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Assay Detail

CHEMBL660486

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

Binding
In vitro evaluation of inhibitory activity against Coagulation factor II in prothrombinase complex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.
Choi-Sledeski YM, Becker MR, Green DM, Davis R, Ewing WR, Mason HJ, Ly C, Spada A, Liang G, Cheney D, Barton J, Chu V, Brown K, Colussi D, Bentley R, Leadley R, Dunwiddie C, Pauls HW.
Bioorg Med Chem Lett (1999) 9 : 2539 -2544
PubMed 10498204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.86 5.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL315218 1 5.87
CHEMBL327600 1 5.85
CHEMBL86343 1 -
CHEMBL83532 1 -
CHEMBL1907672 1 -
CHEMBL419490 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL315218 Ki = 1350.0 nM 5.87
CHEMBL327600 Ki = 1400.0 nM 5.85
CHEMBL86343 Ki > 4000.0 nM -
CHEMBL83532 Ki ~ 4000.0 nM -
CHEMBL1907672 Ki > 4000.0 nM -
CHEMBL419490 Ki ~ 4000.0 nM -