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Assay Detail

CHEMBL658336

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Binding
Binding affinity against Coagulation factor X in an enzyme inhibition assay.
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Preparation of pyrrolidine and isoxazolidine benzamidines as potent inhibitors of coagulation factor Xa.
Fevig JM, Buriak J, Stouten PF, Knabb RM, Lam GN, Wong PC, Wexler RR.
Bioorg Med Chem Lett (1999) 9 : 1195 -1200
PubMed 10328312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.67 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18767 1 8.89
CHEMBL18578 1 8.74
CHEMBL279267 1 8.51
CHEMBL18225 2 8.47
CHEMBL276782 1 8.24
CHEMBL279628 1 8.20
CHEMBL429068 1 7.92
CHEMBL277994 1 7.89
CHEMBL275582 1 7.58
CHEMBL18627 1 7.44
CHEMBL19038 1 6.82
CHEMBL19075 1 6.77
CHEMBL19090 1 6.40
CHEMBL277366 1 6.34
CHEMBL435761 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18767 Ki = 1.3 nM 8.89
CHEMBL18578 Ki = 1.8 nM 8.74
CHEMBL279267 Ki = 3.1 nM 8.51
CHEMBL18225 Ki = 3.4 nM 8.47
CHEMBL18225 Ki = 4.8 nM 8.32
CHEMBL276782 Ki = 5.8 nM 8.24
CHEMBL279628 Ki = 6.3 nM 8.20
CHEMBL429068 Ki = 12.0 nM 7.92
CHEMBL277994 Ki = 13.0 nM 7.89
CHEMBL275582 Ki = 26.0 nM 7.58
CHEMBL18627 Ki = 36.0 nM 7.44
CHEMBL19038 Ki = 150.0 nM 6.82
CHEMBL19075 Ki = 170.0 nM 6.77
CHEMBL19090 Ki = 400.0 nM 6.40
CHEMBL277366 Ki = 460.0 nM 6.34
CHEMBL435761 Ki = 600.0 nM 6.22