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Assay Detail

CHEMBL931789

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

Binding
Inhibition of human factor 10a
28
Total Activities
27
Compounds Tested
2
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

Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.
Imaeda Y, Miyawaki T, Sakamoto H, Itoh F, Konishi N, Hiroe K, Kawamura M, Tanaka T, Kubo K.
Bioorg Med Chem (2008) 16 : 2243 -2260
PubMed 18077174 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.92 7.48
Ki 1 7.82 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261646 2 7.82
CHEMBL270527 1 7.48
CHEMBL401529 1 7.43
CHEMBL271991 1 7.30
CHEMBL429249 1 7.27
CHEMBL271366 1 7.22
CHEMBL272783 1 7.20
CHEMBL272042 1 7.19
CHEMBL411027 1 7.10
CHEMBL405898 1 7.07
CHEMBL273112 1 7.02
CHEMBL429936 1 7.02
CHEMBL271944 1 6.96
CHEMBL271132 1 6.92
CHEMBL407407 1 6.92
CHEMBL19902 DX-9065A 1 6.89
CHEMBL270941 1 6.85
CHEMBL271604 1 6.80
CHEMBL272392 1 6.60
CHEMBL270323 1 6.33
CHEMBL270526 1 6.14
CHEMBL271784 1 6.14
CHEMBL412049 1 6.08
CHEMBL272570 1 -
CHEMBL409521 1 -
CHEMBL270324 1 -
CHEMBL272654 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261646 Ki = 15.0 nM 7.82
CHEMBL270527 IC50 = 33.0 nM 7.48
CHEMBL401529 IC50 = 37.0 nM 7.43
CHEMBL271991 IC50 = 50.0 nM 7.30
CHEMBL429249 IC50 = 54.0 nM 7.27
CHEMBL271366 IC50 = 60.0 nM 7.22
CHEMBL261646 IC50 = 61.0 nM 7.21
CHEMBL272783 IC50 = 63.0 nM 7.20
CHEMBL272042 IC50 = 64.0 nM 7.19
CHEMBL411027 IC50 = 79.0 nM 7.10
CHEMBL405898 IC50 = 85.0 nM 7.07
CHEMBL273112 IC50 = 95.0 nM 7.02
CHEMBL429936 IC50 = 95.0 nM 7.02
CHEMBL271944 IC50 = 110.0 nM 6.96
CHEMBL271132 IC50 = 120.0 nM 6.92
CHEMBL407407 IC50 = 120.0 nM 6.92
CHEMBL19902 DX-9065A IC50 = 130.0 nM 6.89
CHEMBL270941 IC50 = 140.0 nM 6.85
CHEMBL271604 IC50 = 160.0 nM 6.80
CHEMBL272392 IC50 = 250.0 nM 6.60
CHEMBL270323 IC50 = 470.0 nM 6.33
CHEMBL270526 IC50 = 720.0 nM 6.14
CHEMBL271784 IC50 = 720.0 nM 6.14
CHEMBL412049 IC50 = 840.0 nM 6.08
CHEMBL270324 IC50 > 5000.0 nM -
CHEMBL409521 IC50 > 5000.0 nM -
CHEMBL272654 IC50 > 5000.0 nM -
CHEMBL272570 IC50 > 5000.0 nM -