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Assay Detail

CHEMBL3396934

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

ADMET
Reversible inhibition of CYP3A4 in human liver microsomes using midazolam as substrate
10
Total Activities
10
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

Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.
Zak M, Liederer BM, Sampath D, Yuen PW, Bair KW, Baumeister T, Buckmelter AJ, Clodfelter KH, Cheng E, Crocker L, Fu B, Han B, Li G, Ho YC, Lin J, Liu X, Ly J, O'Brien T, Reynolds DJ, Skelton N, Smith CC, Tay S, Wang W, Wang Z, Xiao Y, Zhang L, Zhao G, Zheng X, Dragovich PS.
Bioorg Med Chem Lett (2015) 25 : 529 -541
PubMed 25556090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.24 5.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3394730 1 5.24
CHEMBL3394719 1 -
CHEMBL3394721 1 -
CHEMBL3394722 1 -
CHEMBL3394724 1 -
CHEMBL3394729 1 -
CHEMBL3394734 1 -
CHEMBL3394736 1 -
CHEMBL3394738 1 -
CHEMBL3394741 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3394730 IC50 = 5700.0 nM 5.24
CHEMBL3394719 IC50 > 10000.0 nM -
CHEMBL3394721 IC50 > 10000.0 nM -
CHEMBL3394722 IC50 > 10000.0 nM -
CHEMBL3394724 IC50 > 10000.0 nM -
CHEMBL3394729 IC50 > 10000.0 nM -
CHEMBL3394734 IC50 > 10000.0 nM -
CHEMBL3394736 IC50 > 10000.0 nM -
CHEMBL3394738 IC50 > 10000.0 nM -
CHEMBL3394741 IC50 > 10000.0 nM -