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Assay Detail

CHEMBL4196336

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

Binding
Inhibition of human thrombin using tosyl-glycyl-prolyl-arginine-4-nitranilide acetate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.
Xie Z, Tian Y, Lv X, Xiao X, Zhan M, Cheng K, Li S, Liao C.
Eur J Med Chem (2018) 146 : 299 -317
PubMed 29407959 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.53 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48635 1 8.27
CHEMBL48361 DABIGATRAN 3.0 1 8.03
CHEMBL298500 1 7.96
CHEMBL417360 1 7.50
CHEMBL51528 1 7.24
CHEMBL23430 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48635 IC50 = 5.4 nM 8.27
CHEMBL48361 DABIGATRAN IC50 = 9.3 nM 8.03
CHEMBL298500 IC50 = 11.0 nM 7.96
CHEMBL417360 IC50 = 32.0 nM 7.50
CHEMBL51528 IC50 = 58.0 nM 7.24
CHEMBL23430 IC50 = 690.0 nM 6.16