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Assay Detail

CHEMBL4711820

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

Binding
Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by horse-radish peroxidase/Amplex Red coupled fluorimetric analysis
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BTI-TN-5B1-4
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] A (CHEMBL1951)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrimido[1,2-b]indazole derivatives: Selective inhibitors of human monoamine oxidase B with neuroprotective activity.
Jismy B,El Qami A,Pišlar A,Frlan R,Kos J,Gobec S,Knez D,Abarbri M
Eur J Med Chem (2021) 209 : 112911 -112911
PubMed 33071056 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.29 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL8706 CLORGILINE 2.0 1 8.47
CHEMBL340807 HARMALINE 1 7.48
CHEMBL4744827 1 4.68
CHEMBL887 RASAGILINE 4.0 1 4.53
CHEMBL396778 SAFINAMIDE 4.0 1 -
CHEMBL4754874 1 -
CHEMBL4783558 1 -
CHEMBL4794759 1 -
CHEMBL4795009 1 -
CHEMBL4758739 1 -
CHEMBL4779904 1 -
CHEMBL4791844 1 -
CHEMBL4759301 1 -
CHEMBL4796620 1 -
CHEMBL4748333 1 -
CHEMBL4746018 1 -
CHEMBL4783092 1 -
CHEMBL4750291 1 -
CHEMBL4753501 1 -
CHEMBL4778686 1 -
CHEMBL4785345 1 -
CHEMBL4757484 1 -
CHEMBL4748078 1 -
CHEMBL4763130 1 -
CHEMBL4798781 1 -
CHEMBL4760176 1 -
CHEMBL4752356 1 -
CHEMBL4780349 1 -
CHEMBL4753863 1 -
CHEMBL4746352 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL8706 CLORGILINE IC50 = 3.4 nM 8.47
CHEMBL340807 HARMALINE IC50 = 32.9 nM 7.48
CHEMBL4744827 IC50 = 21100.0 nM 4.68
CHEMBL887 RASAGILINE IC50 = 29500.0 nM 4.53
CHEMBL4794759 IC50 > 100000.0 nM -
CHEMBL4776405 IC50 > 100000.0 nM -
CHEMBL4795009 IC50 > 100000.0 nM -
CHEMBL4758739 IC50 > 100000.0 nM -
CHEMBL4779904 IC50 > 100000.0 nM -
CHEMBL4791844 IC50 > 100000.0 nM -
CHEMBL4759301 IC50 > 100000.0 nM -
CHEMBL4796620 IC50 > 100000.0 nM -
CHEMBL4748333 IC50 > 100000.0 nM -
CHEMBL4746018 IC50 > 100000.0 nM -
CHEMBL4783092 IC50 > 100000.0 nM -
CHEMBL4754874 IC50 > 100000.0 nM -
CHEMBL4746955 IC50 > 100000.0 nM -
CHEMBL4750851 IC50 > 100000.0 nM -
CHEMBL4749504 IC50 > 100000.0 nM -
CHEMBL4783558 IC50 > 100000.0 nM -
CHEMBL396778 SAFINAMIDE IC50 > 10000.0 nM -
CHEMBL4750291 IC50 > 100000.0 nM -
CHEMBL4753501 IC50 > 100000.0 nM -
CHEMBL4778686 IC50 > 100000.0 nM -
CHEMBL4785345 IC50 > 100000.0 nM -
CHEMBL4757484 IC50 > 100000.0 nM -
CHEMBL4748078 IC50 > 100000.0 nM -
CHEMBL4763130 IC50 > 100000.0 nM -
CHEMBL4798781 IC50 > 100000.0 nM -
CHEMBL4760176 IC50 > 100000.0 nM -
CHEMBL4752356 IC50 > 100000.0 nM -
CHEMBL4780349 IC50 > 100000.0 nM -
CHEMBL4753863 IC50 > 100000.0 nM -
CHEMBL4746352 IC50 > 100000.0 nM -