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Assay Detail

CHEMBL2424091

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

Binding
Inhibition of plasma clot-bound thrombin (unknown origin) using S2238 as substrate
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.
Park HD, Lee SH, Kim TH, Lee SH, Cho KH, Kim A.
Bioorg Med Chem Lett (2013) 23 : 4779 -4784
PubMed 23899618 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.47 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2419745 1 8.30
CHEMBL266349 MELAGATRAN 4.0 1 7.07
CHEMBL1166 ARGATROBAN 4.0 1 7.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2419745 IC50 = 5.0 nM 8.30
CHEMBL266349 MELAGATRAN IC50 = 85.2 nM 7.07
CHEMBL1166 ARGATROBAN IC50 = 92.4 nM 7.03