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Assay Detail

CHEMBL3385921

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

Functional
Anticoagulant activity in recombinant tissue factor and procoagulant phospholipids-stimulated human citrated plasma assessed as inhibition of thrombin peak by fluorometry based calibrated automated thrombography
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
Confidence 1 — Organism
Curated By Autocuration

Target

Plasma (CHEMBL613424)
Type TISSUE
Organism Homo sapiens

Publication

How a β-D-glucoside side chain enhances binding affinity to thrombin of inhibitors bearing 2-chlorothiophene as P1 moiety: crystallography, fragment deconstruction study, and evaluation of antithrombotic properties.
Belviso BD, Caliandro R, de Candia M, Zaetta G, Lopopolo G, Incampo F, Colucci M, Altomare CD.
J Med Chem (2014) 57 : 8563 -8575
PubMed 25268757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.79 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3343301 1 6.52
CHEMBL3343300 1 5.92
CHEMBL1166 ARGATROBAN 4.0 1 5.72
CHEMBL3343299 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3343301 IC50 = 300.0 nM 6.52
CHEMBL3343300 IC50 = 1200.0 nM 5.92
CHEMBL1166 ARGATROBAN IC50 = 1900.0 nM 5.72
CHEMBL3343299 IC50 = 10000.0 nM 5.00