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Assay Detail

CHEMBL900672

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Functional
Inhibition of thrombus formation in rabbit arteriovenous shunt thrombosis model
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 1 — Organism
Curated By Intermediate

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
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
IC50 12 6.65 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL235265 1 6.92
CHEMBL378093 1 6.85
CHEMBL391484 1 6.76
CHEMBL237419 1 6.75
CHEMBL231779 APIXABAN 4.0 1 6.48
CHEMBL206335 RAZAXABAN 2.0 1 6.47
CHEMBL237226 1 6.35
CHEMBL279187 1 -
CHEMBL237420 1 -
CHEMBL443578 1 -
CHEMBL237228 1 -
CHEMBL235710 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL235265 IC50 = 120.0 nM 6.92
CHEMBL378093 IC50 = 140.0 nM 6.85
CHEMBL391484 IC50 = 175.0 nM 6.76
CHEMBL237419 IC50 = 180.0 nM 6.75
CHEMBL231779 APIXABAN IC50 = 329.0 nM 6.48
CHEMBL206335 RAZAXABAN IC50 = 340.0 nM 6.47
CHEMBL237226 IC50 = 445.0 nM 6.35
CHEMBL279187 IC50 - -
CHEMBL237420 IC50 - -
CHEMBL443578 IC50 - -
CHEMBL237228 IC50 - -
CHEMBL235710 IC50 - -