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Assay Detail

CHEMBL4839400

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

ADMET
Competitive inhibition of CYP3A4 in human liver microsomes using midazolam as substrate by LC-MS/MS 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 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

BAY-8400: A Novel Potent and Selective DNA-PK Inhibitor which Shows Synergistic Efficacy in Combination with Targeted Alpha Therapies.
Berger M, Wortmann L, Buchgraber P, Lücking U, Zitzmann-Kolbe S, Wengner AM, Bader B, Bömer U, Briem H, Eis K, Rehwinkel H, Bartels F, Moosmayer D, Eberspächer U, Lienau P, Hammer S, Schatz CA, Wang Q, Wang Q, Mumberg D, Nising CF, Siemeister G.
J Med Chem (2021) 64 : 12723 -12737
PubMed 34428039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.82 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4851439 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4851439 IC50 = 15000.0 nM 4.82