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Assay Detail

CHEMBL906324

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

Binding
Displacement of [3H]PGE2 from human recombinant EP1 receptor expressed in CHOK1 cell membrane
30
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Prostaglandin E2 receptor EP1 subtype (CHEMBL1811)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,5-Biaryl pyrrole derivatives as EP1 receptor antagonists. Structure-activity relationships of 6-substituted and 5,6-disubstituted benzoic acid derivatives.
Hall A, Brown SH, Chessell IP, Chowdhury A, Clayton NM, Coleman T, Giblin GM, Hammond B, Healy MP, Johnson MR, Metcalf A, Michel AD, Naylor A, Novelli R, Spalding DJ, Sweeting J, Winyard L.
Bioorg Med Chem Lett (2007) 17 : 916 -920
PubMed 17175160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 8.45 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387969 1 9.40
CHEMBL228586 1 9.40
CHEMBL387878 1 9.20
CHEMBL228593 1 9.10
CHEMBL228963 1 8.90
CHEMBL230765 1 8.90
CHEMBL395248 1 8.90
CHEMBL395488 1 8.70
CHEMBL426913 1 8.70
CHEMBL230766 1 8.70
CHEMBL228638 1 8.70
CHEMBL414978 1 8.60
CHEMBL230875 1 8.60
CHEMBL397655 1 8.60
CHEMBL388294 1 8.50
CHEMBL228644 1 8.40
CHEMBL228592 1 8.40
CHEMBL228746 1 8.30
CHEMBL231184 1 8.30
CHEMBL374824 1 8.30
CHEMBL228695 1 8.20
CHEMBL208791 2 8.20
CHEMBL388478 1 8.10
CHEMBL390081 1 7.90
CHEMBL230874 1 7.90
CHEMBL388510 1 7.80
CHEMBL230873 1 7.80
CHEMBL397226 1 7.60
CHEMBL269514 1 7.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387969 IC50 = 0.3981 nM 9.40
CHEMBL228586 IC50 = 0.3981 nM 9.40
CHEMBL387878 IC50 = 0.631 nM 9.20
CHEMBL228593 IC50 = 0.7943 nM 9.10
CHEMBL228963 IC50 = 1.259 nM 8.90
CHEMBL230765 IC50 = 1.259 nM 8.90
CHEMBL395248 IC50 = 1.259 nM 8.90
CHEMBL426913 IC50 = 1.995 nM 8.70
CHEMBL230766 IC50 = 1.995 nM 8.70
CHEMBL395488 IC50 = 1.995 nM 8.70
CHEMBL228638 IC50 = 1.995 nM 8.70
CHEMBL230875 IC50 = 2.512 nM 8.60
CHEMBL397655 IC50 = 2.512 nM 8.60
CHEMBL414978 IC50 = 2.512 nM 8.60
CHEMBL388294 IC50 = 3.162 nM 8.50
CHEMBL228644 IC50 = 3.981 nM 8.40
CHEMBL228592 IC50 = 3.981 nM 8.40
CHEMBL374824 IC50 = 5.012 nM 8.30
CHEMBL228746 IC50 = 5.012 nM 8.30
CHEMBL231184 IC50 = 5.012 nM 8.30
CHEMBL208791 IC50 = 6.31 nM 8.20
CHEMBL228695 IC50 = 6.31 nM 8.20
CHEMBL208791 IC50 = 6.31 nM 8.20
CHEMBL388478 IC50 = 7.943 nM 8.10
CHEMBL390081 IC50 = 12.59 nM 7.90
CHEMBL230874 IC50 = 12.59 nM 7.90
CHEMBL230873 IC50 = 15.85 nM 7.80
CHEMBL388510 IC50 = 15.85 nM 7.80
CHEMBL397226 IC50 = 25.12 nM 7.60
CHEMBL269514 IC50 = 79.43 nM 7.10