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Assay Detail

CHEMBL4385036

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

Binding
Inhibition of Sprague-Dawley rat liver MAO-B using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] B (CHEMBL2993)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 11 7.32 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4450595 1 8.38
CHEMBL887 RASAGILINE 4.0 1 8.37
CHEMBL4439889 1 8.31
CHEMBL972 SELEGILINE 4.0 1 8.21
CHEMBL3707394 SEMBRAGILINE 2.0 1 7.83
CHEMBL4450144 1 7.07
CHEMBL4532884 1 6.82
CHEMBL4456254 1 6.80
CHEMBL4467747 1 6.65
CHEMBL4451278 1 6.24
CHEMBL4441316 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4450595 IC50 = 4.2 nM 8.38
CHEMBL887 RASAGILINE IC50 = 4.31 nM 8.37
CHEMBL4439889 IC50 = 4.9 nM 8.31
CHEMBL972 SELEGILINE IC50 = 6.11 nM 8.21
CHEMBL3707394 SEMBRAGILINE IC50 = 14.7 nM 7.83
CHEMBL4450144 IC50 = 85.5 nM 7.07
CHEMBL4532884 IC50 = 153.0 nM 6.82
CHEMBL4456254 IC50 = 158.0 nM 6.80
CHEMBL4467747 IC50 = 224.0 nM 6.65
CHEMBL4451278 IC50 = 574.0 nM 6.24
CHEMBL4441316 IC50 = 1303.0 nM 5.88