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Assay Detail

CHEMBL923682

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

Binding
Inhibition of human factor 10a
21
Total Activities
20
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 piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.
Imaeda Y, Kawamoto T, Tobisu M, Konishi N, Hiroe K, Kawamura M, Tanaka T, Kubo K.
Bioorg Med Chem (2008) 16 : 3125 -3140
PubMed 18164204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.41 8.05
Ki 1 8.10 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259603 2 8.10
CHEMBL405361 1 7.92
CHEMBL260152 1 7.75
CHEMBL409115 1 7.75
CHEMBL265456 1 7.70
CHEMBL409851 1 7.68
CHEMBL410528 1 7.66
CHEMBL258716 1 7.62
CHEMBL261775 1 7.62
CHEMBL261774 1 7.54
CHEMBL409850 1 7.46
CHEMBL261323 1 7.39
CHEMBL261324 1 7.35
CHEMBL265455 1 7.24
CHEMBL261646 1 7.21
CHEMBL259663 1 7.11
CHEMBL261524 1 7.06
CHEMBL260360 1 7.03
CHEMBL19902 DX-9065A 1 6.89
CHEMBL428081 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259603 Ki = 8.0 nM 8.10
CHEMBL259603 IC50 = 9.0 nM 8.05
CHEMBL405361 IC50 = 12.0 nM 7.92
CHEMBL260152 IC50 = 18.0 nM 7.75
CHEMBL409115 IC50 = 18.0 nM 7.75
CHEMBL265456 IC50 = 20.0 nM 7.70
CHEMBL409851 IC50 = 21.0 nM 7.68
CHEMBL410528 IC50 = 22.0 nM 7.66
CHEMBL258716 IC50 = 24.0 nM 7.62
CHEMBL261775 IC50 = 24.0 nM 7.62
CHEMBL261774 IC50 = 29.0 nM 7.54
CHEMBL409850 IC50 = 35.0 nM 7.46
CHEMBL261323 IC50 = 41.0 nM 7.39
CHEMBL261324 IC50 = 45.0 nM 7.35
CHEMBL265455 IC50 = 57.0 nM 7.24
CHEMBL261646 IC50 = 61.0 nM 7.21
CHEMBL259663 IC50 = 78.0 nM 7.11
CHEMBL261524 IC50 = 87.0 nM 7.06
CHEMBL260360 IC50 = 93.0 nM 7.03
CHEMBL19902 DX-9065A IC50 = 130.0 nM 6.89
CHEMBL428081 IC50 = 840.0 nM 6.08