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Assay Detail

CHEMBL879391

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Binding
Inhibition of bovine brain mitochondrial Monoamine oxidase A (MAO-A) compared to toloxatone
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Amine oxidase [flavin-containing] A (CHEMBL3254)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

3-(1H-Pyrrol-1-yl)-2-oxazolidinones as reversible, highly potent, and selective inhibitors of monoamine oxidase type A.
Mai A, Artico M, Esposito M, Sbardella G, Massa S, Befani O, Turini P, Giovannini V, Mondovì B.
J Med Chem (2002) 45 : 1180 -1183
PubMed 11881986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.31 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18101 (R/R)BEFLOXATONE 1 8.60
CHEMBL18334 1 8.31
CHEMBL17653 1 7.05
CHEMBL18019 1 6.70
CHEMBL1794849 1 6.57
CHEMBL18116 TOLOXATONE 4.0 1 6.42
CHEMBL18390 1 6.00
CHEMBL17562 1 5.92
CHEMBL17643 1 5.92
CHEMBL279544 1 5.60
CHEMBL274947 1 4.40
CHEMBL17981 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18101 (R/R)BEFLOXATONE Ki = 2.5 nM 8.60
CHEMBL18334 Ki = 4.9 nM 8.31
CHEMBL17653 Ki = 90.0 nM 7.05
CHEMBL18019 Ki = 200.0 nM 6.70
CHEMBL1794849 Ki = 270.0 nM 6.57
CHEMBL18116 TOLOXATONE Ki = 380.0 nM 6.42
CHEMBL18390 Ki = 1000.0 nM 6.00
CHEMBL17562 Ki = 1200.0 nM 5.92
CHEMBL17643 Ki = 1200.0 nM 5.92
CHEMBL279544 Ki = 2500.0 nM 5.60
CHEMBL274947 Ki = 40000.0 nM 4.40
CHEMBL17981 Ki = 53000.0 nM 4.28