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Assay Detail

CHEMBL1045320

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

ADMET
Inhibition of human CYP2C19
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cytochrome P450 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding.
Singh J, Zeller W, Zhou N, Hategan G, Mishra RK, Polozov A, Yu P, Onua E, Zhang J, Ramírez JL, Sigthorsson G, Thorsteinnsdottir M, Kiselyov AS, Zembower DE, Andrésson T, Gurney ME.
J Med Chem (2010) 53 : 18 -36
PubMed 19957930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.18 5.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565591 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565591 IC50 = 6600.0 nM 5.18