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Assay Detail

CHEMBL912581

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Binding
Inhibition of MAO-A in bovine brain mitochondria by fluorimetric method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Brain
Subcellular Mitochondria
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Amine oxidase [flavin-containing] A (CHEMBL3254)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Monoamine oxidase isoform-dependent tautomeric influence in the recognition of 3,5-diaryl pyrazole inhibitors.
Chimenti F, Fioravanti R, Bolasco A, Manna F, Chimenti P, Secci D, Befani O, Turini P, Ortuso F, Alcaro S.
J Med Chem (2007) 50 : 425 -428
PubMed 17266193 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.46 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL375966 1 9.00
CHEMBL218323 1 8.69
CHEMBL218324 1 8.52
CHEMBL221593 1 7.85
CHEMBL218059 1 6.52
CHEMBL18116 TOLOXATONE 4.0 1 6.42
CHEMBL424940 1 5.82
CHEMBL375616 1 5.64
CHEMBL221293 1 5.52
CHEMBL385397 1 5.39
CHEMBL221629 1 5.20
CHEMBL86304 MOCLOBEMIDE 4.0 1 4.94
CHEMBL972 SELEGILINE 4.0 1 4.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL375966 IC50 = 1.0 nM 9.00
CHEMBL218323 IC50 = 2.042 nM 8.69
CHEMBL218324 IC50 = 3.02 nM 8.52
CHEMBL221593 IC50 = 14.13 nM 7.85
CHEMBL218059 IC50 = 302.0 nM 6.52
CHEMBL18116 TOLOXATONE IC50 = 380.19 nM 6.42
CHEMBL424940 IC50 = 1513.56 nM 5.82
CHEMBL375616 IC50 = 2290.87 nM 5.64
CHEMBL221293 IC50 = 3019.95 nM 5.52
CHEMBL385397 IC50 = 4073.8 nM 5.39
CHEMBL221629 IC50 = 6309.57 nM 5.20
CHEMBL86304 MOCLOBEMIDE IC50 = 11481.54 nM 4.94
CHEMBL972 SELEGILINE IC50 = 38018.94 nM 4.42