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Assay Detail

CHEMBL1251644

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

Binding
Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay
ChEMBL ↗
101
Total Activities
60
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] B (CHEMBL2039) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, semipreparative HPLC separation, biological evaluation, and 3D-QSAR of hydrazothiazole derivatives as human monoamine oxidase B inhibitors.
Chimenti F, Secci D, Bolasco A, Chimenti P, Granese A, Carradori S, Maccioni E, Cardia MC, Yáñez M, Orallo F, Alcaro S, Ortuso F, Cirilli R, Ferretti R, Distinto S, Kirchmair J, Langer T.
Bioorg Med Chem (2010) 18 : 5063 -5070
PubMed 20579890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 101 6.74 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1253680 — — 2 8.52
CHEMBL1253845 — — 2 8.45
CHEMBL1253699 — — 2 8.42
CHEMBL453703 — — 1 8.00
CHEMBL1243026 — — 1 8.00
CHEMBL1253926 — — 2 7.96
CHEMBL1240558 — — 1 7.85
CHEMBL1253847 — — 2 7.80
CHEMBL498694 — — 1 7.78
CHEMBL1243371 — — 1 7.77
CHEMBL972 SELEGILINE 4.0 1 7.70
CHEMBL1242938 — — 2 7.66
CHEMBL1243399 — — 1 7.58
CHEMBL248050 — — 2 7.57
CHEMBL1242991 — — 2 7.52
CHEMBL1243025 — — 1 7.50
CHEMBL1243400 — — 2 7.50
CHEMBL1242992 — — 2 7.44
CHEMBL1253613 — — 2 7.40
CHEMBL1254934 — — 2 7.37
CHEMBL1254017 — — 2 7.34
CHEMBL1242964 — — 1 7.33
CHEMBL497674 — — 1 7.32
CHEMBL1254851 — — 2 7.28
CHEMBL1253763 — — 2 7.21
CHEMBL1243401 — — 2 7.20
CHEMBL1254850 — — 2 7.07
CHEMBL1255019 — — 2 7.04
CHEMBL247834 — — 2 7.03
CHEMBL220495 — — 2 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1253680 — IC50 = 3.0 nM 8.52
CHEMBL1253680 — IC50 = 3.236 nM 8.49
CHEMBL1253845 — IC50 = 3.548 nM 8.45
CHEMBL1253699 — IC50 = 3.802 nM 8.42
CHEMBL1253845 — IC50 = 4.0 nM 8.40
CHEMBL1253699 — IC50 = 4.0 nM 8.40
CHEMBL1243026 — IC50 = 10.0 nM 8.00
CHEMBL453703 — IC50 = 10.0 nM 8.00
CHEMBL1253926 — IC50 = 11.0 nM 7.96
CHEMBL1253926 — IC50 = 11.48 nM 7.94
CHEMBL1240558 — IC50 = 14.0 nM 7.85
CHEMBL1253847 — IC50 = 16.0 nM 7.80
CHEMBL1253847 — IC50 = 16.22 nM 7.79
CHEMBL498694 — IC50 = 16.6 nM 7.78
CHEMBL1243371 — IC50 = 17.0 nM 7.77
CHEMBL972 SELEGILINE IC50 = 20.0 nM 7.70
CHEMBL1242938 — IC50 = 21.88 nM 7.66
CHEMBL1242938 — IC50 = 22.0 nM 7.66
CHEMBL1243399 — IC50 = 26.0 nM 7.58
CHEMBL248050 — IC50 = 27.0 nM 7.57
CHEMBL248050 — IC50 = 27.54 nM 7.56
CHEMBL1242991 — IC50 = 30.0 nM 7.52
CHEMBL1243400 — IC50 = 32.0 nM 7.50
CHEMBL1243025 — IC50 = 32.0 nM 7.50
CHEMBL1243400 — IC50 = 32.36 nM 7.49
CHEMBL1242992 — IC50 = 36.0 nM 7.44
CHEMBL1253613 — IC50 = 40.0 nM 7.40
CHEMBL1253613 — IC50 = 40.74 nM 7.39
CHEMBL1254934 — IC50 = 43.0 nM 7.37
CHEMBL1254934 — IC50 = 43.65 nM 7.36
CHEMBL1254017 — IC50 = 45.71 nM 7.34
CHEMBL1254017 — IC50 = 46.0 nM 7.34
CHEMBL1242964 — IC50 = 47.0 nM 7.33
CHEMBL1242991 — IC50 = 47.86 nM 7.32
CHEMBL497674 — IC50 = 47.86 nM 7.32
CHEMBL1254851 — IC50 = 52.48 nM 7.28
CHEMBL1254851 — IC50 = 53.0 nM 7.28
CHEMBL1253763 — IC50 = 61.0 nM 7.21
CHEMBL1253763 — IC50 = 61.66 nM 7.21
CHEMBL1243401 — IC50 = 63.1 nM 7.20
CHEMBL1243401 — IC50 = 63.0 nM 7.20
CHEMBL1242992 — IC50 = 66.07 nM 7.18
CHEMBL1254850 — IC50 = 85.11 nM 7.07
CHEMBL1254850 — IC50 = 86.0 nM 7.07
CHEMBL1255019 — IC50 = 91.2 nM 7.04
CHEMBL1255019 — IC50 = 91.0 nM 7.04
CHEMBL247834 — IC50 = 94.0 nM 7.03
CHEMBL247834 — IC50 = 95.5 nM 7.02
CHEMBL220495 — IC50 = 116.0 nM 6.94
CHEMBL220495 — IC50 = 117.49 nM 6.93