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Assay Detail

CHEMBL4141645

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

Binding
Inhibition of MAO-A in rat liver mitochondria using p-tyramine as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins in presence of MAO-B inhibitor deprenyl by Amplex red dye-based fluorescence assay
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis, monoamine oxidase inhibition activity and molecular docking studies of novel 4-hydroxy-N'-[benzylidene or 1-phenylethylidene]-2-H/methyl/benzyl-1,2-benzothiazine-3-carbohydrazide 1,1-dioxides.
Saddique FA, Zaib S, Jalil S, Aslam S, Ahmad M, Sultan S, Naz H, Iqbal M, Iqbal J.
Eur J Med Chem (2018) 143 : 1373 -1386
PubMed 29126721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 5.56 8.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8706 CLORGILINE 2.0 1 8.35
CHEMBL4169543 1 6.96
CHEMBL1782842 1 6.92
CHEMBL475017 1 6.75
CHEMBL4167042 1 6.62
CHEMBL4172849 1 6.50
CHEMBL4176805 1 6.48
CHEMBL475188 1 6.46
CHEMBL4165825 1 6.42
CHEMBL4164943 1 6.36
CHEMBL4161683 1 6.02
CHEMBL4167829 1 5.96
CHEMBL4166188 1 5.91
CHEMBL1782841 1 5.80
CHEMBL471758 1 5.72
CHEMBL4163328 1 5.53
CHEMBL4161532 1 5.31
CHEMBL471769 1 5.29
CHEMBL4165104 1 5.29
CHEMBL470744 1 5.24
CHEMBL4169453 1 5.21
CHEMBL4177110 1 5.18
CHEMBL4169131 1 5.13
CHEMBL4167325 1 5.02
CHEMBL4173753 1 4.97
CHEMBL1782829 1 4.95
CHEMBL4167525 1 4.94
CHEMBL4171408 1 4.77
CHEMBL4169612 1 4.73
CHEMBL4176639 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8706 CLORGILINE IC50 = 4.5 nM 8.35
CHEMBL4169543 IC50 = 110.0 nM 6.96
CHEMBL1782842 IC50 = 120.0 nM 6.92
CHEMBL475017 IC50 = 177.0 nM 6.75
CHEMBL4167042 IC50 = 240.0 nM 6.62
CHEMBL4172849 IC50 = 320.0 nM 6.50
CHEMBL4176805 IC50 = 330.0 nM 6.48
CHEMBL475188 IC50 = 350.0 nM 6.46
CHEMBL4165825 IC50 = 380.0 nM 6.42
CHEMBL4164943 IC50 = 440.0 nM 6.36
CHEMBL4161683 IC50 = 960.0 nM 6.02
CHEMBL4167829 IC50 = 1110.0 nM 5.96
CHEMBL4166188 IC50 = 1220.0 nM 5.91
CHEMBL1782841 IC50 = 1580.0 nM 5.80
CHEMBL471758 IC50 = 1910.0 nM 5.72
CHEMBL4163328 IC50 = 2970.0 nM 5.53
CHEMBL4161532 IC50 = 4850.0 nM 5.31
CHEMBL471769 IC50 = 5070.0 nM 5.29
CHEMBL4165104 IC50 = 5070.0 nM 5.29
CHEMBL470744 IC50 = 5760.0 nM 5.24
CHEMBL4169453 IC50 = 6120.0 nM 5.21
CHEMBL4177110 IC50 = 6670.0 nM 5.18
CHEMBL4169131 IC50 = 7480.0 nM 5.13
CHEMBL4167325 IC50 = 9510.0 nM 5.02
CHEMBL4173753 IC50 = 10800.0 nM 4.97
CHEMBL1782829 IC50 = 11200.0 nM 4.95
CHEMBL4167525 IC50 = 11400.0 nM 4.94
CHEMBL4171408 IC50 = 16900.0 nM 4.77
CHEMBL4169612 IC50 = 18700.0 nM 4.73
CHEMBL4176639 IC50 = 18900.0 nM 4.72
CHEMBL4166029 IC50 = 21100.0 nM 4.68
CHEMBL4176626 IC50 = 26600.0 nM 4.58
CHEMBL4173005 IC50 = 28300.0 nM 4.55
CHEMBL4159611 IC50 = 29800.0 nM 4.53
CHEMBL4162583 IC50 = 53400.0 nM 4.27
CHEMBL8663 IC50 = 67250.0 nM 4.17
CHEMBL4163586 IC50 >= 100000.0 nM -
CHEMBL4160794 IC50 >= 100000.0 nM -
CHEMBL4173275 IC50 >= 100000.0 nM -
CHEMBL1782814 IC50 >= 100000.0 nM -
CHEMBL4176387 IC50 >= 100000.0 nM -
CHEMBL4171487 IC50 >= 100000.0 nM -
CHEMBL4159508 IC50 >= 100000.0 nM -
CHEMBL4164808 IC50 >= 100000.0 nM -
CHEMBL4168526 IC50 >= 100000.0 nM -