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Assay Detail

CHEMBL816074

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Binding
Inhibitory activity against thrombin induced platelet aggregation
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

Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.
Costanzo MJ, Maryanoff BE, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Kauffman JA, Lewis JM, Krishnan R, Tulinsky A.
J Med Chem (1996) 39 : 3039 -3043
PubMed 8759623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.52 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273196 EFEGATRAN 2.0 1 7.64
CHEMBL270437 1 7.64
CHEMBL1166 ARGATROBAN 4.0 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273196 EFEGATRAN IC50 = 23.0 nM 7.64
CHEMBL270437 IC50 = 23.0 nM 7.64
CHEMBL1166 ARGATROBAN IC50 = 52.0 nM 7.28