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Assay Detail

CHEMBL4841645

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

ADMET
Inhibition of CYP3A4M in human liver microsomes using midazolam as substrate incubated for 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

Discovery of 1-Amino-1<i>H</i>-imidazole-5-carboxamide Derivatives as Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitors.
Ma C, Li Q, Zhao M, Fan G, Zhao J, Zhang D, Yang S, Zhang S, Gao D, Mao L, Zhu L, Li W, Xu G, Jiang Y, Ding Q.
J Med Chem (2021) 64 : 16242 -16270
PubMed 34672559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.15 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157101 KETOCONAZOLE 4.0 1 8.15
CHEMBL4864983 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157101 KETOCONAZOLE IC50 = 7.0 nM 8.15
CHEMBL4864983 IC50 > 10000.0 nM -