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Assay Detail

CHEMBL660487

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

Binding
Inhibition of Coagulation factor II
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Prothrombin (CHEMBL204)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.
Dominguez C, Duffy DE, Han Q, Alexander RS, Galemmo RA, Park JM, Wong PC, Amparo EC, Knabb RM, Luettgen J, Wexler RR.
Bioorg Med Chem Lett (1999) 9 : 925 -930
PubMed 10230612 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.72 10.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL290376 1 10.38
CHEMBL175398 1 8.15
CHEMBL422722 1 8.13
CHEMBL174456 1 7.75
CHEMBL366643 1 7.72
CHEMBL367626 1 7.62
CHEMBL170063 1 7.62
CHEMBL174008 1 7.55
CHEMBL173612 1 6.85
CHEMBL171390 1 6.68
CHEMBL368131 1 6.52
CHEMBL173765 1 -
CHEMBL177038 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL290376 Ki = 0.042 nM 10.38
CHEMBL175398 Ki = 7.0 nM 8.15
CHEMBL422722 Ki = 7.4 nM 8.13
CHEMBL174456 Ki = 18.0 nM 7.75
CHEMBL366643 Ki = 19.0 nM 7.72
CHEMBL367626 Ki = 24.0 nM 7.62
CHEMBL170063 Ki = 24.0 nM 7.62
CHEMBL174008 Ki = 28.0 nM 7.55
CHEMBL173612 Ki = 140.0 nM 6.85
CHEMBL171390 Ki = 210.0 nM 6.68
CHEMBL368131 Ki = 300.0 nM 6.52
CHEMBL173765 Ki > 21000.0 nM -
CHEMBL177038 Ki > 21000.0 nM -