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Assay Detail

CHEMBL4422960

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

ADMET
Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 30 mins followed by substrate addition measured after 10 mins in presence of NADPH by LC-MS/MS analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel non-xanthine antagonist of the A<sub>2B</sub> adenosine receptor: From HTS hit to lead structure.
Härter M, Kalthof B, Delbeck M, Lustig K, Gerisch M, Schulz S, Kast R, Meibom D, Lindner N.
Eur J Med Chem (2019) 163 : 763 -778
PubMed 30576906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.80 4.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451942 1 4.80
CHEMBL4522981 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451942 IC50 = 16000.0 nM 4.80
CHEMBL4522981 IC50 > 20000.0 nM -