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Assay Detail

CHEMBL4354288

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

Binding
Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method
33
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BTI-TN-5B1-4
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Carboxamides vs. methanimines: Crystal structures, binding interactions, photophysical studies, and biological evaluation of (indazole-5-yl)methanimines as monoamine oxidase B and acetylcholinesterase inhibitors.
Tzvetkov NT, Stammler HG, Georgieva MG, Russo D, Faraone I, Balacheva AA, Hristova S, Atanasov AG, Milella L, Antonov L, Gastreich M.
Eur J Med Chem (2019) 179 : 404 -422
PubMed 31265934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.78 9.41
Ki 13 9.27 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3319256 2 9.77
CHEMBL3319244 2 9.59
CHEMBL3319272 2 9.57
CHEMBL3319247 2 9.54
CHEMBL3317469 2 9.52
CHEMBL3319273 2 9.34
CHEMBL4104691 2 9.32
CHEMBL4539722 3 9.24
CHEMBL4466571 3 9.24
CHEMBL4567537 3 9.08
CHEMBL4449231 3 9.03
CHEMBL396778 SAFINAMIDE 4.0 3 8.64
CHEMBL3319254 2 8.62
CHEMBL972 SELEGILINE 4.0 1 8.26
CHEMBL887 RASAGILINE 4.0 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3319256 Ki = 0.17 nM 9.77
CHEMBL3319244 Ki = 0.26 nM 9.59
CHEMBL3319272 Ki = 0.27 nM 9.57
CHEMBL3319247 Ki = 0.29 nM 9.54
CHEMBL3317469 Ki = 0.3 nM 9.52
CHEMBL3319256 IC50 = 0.389 nM 9.41
CHEMBL3319273 Ki = 0.46 nM 9.34
CHEMBL4104691 Ki = 0.48 nM 9.32
CHEMBL4466571 Ki = 0.57 nM 9.24
CHEMBL4539722 Ki = 0.57 nM 9.24
CHEMBL3319244 IC50 = 0.5888 nM 9.23
CHEMBL3319272 IC50 = 0.6166 nM 9.21
CHEMBL3319247 IC50 = 0.6607 nM 9.18
CHEMBL3317469 IC50 = 0.6761 nM 9.17
CHEMBL4567537 Ki = 0.84 nM 9.08
CHEMBL4449231 Ki = 0.93 nM 9.03
CHEMBL3319273 IC50 = 1.023 nM 8.99
CHEMBL4104691 IC50 = 1.072 nM 8.97
CHEMBL4539722 IC50 = 1.288 nM 8.89
CHEMBL4466571 IC50 = 1.288 nM 8.89
CHEMBL4466571 IC50 = 1.29 nM 8.89
CHEMBL4539722 IC50 = 1.28 nM 8.89
CHEMBL4567537 IC50 = 1.905 nM 8.72
CHEMBL4567537 IC50 = 1.91 nM 8.72
CHEMBL4449231 IC50 = 2.089 nM 8.68
CHEMBL4449231 IC50 = 2.1 nM 8.68
CHEMBL396778 SAFINAMIDE Ki = 2.29 nM 8.64
CHEMBL3319254 Ki = 2.39 nM 8.62
CHEMBL396778 SAFINAMIDE IC50 = 5.18 nM 8.29
CHEMBL396778 SAFINAMIDE IC50 = 5.129 nM 8.29
CHEMBL3319254 IC50 = 5.37 nM 8.27
CHEMBL972 SELEGILINE IC50 = 5.5 nM 8.26
CHEMBL887 RASAGILINE IC50 = 13.0 nM 7.89