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Assay Detail

CHEMBL868639

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

Binding
Binding affinity to human F2a
18
Total Activities
18
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

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

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
Ki 18 6.94 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378093 1 7.46
CHEMBL211410 1 7.37
CHEMBL378092 1 7.24
CHEMBL213252 1 7.24
CHEMBL378222 1 7.23
CHEMBL213888 1 7.15
CHEMBL263767 1 7.14
CHEMBL436791 1 7.12
CHEMBL386294 1 7.01
CHEMBL379588 1 6.92
CHEMBL428982 1 6.89
CHEMBL380405 1 6.89
CHEMBL209376 1 6.82
CHEMBL265087 1 6.64
CHEMBL379397 1 6.60
CHEMBL212202 1 6.55
CHEMBL385679 1 6.42
CHEMBL206335 RAZAXABAN 2.0 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378093 Ki = 35.0 nM 7.46
CHEMBL211410 Ki = 43.0 nM 7.37
CHEMBL378092 Ki = 58.0 nM 7.24
CHEMBL213252 Ki = 57.0 nM 7.24
CHEMBL378222 Ki = 59.0 nM 7.23
CHEMBL213888 Ki = 71.0 nM 7.15
CHEMBL263767 Ki = 72.0 nM 7.14
CHEMBL436791 Ki = 75.0 nM 7.12
CHEMBL386294 Ki = 97.0 nM 7.01
CHEMBL379588 Ki = 120.0 nM 6.92
CHEMBL428982 Ki = 130.0 nM 6.89
CHEMBL380405 Ki = 130.0 nM 6.89
CHEMBL209376 Ki = 150.0 nM 6.82
CHEMBL265087 Ki = 230.0 nM 6.64
CHEMBL379397 Ki = 250.0 nM 6.60
CHEMBL212202 Ki = 280.0 nM 6.55
CHEMBL385679 Ki = 380.0 nM 6.42
CHEMBL206335 RAZAXABAN Ki = 540.0 nM 6.27