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Assay Detail

CHEMBL4052345

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

Binding
Inhibition of recombinant mouse LOXL2 expressed in mouse whole blood assessed as reduction of H2O2 production from oxidative deamination of DAP preincubated for 2 hrs followed by substrate addition measured every 2 mins for 1 hr by amplex red reagent-based fluorescence assay
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Lysyl oxidase homolog 2 (CHEMBL4105831)
Type SINGLE PROTEIN
Organism Mus musculus

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 2 6.54 7.00
IC90 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4063337 1 7.00
CHEMBL4079398 2 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4063337 IC50 = 100.0 nM 7.00
CHEMBL4079398 IC50 = 860.0 nM 6.07
CHEMBL4079398 IC90 = 5600.0 nM -