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Assay Detail

CHEMBL808335

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Binding
Inhibitory activity against Thrombin
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex.
South MS, Case BL, Wood RS, Jones DE, Hayes MJ, Girard TJ, Lachance RM, Nicholson NS, Clare M, Stevens AM, Stegeman RA, Stallings WC, Kurumbail RG, Parlow JJ.
Bioorg Med Chem Lett (2003) 13 : 2319 -2325
PubMed 12824026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.29 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308948 1 6.96
CHEMBL75084 1 6.82
CHEMBL77490 1 5.10
CHEMBL77076 1 -
CHEMBL77982 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308948 IC50 = 110.0 nM 6.96
CHEMBL75084 IC50 = 150.0 nM 6.82
CHEMBL77490 IC50 = 8000.0 nM 5.10
CHEMBL77076 IC50 > 100000.0 nM -
CHEMBL77982 IC50 < 40.0 nM -