Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 145971909 | 164795 | None | 0 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 11 | 3 | 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 | 164795 | None | 0 | Human | Functional | pEC50 | = | 10.2 | 10.2 | 11 | 3 | 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 | 163803 | None | 0 | Human | Functional | pEC50 | = | 10.1 | 10.1 | 10 | 3 | 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 | 163803 | None | 0 | Human | Functional | pEC50 | = | 10.1 | 10.1 | 10 | 3 | 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 | 139563 | None | 0 | Human | Functional | pEC50 | = | 10.0 | 10.0 | - | 1 | 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 | 139563 | None | 0 | Human | Functional | pEC50 | = | 10.0 | 10.0 | - | 1 | 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 | 163847 | None | 0 | Human | Functional | pEC50 | = | 10.0 | 10.0 | 27 | 3 | 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 | 163847 | None | 0 | Human | Functional | pEC50 | = | 10.0 | 10.0 | 27 | 3 | 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 | 139491 | None | 0 | Human | Functional | pEC50 | = | 9.9 | 9.9 | - | 1 | 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 | 139491 | None | 0 | Human | Functional | pEC50 | = | 9.9 | 9.9 | - | 1 | 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 | 152633 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | 24 | 3 | 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 | 152633 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | 24 | 3 | 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 | 153366 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | 35 | 3 | 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 | 153366 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | 35 | 3 | 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 | 139537 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | - | 1 | 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 | 139537 | None | 0 | Human | Functional | pEC50 | = | 9.8 | 9.8 | - | 1 | Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay |
ChEMBL | 437 | 5 | 2 | 6 | 4.4 | Cc1cc(OC[C@H]2[C@H](O)C[C@@H]3O[C@@H](c4nc(C(=O)O)cs4)CC[C@@H]32)cc(C)c1Cl | 10.1016/j.bmcl.2016.03.110 | ||
| 1883 | 3082 | None | 47 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | -2 | 12 | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1016/j.bmcl.2009.01.059 | ||
| 1916 | 3082 | None | 47 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | -2 | 12 | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1016/j.bmcl.2009.01.059 | ||
| 5280360 | 3082 | None | 47 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | -2 | 12 | 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 | ||
| 5280360.0 | 3082 | None | 47 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | -2 | 12 | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1016/j.bmcl.2009.01.059 | ||
| 913 | 3082 | None | 47 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | -2 | 12 | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1016/j.bmcl.2009.01.059 | ||
| CHEMBL548 | 3082 | None | 47 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | -2 | 12 | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1016/j.bmcl.2009.01.059 | ||
| DB00917 | 3082 | None | 47 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | -2 | 12 | 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 | 198358 | None | 0 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | 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 | 198358 | None | 0 | Rat | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | 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 | 139513 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | 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 | 139513 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | 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 | 139408 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | 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 | 139408 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Agonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assayAgonist activity at human EP2 receptor expressed in CHO cells assessed as cAMP level by HTRF assay |
ChEMBL | 477 | 5 | 2 | 6 | 5.1 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccc(Cl)c(Cl)c3Cl)O2)n1 | 10.1016/j.bmcl.2016.03.110 | ||
| 1929 | 1605 | None | 49 | Rat | Functional | pEC50 | = | 9.5 | 9.5 | 2 | 2 | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release |
ChEMBL | 468 | 9 | 1 | 5 | 4.2 | OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C | 10.1016/j.bmcl.2009.01.059 | ||
| 9890801 | 1605 | None | 49 | Rat | Functional | pEC50 | = | 9.5 | 9.5 | 2 | 2 | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release |
ChEMBL | 468 | 9 | 1 | 5 | 4.2 | OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C | 10.1016/j.bmcl.2009.01.059 | ||
| CHEMBL563646 | 1605 | None | 49 | Rat | Functional | pEC50 | = | 9.5 | 9.5 | 2 | 2 | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP releaseAgonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release |
ChEMBL | 468 | 9 | 1 | 5 | 4.2 | OC(=O)COc1cccc(c1)CN(S(=O)(=O)c1cccnc1)Cc1ccc(cc1)C(C)(C)C | 10.1016/j.bmcl.2009.01.059 | ||
| DB12022 | 1605 | None | 49 | Rat | Functional | pEC50 | = | 9.5 | 9.5 | 2 | 2 | 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 | 164458 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 9 | 3 | 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 | 164458 | None | 0 | Human | Functional | pEC50 | = | 9.4 | 9.4 | 9 | 3 | 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 | 163935 | None | 0 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 5 | 3 | 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 | 163935 | None | 0 | Human | Functional | pEC50 | = | 9.3 | 9.3 | 5 | 3 | 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 | 140409 | None | 0 | Human | Functional | pEC50 | = | 9.3 | 9.3 | - | 1 | 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 | 140409 | None | 0 | Human | Functional | pEC50 | = | 9.3 | 9.3 | - | 1 | 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 | 139506 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | 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 | 139506 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | 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 | 149689 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 4 | 4 | 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 | 149689 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 4 | 4 | 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 | 137339 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 1 | 3 | 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 | 137339 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 1 | 3 | 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 | 139577 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | 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 | 139577 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | 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 | 139516 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 7079 | 2 | 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 | 139516 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | 7079 | 2 | 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 | 139450 | None | 0 | Human | Functional | pEC50 | = | 9.1 | 9.1 | - | 1 | 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 | ||
Showing 1 to 50 of 943 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 11855868 | 152633 | None | 0 | Human | Binding | pEC50 | = | 9.8 | 9.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 429 | 11 | 2 | 4 | 5.6 | CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 | nan | ||
| CHEMBL3971632 | 152633 | None | 0 | Human | Binding | pEC50 | = | 9.8 | 9.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 429 | 11 | 2 | 4 | 5.6 | CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 | nan | ||
| 127037150 | 137647 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor |
ChEMBL | 426 | 12 | 2 | 6 | 4.1 | CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 | 10.1016/j.bmcl.2015.12.039 | ||
| CHEMBL3754586 | 137647 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor |
ChEMBL | 426 | 12 | 2 | 6 | 4.1 | CCCC[C@H](C)C[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 | 10.1016/j.bmcl.2015.12.039 | ||
| 16725337 | 149689 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 443 | 12 | 2 | 4 | 6.0 | CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 | nan | ||
| CHEMBL3947001 | 149689 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 443 | 12 | 2 | 4 | 6.0 | CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 | nan | ||
| 59554827 | 137380 | None | 0 | Human | Binding | pEC50 | = | 9.0 | 9.0 | - | 0 | Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor |
ChEMBL | 426 | 11 | 2 | 6 | 4.1 | CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 | 10.1016/j.bmcl.2015.12.039 | ||
| CHEMBL3752377 | 137380 | None | 0 | Human | Binding | pEC50 | = | 9.0 | 9.0 | - | 0 | Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor |
ChEMBL | 426 | 11 | 2 | 6 | 4.1 | CCCCC(C)(C)[C@H](O)/C=C/[C@H]1CCC(=O)N1CCSc1nc(C(=O)O)cs1 | 10.1016/j.bmcl.2015.12.039 | ||
| 11502897 | 142880 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 431 | 11 | 2 | 5 | 4.8 | CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
| CHEMBL3892847 | 142880 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 431 | 11 | 2 | 5 | 4.8 | CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
| 11855865 | 153366 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 445 | 12 | 2 | 5 | 5.2 | CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
| CHEMBL3977724 | 153366 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 445 | 12 | 2 | 5 | 5.2 | CCCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)s2)cc1 | nan | ||
| 11855870 | 146368 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 427 | 11 | 1 | 4 | 5.7 | CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 | nan | ||
| CHEMBL3920756 | 146368 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 427 | 11 | 1 | 4 | 5.7 | CCCCCC(=O)c1ccc(N2C(=O)CC[C@@H]2CCCc2ccc(C(=O)O)s2)cc1 | nan | ||
| 1932 | 2942 | None | 4 | Human | Binding | pEC50 | = | 8.7 | 8.7 | 1 | 6 | Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay |
ChEMBL | 410 | 12 | 3 | 3 | 4.8 | C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O | 10.1021/jm401431x | ||
| 5311228 | 2942 | None | 4 | Human | Binding | pEC50 | = | 8.7 | 8.7 | 1 | 6 | Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay |
ChEMBL | 410 | 12 | 3 | 3 | 4.8 | C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O | 10.1021/jm401431x | ||
| CHEMBL3286796 | 2942 | None | 4 | Human | Binding | pEC50 | = | 8.7 | 8.7 | 1 | 6 | Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay |
ChEMBL | 410 | 12 | 3 | 3 | 4.8 | C=CCC1(CCC1)[C@H](C/C=C/[C@H]1[C@H](O)C[C@H]([C@@H]1C/C=C\CCCC(=O)O)Cl)O | 10.1021/jm401431x | ||
| 90054482 | 144004 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 463 | 10 | 2 | 4 | 4.4 | C[C@@H](Cc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| CHEMBL3902065 | 144004 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 463 | 10 | 2 | 4 | 4.4 | C[C@@H](Cc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| 90054490 | 152279 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 519 | 14 | 2 | 4 | 6.0 | C[C@@H](CCCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| CHEMBL3968443 | 152279 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 519 | 14 | 2 | 4 | 6.0 | C[C@@H](CCCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| 127051063 | 140409 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay |
ChEMBL | 443 | 5 | 2 | 6 | 4.2 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 | 10.1021/acsmedchemlett.5b00455 | ||
| CHEMBL3806284 | 140409 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assayAgonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay |
ChEMBL | 443 | 5 | 2 | 6 | 4.2 | O=C(O)c1csc([C@H]2CC[C@H]3[C@H](C[C@@H](O)[C@@H]3COc3ccccc3C(F)(F)F)O2)n1 | 10.1021/acsmedchemlett.5b00455 | ||
| 11855590 | 144462 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 387 | 8 | 2 | 5 | 3.4 | CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 | nan | ||
| CHEMBL3905811 | 144462 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 387 | 8 | 2 | 5 | 3.4 | CC(C)C(O)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 | nan | ||
| 90054450 | 143863 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 493 | 13 | 2 | 4 | 5.4 | C[C@@H](CCCc1ccccc1)[C@H](O)CC[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| CHEMBL3900979 | 143863 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 493 | 13 | 2 | 4 | 5.4 | C[C@@H](CCCc1ccccc1)[C@H](O)CC[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| 11855591 | 144524 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 435 | 9 | 2 | 5 | 4.0 | O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 | nan | ||
| CHEMBL3906402 | 144524 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 435 | 9 | 2 | 5 | 4.0 | O=C(O)c1ccc(COC[C@H]2CCC(=O)N2c2ccc(C(O)Cc3ccccc3)cc2)o1 | nan | ||
| 72948479 | 153122 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 1 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 491 | 12 | 2 | 4 | 5.2 | C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| CHEMBL3975743 | 153122 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 1 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 491 | 12 | 2 | 4 | 5.2 | C[C@@H](CCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| 70667255 | 151563 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 427 | 10 | 2 | 4 | 5.4 | CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 | nan | ||
| CHEMBL3962183 | 151563 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 1 | Agonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulationAgonist activity at recombinant human EP2 receptor expressed in HEK293-EBNA cells co-expressing Gqs5 assessed as induction of c-AMP accumulation |
ChEMBL | 427 | 10 | 2 | 4 | 5.4 | CCCCCC(O)c1ccc(N2C(=O)CC[C@@H]2C=CCc2ccc(C(=O)O)s2)cc1 | nan | ||
| 90054430 | 149452 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 505 | 13 | 2 | 4 | 5.6 | C[C@@H](CCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| CHEMBL3945327 | 149452 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 505 | 13 | 2 | 4 | 5.6 | C[C@@H](CCCCc1ccccc1)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCCc1ccc(C(=O)O)s1 | nan | ||
| 5283056 | 205318 | None | 28 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O | nan | ||
| CHEMBL62570 | 205318 | None | 28 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 354 | 13 | 3 | 4 | 3.5 | CCCCC[C@@H](O)/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1CCCCCCC(=O)O | nan | ||
| 66858111 | 137538 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor |
ChEMBL | 488 | 11 | 2 | 7 | 4.5 | O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCc3ccccc3)CCC2)n1 | 10.1016/j.bmcl.2015.12.039 | ||
| CHEMBL3753622 | 137538 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor |
ChEMBL | 488 | 11 | 2 | 7 | 4.5 | O=C(O)c1csc(SCCN2C(=O)OC[C@@H]2/C=C/[C@@H](O)C2(CCc3ccccc3)CCC2)n1 | 10.1016/j.bmcl.2015.12.039 | ||
| 72950425 | 143137 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 419 | 8 | 2 | 3 | 3.5 | CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 | nan | ||
| CHEMBL3895047 | 143137 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 419 | 8 | 2 | 3 | 3.5 | CCC#CC[C@H](C)[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 | nan | ||
| 11328569 | 137555 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor |
ChEMBL | 456 | 12 | 2 | 8 | 3.3 | COCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 | 10.1016/j.bmcl.2015.12.039 | ||
| CHEMBL3753788 | 137555 | None | 0 | Human | Binding | pEC50 | = | 7.8 | 7.8 | - | 0 | Agonist activity at human EP2 receptorAgonist activity at human EP2 receptor |
ChEMBL | 456 | 12 | 2 | 8 | 3.3 | COCCCC1([C@H](O)/C=C/[C@H]2COC(=O)N2CCSc2nc(C(=O)O)cs2)CCC1 | 10.1016/j.bmcl.2015.12.039 | ||
| 11855324 | 142692 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins |
ChEMBL | 371 | 6 | 1 | 4 | 4.0 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 | nan | ||
| CHEMBL3891401 | 142692 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 minsDisplacement of [3H]PGE2 from from human EP2 receptor expressed in HEK293 cells at pH 6.0 membranes incubated for 60 mins |
ChEMBL | 371 | 6 | 1 | 4 | 4.0 | CC(C)(C)c1ccc(N2C(=O)CC[C@@H]2COCc2ccc(C(=O)O)o2)cc1 | nan | ||
| 72950929 | 146670 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 1 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 395 | 10 | 2 | 3 | 3.7 | CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 | nan | ||
| CHEMBL3923027 | 146670 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 1 | SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid.SEAP Activity Assay: 1. Seed cells on an EP2 or EP4 STEP plate at a density of 40,000-80,000 cells/well in 200 ul of reduced serum medium containing 0.5% FBS. Place the plate in a 37° C. incubator with 5% CO2 and incubate overnight. 2. After 16-18 hours of incubation, aspirate the culture media from each well. 3. Add 200 ul of culture medium containing different concentration of test compounds to the assigned wells. For each test compound, at least 8 concentrations starting at highest 10 M and lowest 0.01 pM were tested. In addition each concentration had triplicates. A PGE2 curve (concentrations from lowest to highest, 0 pM, 0.384 pM, 1.92 pM, 9.6 pM, 48 pM, 240 pM, 1200 pM, and 6000 pM) was always run in parallel with test compounds. 4. After 6-8 hours of stimulation with test compounds and PGE2, 10 ul of culture media from each well was transferred to a corresponding well of a 96-well solid black plate. Cover the plate with the lid. |
ChEMBL | 395 | 10 | 2 | 3 | 3.7 | CCCCC[C@H](O)/C=C/[C@H]1CC(F)(F)C(=O)N1CCc1ccc(C(=O)O)cc1 | nan | ||
| 1883 | 3082 | None | 47 | Human | Binding | pEC50 | = | 8.7 | 8.7 | -6 | 24 | Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm401431x | ||
| 1916 | 3082 | None | 47 | Human | Binding | pEC50 | = | 8.7 | 8.7 | -6 | 24 | Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm401431x | ||
| 5280360 | 3082 | None | 47 | Human | Binding | pEC50 | = | 8.7 | 8.7 | -6 | 24 | Agonist activity at EP2 receptor (unknown origin) by functional assayAgonist activity at EP2 receptor (unknown origin) by functional assay |
ChEMBL | 352 | 12 | 3 | 4 | 3.3 | CCCCC[C@@H](/C=C/[C@H]1[C@H](O)CC(=O)[C@@H]1C/C=C\CCCC(=O)O)O | 10.1021/jm401431x | ||
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