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Assay Detail

CHEMBL869244

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

Functional
Antithrombotic activity in rabbit arterio-venous shunt thrombosis model
8
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa.
Pinto DJ, Orwat MJ, Quan ML, Han Q, Galemmo RA, Amparo E, Wells B, Ellis C, He MY, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, Mersinger L, Kettner C, Bai S, He K, Wexler RR, Lam PY.
Bioorg Med Chem Lett (2006) 16 : 4141 -4147
PubMed 16730984 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.39 6.87
ID50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378093 1 6.87
CHEMBL211410 1 6.65
CHEMBL206335 RAZAXABAN 2.0 1 6.47
CHEMBL213888 1 6.29
CHEMBL263767 1 6.22
CHEMBL436791 1 6.22
CHEMBL402881 1 6.00
CHEMBL380405 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378093 IC50 = 135.0 nM 6.87
CHEMBL211410 IC50 = 223.0 nM 6.65
CHEMBL206335 RAZAXABAN IC50 = 340.0 nM 6.47
CHEMBL213888 IC50 = 510.0 nM 6.29
CHEMBL263767 IC50 = 600.0 nM 6.22
CHEMBL436791 IC50 = 600.0 nM 6.22
CHEMBL402881 IC50 = 1000.0 nM 6.00
CHEMBL380405 ID50 = 0.6 ug/hr.kg -