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Assay Detail

CHEMBL4385039

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 using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by Cheng-Prusoff equation analysis
13
Total Activities
13
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] B (CHEMBL2039)
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
Ki 13 7.60 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4450595 1 9.30
CHEMBL4439889 1 8.84
CHEMBL396778 SAFINAMIDE 4.0 1 8.64
CHEMBL4450144 1 8.32
CHEMBL3319242 1 8.26
CHEMBL4467747 1 7.89
CHEMBL4532884 1 7.69
CHEMBL4456254 1 7.50
CHEMBL4451278 1 7.27
CHEMBL4441316 1 6.91
CHEMBL4467709 1 6.41
CHEMBL3319241 1 5.94
CHEMBL3319240 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4450595 Ki = 0.5 nM 9.30
CHEMBL4439889 Ki = 1.45 nM 8.84
CHEMBL396778 SAFINAMIDE Ki = 2.29 nM 8.64
CHEMBL4450144 Ki = 4.82 nM 8.32
CHEMBL3319242 Ki = 5.48 nM 8.26
CHEMBL4467747 Ki = 12.8 nM 7.89
CHEMBL4532884 Ki = 20.4 nM 7.69
CHEMBL4456254 Ki = 31.8 nM 7.50
CHEMBL4451278 Ki = 53.5 nM 7.27
CHEMBL4441316 Ki = 122.0 nM 6.91
CHEMBL4467709 Ki = 390.0 nM 6.41
CHEMBL3319241 Ki = 1145.0 nM 5.94
CHEMBL3319240 Ki = 1459.0 nM 5.84