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Assay Detail

CHEMBL815797

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

Binding
In vitro evaluation for the concentration needed for inhibiting thrombin by 50%
19
Total Activities
19
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

Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.
Nagahara T, Yokoyama Y, Inamura K, Katakura S, Komoriya S, Yamaguchi H, Hara T, Iwamoto M.
J Med Chem (1994) 37 : 1200 -1207
PubMed 8164262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 4.75 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19368 1 5.40
CHEMBL279962 1 5.30
CHEMBL280158 1 5.05
CHEMBL279077 1 4.82
CHEMBL279367 1 4.70
CHEMBL280162 1 4.68
CHEMBL19594 1 4.66
CHEMBL19152 1 4.44
CHEMBL279270 1 4.42
CHEMBL19626 1 4.00
CHEMBL19139 1 -
CHEMBL277240 1 -
CHEMBL19660 1 -
CHEMBL280157 1 -
CHEMBL279959 1 -
CHEMBL276989 1 -
CHEMBL19365 1 -
CHEMBL277267 1 -
CHEMBL19902 DX-9065A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19368 IC50 = 4000.0 nM 5.40
CHEMBL279962 IC50 = 5000.0 nM 5.30
CHEMBL280158 IC50 = 9000.0 nM 5.05
CHEMBL279077 IC50 = 15000.0 nM 4.82
CHEMBL279367 IC50 = 20000.0 nM 4.70
CHEMBL280162 IC50 = 21000.0 nM 4.68
CHEMBL19594 IC50 = 22000.0 nM 4.66
CHEMBL19152 IC50 = 36000.0 nM 4.44
CHEMBL279270 IC50 = 38000.0 nM 4.42
CHEMBL19626 IC50 = 100000.0 nM 4.00
CHEMBL19139 IC50 > 1600000.0 nM -
CHEMBL277240 IC50 > 400000.0 nM -
CHEMBL19660 IC50 > 1200000.0 nM -
CHEMBL280157 IC50 = 230000.0 nM -
CHEMBL279959 IC50 > 100000.0 nM -
CHEMBL276989 IC50 > 1000000.0 nM -
CHEMBL19365 IC50 > 1000000.0 nM -
CHEMBL277267 IC50 > 600000.0 nM -
CHEMBL19902 DX-9065A IC50 > 2000000.0 nM -