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Assay Detail

CHEMBL912582

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Binding
Inhibition of MAO-B in bovine brain mitochondria 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] B (CHEMBL2756)
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 6.80 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL424940 1 9.00
CHEMBL218059 1 8.22
CHEMBL221293 1 8.05
CHEMBL375966 1 8.00
CHEMBL385397 1 7.52
CHEMBL218324 1 7.39
CHEMBL375616 1 7.00
CHEMBL221593 1 6.35
CHEMBL972 SELEGILINE 4.0 1 6.00
CHEMBL218323 1 5.22
CHEMBL18116 TOLOXATONE 4.0 1 4.82
CHEMBL221629 1 4.00
CHEMBL86304 MOCLOBEMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL424940 IC50 = 1.0 nM 9.00
CHEMBL218059 IC50 = 6.026 nM 8.22
CHEMBL221293 IC50 = 8.913 nM 8.05
CHEMBL375966 IC50 = 10.0 nM 8.00
CHEMBL385397 IC50 = 30.2 nM 7.52
CHEMBL218324 IC50 = 40.74 nM 7.39
CHEMBL375616 IC50 = 100.0 nM 7.00
CHEMBL221593 IC50 = 446.68 nM 6.35
CHEMBL972 SELEGILINE IC50 = 1000.0 nM 6.00
CHEMBL218323 IC50 = 6025.6 nM 5.22
CHEMBL18116 TOLOXATONE IC50 = 15135.61 nM 4.82
CHEMBL221629 IC50 = 100000.0 nM 4.00
CHEMBL86304 MOCLOBEMIDE IC50 = 10000000.0 nM -