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Assay Detail

CHEMBL1069162

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

Binding
Competitive inhibition of MAOA in rat liver homogenate by spectrophotometrically
24
Total Activities
12
Compounds Tested
2
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

Synthesis and molecular modeling of some novel hexahydroindazole derivatives as potent monoamine oxidase inhibitors.
Gökhan-Kelekçi N, Simşek OO, Ercan A, Yelekçi K, Sahin ZS, Işik S, Uçar G, Bilgin AA.
Bioorg Med Chem (2009) 17 : 6761 -6772
PubMed 19682910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.08 6.16
Ki 12 6.25 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL594029 2 8.38
CHEMBL86304 MOCLOBEMIDE 4.0 2 8.26
CHEMBL593341 2 7.41
CHEMBL607513 2 6.19
CHEMBL596228 2 6.06
CHEMBL596340 2 5.76
CHEMBL592976 2 5.52
CHEMBL596453 2 5.41
CHEMBL596313 2 5.37
CHEMBL596339 2 5.30
CHEMBL607552 2 5.05
CHEMBL972 SELEGILINE 4.0 2 4.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL594029 Ki = 4.22 nM 8.38
CHEMBL86304 MOCLOBEMIDE Ki = 5.53 nM 8.26
CHEMBL593341 Ki = 39.15 nM 7.41
CHEMBL607513 Ki = 650.0 nM 6.19
CHEMBL593341 IC50 = 700.0 nM 6.16
CHEMBL594029 IC50 = 780.0 nM 6.11
CHEMBL596228 Ki = 880.0 nM 6.06
CHEMBL596340 Ki = 1720.0 nM 5.76
CHEMBL607513 IC50 = 1780.0 nM 5.75
CHEMBL596228 IC50 = 2050.0 nM 5.69
CHEMBL596340 IC50 = 3010.0 nM 5.52
CHEMBL592976 Ki = 2990.0 nM 5.52
CHEMBL596453 Ki = 3900.0 nM 5.41
CHEMBL596313 Ki = 4260.0 nM 5.37
CHEMBL596339 Ki = 5010.0 nM 5.30
CHEMBL86304 MOCLOBEMIDE IC50 = 5700.0 nM 5.24
CHEMBL607552 Ki = 8820.0 nM 5.05
CHEMBL596339 IC50 = 62340.0 nM 4.21
CHEMBL596453 IC50 = 80220.0 nM 4.10
CHEMBL972 SELEGILINE IC50 = 90550.0 nM 4.04
CHEMBL592976 IC50 = 95200.0 nM 4.02
CHEMBL596313 IC50 = 110450.0 nM -
CHEMBL972 SELEGILINE Ki = 105660.0 nM -
CHEMBL607552 IC50 = 108340.0 nM -