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Assay Detail

CHEMBL5049166

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

Binding
Inhibition of human recombinant MAO-B expressed in supersomes assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate by spectrofluorimetric analysis
20
Total Activities
20
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

Probing Fluorinated Motifs onto Dual AChE-MAO B Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Early-ADME Studies.
Rullo M, Cipolloni M, Catto M, Colliva C, Miniero DV, Latronico T, de Candia M, Benicchi T, Linusson A, Giacchè N, Altomare CD, Pisani L.
J Med Chem (2022) 65 : 3962 -3977
PubMed 35195417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.99 8.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5082824 1 8.09
CHEMBL5090153 1 8.00
CHEMBL3586771 1 8.00
CHEMBL5083014 1 7.92
CHEMBL396778 SAFINAMIDE 4.0 1 7.75
CHEMBL4571763 1 7.52
CHEMBL5081663 1 7.14
CHEMBL4598256 1 6.96
CHEMBL5085674 1 6.89
CHEMBL5083613 1 6.89
CHEMBL5090504 1 6.85
CHEMBL5078658 1 6.80
CHEMBL5072382 1 6.58
CHEMBL5094348 1 6.46
CHEMBL5079544 1 6.38
CHEMBL4464759 1 6.32
CHEMBL5081574 1 6.28
CHEMBL5083737 1 6.25
CHEMBL4453856 1 5.82
CHEMBL502 DONEPEZIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5082824 IC50 = 8.2 nM 8.09
CHEMBL5090153 IC50 = 10.0 nM 8.00
CHEMBL3586771 IC50 = 10.0 nM 8.00
CHEMBL5083014 IC50 = 12.0 nM 7.92
CHEMBL396778 SAFINAMIDE IC50 = 18.0 nM 7.75
CHEMBL4571763 IC50 = 30.0 nM 7.52
CHEMBL5081663 IC50 = 73.0 nM 7.14
CHEMBL4598256 IC50 = 110.0 nM 6.96
CHEMBL5085674 IC50 = 130.0 nM 6.89
CHEMBL5083613 IC50 = 130.0 nM 6.89
CHEMBL5090504 IC50 = 140.0 nM 6.85
CHEMBL5078658 IC50 = 160.0 nM 6.80
CHEMBL5072382 IC50 = 260.0 nM 6.58
CHEMBL5094348 IC50 = 350.0 nM 6.46
CHEMBL5079544 IC50 = 420.0 nM 6.38
CHEMBL4464759 IC50 = 480.0 nM 6.32
CHEMBL5081574 IC50 = 530.0 nM 6.28
CHEMBL5083737 IC50 = 560.0 nM 6.25
CHEMBL4453856 IC50 = 1500.0 nM 5.82
CHEMBL502 DONEPEZIL IC50 - -