Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
145971909 164137 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 164137 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 163145 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 163145 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 138933 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 138933 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 163189 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 163189 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 138861 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 138861 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 152000 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 152000 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 152731 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 152731 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 138907 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 138907 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 194218 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 194218 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 138883 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 138883 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 138778 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 138778 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 1569 46 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 1569 46 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 1569 46 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 1569 46 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 163800 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 163800 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 163277 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 163277 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 139779 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 139779 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 138876 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 138876 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 149057 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 149057 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 136715 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 136715 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 138947 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 138947 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 138886 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 138886 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 138820 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 138820 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 138820 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 138820 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 139751 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 139751 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 150901 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 150901 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 143569 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 143569 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 193244 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 193244 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 163444 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 163444 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 2870 20 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 2870 20 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 2870 20 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 139764 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 139764 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 142249 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 142249 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 145735 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 145735 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 152000 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 152000 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 152731 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 152731 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 171153 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 171153 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 152000 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 152000 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 138956 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 138956 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 139668 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 139668 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 145140 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 145140 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 143147 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 143147 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 152351 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 152351 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 2888 1 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 2888 1 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 2888 1 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 145740 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 145740 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 152824 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 152824 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 146993 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 146993 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 194292 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 194292 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 150728 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 150728 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 175785 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 175785 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 175785 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 138836 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 138836 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 153810 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 153810 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 201534 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 201534 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 142206 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 142206 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 150460 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 150460 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 138923 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 138923 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 143040 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 143040 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 176098 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 176098 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 176098 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 175948 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 175948 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 175948 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 143829 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 143829 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 143891 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 143891 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 143891 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 143891 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 143431 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 143431 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 143147 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 143147 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 153340 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 153340 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 138842 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 138842 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 138842 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 138842 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 139682 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 139682 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 139701 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 139701 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 175629 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 175629 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 152042 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 152042 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 148400 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 148400 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 100406 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 100406 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 93780 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 93780 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 193703 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 193703 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 144146 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 144146 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 144146 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 144146 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 139678 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 139678 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 148734 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 148734 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 74802 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 74802 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 201506 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 201506 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 148659 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 148659 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 143891 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 143891 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 84270 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 84270 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 138815 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 138815 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 150641 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 150641 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 147724 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 147724 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 142887 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 142887 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 177000 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 177000 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 74803 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 74803 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 155023 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 155023 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 142645 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 142645 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 142715 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 142715 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 144683 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 144683 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 145400 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 145400 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 149350 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 149350 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 149826 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 149826 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 94010 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 94010 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 145735 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 145735 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 145735 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 145735 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 147762 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 147762 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 152016 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 152016 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 74804 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 74804 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 153165 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 153165 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 153798 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 153798 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 1569 46 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 1569 46 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 1569 46 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 1569 46 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 142236 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 142236 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 142362 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 142362 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 146843 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 146843 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 141989 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 141989 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 170828 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 170828 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 143095 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 143095 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 143322 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 143322 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 151360 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 151360 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 70947 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 70947 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 84270 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 84270 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 70947 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 70947 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 145438 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 145438 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 145438 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 145438 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 95105 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 95105 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 175893 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 175893 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 175893 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 94078 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 94078 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 138818 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 138818 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 143568 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 143568 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 163836 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 163836 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 175744 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 175744 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 175744 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 145350 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 145350 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 145568 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 145568 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 148253 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 148253 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 149933 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 149933 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 163559 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 163559 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 201610 19 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 201610 19 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 138926 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 138926 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 193243 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 193243 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 175962 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 175962 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 175962 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 3020 84 None -1 9 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 3020 84 None -1 9 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 3020 84 None -1 9 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 3020 84 None -1 9 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 3020 84 None -1 9 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 175678 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 175678 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 175678 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 175936 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 175936 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 175936 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 175914 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 175914 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 175914 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 201473 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 201473 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 138874 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 138874 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 152731 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 152731 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 193418 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 193418 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 152243 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 152243 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 186871 39 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 186871 39 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 186871 39 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 142730 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 142730 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 152435 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 152435 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 152435 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 152435 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 145863 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 145863 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 145863 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 145863 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 145915 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 145915 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 100553 0 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 100553 0 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 94040 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 94040 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 150641 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 150641 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 150930 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 150930 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 150046 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 150046 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 151116 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 151116 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 153876 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 153876 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 138869 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 138869 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 139756 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 139756 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 151048 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 151048 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 95270 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 95270 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 142625 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 142625 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 146650 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 146650 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 151194 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 151194 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 143851 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 143851 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 70948 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 70948 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 70948 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 70948 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 150459 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 150459 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 152578 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 152578 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 153793 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 153793 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 139691 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 139691 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 144057 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 144057 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 144416 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 144416 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 74805 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 74805 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 143851 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 143851 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 139706 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 139706 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 142061 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 142061 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 147081 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 147081 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 146698 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 146698 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 175798 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 175798 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 175798 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 59368 20 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 59368 20 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 171113 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 171113 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 97405 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 97405 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 143568 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 143568 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 145167 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 145167 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 146481 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 146481 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 147293 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 147293 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 151732 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 151732 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 153394 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 153394 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 139731 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 139731 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 175679 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 175679 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 175679 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 139712 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 139712 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 139727 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 139727 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 138873 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 138873 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 138877 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 138877 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 138873 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 138873 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 139683 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 139683 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 152609 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 152609 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 175921 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 175921 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 175921 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 150625 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 150625 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 163667 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 163667 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 145438 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 145438 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 144136 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 144136 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 201573 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 201573 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 74922 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 74922 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 153241 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 153241 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 167500 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 167500 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 152210 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 152210 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 146887 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 146887 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 193419 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 193419 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 163328 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 163328 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 146016 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 146016 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 151154 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 151154 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 150114 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 150114 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 94041 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 94041 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 175786 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 175786 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 175786 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 142262 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 142262 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 144632 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 144632 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 152824 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 152824 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 176016 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 176016 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 176016 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 147910 0 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 147910 0 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 151308 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 151308 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 74799 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 74799 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 146214 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 146214 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 146650 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 146650 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 146650 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 146650 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 167608 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 167608 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 151507 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 151507 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 143877 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 143877 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 93808 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 93808 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 147724 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 147724 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 152210 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 152210 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 143736 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 143736 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 175766 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 175766 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 175766 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 175951 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 175951 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 175951 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 170555 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 170555 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 150206 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 150206 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 194268 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 194268 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 146812 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 146812 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 146812 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 146812 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 193518 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 193518 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 193881 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 193881 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 144057 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 144057 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 144057 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 144057 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 150666 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 150666 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 169959 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 169959 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 100337 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 100337 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 97404 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 97404 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 194657 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 194657 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 142061 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 142061 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 142061 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 142061 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 175851 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 175851 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 175851 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 145296 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 145296 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 102137 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 102137 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 149343 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 149343 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 194179 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 194179 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 77826 22 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 77826 22 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 74800 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 74800 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 176494 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 176494 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 193958 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 193958 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 144645 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 144645 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 143247 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 143247 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 142772 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 142772 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 149057 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 149057 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 149057 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 149057 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 147601 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 147601 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 148121 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 148121 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 139757 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 139757 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 69116 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 69116 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 176070 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 176070 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 176070 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 148124 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 148124 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 93691 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 93691 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 142982 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 142982 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 144522 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 144522 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 144878 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 144878 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 149158 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 149158 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 150400 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 150400 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 150886 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 150886 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 144146 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 144146 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 145048 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 145048 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 146289 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 146289 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 145529 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 145529 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 145559 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 145559 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 144223 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 144223 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 201517 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 201517 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 145937 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 145937 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 146812 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 146812 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 138781 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 138781 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 147538 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 147538 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 143735 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 143735 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 193962 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 193962 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 150666 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 150666 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 201237 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 201237 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 194299 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 194299 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 93651 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 93651 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 151364 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 151364 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 175717 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 175717 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 175717 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 139717 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 139717 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 164065 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 164065 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 2888 1 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 2888 1 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 2888 1 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 175950 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 175950 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 175950 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 152099 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 152099 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 152122 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 152122 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 175897 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 175897 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 175897 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 148892 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 148892 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 139670 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 139670 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 150044 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 150044 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 139663 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 139663 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 145911 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 145911 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 101869 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 101869 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 144338 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 144338 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 143344 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 143344 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 143344 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 143344 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 150810 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 150810 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 2157 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 2157 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 2157 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 151673 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 151673 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 176069 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 176069 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 176069 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 143727 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 143727 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 143829 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 143829 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 143829 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 143829 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 149480 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 149480 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 145712 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 145712 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 152351 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 152351 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 995 27 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 995 27 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 995 27 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 145863 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 145863 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 152435 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 152435 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 142249 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 142249 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 142249 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 142249 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 148195 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 148195 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 150435 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 150435 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 143727 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 143727 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 143851 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 143851 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 153165 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 153165 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 94010 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 94010 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 152536 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 152536 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 175865 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 175865 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 175865 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 148463 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 148463 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 74923 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 74923 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 194635 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 194635 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 139679 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 139679 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 150625 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 150625 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 146667 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 146667 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 152343 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 152343 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 3021 71 None -6 10 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 69113 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 69113 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 69113 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 69113 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 175757 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 175757 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 175757 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 163925 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 163925 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 145104 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 145104 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 193365 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 193365 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 148550 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 148550 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 121120 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 121120 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 121086 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 121086 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 121096 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 121096 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 121111 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 121111 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 121075 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 121075 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 121090 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 121090 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 121076 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 121076 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 121095 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 121095 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 3723 24 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 3723 24 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 3723 24 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 121092 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 121092 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 121104 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 121104 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 121117 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 121117 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 121119 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 121119 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 121089 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 121089 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 121098 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 121098 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 121112 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 121112 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 121118 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 121118 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 121071 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 121071 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 121072 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 121072 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 121097 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 121097 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 121100 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 121100 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 121108 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 121108 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 121118 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 121118 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 121105 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 121105 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 121102 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 121102 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 121087 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 121087 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 121118 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 121118 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 121077 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 121077 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 121106 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 121106 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 121071 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 121071 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 121071 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 121071 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 121094 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 121094 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 121101 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 121101 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 121074 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 121074 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 121073 3 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 121073 3 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 121099 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 121099 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 40440 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 40440 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 9805 15 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 9805 15 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 121459 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 121459 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 3473 33 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 3473 33 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 3473 33 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 317 66 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 317 66 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 317 66 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 164840 2 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 164840 2 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 57224 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 57224 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 119567 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 119567 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 56916 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 56916 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 197539 21 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 197539 21 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 3020 84 None -4 9 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 3020 84 None -4 9 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 3020 84 None -4 9 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 3020 84 None -4 9 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 3020 84 None -4 9 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 166875 20 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 166875 20 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 1569 46 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 1569 46 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 1569 46 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 1569 46 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 3021 71 None -2 10 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 1569 46 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 1569 46 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 1569 46 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 1569 46 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 3684 45 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 3684 45 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 3684 45 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 3684 45 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 3684 45 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 3684 45 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 3684 45 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 3684 45 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 3725 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 3725 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 3725 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 3725 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 3721 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 3721 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 3721 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 3723 24 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 3723 24 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 3723 24 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 3000 49 None -1 2 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 3000 49 None -1 2 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 3000 49 None -1 2 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 3000 49 None -1 2 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 3000 49 None -1 2 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 3000 49 None -1 2 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 3000 49 None -1 2 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 3000 49 None -1 2 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 3000 49 None 1 2 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 3000 49 None 1 2 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 3000 49 None 1 2 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 3000 49 None 1 2 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 3002 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 3002 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 3724 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 3724 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 3722 42 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 3722 42 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 3722 42 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 Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
11855868 152000 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 152000 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 137022 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 137022 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 149057 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 149057 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 136756 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 136756 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 142249 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 142249 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 152731 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 152731 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 145735 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 145735 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 2886 4 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 2886 4 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 2886 4 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 143373 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 143373 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 151646 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 151646 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 139779 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 139779 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 143829 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 143829 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 143232 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 143232 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 143891 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 143891 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 152487 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 152487 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 150930 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 150930 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 148820 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 148820 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 201163 26 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 201163 26 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 136913 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 136913 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 142506 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 142506 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 136930 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 136930 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 142061 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 142061 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 146037 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 146037 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 138778 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 138778 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 138907 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 138907 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 3684 45 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 3684 45 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 3684 45 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 3684 45 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 136715 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 136715 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 136856 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 136856 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 139731 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 139731 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 150046 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 150046 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 136863 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 136863 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 146650 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 146650 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 144057 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 144057 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 144146 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 144146 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 142061 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 142061 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 136944 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 136944 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 138883 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 138883 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 201473 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 201473 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 145438 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 145438 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 734 15 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 734 15 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 734 15 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 145189 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 145189 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 97341 27 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 97341 27 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 136763 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 136763 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 139678 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 139678 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 1569 46 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 1569 46 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 1569 46 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 1569 46 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 136759 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 136759 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 144146 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 144146 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 146289 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 146289 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 146812 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 146812 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 201610 19 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 201610 19 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 136982 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 136982 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 147859 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 147859 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 139751 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 139751 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 136937 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 136937 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 151442 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 151442 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 149413 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 149413 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 142374 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 142374 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 145863 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 145863 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 152435 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 152435 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 138820 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 138820 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 138820 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 138820 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 142541 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 142541 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 151308 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 151308 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 121118 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 121118 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 121118 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 121118 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 2870 20 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 2870 20 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 2870 20 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 121076 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 121076 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 121084 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 121084 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 121086 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 121086 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 121104 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 121104 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 121071 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 121071 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 121071 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 121071 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 121078 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 121078 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 121093 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 121093 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 192039 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 192039 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 121098 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 121098 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 121107 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 121107 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 165534 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 165534 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 121091 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 121091 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 76682 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 76682 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 178064 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 178064 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 139117 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 139117 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 192007 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 192007 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 155725 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 155725 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 212238 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 nan
10047541 131976 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 131976 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 121116 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 121116 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 144223 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 144223 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 147445 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 147445 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 140365 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 140365 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 182343 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 182343 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 121110 3 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 121110 3 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 121108 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 121108 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 142541 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 142541 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 121088 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 121088 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 121090 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 121090 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 145712 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 145712 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 14721 7 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 14721 7 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 14721 7 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 193365 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 193365 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 121113 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 121113 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 156868 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 156868 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 105772 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 105772 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 105772 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 121081 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 121081 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 145559 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 145559 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 139063 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 139063 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 158759 15 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 158759 15 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 6089 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 6089 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 121120 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 121120 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 121074 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 121074 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 121117 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 121117 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 121073 3 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 121073 3 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 121075 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 121075 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 121077 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 121077 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 121111 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 121111 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 193703 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 193703 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 150206 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 150206 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 182678 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 182678 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 158108 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 158108 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 59726 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 59726 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 100008 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 100008 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 193437 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 193437 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 3522 51 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 3522 51 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 3522 51 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 3522 51 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 193419 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 193419 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 121097 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 121097 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 89890 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 89890 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 194218 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 194218 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 121087 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 121087 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 194179 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 194179 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 121106 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 121106 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 121089 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 121089 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 121096 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 121096 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 121079 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 121079 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 121080 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 121080 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 121085 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 121085 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 194721 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 194721 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 193403 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 193403 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 194314 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 194314 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 154277 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 154277 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 193962 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 193962 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 195152 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 195152 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 158264 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 158264 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 153340 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 153340 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 941 35 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 941 35 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 941 35 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 941 35 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 136149 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 136149 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 193958 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 193958 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 121094 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 121094 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 121100 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 121100 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 121115 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 121115 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 1377 22 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 1377 22 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 1377 22 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 166875 20 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 166875 20 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 152207 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 152207 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 186223 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 186223 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 158420 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 158420 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 182215 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 182215 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 138379 7 None - 0 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 138379 7 None - 0 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 138379 7 None - 0 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 138379 7 None - 0 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 195187 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 195187 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 151985 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 151985 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 130083 22 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 130083 22 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 194292 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 194292 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 3000 49 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 nan
5817 3000 49 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 nan
CHEMBL3286797 3000 49 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 nan
DB12024 3000 49 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 nan
1883 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 1569 46 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 1569 46 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 1569 46 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 1569 46 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 193881 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 193881 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 193243 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 193243 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 153793 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 153793 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 121103 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 121103 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 193822 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 193822 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 121099 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 121099 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 121082 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 121082 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 121083 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 121083 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 121114 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 121114 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 152536 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 152536 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 193244 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 193244 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 194635 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 194635 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 138707 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 138707 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 121095 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 121095 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 89894 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 89894 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 194299 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 194299 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 89914 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 89914 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 140340 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 140340 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 121071 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 121071 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 121072 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 121072 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 121092 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 121092 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 194268 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 194268 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 931 52 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 931 52 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 931 52 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 89915 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 89915 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 179930 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 179930 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 193418 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 193418 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 121118 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 121118 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 121119 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 121119 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 121101 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 121101 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 121112 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 121112 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 121102 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 121102 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 193518 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 193518 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 165409 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 165409 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 145911 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 145911 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 121105 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 121105 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 194267 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 194267 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 194657 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 194657 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 179931 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 179931 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 89893 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 89893 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 176116 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 176116 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 3000 49 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 nan
5817 3000 49 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 nan
CHEMBL3286797 3000 49 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 nan
DB12024 3000 49 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 nan
9807448 201473 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 201473 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 128668 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 128668 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 128672 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 128672 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 74802 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 74802 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 2886 4 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 2886 4 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 2886 4 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 70948 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 70948 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 70948 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 70948 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 128662 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 128662 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 3684 45 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 3684 45 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 3684 45 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 3684 45 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 152731 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 152731 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 125352 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 125352 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 100471 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 100471 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 100471 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 100471 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 95270 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 95270 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 201559 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 201559 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 204618 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 204618 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 143727 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 143727 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 81455 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 81455 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 201506 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 201506 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 97341 27 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 97341 27 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 16350 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 16350 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 97341 27 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 97341 27 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 64257 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 64257 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 201044 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 201044 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 69009 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 69009 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 198888 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 198888 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 161357 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 161357 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 205193 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 205193 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 150625 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 150625 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 142249 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 142249 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 142249 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 142249 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 317 66 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 317 66 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 317 66 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 143851 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 143851 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 199536 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 199536 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 100102 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 100102 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 84270 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 84270 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 198072 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 198072 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 199525 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 199525 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 102237 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 102237 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 198900 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 198900 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 164840 2 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 164840 2 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 105772 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 105772 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 105772 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 174082 15 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 174082 15 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 153165 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 153165 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 94010 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 94010 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 152210 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 152210 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 69110 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 69110 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 69110 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 69110 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 143147 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 143147 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 128669 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 128669 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 167608 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 167608 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 69119 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 69119 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 84270 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 84270 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 122765 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 122765 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 126791 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 126791 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 198381 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 198381 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 205285 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 205285 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 152824 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 152824 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 94040 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 94040 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 2239 68 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 2239 68 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 2239 68 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 2239 68 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 2239 68 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 150930 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 150930 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 150641 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 150641 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 201620 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 201620 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 204517 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 204517 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 16353 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 16353 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 16353 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 16353 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 137343 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 137343 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 69014 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 69014 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 148659 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 148659 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 102000 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 102000 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 102000 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 111059 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 111059 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 95105 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 95105 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 143851 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 143851 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 162960 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 162960 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 152000 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 152000 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 69117 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 69117 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 152000 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 152000 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 74805 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 74805 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 169499 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 169499 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 16453 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 16453 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 201478 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 201478 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 197470 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 197470 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 102274 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 102274 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 144683 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 144683 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 144878 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 144878 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 145400 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 145400 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 152609 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 152609 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 105772 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 105772 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 105772 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 105772 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 105772 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 105772 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 198867 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 198867 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 1569 46 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 1569 46 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 1569 46 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 1569 46 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 167815 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 167815 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 83714 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 83714 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 96058 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 96058 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 204109 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 204109 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 145863 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 145863 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 145863 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 145863 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 144057 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 144057 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 144057 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 144057 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 64467 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 64467 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 16346 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 16346 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 65763 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 65763 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 124522 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 124522 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 69015 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 69015 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 74793 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 74793 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 63441 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 63441 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 94079 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 94079 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 14721 7 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 14721 7 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 14721 7 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 152351 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 152351 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 16344 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 16344 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 170599 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 170599 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 198285 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 198285 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 158759 15 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 158759 15 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 153875 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 153875 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 142061 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 142061 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 69116 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 69116 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 69116 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 69116 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 152731 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 152731 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 70946 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 70946 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 2480 39 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 2480 39 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 2480 39 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 142645 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 142645 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 74799 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 74799 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 74803 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 74803 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 201473 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 201473 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 128663 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 128663 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 100406 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 100406 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 64862 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 64862 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 204540 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 204540 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 64868 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 64868 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 74795 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 74795 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 198909 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 198909 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 146650 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 146650 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 146650 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 146650 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 153860 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 153860 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 97405 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 97405 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 74807 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 74807 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 64065 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 64065 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 66224 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 66224 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 204676 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 204676 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 63727 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 63727 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 64868 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 64868 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 82652 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 82652 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 82653 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 82653 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 74789 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 74789 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 198157 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 198157 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 100425 4 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 100425 4 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 110963 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 110963 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 70949 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 70949 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 70949 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 70949 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 74806 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 74806 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 74923 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 74923 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 64479 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 64479 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 84505 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 84505 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 93651 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 93651 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 167484 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 167484 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 176917 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 176917 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 143727 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 143727 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 19080 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 19080 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 143344 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 143344 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 143344 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 143344 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 143891 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 143891 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 143891 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 143891 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 74801 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 74801 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 140783 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 140783 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 140783 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 140783 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 16967 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 16967 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 64459 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 64459 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 106393 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 106393 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 205451 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 205451 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 155024 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 155024 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 74924 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 74924 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 59368 20 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 59368 20 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 69111 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 69111 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 69111 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 69111 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 97341 27 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 97341 27 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 167500 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 167500 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 141207 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 141207 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 93780 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 93780 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 201517 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 201517 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 147724 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 147724 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 65923 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 65923 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 64068 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 64068 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 16620 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 16620 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 16634 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 16634 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 105672 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 105672 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 16351 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 16351 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 16354 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 16354 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 16354 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 16354 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 82988 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 82988 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 84290 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 84290 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 84335 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 84335 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 84335 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 84335 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 101873 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 101873 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 97259 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 97259 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 97404 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 97404 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 201111 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 201111 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 100846 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 100846 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 128049 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 128049 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 144146 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 144146 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 204115 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 204115 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 66314 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 66314 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 64095 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 64095 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 204618 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 204618 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 143431 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 143431 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 93691 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 93691 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 74804 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 74804 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 121517 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 121517 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 201464 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 201464 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 136149 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 136149 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 199921 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 199921 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 144645 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 144645 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 93721 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 93721 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 153876 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 153876 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 201280 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 201280 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 16376 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 16376 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 18331 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 18331 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 106065 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 106065 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 204594 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 204594 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 204698 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 204698 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 16348 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 16348 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 66512 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 66512 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 172108 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 172108 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 120336 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 120336 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 120336 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 69115 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 69115 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 69115 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 69115 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 70947 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 70947 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 70947 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 70947 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 128671 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 128671 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 201473 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 201473 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
67078580 128665 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 128665 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 128667 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 128667 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 201534 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 201534 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 154963 8 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 154963 8 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 105514 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 105514 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 92985 27 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 92985 27 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 43371 24 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 43371 24 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 8977 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 8977 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 93779 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 93779 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 145735 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 145735 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 145735 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 145735 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 141066 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 141066 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 64069 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 64069 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 201425 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 201425 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 201213 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 201213 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 106605 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 106605 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 35011 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 35011 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 153165 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 153165 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 152824 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 152824 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 69114 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 69114 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 69114 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 69114 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 178332 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 178332 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 150046 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 150046 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 126012 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 126012 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 100553 0 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 100553 0 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 64067 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 64067 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 65772 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 65772 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 201260 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 201260 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 198360 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 198360 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 56563 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 56563 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 201233 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 201233 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 64066 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 64066 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 84270 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 84270 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 160715 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 160715 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 152351 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 152351 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 137369 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 137369 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 16729 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 16729 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 74792 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 74792 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 64460 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 64460 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 16373 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 16373 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 167754 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 167754 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 34239 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 34239 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 143147 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 143147 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 200416 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 200416 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 201237 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 201237 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 64084 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 64084 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 116391 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 116391 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 84705 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 84705 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 201610 19 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 201610 19 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 165329 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 165329 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 167369 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 167369 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 197757 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 197757 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 152435 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 152435 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 152435 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 152435 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 76677 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 76677 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 76677 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 76677 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 122088 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 122088 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 201542 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 201542 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 183693 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 183693 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 128666 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 128666 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 102137 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 102137 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 142061 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 142061 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 142061 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 142061 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 166278 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 166278 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 126632 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 126632 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 165612 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 165612 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 69109 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 69109 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 69109 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 69109 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 16706 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 16706 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 63291 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 63291 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 100895 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 100895 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 69118 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 69118 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 177934 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 177934 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 100960 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 100960 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 94010 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 94010 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 81454 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 81454 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 101869 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 101869 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 199175 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 199175 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 169898 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 169898 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 64478 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 64478 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 155023 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 155023 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 123918 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 123918 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 162960 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 162960 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 16703 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 16703 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 113289 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 113289 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 149350 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 149350 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 199689 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 199689 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 145915 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 145915 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 68991 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 68991 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 123316 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 123316 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 84335 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 84335 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 201454 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 201454 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 204616 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 204616 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 2157 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 2157 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 2157 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 1569 46 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 1569 46 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 1569 46 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 1569 46 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 64071 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 64071 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 142982 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 142982 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 144522 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 144522 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 149158 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 149158 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 150400 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 150400 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 150886 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 150886 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 144146 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 144146 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 144146 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 144146 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 150666 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 150666 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 84265 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 84265 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 64458 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 64458 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 66282 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 66282 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 8651 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 8651 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 16342 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 16342 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 64461 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 64461 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 201501 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 201501 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 143568 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 143568 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 95018 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 95018 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 66614 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 66614 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 65760 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 65760 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 82349 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 82349 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 93720 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 93720 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 16341 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 16341 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 170731 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 170731 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 74922 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 74922 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 154287 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 154287 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 93750 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 93750 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 147380 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 147380 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 165395 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 165395 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 198161 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 198161 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 145438 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 145438 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 145438 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 145438 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 168520 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 168520 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 173392 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 173392 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 204529 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 204529 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 2507 37 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 2507 37 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 2507 37 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 199751 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 199751 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 161147 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 161147 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 124896 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 124896 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 93560 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 93560 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 94041 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 94041 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 64072 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 64072 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 142715 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 142715 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 149480 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 149480 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 93722 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 93722 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 112077 30 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 112077 30 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 70943 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 70943 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 74790 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 74790 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 64468 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 64468 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 2888 1 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 2888 1 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 2888 1 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 2888 1 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 2888 1 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 2888 1 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 2888 1 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 2888 1 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 2888 1 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 93692 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 93692 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 154286 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 154286 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 78200 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 78200 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 16345 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 16345 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 82722 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 82722 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 82723 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 82723 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 34826 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 34826 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 74925 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 74925 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 16343 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 16343 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 69010 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 69010 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 198010 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 198010 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 162197 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 162197 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 70940 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 70940 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 128664 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 128664 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
59465571 145740 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 145740 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 151154 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 151154 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 106407 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 106407 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 16347 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 16347 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 144338 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 144338 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 163808 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 163808 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 74794 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 74794 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 2507 37 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 2507 37 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 2507 37 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 734 15 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 734 15 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 734 15 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 201573 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 201573 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 63531 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 63531 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 183937 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 183937 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 100395 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 100395 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 142206 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 142206 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 198868 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 198868 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 93561 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 93561 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 201453 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 201453 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 84280 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 84280 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 93808 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 93808 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 16355 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 16355 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 16355 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 16355 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 82801 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 82801 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 16599 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 16599 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 102355 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 102355 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 100255 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 100255 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 63948 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 63948 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 149057 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 149057 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 149057 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 149057 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 199837 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 199837 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 82353 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 82353 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 141020 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 141020 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 141116 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 141116 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 6745 12 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 6745 12 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 77622 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 77622 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 16367 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 16367 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 17836 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 17836 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 16367 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 16367 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 117555 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 117555 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 93751 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 93751 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 69112 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 69112 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 69112 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 69112 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 68990 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 68990 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 178460 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 178460 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 16341 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 16341 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 82568 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 82568 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 137325 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 137325 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 204672 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 204672 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 83708 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 83708 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 16349 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 16349 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 82730 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 82730 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 141207 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 141207 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 59368 20 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 59368 20 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 94078 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 94078 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 65998 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 65998 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 128673 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 128673 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 74800 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 74800 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 69113 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 69113 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 69113 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 69113 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 69113 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 69113 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 128670 3 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 128670 3 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 126712 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 126712 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 199881 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 199881 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 70942 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 70942 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 100337 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 100337 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 93778 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 93778 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 197980 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 197980 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 198922 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 198922 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 142206 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 142206 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 152609 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 152609 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 63519 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 63519 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 83713 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 83713 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 143851 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 143851 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 125352 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 125352 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 125352 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 125352 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 63732 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 63732 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 214265 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 214636 0 Functional -1348 31 Dog 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
5090 214636 0 Functional -35 31 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
5311035 97341 27 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 97341 27 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 912 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 912 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
631 912 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 912 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 214263 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 214264 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 214264 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 214262 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 214268 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 314 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 314 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 2496 60 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 2496 60 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 2496 60 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 2496 60 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 2496 60 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 317 66 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 317 66 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 317 66 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 214636 0 Functional -35 31 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
5090 214636 0 Functional -35 31 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
5077 3509 72 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 3509 72 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 3509 72 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 3509 72 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 3509 72 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 186871 39 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 186871 39 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 186871 39 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 186871 39 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 186871 39 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 186871 39 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 912 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 912 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
631 912 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 912 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 186871 39 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 186871 39 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 186871 39 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 215978 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 2239 68 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 2239 68 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 2239 68 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 2239 68 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 2239 68 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 214634 0 None 125 27 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 214636 0 None 28 31 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 314 3 0 4 2.6 CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 None
1817 2496 60 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 2496 60 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 2496 60 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 2496 60 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 2496 60 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 1988 116 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 2569 47 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 2569 47 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 2569 47 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 1968 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 1968 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 1968 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 1968 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 734 15 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 734 15 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 734 15 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 734 15 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 734 15 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 734 15 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3020 84 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3021 71 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 3026 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 3026 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 3781 55 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 2870 20 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 2870 20 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 2870 20 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 2886 4 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 2886 4 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 2886 4 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 3825 26 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 3825 26 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 3825 26 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 3825 26 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 2496 60 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 2496 60 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 2496 60 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 2496 60 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 2496 60 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 3018 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 3018 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 3018 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 3018 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 3018 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 3825 26 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 3825 26 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 3825 26 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 3825 26 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 3018 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 3018 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 3018 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 3018 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 3018 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 2890 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 2890 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 3022 46 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 2419 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 2419 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 2419 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 2419 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 1968 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 1968 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 1968 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 1968 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 2887 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 2887 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 781 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 781 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 781 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 1968 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 1968 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 1968 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 1968 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 29 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 29 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 317 66 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 317 66 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 317 66 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 912 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 912 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
631 912 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 912 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 2419 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 2419 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 314 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 314 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 781 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 781 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 781 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 2051 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 2051 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 2051 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 27 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 27 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 27 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 3269 15 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 3269 15 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 3269 15 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 3269 15 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 317 66 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 317 66 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 317 66 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 317 66 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 317 66 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 317 66 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 314 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 314 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 29 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 29 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 734 15 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 734 15 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 734 15 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 2495 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 2495 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 2495 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 25 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 25 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 25 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