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Assay Detail

CHEMBL5582355

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

ADMET
Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate preincubated for 5 mins followed by NADPH addition and measured after 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 2C8 (CHEMBL3721)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Evaluation of 3-Phenyloxetane Derivative Agonists of the Glucagon-Like Peptide-1 Receptor.
Zhang Z, Pan H, Guo L, Cai C, Chen T, Zhang Z, Yang X, Zheng H, Jiang C, Wang Z, Yang Y, Wang Z, Zhang X, Zhang Y, Liu D.
J Med Chem (2024) 67 : 14820 -14839
PubMed 39140772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.28 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5590455 1 6.66
CHEMBL4518483 DANUGLIPRON 2.0 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5590455 IC50 = 220.0 nM 6.66
CHEMBL4518483 DANUGLIPRON IC50 = 1250.0 nM 5.90