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Assay Detail

CHEMBL897085

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 CHO cells
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
Hall A, Atkinson S, Brown SH, Chessell IP, Chowdhury A, Giblin GM, Goldsmith P, Healy MP, Jandu KS, Johnson MR, Michel AD, Naylor A, Sweeting JA.
Bioorg Med Chem Lett (2007) 17 : 1200 -1205
PubMed 17196385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 7.44 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL233768 1 8.80
CHEMBL232340 1 8.60
CHEMBL232117 1 8.60
CHEMBL232341 1 8.60
CHEMBL391286 1 8.40
CHEMBL233137 1 8.40
CHEMBL391287 1 8.30
CHEMBL391026 1 8.30
CHEMBL232932 1 8.10
CHEMBL232543 1 8.10
CHEMBL377852 1 8.10
CHEMBL231723 1 8.00
CHEMBL401023 1 7.90
CHEMBL439381 1 7.80
CHEMBL233138 1 7.80
CHEMBL393187 1 7.70
CHEMBL232930 1 7.70
CHEMBL231722 1 7.70
CHEMBL232544 1 7.60
CHEMBL233140 1 7.60
CHEMBL233975 1 7.60
CHEMBL234176 1 7.60
CHEMBL232931 1 7.50
CHEMBL391931 1 7.40
CHEMBL234181 1 7.40
CHEMBL233160 1 7.40
CHEMBL392047 1 7.40
CHEMBL233565 1 7.40
CHEMBL234174 1 7.30
CHEMBL399800 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL233768 IC50 = 1.585 nM 8.80
CHEMBL232340 IC50 = 2.512 nM 8.60
CHEMBL232341 IC50 = 2.512 nM 8.60
CHEMBL232117 IC50 = 2.512 nM 8.60
CHEMBL391286 IC50 = 3.981 nM 8.40
CHEMBL233137 IC50 = 3.981 nM 8.40
CHEMBL391287 IC50 = 5.012 nM 8.30
CHEMBL391026 IC50 = 5.012 nM 8.30
CHEMBL232932 IC50 = 7.943 nM 8.10
CHEMBL377852 IC50 = 7.943 nM 8.10
CHEMBL232543 IC50 = 7.943 nM 8.10
CHEMBL231723 IC50 = 10.0 nM 8.00
CHEMBL401023 IC50 = 12.59 nM 7.90
CHEMBL233138 IC50 = 15.85 nM 7.80
CHEMBL439381 IC50 = 15.85 nM 7.80
CHEMBL393187 IC50 = 19.95 nM 7.70
CHEMBL231722 IC50 = 19.95 nM 7.70
CHEMBL232930 IC50 = 19.95 nM 7.70
CHEMBL232544 IC50 = 25.12 nM 7.60
CHEMBL233140 IC50 = 25.12 nM 7.60
CHEMBL233975 IC50 = 25.12 nM 7.60
CHEMBL234176 IC50 = 25.12 nM 7.60
CHEMBL232931 IC50 = 31.62 nM 7.50
CHEMBL233565 IC50 = 39.81 nM 7.40
CHEMBL392047 IC50 = 39.81 nM 7.40
CHEMBL233160 IC50 = 39.81 nM 7.40
CHEMBL391931 IC50 = 39.81 nM 7.40
CHEMBL234181 IC50 = 39.81 nM 7.40
CHEMBL234174 IC50 = 50.12 nM 7.30
CHEMBL399800 IC50 = 50.12 nM 7.30
CHEMBL393416 IC50 = 63.1 nM 7.20
CHEMBL233159 IC50 = 63.1 nM 7.20
CHEMBL233141 IC50 = 63.1 nM 7.20
CHEMBL233146 IC50 = 63.1 nM 7.20
CHEMBL233361 IC50 = 63.1 nM 7.20
CHEMBL438126 IC50 = 63.1 nM 7.20
CHEMBL232537 IC50 = 63.1 nM 7.20
CHEMBL394173 IC50 = 79.43 nM 7.10
CHEMBL234182 IC50 = 125.89 nM 6.90
CHEMBL393743 IC50 = 125.89 nM 6.90
CHEMBL232733 IC50 = 125.89 nM 6.90
CHEMBL233772 IC50 = 158.49 nM 6.80
CHEMBL232734 IC50 = 199.53 nM 6.70
CHEMBL233359 IC50 = 199.53 nM 6.70
CHEMBL234183 IC50 = 251.19 nM 6.60
CHEMBL391228 IC50 = 316.23 nM 6.50
CHEMBL391456 IC50 = 501.19 nM 6.30
CHEMBL439388 IC50 = 501.19 nM 6.30
CHEMBL391930 IC50 = 501.19 nM 6.30
CHEMBL393374 IC50 = 501.19 nM 6.30