Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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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 164676 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 164676 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 163684 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 163684 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 139451 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 139451 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 163728 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 163728 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 139379 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 139379 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 152520 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 152520 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 153253 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 153253 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 139425 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 139425 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 3060 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
1916 3060 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
5280360 3060 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
913 3060 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
CHEMBL548 3060 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
DB00917 3060 75 None -2 12 Rat 9.7 pEC50 = 9.7 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmcl.2009.01.059
18376258 195879 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 195879 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 139401 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 139401 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 139296 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 139296 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 1592 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
9890801 1592 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
CHEMBL563646 1592 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
DB12022 1592 55 None 2 2 Rat 9.5 pEC50 = 9.5 Functional
Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1016/j.bmcl.2009.01.059
67082748 164339 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 164339 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 163816 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 163816 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 140297 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 140297 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 139394 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 139394 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 149577 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 149577 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 137227 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 137227 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 139465 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 139465 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 139404 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 139404 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 139338 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 139338 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 139338 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 139338 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 140269 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 140269 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 151421 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 151421 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 144088 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 144088 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 194900 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 194900 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 163983 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 163983 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 2905 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
44230575 2905 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
CHEMBL3707245 2905 28 None 1659 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 478 10 2 8 2.6 OC(=O)CNc1cccc(n1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)n1cccn1 10.1021/acs.jmedchem.8b00808
126495463 140282 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 140282 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 142768 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 142768 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 146255 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 146255 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 152520 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 152520 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 153253 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 153253 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 171705 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 171705 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 152520 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 152520 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 139474 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 139474 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 3060 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
1916 3060 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
5280360 3060 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
913 3060 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
CHEMBL548 3060 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
DB00917 3060 75 None -6 12 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF methodAgonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acsmedchemlett.5b00455
126495398 140186 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 140186 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 145660 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 145660 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 143666 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 143666 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 152872 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 152872 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 2923 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
9824353 2923 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL292964 2923 2 None -66069 4 Human 5.0 pEC50 = 5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 436 13 3 6 2.8 COCc1cccc(c1)C[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCSCCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
59465571 146260 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 146260 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 153346 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 153346 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 147513 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 147513 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 195953 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 195953 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 151248 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 151248 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 176345 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 176345 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 176345 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 139354 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 139354 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 154332 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 154332 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 203211 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 203211 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 142725 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 142725 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 150980 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 150980 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 139441 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 139441 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 143559 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 143559 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 176658 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 176658 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 176658 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 176508 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 176508 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 176508 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 144349 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 144349 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 144411 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 144411 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 144411 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 144411 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 143950 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 143950 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 143666 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 143666 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 153862 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 153862 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 139360 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 139360 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 139360 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 139360 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 140200 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 140200 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 140219 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 140219 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 176189 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 176189 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 152562 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 152562 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 148920 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 148920 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 100859 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 100859 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 94199 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 94199 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 195360 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 195360 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 144666 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 144666 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 144666 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 144666 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 140196 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 140196 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 149254 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 149254 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 75138 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 75138 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 203182 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 203182 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 149179 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 149179 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 144411 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 144411 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 84679 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 84679 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 139333 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 139333 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 151161 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 151161 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 148244 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 148244 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 143406 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 143406 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 177560 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 177560 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 75139 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 75139 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 155551 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 155551 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 143164 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 143164 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 143234 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 143234 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 145203 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 145203 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 145920 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 145920 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 149870 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 149870 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 150347 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 150347 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 94430 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 94430 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 146255 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 146255 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 146255 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 146255 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 148282 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 148282 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 152536 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 152536 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 75140 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 75140 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 153687 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 153687 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 154320 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 154320 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 1592 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
9890801 1592 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
CHEMBL563646 1592 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
DB12022 1592 55 None -2 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 minsAgonist activity at recombinant human EP2 receptor expressed in HEK293 cells assessed as induction of cAMP accumulation after 30 mins
ChEMBL 468 9 1 5 4.2 OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C 10.1021/acs.jmedchem.8b00808
89444254 142755 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 142755 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 142881 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 142881 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 147363 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 147363 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 142508 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 142508 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 171380 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 171380 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 143614 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 143614 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 143841 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 143841 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 151880 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 151880 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 71277 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 71277 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 84679 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 84679 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 71277 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 71277 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 145958 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 145958 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 145958 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 145958 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 95533 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 95533 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 3060 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
1916 3060 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
5280360 3060 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
913 3060 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
CHEMBL548 3060 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
DB00917 3060 75 None -2 12 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at rat EP2 receptorAgonist activity at rat EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1016/j.bmc.2012.02.018
53259985 176453 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 176453 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 176453 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 94498 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 94498 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 139336 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 139336 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 144087 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 144087 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 164375 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 164375 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 176304 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 176304 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 176304 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 145870 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 145870 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 146088 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 146088 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 148773 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 148773 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 150454 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 150454 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 164098 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 164098 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 203287 24 None -10 4 Mouse 8.7 pEC50 = 8.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
CHEMBL64804 203287 24 None -10 4 Mouse 8.7 pEC50 = 8.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O 10.1016/s0960-894x(01)00359-6
118352285 139444 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 139444 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 194899 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 194899 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 176522 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 176522 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 176522 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 3059 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
1882 3059 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
5280723 3059 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
CHEMBL495 3059 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
DB00770 3059 88 None -1 10 Mouse 8.6 pEC50 = 8.6 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 354 13 3 4 3.5 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O)O 10.1016/s0960-894x(01)00359-6
53260134 176238 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 176238 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 176238 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 176496 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 176496 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 176496 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 176474 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 176474 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 176474 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 203149 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 203149 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 139392 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 139392 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 153253 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 153253 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 195075 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 195075 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 152763 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 152763 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 187440 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
5311181 187440 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
CHEMBL494 187440 46 None -1348 7 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysisAgonist activity at human EP2 expressed in HEK293 cells assessed as increase in cAMP level incubated for 20 mins measured after 60 mins addition of cAMP detect reagent by HTRF analysis
ChEMBL 360 8 3 3 3.5 CC#CCC(C)[C@H](O)/C=C/[C@@H]1[C@H]2C/C(=C/CCCC(=O)O)C[C@H]2C[C@H]1O 10.1016/j.ejmech.2022.114154
59465583 143249 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 143249 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 152956 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 152956 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 152956 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 152956 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 146383 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 146383 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 146383 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 146383 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 146435 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 146435 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 101008 1 None - 1 Mouse 6.7 pEC50 = 6.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
CHEMBL294585 101008 1 None - 1 Mouse 6.7 pEC50 = 6.7 Functional
Effective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptorEffective concentration which increases intracellular c-AMP production in mouse Prostanoid EP2 receptor
ChEMBL 392 12 3 4 4.0 CCCC1([C@@H](O)C/C=C/[C@H]2[C@H](O)CC(=O)[C@@H]2C/C=C\CCCC(=O)O)CCC1 10.1016/s0960-894x(01)00359-6
9975502 94460 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 94460 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 151161 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 151161 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 151450 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 151450 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 150567 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 150567 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 151636 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 151636 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 154398 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 154398 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 139387 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 139387 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 140274 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 140274 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 151568 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 151568 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 95698 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 95698 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 143144 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 143144 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 147170 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 147170 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 151714 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 151714 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 144371 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 144371 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 71278 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 71278 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 71278 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 71278 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 150979 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 150979 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 153100 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 153100 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 154315 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 154315 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 140209 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 140209 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 144577 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 144577 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 144936 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 144936 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 75141 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 75141 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 144371 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 144371 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 140224 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 140224 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 142580 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 142580 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 147601 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 147601 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 147218 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 147218 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 176358 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 176358 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 176358 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 59665 23 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
CHEMBL1722929 59665 23 None -3 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 388 13 2 3 5.8 CCCCCC(O)c1ccc([C@H]2CCC(=O)[C@@H]2CCCCCCC(=O)O)cc1 nan
155532079 171665 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 171665 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 97839 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 97839 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 144087 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 144087 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 145687 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 145687 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 147001 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 147001 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 147813 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 147813 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 152252 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 152252 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 153916 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 153916 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 140249 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 140249 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 176239 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 176239 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 176239 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 140230 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 140230 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 140245 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 140245 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 139391 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 139391 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 139395 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 139395 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 139391 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 139391 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 140201 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 140201 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 153131 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 153131 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 176481 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 176481 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 176481 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 151145 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 151145 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 164206 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 164206 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 145958 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 145958 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 144656 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 144656 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 203250 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 203250 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 75258 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 75258 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 153763 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 153763 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 168050 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 168050 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 3060 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
1916 3060 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
5280360 3060 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
913 3060 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
CHEMBL548 3060 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
DB00917 3060 75 None -6 12 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISAAgonist activity at human EP2 receptor expressed in HEK293T/17 cells assessed as increase in intracellular cAMP level incubated for 30 mins by ELISA
ChEMBL 352 12 3 4 3.3 CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O 10.1021/acs.jmedchem.9b00336
17757350 152730 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 152730 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 147407 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 147407 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 195076 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 195076 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 163867 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 163867 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 146536 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 146536 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 151674 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 151674 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 150635 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 150635 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 94461 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 94461 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 176346 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 176346 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 176346 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 142781 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 142781 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 145152 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 145152 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 153346 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 153346 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 176576 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 176576 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 176576 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 148430 1 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 3 4 4.9 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
CHEMBL3937945 148430 1 None -2 2 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assayAgonist activity at human recombinant EP2 receptor expressed in HEK293 cells assessed as effect on calcium accumulation by Fluo-4 AM dye based FLIPR assay
ChEMBL 428 11 3 4 4.9 CCCC1(C(O)c2cccc([C@H]3[C@H](O)CC(=O)[C@@H]3C/C=C\CCCC(=O)O)c2)CCC1 nan
118689427 151828 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 151828 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 75135 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 75135 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 146734 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 146734 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 147170 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 147170 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 147170 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 147170 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 168158 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 168158 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 152027 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 152027 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 144397 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 144397 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 94227 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 94227 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 148244 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 148244 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 152730 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 152730 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 144255 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 144255 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 176326 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 176326 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 176326 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 176511 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 176511 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