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Assay Detail

CHEMBL845034

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Binding
Inhibition of human thrombin by chromogenic assay
24
Total Activities
24
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

Structure-based design of novel potent nonpeptide thrombin inhibitors.
Hauel NH, Nar H, Priepke H, Ries U, Stassen JM, Wienen W.
J Med Chem (2002) 45 : 1757 -1766
PubMed 11960487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.61 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48635 1 8.27
CHEMBL48361 DABIGATRAN 3.0 1 8.03
CHEMBL49445 1 8.00
CHEMBL48914 1 8.00
CHEMBL298500 1 7.96
CHEMBL417360 1 7.50
CHEMBL299515 1 7.27
CHEMBL51528 1 7.24
CHEMBL46434 1 6.92
CHEMBL299580 1 6.89
CHEMBL51173 1 6.70
CHEMBL424593 1 6.58
CHEMBL49216 1 6.48
CHEMBL51050 1 6.29
CHEMBL300305 1 6.22
CHEMBL50790 1 5.89
CHEMBL46780 1 5.82
CHEMBL299743 1 5.80
CHEMBL300937 1 5.75
CHEMBL48882 1 5.62
CHEMBL48517 1 5.40
CHEMBL49181 1 4.72
CHEMBL298578 1 4.62
CHEMBL48717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48635 IC50 = 5.4 nM 8.27
CHEMBL48361 DABIGATRAN IC50 = 9.3 nM 8.03
CHEMBL49445 IC50 = 10.0 nM 8.00
CHEMBL48914 IC50 = 10.0 nM 8.00
CHEMBL298500 IC50 = 11.0 nM 7.96
CHEMBL417360 IC50 = 32.0 nM 7.50
CHEMBL299515 IC50 = 54.0 nM 7.27
CHEMBL51528 IC50 = 58.0 nM 7.24
CHEMBL46434 IC50 = 120.0 nM 6.92
CHEMBL299580 IC50 = 130.0 nM 6.89
CHEMBL51173 IC50 = 200.0 nM 6.70
CHEMBL424593 IC50 = 260.0 nM 6.58
CHEMBL49216 IC50 = 330.0 nM 6.48
CHEMBL51050 IC50 = 510.0 nM 6.29
CHEMBL300305 IC50 = 600.0 nM 6.22
CHEMBL50790 IC50 = 1300.0 nM 5.89
CHEMBL46780 IC50 = 1500.0 nM 5.82
CHEMBL299743 IC50 = 1600.0 nM 5.80
CHEMBL300937 IC50 = 1800.0 nM 5.75
CHEMBL48882 IC50 = 2400.0 nM 5.62
CHEMBL48517 IC50 = 4000.0 nM 5.40
CHEMBL49181 IC50 = 19000.0 nM 4.72
CHEMBL298578 IC50 = 24000.0 nM 4.62
CHEMBL48717 IC50 > 100000.0 nM -