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Assay Detail

CHEMBL3807136

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

Binding
Inhibition of human recombinant DAAO using D-alanine as substrate assessed as pyruvate production incubated for 60 mins by microplate reader analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

D-amino-acid oxidase (CHEMBL5485)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and analgesic evaluation of 8-chloro-1,4-dihydropyrido[2,3-b]pyrazine-2,3-dione as a novel potent d-amino acid oxidase inhibitor.
Xie D, Lu J, Xie J, Cui J, Li TF, Wang YC, Chen Y, Gong N, Li XY, Fu L, Wang YX.
Eur J Med Chem (2016) 117 : 19 -32
PubMed 27089209 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.56 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL146227 1 7.37
CHEMBL445990 1 6.96
CHEMBL3804851 1 6.68
CHEMBL3804953 1 6.64
CHEMBL3805642 1 6.47
CHEMBL92084 1 5.95
CHEMBL3805223 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL146227 IC50 = 43.0 nM 7.37
CHEMBL445990 IC50 = 110.0 nM 6.96
CHEMBL3804851 IC50 = 210.0 nM 6.68
CHEMBL3804953 IC50 = 230.0 nM 6.64
CHEMBL3805642 IC50 = 340.0 nM 6.47
CHEMBL92084 IC50 = 1130.0 nM 5.95
CHEMBL3805223 IC50 = 1380.0 nM 5.86