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Assay Detail

CHEMBL1833288

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

ADMET
Inhibition of CYP3A4 in human liver microsomes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 3-(1H-imidazol- and triazol-1-yl)-2,2-dimethyl-3-[4-(naphthalen-2-ylamino)phenyl]propyl derivatives as small molecule inhibitors of retinoic acid 4-hydroxylase (CYP26).
Gomaa MS, Bridgens CE, Veal GJ, Redfern CP, Brancale A, Armstrong JL, Simons C.
J Med Chem (2011) 54 : 6803 -6811
PubMed 21838328 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.47 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1831092 1 6.48
CHEMBL517438 1 6.46
CHEMBL1766005 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1831092 IC50 = 330.0 nM 6.48
CHEMBL517438 IC50 = 350.0 nM 6.46
CHEMBL1766005 IC50 < 100.0 nM -