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Assay Detail

CHEMBL4385035

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

Binding
Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
12
Total Activities
12
Compounds Tested
1
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] A (CHEMBL1951)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

(Pyrrolo-pyridin-5-yl)benzamides: BBB permeable monoamine oxidase B inhibitors with neuroprotective effect on cortical neurons.
Tzvetkov NT, Stammler HG, Hristova S, Atanasov AG, Antonov L.
Eur J Med Chem (2019) 162 : 793 -809
PubMed 30522087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.51 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL887 RASAGILINE 4.0 1 6.17
CHEMBL972 SELEGILINE 4.0 1 5.85
CHEMBL3707394 SEMBRAGILINE 2.0 1 5.41
CHEMBL396778 SAFINAMIDE 4.0 1 4.59
CHEMBL4467747 1 -
CHEMBL4456254 1 -
CHEMBL4451278 1 -
CHEMBL4441316 1 -
CHEMBL4450595 1 -
CHEMBL4439889 1 -
CHEMBL4450144 1 -
CHEMBL4532884 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL887 RASAGILINE IC50 = 680.0 nM 6.17
CHEMBL972 SELEGILINE IC50 = 1424.0 nM 5.85
CHEMBL3707394 SEMBRAGILINE IC50 = 3852.0 nM 5.41
CHEMBL396778 SAFINAMIDE IC50 = 25900.0 nM 4.59
CHEMBL4467747 IC50 > 10000.0 nM -
CHEMBL4456254 IC50 > 10000.0 nM -
CHEMBL4451278 IC50 > 10000.0 nM -
CHEMBL4441316 IC50 > 10000.0 nM -
CHEMBL4450595 IC50 > 10000.0 nM -
CHEMBL4439889 IC50 > 10000.0 nM -
CHEMBL4450144 IC50 > 10000.0 nM -
CHEMBL4532884 IC50 > 10000.0 nM -