Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5100458

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

ADMET
Inhibition of CYP3A4 in human liver Microsome using midazolam as substrate in presence of NADPH by LC-MS/MS analysis
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

Structure-Activity Studies of 1<i>H</i>-Imidazo[4,5-<i>c</i>]quinolin-4-amine Derivatives as A<sub>3</sub> Adenosine Receptor Positive Allosteric Modulators.
Fallot LB, Suresh RR, Fisher CL, Salmaso V, O'Connor RD, Kaufman N, Gao ZG, Auchampach JA, Jacobson KA.
J Med Chem (2022) 65 : 15238 -15262
PubMed 36367749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.61 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL91 MICONAZOLE 4.0 1 9.00
CHEMBL5170790 1 4.21
CHEMBL5190388 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL91 MICONAZOLE IC50 = 1.0 nM 9.00
CHEMBL5170790 IC50 = 61600.0 nM 4.21
CHEMBL5190388 IC50 > 30000.0 nM -