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Assay Detail

CHEMBL865352

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Binding
Inhibition of [3H]PGE2 binding to EP1 receptor expressed in CHO cells
ChEMBL ↗
54
Total Activities
53
Compounds Tested
2
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

Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists.
Hall A, Atkinson S, Brown SH, Chessell IP, Chowdhury A, Clayton NM, Coleman T, Giblin GM, Gleave RJ, Hammond B, Healy MP, Johnson MR, Michel AD, Naylor A, Novelli R, Spalding DJ, Tang SP.
Bioorg Med Chem Lett (2006) 16 : 3657 -3662
PubMed 16697196 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 7.65 9.00
Ki 1 9.15 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377852 — — 2 9.15
CHEMBL211534 — — 1 9.00
CHEMBL210394 — — 1 8.80
CHEMBL209685 — — 1 8.60
CHEMBL212672 — — 1 8.50
CHEMBL211088 — — 1 8.40
CHEMBL212688 — — 1 8.30
CHEMBL211059 — — 1 8.30
CHEMBL378120 — — 1 8.30
CHEMBL209800 — — 1 8.30
CHEMBL208934 — — 1 8.30
CHEMBL208912 — — 1 8.20
CHEMBL378641 — — 1 8.20
CHEMBL208791 — — 1 8.20
CHEMBL209078 — — 1 8.10
CHEMBL377649 — — 1 8.10
CHEMBL210261 — — 1 8.00
CHEMBL211700 — — 1 8.00
CHEMBL383090 — — 1 8.00
CHEMBL212471 — — 1 7.90
CHEMBL379753 — — 1 7.90
CHEMBL380046 — — 1 7.90
CHEMBL208684 — — 1 7.80
CHEMBL377910 — — 1 7.80
CHEMBL208882 — — 1 7.80
CHEMBL208797 — — 1 7.70
CHEMBL211776 — — 1 7.70
CHEMBL209746 — — 1 7.60
CHEMBL212742 — — 1 7.60
CHEMBL377338 — — 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377852 — Ki = 0.7079 nM 9.15
CHEMBL211534 — IC50 = 1.0 nM 9.00
CHEMBL210394 — IC50 = 1.585 nM 8.80
CHEMBL209685 — IC50 = 2.512 nM 8.60
CHEMBL212672 — IC50 = 3.162 nM 8.50
CHEMBL211088 — IC50 = 3.981 nM 8.40
CHEMBL212688 — IC50 = 5.012 nM 8.30
CHEMBL211059 — IC50 = 5.012 nM 8.30
CHEMBL209800 — IC50 = 5.012 nM 8.30
CHEMBL378120 — IC50 = 5.012 nM 8.30
CHEMBL208934 — IC50 = 5.012 nM 8.30
CHEMBL208791 — IC50 = 6.31 nM 8.20
CHEMBL378641 — IC50 = 6.31 nM 8.20
CHEMBL208912 — IC50 = 6.31 nM 8.20
CHEMBL377852 — IC50 = 7.943 nM 8.10
CHEMBL377649 — IC50 = 7.943 nM 8.10
CHEMBL209078 — IC50 = 7.943 nM 8.10
CHEMBL383090 — IC50 = 10.0 nM 8.00
CHEMBL210261 — IC50 = 10.0 nM 8.00
CHEMBL211700 — IC50 = 10.0 nM 8.00
CHEMBL380046 — IC50 = 12.59 nM 7.90
CHEMBL379753 — IC50 = 12.59 nM 7.90
CHEMBL212471 — IC50 = 12.59 nM 7.90
CHEMBL208684 — IC50 = 15.85 nM 7.80
CHEMBL377910 — IC50 = 15.85 nM 7.80
CHEMBL208882 — IC50 = 15.85 nM 7.80
CHEMBL211776 — IC50 = 19.95 nM 7.70
CHEMBL208797 — IC50 = 19.95 nM 7.70
CHEMBL377338 — IC50 = 25.12 nM 7.60
CHEMBL212742 — IC50 = 25.12 nM 7.60
CHEMBL380197 — IC50 = 25.12 nM 7.60
CHEMBL209746 — IC50 = 25.12 nM 7.60
CHEMBL378226 — IC50 = 31.62 nM 7.50
CHEMBL378090 — IC50 = 39.81 nM 7.40
CHEMBL212680 — IC50 = 39.81 nM 7.40
CHEMBL210987 — IC50 = 39.81 nM 7.40
CHEMBL379514 — IC50 = 39.81 nM 7.40
CHEMBL377134 — IC50 = 50.12 nM 7.30
CHEMBL377034 — IC50 = 50.12 nM 7.30
CHEMBL210994 — IC50 = 79.43 nM 7.10
CHEMBL379155 — IC50 = 79.43 nM 7.10
CHEMBL208660 — IC50 = 100.0 nM 7.00
CHEMBL208891 — IC50 = 100.0 nM 7.00
CHEMBL379143 — IC50 = 100.0 nM 7.00
CHEMBL378464 — IC50 = 100.0 nM 7.00
CHEMBL377831 — IC50 = 125.89 nM 6.90
CHEMBL209326 — IC50 = 199.53 nM 6.70
CHEMBL212679 — IC50 = 199.53 nM 6.70
CHEMBL376996 — IC50 = 251.19 nM 6.60
CHEMBL377245 — IC50 = 398.11 nM 6.40