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Assay Detail

CHEMBL4415872

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

ADMET
Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysis
3
Total Activities
3
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 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na<sub>V</sub>1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy.
Focken T, Burford K, Grimwood ME, Zenova A, Andrez JC, Gong W, Wilson M, Taron M, Decker S, Lofstrand V, Chowdhury S, Shuart N, Lin S, Goodchild SJ, Young C, Soriano M, Tari PK, Waldbrook M, Nelkenbrecher K, Kwan R, Lindgren A, de Boer G, Lee S, Sojo L, DeVita RJ, Cohen CJ, Wesolowski SS, Johnson JP, Dehnhardt CM, Empfield JR.
J Med Chem (2019) 62 : 9618 -9641
PubMed 31525968 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.39 4.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471825 1 4.57
CHEMBL4460028 1 4.30
CHEMBL4435054 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471825 IC50 = 27000.0 nM 4.57
CHEMBL4460028 IC50 = 50000.0 nM 4.30
CHEMBL4435054 IC50 = 50000.0 nM 4.30