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Assay Detail

CHEMBL4700815

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
1
Total Activities
1
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 and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.
Boy KM,Guernon JM,Zuev DS,Xu L,Zhang Y,Shi J,Marcin LR,Higgins MA,Wu YJ,Krishnananthan S,Li J,Trehan A,Smith D,Toyn JH,Meredith JE,Burton CR,Kimura SR,Zvyaga T,Zhuo X,Lentz KA,Grace JE,Denton R,Morrison JS,Mathur A,Albright CF,Ahlijanian MK,Olson RE,Thompson LA,Macor JE
ACS Med Chem Lett (2019) 10 : 312 -317
PubMed 30891132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 4.08 4.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209316 1 4.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209316 Ki = 83000.0 nM 4.08