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Assay Detail

CHEMBL4843282

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

ADMET
Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate incubated for 10 mins in presence of NADPH by LCMS/MS analysis
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 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.
Hamilton MM, Mseeh F, McAfoos TJ, Leonard PG, Reyna NJ, Harris AL, Xu A, Han M, Soth MJ, Czako B, Theroff JP, Mandal PK, Burke JP, Virgin-Downey B, Petrocchi A, Pfaffinger D, Rogers NE, Parker CA, Yu SS, Jiang Y, Krapp S, Lammens A, Trevitt G, Tremblay MR, Mikule K, Wilcoxen K, Cross JB, Jones P, Marszalek JR, Lewis RT.
J Med Chem (2021) 64 : 11302 -11329
PubMed 34292726 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.70 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4848055 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4848055 IC50 = 200.0 nM 6.70