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Assay Detail

CHEMBL4333063

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

ADMET
Inhibition of CYP3A in human liver microsomes assessed as reduction in midazolam 1'-hydroxylation by tandem mass spectrometry analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Tissue Liver
Subcellular Microsomes
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Cytochrome P450 3A (CHEMBL2364675)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.
Lee D, Pagire HS, Pagire SH, Bae EJ, Dighe M, Kim M, Lee KM, Jang YK, Jaladi AK, Jung KY, Yoo EK, Gim HE, Lee S, Choi WI, Chi YI, Song JS, Bae MA, Jeon YH, Lee GH, Liu KH, Lee T, Park S, Jeon JH, Lee IK, Ahn JH.
J Med Chem (2019) 62 : 575 -588
PubMed 30623649 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.44 4.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471264 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471264 IC50 = 36600.0 nM 4.44