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Assay Detail

CHEMBL4196310

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

Binding
Inhibition of human thrombin using H-D-phenylalanyl-L-pipecolyl-L-arginine-p-nitroaniline dihydrochloride as substrate after 60 mins
8
Total Activities
8
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 8 5.41 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL75084 1 6.80
CHEMBL125781 1 6.02
CHEMBL133623 1 5.12
CHEMBL77490 1 5.10
CHEMBL4202662 1 4.00
CHEMBL77076 1 -
CHEMBL4215577 1 -
CHEMBL142205 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL75084 IC50 = 160.0 nM 6.80
CHEMBL125781 IC50 = 950.0 nM 6.02
CHEMBL133623 IC50 = 7630.0 nM 5.12
CHEMBL77490 IC50 = 8000.0 nM 5.10
CHEMBL4202662 IC50 = 100000.0 nM 4.00
CHEMBL77076 IC50 > 100000.0 nM -
CHEMBL4215577 IC50 > 30000.0 nM -
CHEMBL142205 IC50 > 30000.0 nM -