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Assay Detail

CHEMBL4027673

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 upto 10 uM after 20 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 2C8 (CHEMBL3721)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity.
Li B, Ni S, Mao F, Chen F, Liu Y, Wei H, Chen W, Zhu J, Lan L, Li J.
J Med Chem (2018) 61 : 224 -250
PubMed 29243920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.50 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL787 MONTELUKAST 4.0 1 6.00
CHEMBL4086008 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL787 MONTELUKAST IC50 = 1000.0 nM 6.00
CHEMBL4086008 IC50 = 10000.0 nM 5.00