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Assay Detail

CHEMBL5541708

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

ADMET
Inhibition of CYP3A4/5 in human liver microsomes incubated for 15 mins by LC-MS/MS analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 3A4/3A5 (CHEMBL2111472)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Identification of Piperazinyl-Difluoro-indene Derivatives Containing Pyridyl Groups as Potent FGFR Inhibitors against FGFR Mutant Tumor: Design, Synthesis, and Biological Evaluation.
Ding W, Yan L, Sheng L, Chen S, Li Y, Cheng S, Luo L, Huang H, Shao H, Zhang D.
J Med Chem (2024) 67 : 2941 -2962
PubMed 38294952 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.67 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157101 KETOCONAZOLE 4.0 1 7.70
CHEMBL5570406 1 5.42
CHEMBL5571836 1 4.81
CHEMBL5572540 1 4.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157101 KETOCONAZOLE IC50 = 20.0 nM 7.70
CHEMBL5570406 IC50 = 3800.0 nM 5.42
CHEMBL5571836 IC50 = 15500.0 nM 4.81
CHEMBL5572540 IC50 = 18100.0 nM 4.74