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Assay Detail

CHEMBL4373233

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

ADMET
Inhibition of CYP2C8 in human liver microsomes
15
Total Activities
15
Compounds Tested
2
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

Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.
Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C.
J Med Chem (2019) 62 : 831 -856
PubMed 30576602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 13 - -
IC50 2 6.00 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4279180 1 6.00
CHEMBL4550045 1 6.00
CHEMBL4570932 1 -
CHEMBL4466131 1 -
CHEMBL4527346 1 -
CHEMBL4292013 1 -
CHEMBL4290933 1 -
CHEMBL4276864 1 -
CHEMBL4283748 1 -
CHEMBL4475017 1 -
CHEMBL4447807 1 -
CHEMBL4287506 1 -
CHEMBL4524193 1 -
CHEMBL4280298 1 -
CHEMBL4460464 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4279180 IC50 = 1000.0 nM 6.00
CHEMBL4550045 IC50 = 1000.0 nM 6.00
CHEMBL4570932 Inhibition - % -
CHEMBL4466131 Inhibition - % -
CHEMBL4527346 Inhibition - % -
CHEMBL4292013 Inhibition - % -
CHEMBL4290933 Inhibition - % -
CHEMBL4276864 Inhibition - % -
CHEMBL4283748 Inhibition - % -
CHEMBL4475017 Inhibition - % -
CHEMBL4447807 Inhibition - % -
CHEMBL4287506 Inhibition - % -
CHEMBL4524193 Inhibition - % -
CHEMBL4280298 Inhibition - % -
CHEMBL4460464 Inhibition - % -