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Assay Detail

CHEMBL5152644

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

Binding
Inhibition of recombinant human MAO-B using using kynuramine as substrate assessed as inhibition of 4-hydroxyquinoline formation incubated for 20 mins by fluorescence spectrophotometric analysis
13
Total Activities
13
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] B (CHEMBL2039)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The inhibition of monoamine oxidase by 2H-1,4-benzothiazin-3(4H)-ones.
Hitge R, Petzer JP, Petzer A.
Bioorg Med Chem Lett (2022) 77 : 129038 -129038
PubMed 36307034 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.76 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5199383 1 8.57
CHEMBL5174857 1 8.39
CHEMBL5203446 1 8.09
CHEMBL5174014 1 8.02
CHEMBL5194774 1 7.70
CHEMBL5175823 1 7.62
CHEMBL5176809 1 7.15
CHEMBL5170948 1 6.78
CHEMBL140 CURCUMIN 3.0 1 5.59
CHEMBL5199502 1 5.54
CHEMBL326294 ISATIN 1 5.41
CHEMBL5180307 1 4.70
CHEMBL103879 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5199383 IC50 = 2.7 nM 8.57
CHEMBL5174857 IC50 = 4.1 nM 8.39
CHEMBL5203446 IC50 = 8.2 nM 8.09
CHEMBL5174014 IC50 = 9.6 nM 8.02
CHEMBL5194774 IC50 = 20.0 nM 7.70
CHEMBL5175823 IC50 = 24.0 nM 7.62
CHEMBL5176809 IC50 = 71.0 nM 7.15
CHEMBL5170948 IC50 = 167.0 nM 6.78
CHEMBL140 CURCUMIN IC50 = 2580.0 nM 5.59
CHEMBL5199502 IC50 = 2870.0 nM 5.54
CHEMBL326294 ISATIN IC50 = 3900.0 nM 5.41
CHEMBL5180307 IC50 = 20000.0 nM 4.70
CHEMBL103879 IC50 = 42600.0 nM 4.37