Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL900676

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

Binding
Binding affinity to rabbit F10a
4
Total Activities
4
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-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Koch S, Rossi KA, Alexander RS, Smallwood A, Wong PC, Rendina AR, Luettgen JM, Knabb RM, He K, Xin B, Wexler RR, Lam PY.
J Med Chem (2007) 50 : 5339 -5356
PubMed 17914785 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 9.58 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378093 1 10.22
CHEMBL231779 APIXABAN 4.0 1 9.77
CHEMBL206335 RAZAXABAN 2.0 1 9.72
CHEMBL235710 1 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378093 Ki = 0.06 nM 10.22
CHEMBL231779 APIXABAN Ki = 0.17 nM 9.77
CHEMBL206335 RAZAXABAN Ki = 0.19 nM 9.72
CHEMBL235710 Ki = 2.6 nM 8.59