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Assay Detail

CHEMBL4369243

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

Binding
Inhibition of MAOA (unknown origin) using kynuramine as substrate preincubated for 30 mins followed by substrate addition
17
Total Activities
17
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] A (CHEMBL1951)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selected aryl thiosemicarbazones as a new class of multi-targeted monoamine oxidase inhibitors.
Mathew B, Baek SC, Grace Thomas Parambi D, Pil Lee J, Joy M, Annie Rilda PR, Randev RV, Nithyamol P, Vijayan V, Inasu ST, Mathew GE, Lohidakshan KK, Kumar Krishnan G, Kim H.
Medchemcomm (2018) 9 : 1871 -1881
PubMed 30568755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.06 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8706 CLORGILINE 2.0 1 8.15
CHEMBL18116 TOLOXATONE 4.0 1 6.04
CHEMBL673 PARGYLINE 4.0 1 5.88
CHEMBL241902 1 5.74
CHEMBL398206 1 5.30
CHEMBL1096480 1 5.22
CHEMBL279390 LAZABEMIDE 2.0 1 -
CHEMBL2369206 1 -
CHEMBL393467 1 -
CHEMBL1818874 1 -
CHEMBL1818875 1 -
CHEMBL1910220 1 -
CHEMBL391982 1 -
CHEMBL193804 1 -
CHEMBL1096479 1 -
CHEMBL242113 1 -
CHEMBL243185 PHENYLTHIOSEMICARBAZONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8706 CLORGILINE IC50 = 7.1 nM 8.15
CHEMBL18116 TOLOXATONE IC50 = 920.0 nM 6.04
CHEMBL673 PARGYLINE IC50 = 1310.0 nM 5.88
CHEMBL241902 IC50 = 1820.0 nM 5.74
CHEMBL398206 IC50 = 4990.0 nM 5.30
CHEMBL1096480 IC50 = 5980.0 nM 5.22
CHEMBL279390 LAZABEMIDE IC50 > 80000.0 nM -
CHEMBL2369206 IC50 > 10000.0 nM -
CHEMBL393467 IC50 > 10000.0 nM -
CHEMBL1818874 IC50 > 10000.0 nM -
CHEMBL1818875 IC50 > 10000.0 nM -
CHEMBL1910220 IC50 > 10000.0 nM -
CHEMBL391982 IC50 > 10000.0 nM -
CHEMBL193804 IC50 > 10000.0 nM -
CHEMBL1096479 IC50 > 10000.0 nM -
CHEMBL242113 IC50 > 10000.0 nM -
CHEMBL243185 PHENYLTHIOSEMICARBAZONE IC50 > 10000.0 nM -