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Assay Detail

CHEMBL839596

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Binding
Binding affinity determined against human activated protein C
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Vitamin K-dependent protein C (CHEMBL4444)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
Quan ML, Lam PY, Han Q, Pinto DJ, He MY, Li R, Ellis CD, Clark CG, Teleha CA, Sun JH, Alexander RS, Bai S, Luettgen JM, Knabb RM, Wong PC, Wexler RR.
J Med Chem (2005) 48 : 1729 -1744
PubMed 15771420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.00 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176140 1 5.75
CHEMBL558198 RAZAXABAN HYDROCHLORIDE -1.0 1 4.71
CHEMBL554926 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176140 Ki = 1800.0 nM 5.75
CHEMBL558198 RAZAXABAN HYDROCHLORIDE Ki = 19700.0 nM 4.71
CHEMBL554926 Ki = 28000.0 nM 4.55