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Assay Detail

CHEMBL4052353

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ADMET
Inhibition of CYP2C9 human liver microsomes after 10 mins by LC-MS/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 2C9 (CHEMBL3397)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2).
Rowbottom MW, Bain G, Calderon I, Lasof T, Lonergan D, Lai A, Huang F, Darlington J, Prodanovich P, Santini AM, King CD, Goulet L, Shannon KE, Ma GL, Nguyen K, MacKenna DA, Evans JF, Hutchinson JH.
J Med Chem (2017) 60 : 4403 -4423
PubMed 28471663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.77 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4063337 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4063337 IC50 = 1700.0 nM 5.77