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Assay Detail

CHEMBL964393

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

ADMET
Inhibition of CYP2C9
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Cytochrome P450 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]pyridine acid pump antagonists (APAs).
Bailey N, Bamford MJ, Brissy D, Brookfield J, Demont E, Elliott R, Garton N, Farre-Gutierrez I, Hayhow T, Hutley G, Naylor A, Panchal TA, Seow HX, Spalding D, Takle AK.
Bioorg Med Chem Lett (2009) 19 : 3602 -3606
PubMed 19467868 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.24 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL447822 1 6.20
CHEMBL453246 1 6.07
CHEMBL526841 1 5.96
CHEMBL523752 1 5.82
CHEMBL496606 1 5.60
CHEMBL521724 1 5.60
CHEMBL498026 1 5.54
CHEMBL496426 1 5.50
CHEMBL496624 1 5.50
CHEMBL496806 1 5.47
CHEMBL238146 1 5.44
CHEMBL498220 1 5.43
CHEMBL498114 1 5.38
CHEMBL496387 1 5.38
CHEMBL510171 1 5.34
CHEMBL523563 1 5.33
CHEMBL498251 1 5.28
CHEMBL497419 1 5.25
CHEMBL525001 1 5.25
CHEMBL521889 1 5.24
CHEMBL496035 1 5.19
CHEMBL496227 1 5.07
CHEMBL495787 1 5.00
CHEMBL497418 1 4.89
CHEMBL497011 LINAPRAZAN 2.0 1 4.85
CHEMBL496400 1 4.85
CHEMBL498252 1 4.85
CHEMBL495786 1 4.77
CHEMBL496605 1 4.77
CHEMBL496386 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL447822 IC50 = 630.0 nM 6.20
CHEMBL453246 IC50 = 860.0 nM 6.07
CHEMBL526841 IC50 = 1100.0 nM 5.96
CHEMBL523752 IC50 = 1500.0 nM 5.82
CHEMBL496606 IC50 = 2500.0 nM 5.60
CHEMBL521724 IC50 = 2500.0 nM 5.60
CHEMBL498026 IC50 = 2900.0 nM 5.54
CHEMBL496426 IC50 = 3200.0 nM 5.50
CHEMBL496624 IC50 = 3200.0 nM 5.50
CHEMBL496806 IC50 = 3400.0 nM 5.47
CHEMBL238146 IC50 = 3600.0 nM 5.44
CHEMBL498220 IC50 = 3700.0 nM 5.43
CHEMBL498114 IC50 = 4200.0 nM 5.38
CHEMBL496387 IC50 = 4200.0 nM 5.38
CHEMBL510171 IC50 = 4600.0 nM 5.34
CHEMBL523563 IC50 = 4700.0 nM 5.33
CHEMBL498251 IC50 = 5300.0 nM 5.28
CHEMBL497419 IC50 = 5600.0 nM 5.25
CHEMBL525001 IC50 = 5600.0 nM 5.25
CHEMBL521889 IC50 = 5800.0 nM 5.24
CHEMBL496035 IC50 = 6500.0 nM 5.19
CHEMBL496227 IC50 = 8600.0 nM 5.07
CHEMBL495787 IC50 = 10000.0 nM 5.00
CHEMBL497418 IC50 = 13000.0 nM 4.89
CHEMBL498252 IC50 = 14000.0 nM 4.85
CHEMBL496400 IC50 = 14000.0 nM 4.85
CHEMBL497011 LINAPRAZAN IC50 = 14000.0 nM 4.85
CHEMBL495786 IC50 = 17000.0 nM 4.77
CHEMBL496605 IC50 = 17000.0 nM 4.77
CHEMBL496386 IC50 = 19000.0 nM 4.72
CHEMBL498434 IC50 = 21000.0 nM 4.68
CHEMBL496402 IC50 = 23000.0 nM 4.64
CHEMBL498840 IC50 = 97000.0 nM 4.01
CHEMBL495999 IC50 - -
CHEMBL496204 IC50 - -