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Assay Detail

CHEMBL661667

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Binding
Tested in vitro for inhibition of rabbit Coagulation factor X
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Coagulation factor X (CHEMBL5062)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Discovery of 1-(2-aminomethylphenyl)-3-trifluoromethyl-N- [3-fluoro-2'-(aminosulfonyl)[1,1'-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a potent, selective, and orally bioavailable factor Xa inhibitor(1).
Pruitt JR, Pinto DJ, Galemmo RA, Alexander RS, Rossi KA, Wells BL, Drummond S, Bostrom LL, Burdick D, Bruckner R, Chen H, Smallwood A, Wong PC, Wright MR, Bai S, Luettgen JM, Knabb RM, Lam PY, Wexler RR.
J Med Chem (2003) 46 : 5298 -5315
PubMed 14640539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.67 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559015 1 9.52
CHEMBL348441 1 8.59
CHEMBL151939 1 8.54
CHEMBL146910 1 8.37
CHEMBL148944 1 8.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559015 Ki = 0.3 nM 9.52
CHEMBL348441 Ki = 2.6 nM 8.59
CHEMBL151939 Ki = 2.9 nM 8.54
CHEMBL146910 Ki = 4.3 nM 8.37
CHEMBL148944 Ki = 4.6 nM 8.34