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Assay Detail

CHEMBL5541704

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

ADMET
Inhibition of CYP1A2 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 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 1A2 (CHEMBL3356)
Type SINGLE PROTEIN
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 5.66 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26260 BETA-NAPHTHOFLAVONE 1 6.89
CHEMBL5570406 1 4.42
CHEMBL5571836 1 -
CHEMBL5572540 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26260 BETA-NAPHTHOFLAVONE IC50 = 130.0 nM 6.89
CHEMBL5570406 IC50 = 38400.0 nM 4.42
CHEMBL5571836 IC50 > 50000.0 nM -
CHEMBL5572540 IC50 > 50000.0 nM -