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Assay Detail

CHEMBL1104419

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

Functional
Antagonist activity at mouse EP3 receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by FDSS in presence of 1% bovine serum albumin
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Tissue Serum
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E2 receptor EP3 subtype (CHEMBL4336)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists.
Asada M, Obitsu T, Kinoshita A, Nakai Y, Nagase T, Sugimoto I, Tanaka M, Takizawa H, Yoshikawa K, Sato K, Narita M, Ohuchida S, Nakai H, Toda M.
Bioorg Med Chem Lett (2010) 20 : 2639 -2643
PubMed 20346663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.61 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1092432 1 9.40
CHEMBL1091741 1 8.92
CHEMBL1091743 1 8.85
CHEMBL1090937 1 8.42
CHEMBL1091740 1 8.26
CHEMBL1091744 1 8.19
CHEMBL1091739 1 8.11
CHEMBL1091738 1 8.00
CHEMBL1091742 1 7.75
CHEMBL1092431 1 7.62
CHEMBL1090938 1 7.62
CHEMBL1092097 1 7.33
CHEMBL1092976 1 7.29
CHEMBL1093820 1 7.23
CHEMBL1093842 1 7.06
CHEMBL1093819 1 6.96
CHEMBL1092266 1 6.85
CHEMBL1093841 1 6.82
CHEMBL1093537 1 6.72
CHEMBL605833 1 6.24
CHEMBL1092267 1 6.09
CHEMBL1091959 1 -
CHEMBL1093911 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1092432 IC50 = 0.4 nM 9.40
CHEMBL1091741 IC50 = 1.2 nM 8.92
CHEMBL1091743 IC50 = 1.4 nM 8.85
CHEMBL1090937 IC50 = 3.8 nM 8.42
CHEMBL1091740 IC50 = 5.5 nM 8.26
CHEMBL1091744 IC50 = 6.4 nM 8.19
CHEMBL1091739 IC50 = 7.8 nM 8.11
CHEMBL1091738 IC50 = 10.0 nM 8.00
CHEMBL1091742 IC50 = 18.0 nM 7.75
CHEMBL1092431 IC50 = 24.0 nM 7.62
CHEMBL1090938 IC50 = 24.0 nM 7.62
CHEMBL1092097 IC50 = 47.0 nM 7.33
CHEMBL1092976 IC50 = 51.0 nM 7.29
CHEMBL1093820 IC50 = 59.0 nM 7.23
CHEMBL1093842 IC50 = 88.0 nM 7.06
CHEMBL1093819 IC50 = 110.0 nM 6.96
CHEMBL1092266 IC50 = 140.0 nM 6.85
CHEMBL1093841 IC50 = 150.0 nM 6.82
CHEMBL1093537 IC50 = 190.0 nM 6.72
CHEMBL605833 IC50 = 580.0 nM 6.24
CHEMBL1092267 IC50 = 820.0 nM 6.09
CHEMBL1091959 IC50 > 10000.0 nM -
CHEMBL1093911 IC50 > 10000.0 nM -