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Assay Detail

CHEMBL1072755

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

Binding
Inhibition of human factor 10a
14
Total Activities
14
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

Coagulation factor X (CHEMBL244)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenyltriazolinones as potent factor Xa inhibitors.
Quan ML, Pinto DJ, Rossi KA, Sheriff S, Alexander RS, Amparo E, Kish K, Knabb RM, Luettgen JM, Morin P, Smallwood A, Woerner FJ, Wexler RR.
Bioorg Med Chem Lett (2010) 20 : 1373 -1377
PubMed 20100660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.90 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231779 APIXABAN 4.0 1 10.10
CHEMBL176140 1 9.82
CHEMBL206335 RAZAXABAN 2.0 1 9.72
CHEMBL579107 1 9.60
CHEMBL578098 1 9.40
CHEMBL591955 1 9.30
CHEMBL577677 1 9.08
CHEMBL592401 1 8.96
CHEMBL592400 1 8.70
CHEMBL578474 1 8.66
CHEMBL578906 1 8.09
CHEMBL601216 1 8.05
CHEMBL591726 1 7.82
CHEMBL592159 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231779 APIXABAN Ki = 0.08 nM 10.10
CHEMBL176140 Ki = 0.15 nM 9.82
CHEMBL206335 RAZAXABAN Ki = 0.19 nM 9.72
CHEMBL579107 Ki = 0.25 nM 9.60
CHEMBL578098 Ki = 0.4 nM 9.40
CHEMBL591955 Ki = 0.5 nM 9.30
CHEMBL577677 Ki = 0.84 nM 9.08
CHEMBL592401 Ki = 1.1 nM 8.96
CHEMBL592400 Ki = 2.0 nM 8.70
CHEMBL578474 Ki = 2.2 nM 8.66
CHEMBL578906 Ki = 8.1 nM 8.09
CHEMBL601216 Ki = 9.0 nM 8.05
CHEMBL591726 Ki = 15.0 nM 7.82
CHEMBL592159 Ki = 46.0 nM 7.34