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Assay Detail

CHEMBL3281104

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

Binding
Inhibition of human thrombin-mediated blood clotting formation in presence of human fibrinogen
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel bis(benzamidino) compounds with an aromatic central link. Inhibitors of thrombin, pancreatic kallikrein, trypsin, and complement.
Geratz JD, Cheng MC, Tidwell RR.
J Med Chem (1976) 19 : 634 -639
PubMed 1271404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.94 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3277934 1 6.14
CHEMBL3277923 1 6.00
CHEMBL3277936 1 5.40
CHEMBL3277921 1 5.19
CHEMBL3277925 1 5.10
CHEMBL3277935 1 5.00
CHEMBL3277919 1 4.89
CHEMBL3277933 1 4.82
CHEMBL3277918 1 4.77
CHEMBL3277927 1 4.70
CHEMBL3277931 1 4.70
CHEMBL3277920 1 4.60
CHEMBL3277929 1 4.52
CHEMBL3277930 1 4.14
CHEMBL3277926 1 4.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3277934 IC50 = 730.0 nM 6.14
CHEMBL3277923 IC50 = 1000.0 nM 6.00
CHEMBL3277936 IC50 = 4000.0 nM 5.40
CHEMBL3277921 IC50 = 6500.0 nM 5.19
CHEMBL3277925 IC50 = 8000.0 nM 5.10
CHEMBL3277935 IC50 = 10000.0 nM 5.00
CHEMBL3277919 IC50 = 13000.0 nM 4.89
CHEMBL3277933 IC50 = 15000.0 nM 4.82
CHEMBL3277918 IC50 = 17000.0 nM 4.77
CHEMBL3277927 IC50 = 20000.0 nM 4.70
CHEMBL3277931 IC50 = 20000.0 nM 4.70
CHEMBL3277920 IC50 = 25000.0 nM 4.60
CHEMBL3277929 IC50 = 30000.0 nM 4.52
CHEMBL3277930 IC50 = 72000.0 nM 4.14
CHEMBL3277926 IC50 = 80000.0 nM 4.10