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Assay Detail

CHEMBL1177229

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

ADMET
Inhibition of human recombinant CYP24A1 expressed in chinese hamster V79 cells using [3H-1-beta]calcitriol after 60 mins by scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type V79
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides.
Aboraia AS, Yee SW, Gomaa MS, Shah N, Robotham AC, Makowski B, Prosser D, Brancale A, Jones G, Simons C.
Bioorg Med Chem (2010) 18 : 4939 -4946
PubMed 20594862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.24 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171494 1 6.52
CHEMBL157101 KETOCONAZOLE 4.0 1 6.28
CHEMBL1171662 1 5.55
CHEMBL1171489 1 5.40
CHEMBL1171660 1 5.19
CHEMBL1171105 1 4.97
CHEMBL1171106 1 4.64
CHEMBL1171659 1 4.43
CHEMBL1171107 1 4.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171494 IC50 = 300.0 nM 6.52
CHEMBL157101 KETOCONAZOLE IC50 = 520.0 nM 6.28
CHEMBL1171662 IC50 = 2800.0 nM 5.55
CHEMBL1171489 IC50 = 4000.0 nM 5.40
CHEMBL1171660 IC50 = 6400.0 nM 5.19
CHEMBL1171105 IC50 = 10600.0 nM 4.97
CHEMBL1171106 IC50 = 23000.0 nM 4.64
CHEMBL1171659 IC50 = 36900.0 nM 4.43
CHEMBL1171107 IC50 = 72000.0 nM 4.14