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Assay Detail

CHEMBL5352830

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

Binding
Inhibition of human MAO-B using p-tyramine as substrate incubated for 15 mins by Amplex red and horseradish peroxidase based fluorescence assay
28
Total Activities
28
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

Design and synthesis of chromone-based monoamine oxidase B inhibitors with improved drug-like properties.
Reis J, Fernandes C, Salem H, Maia M, Tomé C, Benfeito S, Teixeira J, Oliveira PJ, Uriarte E, Ortuso F, Alcaro S, Bagetta D, Cagide F, Borges F.
Eur J Med Chem (2022) 239 : 114507 -114507
PubMed 35772321 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 7.32 10.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL972 SELEGILINE 4.0 1 10.77
CHEMBL4074532 1 8.17
CHEMBL5437543 1 8.08
CHEMBL4078090 1 7.99
CHEMBL5403995 1 7.89
CHEMBL5429656 1 7.84
CHEMBL5431945 1 7.81
CHEMBL5416761 1 7.80
CHEMBL5431507 1 7.60
CHEMBL5422519 1 7.55
CHEMBL5417198 1 7.54
CHEMBL5404200 1 7.53
CHEMBL5406057 1 7.50
CHEMBL4070614 1 7.38
CHEMBL5423045 1 7.26
CHEMBL5400189 1 7.16
CHEMBL5421246 1 7.01
CHEMBL4075920 1 6.68
CHEMBL5432117 1 6.62
CHEMBL5415156 1 6.58
CHEMBL5425546 1 6.46
CHEMBL5426795 1 6.22
CHEMBL4102366 1 6.17
CHEMBL5423398 1 5.99
CHEMBL5423186 1 5.32
CHEMBL8706 CLORGILINE 2.0 1 -
CHEMBL396778 SAFINAMIDE 4.0 1 -
CHEMBL887 RASAGILINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL972 SELEGILINE IC50 = 0.017 nM 10.77
CHEMBL4074532 IC50 = 6.8 nM 8.17
CHEMBL5437543 IC50 = 8.3 nM 8.08
CHEMBL4078090 IC50 = 10.3 nM 7.99
CHEMBL5403995 IC50 = 13.0 nM 7.89
CHEMBL5429656 IC50 = 14.3 nM 7.84
CHEMBL5431945 IC50 = 15.4 nM 7.81
CHEMBL5416761 IC50 = 15.7 nM 7.80
CHEMBL5431507 IC50 = 25.0 nM 7.60
CHEMBL5422519 IC50 = 28.4 nM 7.55
CHEMBL5417198 IC50 = 29.1 nM 7.54
CHEMBL5404200 IC50 = 29.8 nM 7.53
CHEMBL5406057 IC50 = 31.3 nM 7.50
CHEMBL4070614 IC50 = 41.8 nM 7.38
CHEMBL5423045 IC50 = 55.1 nM 7.26
CHEMBL5400189 IC50 = 68.9 nM 7.16
CHEMBL5421246 IC50 = 97.2 nM 7.01
CHEMBL4075920 IC50 = 211.0 nM 6.68
CHEMBL5432117 IC50 = 240.0 nM 6.62
CHEMBL5415156 IC50 = 262.0 nM 6.58
CHEMBL5425546 IC50 = 344.0 nM 6.46
CHEMBL5426795 IC50 = 598.0 nM 6.22
CHEMBL4102366 IC50 = 674.0 nM 6.17
CHEMBL5423398 IC50 = 1030.0 nM 5.99
CHEMBL5423186 IC50 = 4829.0 nM 5.32
CHEMBL8706 CLORGILINE IC50 = 63.4 nM -
CHEMBL396778 SAFINAMIDE IC50 = 0.023 nM -
CHEMBL887 RASAGILINE IC50 = 0.05 nM -