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Assay Detail

CHEMBL3375452

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

ADMET
Inhibition of human CYP3A4 testosterone site in human liver microsomes using midazolam as substrate 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 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Halland N, Schmidt F, Weiss T, Saas J, Li Z, Czech J, Dreyer M, Hofmeister A, Mertsch K, Dietz U, Strübing C, Nazare M.
ACS Med Chem Lett (2015) 6 : 73 -78
PubMed 25589934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 4.70 4.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092460 1 4.84
CHEMBL3092467 1 4.73
CHEMBL3092468 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092460 IC50 = 14500.0 nM 4.84
CHEMBL3092467 IC50 = 18600.0 nM 4.73
CHEMBL3092468 IC50 = 28600.0 nM 4.54