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Assay Detail

CHEMBL5158149

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

ADMET
Inhibition of CYP1A2 in human liver microsomes in presence of NADPH incubated for 3 to 20 mins 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 Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 1A2 (CHEMBL3356)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel Bicyclic Imidazolopyridine-Containing Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Improved Efficacy and Favorable Druggability.
Zhao T, Zhang J, Tao Y, Liao H, Zhao F, Liang R, Shi X, Zhang Z, Ji J, Wu T, Pang J, Liu X, Zhan P.
J Med Chem (2022) 65 : 4218 -4237
PubMed 35084182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.57 6.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 6.37
CHEMBL5199889 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 431.0 nM 6.37
CHEMBL5199889 IC50 = 16970.0 nM 4.77