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Assay Detail

CHEMBL816475

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Binding
In vitro inhibitory activity against thrombin
3
Total Activities
3
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

D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety.
Lange UE, Baucke D, Hornberger W, Mack H, Seitz W, Höffken HW.
Bioorg Med Chem Lett (2003) 13 : 2029 -2033
PubMed 12781189 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.78 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3215729 1 8.21
CHEMBL543817 1 7.96
CHEMBL266349 MELAGATRAN 4.0 1 7.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3215729 IC50 = 6.2 nM 8.21
CHEMBL543817 IC50 = 11.0 nM 7.96
CHEMBL266349 MELAGATRAN IC50 = 69.2 nM 7.16