBL364841 125886 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.06.014
10116114 125886 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.08.007
CHEMBL364841 125886 0 None -28 8 Mouse 7.0 pKi = 7 Binding
Displacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]PGE2 from mouse prostaglandin EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
ChEMBL 470 6 1 6 4.5 Cc1cc2c(CC(=O)O)cccc2n1C(=O)c1ccc(OC[C@@H]2CN(C)c3ccccc3O2)cc1 10.1016/j.bmc.2011.08.007
44390806 64078 0 None -24 3 Human 6.0 pKi = 6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 386 8 1 2 5.9 Cc1cccc(C2CC2c2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
CHEMBL180752 64078 0 None -24 3 Human 6.0 pKi = 6 Binding
Binding affinity for human prostanoid EP2 receptorBinding affinity for human prostanoid EP2 receptor
ChEMBL 386 8 1 2 5.9 Cc1cccc(C2CC2c2ccccc2CCC(=O)O)c1OCc1ccccc1 10.1016/j.bmcl.2004.11.051
1883 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
1883 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
1916 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
1916 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
5280360 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
5280360 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
913 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
913 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
CHEMBL548 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
CHEMBL548 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
DB00917 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
DB00917 3082 75 None -6 24 Human 7.8 pKd = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
1883 3082 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
1916 3082 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
5280360 3082 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
913 3082 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
CHEMBL548 3082 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
DB00917 3082 75 None -15 24 Mouse 7.7 pKd None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14699136
1883 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
1883 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
1916 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
1916 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
5280360 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
5280360 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
913 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
913 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
CHEMBL548 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
CHEMBL548 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
DB00917 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9440134
DB00917 3082 75 None -7 24 Rat 8.1 pKd None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
138 3081 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 3081 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 3081 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 3081 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 3081 88 3H-PGE2 -19 18 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
None 216046 0 3H-PGE2 -66 3 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 350 11 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=C2)CCCCC(=O)O)O)O None
5090 15561 106 Functional -1348 30 Dog 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5090 15561 106 Functional -35 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15561 106 Functional -1348 30 Dog 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15561 106 Functional -35 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5311035 97803 29 3H-PGE2 4 9 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
CHEMBL271896 97803 29 3H-PGE2 4 9 Mouse 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 408 13 2 5 4.3 CCCC1([C@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2CCCCCCC(=O)OC)CCC1 None
1883 3082 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1916 3082 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5280360 3082 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
913 3082 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
CHEMBL548 3082 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
DB00917 3082 75 3H-PGE2 -15 24 Mouse 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1917 927 0 3H-PGE2 -22 9 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
5311044 927 0 3H-PGE2 -22 9 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
631 927 0 3H-PGE2 -22 9 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
CHEMBL160629 927 0 3H-PGE2 -22 9 Mouse 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
89077401 216044 0 3H-PGE2 -144 12 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 360 8 3 3 3.5 CC#CCC(C)C(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
133126726 216045 0 3H-PGE2 -151 14 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
24868263 216045 0 3H-PGE2 -151 14 Mouse 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 350 10 3 3 4.1 CCCCCC(C=CC1C(CC2C1CC(=CCCCC(=O)O)C2)O)O None
1440 2027 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1909 2027 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
3715 2027 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
CHEMBL6 2027 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
DB00328 2027 119 Functional -9 6 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
None 216043 0 3H-PGE2 -9 5 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 366 12 2 3 5.2 CCCCCC(C=CC1CC2CC(C1CC=CCCCC(=O)O)S2)O None
None 216049 0 3H-PGE2 -2 3 Mouse 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 512 11 2 4 4.6 C1CC2C(C(C1O2)CC=CCCCC(=O)O)C=CC(COC3=CC=C(C=C3)I)O None
1928 317 0 3H-PGE2 -3 3 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O None
5310998 317 0 3H-PGE2 -3 3 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O None
1817 2542 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 2542 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 2542 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 2542 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 2542 68 3H-PGE2 -6 12 Mouse 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1440 2027 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1440 2027 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1909 2027 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1909 2027 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
3715 2027 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
3715 2027 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
CHEMBL6 2027 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
CHEMBL6 2027 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
DB00328 2027 119 Functional -38 6 Dog 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
DB00328 2027 119 Functional -9 6 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
119461 320 72 3H-PGE2 1 10 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
1896 320 72 3H-PGE2 1 10 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
CHEMBL1317823 320 72 3H-PGE2 1 10 Mouse 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C None
5090 15561 106 Functional -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15561 106 Functional -35 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5090 15561 106 Functional -35 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15561 106 Functional -35 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
5077 3578 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
7552 3578 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
9913767 3578 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
CHEMBL238804 3578 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
DB11362 3578 79 None 1 4 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C None
1884 3083 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
5280363 3083 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
912 3083 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
CHEMBL815 3083 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
DB12789 3083 52 None -36 22 Rat 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
138107701 187464 46 None -5 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
5311181 187464 46 None -5 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
CHEMBL494 187464 46 None -5 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
138107701 187464 46 None -5 15 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
5311181 187464 46 None -5 15 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
CHEMBL494 187464 46 None -5 15 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
1917 927 0 None -22 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
5311044 927 0 None -22 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
631 927 0 None -22 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
CHEMBL160629 927 0 None -22 9 Mouse 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C None
138107701 187464 46 None -5 15 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
5311181 187464 46 None -5 15 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
CHEMBL494 187464 46 None -5 15 Rat 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O None
1884 3083 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
5280363 3083 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
912 3083 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
CHEMBL815 3083 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
DB12789 3083 52 None -37 22 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O None
656511 217716 0 None -1 7 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 539 6 3 8 -0.2 CC1(C)S[C@@H]2[C@H](NC(=O)[C@H](NC(=O)N3CCN(C3=O)S(C)(=O)=O)C3=CC=CC=C3)C(=O)N2[C@H]1C(O)=O None
3356 2280 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
4326 2280 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
9867642 2280 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
CHEMBL426559 2280 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
DB11629 2280 73 None -53 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to human EP2 receptor expressed in HEK293 cellsBinding affinity to human EP2 receptor expressed in HEK293 cells
Drug Central 435 5 1 4 4.4 OC(=O)C[C@H]1CCc2c1n(Cc1ccc(cc1)Cl)c1c2cc(cc1S(=O)(=O)C)F None
123619 216393 0 None 125 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
5090 15561 106 None 28 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15561 106 None 28 30 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
1817 2542 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
1936 2542 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
5282381 2542 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
CHEMBL606 2542 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
DB00929 2542 68 None -7 12 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C None
138 3081 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 3081 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 3081 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 3081 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 3081 88 None -19 18 Mouse 8.1 pKi = 8.1 Binding
Affinity for mouse Prostanoid EP2 receptor expressed in CHO cellsAffinity for mouse Prostanoid EP2 receptor expressed in CHO cells
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1883 3082 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1916 3082 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5280360 3082 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
913 3082 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
CHEMBL548 3082 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
DB00917 3082 75 None -15 24 Mouse 8.1 pKi = 8.1 Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation countingDisplacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1440 2027 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
1909 2027 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
3715 2027 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
CHEMBL6 2027 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
DB00328 2027 119 None 3 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 357 4 1 4 3.9 COc1ccc2c(c1)c(CC(=O)O)c(n2C(=O)c1ccc(cc1)Cl)C None
138 3081 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
1882 3081 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
5280723 3081 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
CHEMBL495 3081 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
DB00770 3081 88 None -8 18 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O None
2720 3854 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
5820 3854 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
6918140 3854 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
CHEMBL1237119 3854 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
DB00374 3854 59 None -1 6 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O None
1883 3082 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
1916 3082 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5280360 3082 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
913 3082 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
CHEMBL548 3082 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
DB00917 3082 75 None -6 24 Human 8.1 pKi = 8.1 Binding
Binding affinity to human prostanoid EP2 receptor by radioligand displacement assayBinding affinity to human prostanoid EP2 receptor by radioligand displacement assay
Drug Central 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O None
5852 2617 55 None -288 4 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 17545310
9931891 2617 55 None -288 4 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 17545310
CHEMBL239226 2617 55 None -288 4 Human 5.2 pKi = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 419 11 1 5 4.9 OC(=O)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 17545310
1895 2007 0 None -125 16 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
6435378 2007 0 None -125 16 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
CHEMBL236025 2007 0 None -125 16 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
DB01088 2007 0 None -125 16 Rat 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9537820
1892 747 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10462542
1892 747 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
25886893 747 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10462542
25886893 747 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
CHEMBL1628262 747 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10462542
CHEMBL1628262 747 20 None -2 9 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10634944
1883 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
1883 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
1883 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
1916 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
1916 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
1916 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
5280360 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
5280360 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
5280360 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
913 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
913 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
913 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
CHEMBL548 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
CHEMBL548 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
CHEMBL548 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
DB00917 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10746663
DB00917 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 14607240
DB00917 3082 75 None -15 24 Mouse 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9313928
1883 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
1883 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
1883 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
1916 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
1916 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
1916 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
5280360 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
5280360 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
5280360 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
913 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
913 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
913 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
CHEMBL548 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
CHEMBL548 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
CHEMBL548 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
DB00917 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10462542
DB00917 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10634944
DB00917 3082 75 None -6 24 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 16604093
138 3081 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
138 3081 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1882 3081 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
1882 3081 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
5280723 3081 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
5280723 3081 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL495 3081 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
CHEMBL495 3081 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
DB00770 3081 88 None -19 18 Mouse 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
DB00770 3081 88 None -8 18 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
138 3081 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
1882 3081 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
5280723 3081 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
CHEMBL495 3081 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
DB00770 3081 88 None -9 18 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 8163486
1883 3082 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
1916 3082 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
5280360 3082 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
913 3082 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
CHEMBL548 3082 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
DB00917 3082 75 None -7 24 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 9537820
10110 3087 0 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 2 3 4.3 OC(=O)COc1cccc(c1)NC(=O)c1cc(ccc1F)c1cccc(c1)F 30341781
59654860 3087 0 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 6 2 3 4.3 OC(=O)COc1cccc(c1)NC(=O)c1cc(ccc1F)c1cccc(c1)F 30341781
2720 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
2720 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
5820 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
5820 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
6918140 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
6918140 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
CHEMBL1237119 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
CHEMBL1237119 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
DB00374 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 22480736
DB00374 3854 59 None -1 6 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 390 10 3 4 3.6 CCCCC[C@@H](CC[C@H]1[C@H](O)C[C@H]2[C@@H]1Cc1cccc(c1C2)OCC(=O)O)O 25542069
10315 2926 28 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 29332128
44230575 2926 28 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 29332128
CHEMBL3707245 2926 28 None - 1 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 29332128
1932 2942 5 None -1 6 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10746663
5311228 2942 5 None -1 6 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10746663
CHEMBL3286796 2942 5 None -1 6 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 12 3 3 4.8 C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O 10746663
1888 3900 29 None -501 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
1974 3900 29 None -501 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
5311493 3900 29 None -501 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
CHEMBL521784 3900 29 None -501 17 Human 4.9 pKi None 4.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 10634944
1817 2542 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
1936 2542 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
5282381 2542 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
CHEMBL606 2542 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
DB00929 2542 68 None -7 12 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 13 2 5 4.0 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)OC)(O)C 10634944
1881 3079 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
1891 3079 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
448457 3079 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
CHEMBL1235252 3079 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
DB02056 3079 0 None -4570 21 Human 5.0 pKi None 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
1888 3900 29 None -316 17 Rat 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
1974 3900 29 None -316 17 Rat 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
5311493 3900 29 None -316 17 Rat 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
CHEMBL521784 3900 29 None -316 17 Rat 5.1 pKi None 5.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 12 2 3 4.3 CCCCC[C@@H](/C=C/[C@H]1[C@@H]2OC[C@H]([C@@H]1C/C=C\CCCC(=O)O)C2)O 9537820
1881 3079 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1891 3079 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
448457 3079 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
CHEMBL1235252 3079 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
DB02056 3079 0 None -2290 21 Rat 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1C(=O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1931 2946 0 None -371 2 Mouse 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 10746663
5311229 2946 0 None -371 2 Mouse 5.4 pKi None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 14 1 4 4.6 CCCCC[C@@H](/C=C/[C@H]1[C@H](OC)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)OC 10746663
1884 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
1884 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
5280363 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
5280363 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
912 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
912 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
CHEMBL815 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
CHEMBL815 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
DB12789 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10462542
DB12789 3083 52 None -37 22 Human 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 10634944
1884 3083 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
5280363 3083 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
912 3083 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
CHEMBL815 3083 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
DB12789 3083 52 None -36 22 Rat 5.6 pKi None 5.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 12 4 4 3.0 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@@H]([C@@H]1C/C=C\CCCC(=O)O)O)O 9537820
1913 2464 0 None -15848 15 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10462542
1913 2464 0 None -15848 15 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10634944
5311223 2464 0 None -15848 15 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10462542
5311223 2464 0 None -15848 15 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 10634944
1895 2007 0 None -199 16 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
6435378 2007 0 None -199 16 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
CHEMBL236025 2007 0 None -199 16 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
DB01088 2007 0 None -199 16 Human 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 10634944
1933 2943 0 None -199 3 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 14 3 7 2.9 COCc1ccccc1CC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O)O 10746663
5311230 2943 0 None -199 3 Mouse 5.7 pKi None 5.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 14 3 7 2.9 COCc1ccccc1CC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1SCCCSCC(=O)O)O 10746663
1893 795 0 None -112 13 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
5311242 795 0 None -112 13 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
CHEMBL148319 795 0 None -112 13 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 9313928
1895 2007 0 None -158 16 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
6435378 2007 0 None -158 16 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
CHEMBL236025 2007 0 None -158 16 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
DB01088 2007 0 None -158 16 Mouse 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 360 8 3 3 3.5 CC#CCC([C@@H](/C=C/C1[C@H](O)C[C@H]2[C@@H]1C/C(=C/CCCC(=O)O)/C2)O)C 9313928
1947 28 0 None -39 3 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 12 4 5 2.2 O[C@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)CCC[C@H](O)C 8078484
5283038 28 0 None -39 3 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 12 4 5 2.2 O[C@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)CCC[C@H](O)C 8078484
119461 320 72 None -3 10 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
1896 320 72 None -3 10 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
CHEMBL1317823 320 72 None -3 10 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 10634944
1917 927 0 None -22 9 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
5311044 927 0 None -22 9 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
631 927 0 None -22 9 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
CHEMBL160629 927 0 None -22 9 Mouse 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 6 3 4 2.2 CCC#CC[C@@H]([C@@H](C#C[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C/COCC(=O)O)/C2)O)C 9313928
1913 2464 0 None -8912 15 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 9537820
5311223 2464 0 None -8912 15 Rat 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 374 12 2 4 4.0 OC(=O)CCCCCC[C@@H]1[C@@H](/C=C/[C@H](COc2ccccc2)O)CCC1=O 9537820
1928 317 0 None -12 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O 10462542
5310998 317 0 None -12 3 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O 10462542
1893 795 0 None -70 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
5311242 795 0 None -70 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
CHEMBL148319 795 0 None -70 13 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 10 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1C/C(=C\CCCC(=O)O)/C2)O 10634944
1934 2090 0 None -63 3 Mouse 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
5311244 2090 0 None -63 3 Mouse 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
CHEMBL4522827 2090 0 None -63 3 Mouse 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 350 11 3 3 4.1 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)C[C@H]2[C@@H]1CC(=C2)CCCCC(=O)O)O 9313928
1912 26 0 None -213 6 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
5283068 26 0 None -213 6 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
CHEMBL1879970 26 0 None -213 6 Rat 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 386 11 3 4 3.3 OC(=O)CCC/C=C\C[C@H]1C(=O)C[C@H]([C@@H]1/C=C/[C@H](CCc1ccccc1)O)O 9537820
1930 3333 25 None -999 3 Mouse 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
9803828 3333 25 None -999 3 Mouse 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
CHEMBL303960 3333 25 None -999 3 Mouse 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
DB16315 3333 25 None -999 3 Mouse 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 450 13 2 7 2.9 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)OC)O 11917107
119461 320 72 None -1 10 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9537820
1896 320 72 None -1 10 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9537820
CHEMBL1317823 320 72 None -1 10 Rat 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9537820
119461 320 72 None 1 10 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9313928
1896 320 72 None 1 10 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9313928
CHEMBL1317823 320 72 None 1 10 Mouse 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 4 3.4 CC(Oc1ccc2c(c1)oc1c(c2=O)cc(cc1)C(=O)O)C 9313928
1928 317 0 None -3 3 Mouse 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O 9313928
5310998 317 0 None -3 3 Mouse 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 388 13 2 3 5.8 CCCCCC(c1ccc(cc1)C1CCC(=O)C1CCCCCCC(=O)O)O 9313928
1947 28 0 None -5 3 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 12 4 5 2.2 O[C@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)CCC[C@H](O)C 9537820
5283038 28 0 None -5 3 Rat 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 12 4 5 2.2 O[C@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)CCC[C@H](O)C 9537820
1892 747 20 None 2 9 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
25886893 747 20 None 2 9 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL1628262 747 20 None 2 9 Rat 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 394 13 3 4 4.3 CCCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1925 7 0 None -39 6 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
5283055 7 0 None -39 6 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
CHEMBL3246389 7 0 None -39 6 Mouse 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9313928
1925 7 0 None -25 6 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
5283055 7 0 None -25 6 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
CHEMBL3246389 7 0 None -25 6 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 13 2 3 4.5 CCCCC[C@@H](/C=C/[C@H]1CCC(=O)[C@@H]1CCCCCCC(=O)O)O 9537820
1935 2541 0 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
6436406 2541 0 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
CHEMBL1201377 2541 0 None -3 3 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 368 13 3 4 3.9 CCCCC(C/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)(O)C 10634944
1926 24 0 None -8 3 Mouse 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928
5283066 24 0 None -8 3 Mouse 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928
CHEMBL1221529 24 0 None -8 3 Mouse 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 12 3 4 3.9 CCCCC([C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O)(C)C 9313928