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Assay Detail

CHEMBL4040840

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

Binding
Inhibition of human recombinant microsomal MAOB expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production after 15 mins by amplex red-based fluorescence assay
30
Total Activities
30
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

Coumarin versus Chromone Monoamine Oxidase B Inhibitors: Quo Vadis?
Fonseca A, Reis J, Silva T, Matos MJ, Bagetta D, Ortuso F, Alcaro S, Uriarte E, Borges F.
J Med Chem (2017) 60 : 7206 -7212
PubMed 28753307 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.49 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4074532 1 8.40
CHEMBL4060916 1 8.38
CHEMBL494798 1 8.29
CHEMBL4076698 1 8.22
CHEMBL494808 1 8.12
CHEMBL4080704 1 8.04
CHEMBL4078090 1 7.99
CHEMBL494800 1 7.96
CHEMBL522532 1 7.86
CHEMBL495466 1 7.82
CHEMBL972 SELEGILINE 4.0 1 7.78
CHEMBL4094520 1 7.77
CHEMBL4089520 1 7.72
CHEMBL4099648 1 7.71
CHEMBL4073128 1 7.67
CHEMBL4072004 1 7.66
CHEMBL396778 SAFINAMIDE 4.0 1 7.64
CHEMBL4070614 1 7.38
CHEMBL4081233 1 7.34
CHEMBL4074339 1 7.34
CHEMBL1598233 1 7.33
CHEMBL887 RASAGILINE 4.0 1 7.30
CHEMBL4089098 1 7.11
CHEMBL4085981 1 6.95
CHEMBL4099251 1 6.82
CHEMBL4075920 1 6.68
CHEMBL4081648 1 6.64
CHEMBL4091517 1 6.29
CHEMBL4097014 1 6.21
CHEMBL4102366 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4074532 IC50 = 3.94 nM 8.40
CHEMBL4060916 IC50 = 4.2 nM 8.38
CHEMBL494798 IC50 = 5.07 nM 8.29
CHEMBL4076698 IC50 = 5.95 nM 8.22
CHEMBL494808 IC50 = 7.52 nM 8.12
CHEMBL4080704 IC50 = 9.03 nM 8.04
CHEMBL4078090 IC50 = 10.31 nM 7.99
CHEMBL494800 IC50 = 11.08 nM 7.96
CHEMBL522532 IC50 = 13.9 nM 7.86
CHEMBL495466 IC50 = 15.32 nM 7.82
CHEMBL972 SELEGILINE IC50 = 16.73 nM 7.78
CHEMBL4094520 IC50 = 17.1 nM 7.77
CHEMBL4089520 IC50 = 18.9 nM 7.72
CHEMBL4099648 IC50 = 19.43 nM 7.71
CHEMBL4073128 IC50 = 21.35 nM 7.67
CHEMBL4072004 IC50 = 21.8 nM 7.66
CHEMBL396778 SAFINAMIDE IC50 = 23.07 nM 7.64
CHEMBL4070614 IC50 = 41.8 nM 7.38
CHEMBL4081233 IC50 = 45.42 nM 7.34
CHEMBL4074339 IC50 = 45.4 nM 7.34
CHEMBL1598233 IC50 = 47.24 nM 7.33
CHEMBL887 RASAGILINE IC50 = 49.66 nM 7.30
CHEMBL4089098 IC50 = 78.22 nM 7.11
CHEMBL4085981 IC50 = 113.5 nM 6.95
CHEMBL4099251 IC50 = 151.6 nM 6.82
CHEMBL4075920 IC50 = 210.8 nM 6.68
CHEMBL4081648 IC50 = 228.6 nM 6.64
CHEMBL4091517 IC50 = 512.6 nM 6.29
CHEMBL4097014 IC50 = 621.7 nM 6.21
CHEMBL4102366 IC50 = 674.2 nM 6.17