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Assay Detail

CHEMBL1107235

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H]PGE2 from human EP3 receptor in presence of 10% human serum
62
Total Activities
62
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E2 receptor EP3 subtype (CHEMBL3710)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,7-Disubstituted oxyindoles are potent and selective EP(3) receptor antagonists.
Zhou N, Polozov AM, O'Connell M, Burgeson J, Yu P, Zeller W, Zhang J, Onua E, Ramirez J, Palsdottir GA, Halldorsdottir GV, Andresson T, Kiselyov AS, Gurney M, Singh J.
Bioorg Med Chem Lett (2010) 20 : 2658 -2664
PubMed 20303752 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 62 7.59 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093897 1 8.72
CHEMBL1089454 1 8.55
CHEMBL1090458 1 8.49
CHEMBL1091164 1 8.48
CHEMBL1090113 1 8.48
CHEMBL1093797 1 8.48
CHEMBL1089455 1 8.39
CHEMBL1089491 1 8.37
CHEMBL1090112 1 8.36
CHEMBL1090222 1 8.35
CHEMBL1093843 1 8.30
CHEMBL1088823 1 8.28
CHEMBL1090460 1 8.27
CHEMBL1088785 1 8.27
CHEMBL1089094 1 8.26
CHEMBL1090501 1 8.25
CHEMBL1088780 1 8.19
CHEMBL1089161 1 8.17
CHEMBL1088822 1 8.16
CHEMBL1093792 1 8.12
CHEMBL1089095 1 8.11
CHEMBL1088846 1 8.09
CHEMBL1092230 1 8.03
CHEMBL1093559 1 8.03
CHEMBL1093125 1 8.03
CHEMBL1090507 1 8.01
CHEMBL1088815 1 7.99
CHEMBL479868 1 7.97
CHEMBL1093133 1 7.90
CHEMBL1090454 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093897 IC50 = 1.9 nM 8.72
CHEMBL1089454 IC50 = 2.8 nM 8.55
CHEMBL1090458 IC50 = 3.2 nM 8.49
CHEMBL1091164 IC50 = 3.3 nM 8.48
CHEMBL1090113 IC50 = 3.3 nM 8.48
CHEMBL1093797 IC50 = 3.3 nM 8.48
CHEMBL1089455 IC50 = 4.1 nM 8.39
CHEMBL1089491 IC50 = 4.3 nM 8.37
CHEMBL1090112 IC50 = 4.4 nM 8.36
CHEMBL1090222 IC50 = 4.5 nM 8.35
CHEMBL1093843 IC50 = 5.0 nM 8.30
CHEMBL1088823 IC50 = 5.2 nM 8.28
CHEMBL1090460 IC50 = 5.4 nM 8.27
CHEMBL1088785 IC50 = 5.4 nM 8.27
CHEMBL1089094 IC50 = 5.5 nM 8.26
CHEMBL1090501 IC50 = 5.6 nM 8.25
CHEMBL1088780 IC50 = 6.5 nM 8.19
CHEMBL1089161 IC50 = 6.8 nM 8.17
CHEMBL1088822 IC50 = 6.9 nM 8.16
CHEMBL1093792 IC50 = 7.6 nM 8.12
CHEMBL1089095 IC50 = 7.7 nM 8.11
CHEMBL1088846 IC50 = 8.1 nM 8.09
CHEMBL1092230 IC50 = 9.4 nM 8.03
CHEMBL1093559 IC50 = 9.3 nM 8.03
CHEMBL1093125 IC50 = 9.4 nM 8.03
CHEMBL1090507 IC50 = 9.8 nM 8.01
CHEMBL1088815 IC50 = 10.2 nM 7.99
CHEMBL479868 IC50 = 10.7 nM 7.97
CHEMBL1093133 IC50 = 12.7 nM 7.90
CHEMBL1090454 IC50 = 15.0 nM 7.82
CHEMBL1093790 IC50 = 17.4 nM 7.76
CHEMBL1093791 IC50 = 19.4 nM 7.71
CHEMBL1090459 IC50 = 20.0 nM 7.70
CHEMBL1093240 IC50 = 20.8 nM 7.68
CHEMBL1089807 IC50 = 23.9 nM 7.62
CHEMBL1090888 IC50 = 27.2 nM 7.57
CHEMBL1090455 IC50 = 33.9 nM 7.47
CHEMBL1088848 IC50 = 35.5 nM 7.45
CHEMBL1090498 IC50 = 39.0 nM 7.41
CHEMBL1091145 IC50 = 42.0 nM 7.38
CHEMBL1088847 IC50 = 47.8 nM 7.32
CHEMBL1092871 IC50 = 55.4 nM 7.26
CHEMBL1091146 IC50 = 55.4 nM 7.26
CHEMBL1093239 IC50 = 64.7 nM 7.19
CHEMBL1090499 IC50 = 64.0 nM 7.19
CHEMBL1091165 IC50 = 82.4 nM 7.08
CHEMBL1091893 IC50 = 92.8 nM 7.03
CHEMBL1093124 IC50 = 95.8 nM 7.02
CHEMBL1090342 IC50 = 96.5 nM 7.01
CHEMBL1090889 IC50 = 125.1 nM 6.90