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Assay Detail

CHEMBL5049165

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

Toxicity
Inhibition of human recombinant MAO-A expressed in supersomes assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate by spectrofluorimetric analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] A (CHEMBL1951)
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 11 5.37 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5085674 1 5.85
CHEMBL5083014 1 5.70
CHEMBL4598256 1 5.62
CHEMBL5090504 1 5.60
CHEMBL4571763 1 5.55
CHEMBL5083737 1 5.38
CHEMBL5081663 1 5.11
CHEMBL5094348 1 5.09
CHEMBL5072382 1 4.96
CHEMBL3586771 1 4.82
CHEMBL502 DONEPEZIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5085674 IC50 = 1400.0 nM 5.85
CHEMBL5083014 IC50 = 2000.0 nM 5.70
CHEMBL4598256 IC50 = 2400.0 nM 5.62
CHEMBL5090504 IC50 = 2500.0 nM 5.60
CHEMBL4571763 IC50 = 2800.0 nM 5.55
CHEMBL5083737 IC50 = 4200.0 nM 5.38
CHEMBL5081663 IC50 = 7800.0 nM 5.11
CHEMBL5094348 IC50 = 8100.0 nM 5.09
CHEMBL5072382 IC50 = 11000.0 nM 4.96
CHEMBL3586771 IC50 = 15000.0 nM 4.82
CHEMBL502 DONEPEZIL IC50 - -