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Assay Detail

CHEMBL2026610

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

Binding
Inhibition of mitochondrial MAO-A in rat liver homogenates using [14C]-(5-hydroxy-triptamine) as substrate preincubated for 30 mins by liquid scintillation counting
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Amine oxidase [flavin-containing] A (CHEMBL3358)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine.
Samadi A, de los Ríos C, Bolea I, Chioua M, Iriepa I, Moraleda I, Bartolini M, Andrisano V, Gálvez E, Valderas C, Unzeta M, Marco-Contelles J.
Eur J Med Chem (2012) 52 : 251 -262
PubMed 22503231 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.72 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2022927 1 9.10
CHEMBL95 TACRINE 4.0 1 7.40
CHEMBL2022924 1 7.00
CHEMBL2022925 1 6.82
CHEMBL2022928 1 6.82
CHEMBL2022926 1 6.72
CHEMBL2021938 1 5.90
CHEMBL2022923 1 4.00
CHEMBL2022929 1 -
CHEMBL2022930 1 -
CHEMBL2022931 1 -
CHEMBL2022932 1 -
CHEMBL2022933 1 -
CHEMBL2022934 1 -
CHEMBL502 DONEPEZIL 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2022927 IC50 = 0.79 nM 9.10
CHEMBL95 TACRINE IC50 = 40.0 nM 7.40
CHEMBL2022924 IC50 = 100.0 nM 7.00
CHEMBL2022925 IC50 = 150.0 nM 6.82
CHEMBL2022928 IC50 = 150.0 nM 6.82
CHEMBL2022926 IC50 = 190.0 nM 6.72
CHEMBL2021938 IC50 = 1250.0 nM 5.90
CHEMBL2022923 IC50 = 99260.0 nM 4.00
CHEMBL2022929 IC50 = 240500.0 nM -
CHEMBL2022930 IC50 = 1050000.0 nM -
CHEMBL2022931 IC50 = 494700.0 nM -
CHEMBL2022932 IC50 = 1001000.0 nM -
CHEMBL2022933 IC50 = 618300.0 nM -
CHEMBL2022934 IC50 = 330200.0 nM -
CHEMBL502 DONEPEZIL IC50 = 850000.0 nM -