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Assay Detail

CHEMBL2161497

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

Binding
Inhibition of human recombinant MAOB using kynuramine as substrate assessed as formation of 4-hydroxyquinoline after 20 mins by fluorescence spectrophotometry
12
Total Activities
12
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

Amine oxidase [flavin-containing] B (CHEMBL2039)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel sulfanylphthalimide analogues as highly potent inhibitors of monoamine oxidase B.
Van der Walt MM, Terre'Blanche G, Petzer A, Petzer JP.
Bioorg Med Chem Lett (2012) 22 : 6632 -6635
PubMed 23010267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.40 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2158241 1 8.35
CHEMBL2158242 1 8.25
CHEMBL2158244 1 8.17
CHEMBL2158243 1 8.13
CHEMBL2158251 1 7.82
CHEMBL2158245 1 7.70
CHEMBL2158249 1 7.52
CHEMBL342357 1 7.37
CHEMBL2158250 1 6.75
CHEMBL2158248 1 6.44
CHEMBL2158247 1 6.34
CHEMBL2158246 1 6.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2158241 IC50 = 4.5 nM 8.35
CHEMBL2158242 IC50 = 5.6 nM 8.25
CHEMBL2158244 IC50 = 6.8 nM 8.17
CHEMBL2158243 IC50 = 7.4 nM 8.13
CHEMBL2158251 IC50 = 15.0 nM 7.82
CHEMBL2158245 IC50 = 20.0 nM 7.70
CHEMBL2158249 IC50 = 30.0 nM 7.52
CHEMBL342357 IC50 = 43.0 nM 7.37
CHEMBL2158250 IC50 = 179.0 nM 6.75
CHEMBL2158248 IC50 = 364.0 nM 6.44
CHEMBL2158247 IC50 = 457.0 nM 6.34
CHEMBL2158246 IC50 = 986.0 nM 6.01