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Assay Detail

CHEMBL662109

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

Binding
In vitro activity against human factor IXa
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Coagulation factor IX (CHEMBL2016)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-[3-(aminomethyl)phenyl]-N-3-fluoro-2'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a highly potent, selective, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Wang S, Fevig JM, Quan ML, Amparo E, Cacciola J, Rossi KA, Alexander RS, Smallwood AM, Luettgen JM, Liang L, Aungst BJ, Wright MR, Knabb RM, Wong PC, Wexler RR, Lam PY.
J Med Chem (2001) 44 : 566 -578
PubMed 11170646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 5.66 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559015 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559015 Ki = 2200.0 nM 5.66