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Assay Detail

CHEMBL1246374

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

Binding
Inhibition of human recombinant MAOA expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay
36
Total Activities
36
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

Synthesis, stereochemical separation, and biological evaluation of selective inhibitors of human MAO-B: 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazines.
Chimenti F, Secci D, Bolasco A, Chimenti P, Granese A, Carradori S, Yáñez M, Orallo F, Sanna ML, Gallinella B, Cirilli R.
J Med Chem (2010) 53 : 6516 -6520
PubMed 20715818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 4.72 5.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399353 1 5.56
CHEMBL1242938 1 5.45
CHEMBL1243125 1 5.37
CHEMBL1242992 1 5.32
CHEMBL1242964 1 5.31
CHEMBL1243400 1 5.26
CHEMBL495714 1 5.24
CHEMBL92401 IPRONIAZID 2.0 1 5.18
CHEMBL1242991 1 5.17
CHEMBL1243401 1 5.14
CHEMBL1243089 1 5.00
CHEMBL1243182 1 4.77
CHEMBL1243180 1 4.69
CHEMBL1243181 1 4.66
CHEMBL1243213 1 4.64
CHEMBL1243212 1 4.64
CHEMBL1243399 1 4.51
CHEMBL1242936 1 4.45
CHEMBL1243214 1 4.43
CHEMBL1241294 1 4.42
CHEMBL1240558 1 4.42
CHEMBL1243088 1 4.41
CHEMBL1241295 1 4.41
CHEMBL326294 ISATIN 1 4.40
CHEMBL1243245 1 4.39
CHEMBL1243058 1 4.39
CHEMBL375539 1 4.38
CHEMBL1243371 1 4.37
CHEMBL1243059 1 4.37
CHEMBL1242937 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399353 IC50 = 2760.0 nM 5.56
CHEMBL1242938 IC50 = 3530.0 nM 5.45
CHEMBL1243125 IC50 = 4260.0 nM 5.37
CHEMBL1242992 IC50 = 4810.0 nM 5.32
CHEMBL1242964 IC50 = 4940.0 nM 5.31
CHEMBL1243400 IC50 = 5500.0 nM 5.26
CHEMBL495714 IC50 = 5770.0 nM 5.24
CHEMBL92401 IPRONIAZID IC50 = 6560.0 nM 5.18
CHEMBL1242991 IC50 = 6830.0 nM 5.17
CHEMBL1243401 IC50 = 7220.0 nM 5.14
CHEMBL1243089 IC50 = 10090.0 nM 5.00
CHEMBL1243182 IC50 = 17140.0 nM 4.77
CHEMBL1243180 IC50 = 20570.0 nM 4.69
CHEMBL1243181 IC50 = 21900.0 nM 4.66
CHEMBL1243212 IC50 = 23120.0 nM 4.64
CHEMBL1243213 IC50 = 22760.0 nM 4.64
CHEMBL1243399 IC50 = 31030.0 nM 4.51
CHEMBL1242936 IC50 = 35220.0 nM 4.45
CHEMBL1243214 IC50 = 37520.0 nM 4.43
CHEMBL1240558 IC50 = 37950.0 nM 4.42
CHEMBL1241294 IC50 = 37840.0 nM 4.42
CHEMBL1243088 IC50 = 38840.0 nM 4.41
CHEMBL1241295 IC50 = 38610.0 nM 4.41
CHEMBL326294 ISATIN IC50 = 40000.0 nM 4.40
CHEMBL1243245 IC50 = 40320.0 nM 4.39
CHEMBL1243058 IC50 = 40570.0 nM 4.39
CHEMBL375539 IC50 = 41230.0 nM 4.38
CHEMBL1243371 IC50 = 42310.0 nM 4.37
CHEMBL1243059 IC50 = 42660.0 nM 4.37
CHEMBL1242937 IC50 = 43550.0 nM 4.36
CHEMBL1243057 IC50 = 43780.0 nM 4.36
CHEMBL1243026 IC50 = 43950.0 nM 4.36
CHEMBL1242965 IC50 = 44700.0 nM 4.35
CHEMBL972 SELEGILINE IC50 = 67250.0 nM 4.17
CHEMBL86304 MOCLOBEMIDE IC50 = 361380.0 nM -
CHEMBL8706 CLORGILINE IC50 = 4.46 nM -