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Assay Detail

CHEMBL3367715

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ADMET
Inhibition of CYP2D6 in supersomes (unknown origin) using AMMC as substrate after 30 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2D6 (CHEMBL289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides.
Laufer R, Ng G, Liu Y, Patel NK, Edwards LG, Lang Y, Li SW, Feher M, Awrey DE, Leung G, Beletskaya I, Plotnikova O, Mason JM, Hodgson R, Wei X, Mao G, Luo X, Huang P, Green E, Kiarash R, Lin DC, Harris-Brandts M, Ban F, Nadeem V, Mak TW, Pan GJ, Qiu W, Chirgadze NY, Pauls HW.
Bioorg Med Chem (2014) 22 : 4968 -4997
PubMed 25043312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.15 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3330409 1 5.30
CHEMBL3330410 1 5.00
CHEMBL3330260 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3330409 IC50 = 5000.0 nM 5.30
CHEMBL3330410 IC50 = 10000.0 nM 5.00
CHEMBL3330260 IC50 > 10000.0 nM -