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Assay Detail

CHEMBL4701734

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

ADMET
Time-dependent inhibition of CYP3A4 in human liver microsomes assessed as inhibition constant by Kitz-Wilson plot 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 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.
Zhang Y,Boy KM,Wu YJ,Ramirez A,Toyn JH,Ahlijanian MK,Albright CF,Zhuo X,Johnson BM,Denton RR,Olson RE,Thompson LA,Macor JE
Bioorg Med Chem Lett (2020) 30 : 127530 -127530
PubMed 32890687 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 4.08 4.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209316 1 4.08
CHEMBL4793756 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209316 Ki = 82500.0 nM 4.08
CHEMBL4793756 Ki = 82500.0 nM 4.08