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Assay Detail

CHEMBL3096735

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

Binding
Inhibition of Sprague-Dawley rat MAO-B using Kynuramine as substrate assessed as formation of 4-hydroxyquinoline preincubated for 5 mins prior to substrate addition measured for 5 mins by spectrophotometry
ChEMBL ↗
65
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Amine oxidase [flavin-containing] B (CHEMBL2993) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Fine molecular tuning at position 4 of 2H-chromen-2-one derivatives in the search of potent and selective monoamine oxidase B inhibitors.
Pisani L, Catto M, Nicolotti O, Grossi G, Di Braccio M, Soto-Otero R, Mendez-Alvarez E, Stefanachi A, Gadaleta D, Carotti A.
Eur J Med Chem (2013) 70 : 723 -739
PubMed 24231308 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 6.87 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3094016 — — 2 8.51
CHEMBL3094037 — — 1 8.28
CHEMBL3093993 — — 1 8.24
CHEMBL575934 — — 1 8.13
CHEMBL3093992 — — 1 8.11
CHEMBL3094007 — — 1 8.06
CHEMBL3094017 — — 1 8.05
CHEMBL3094131 — — 1 7.96
CHEMBL239507 — — 1 7.89
CHEMBL3094038 — — 1 7.85
CHEMBL572534 — — 1 7.82
CHEMBL575093 — — 1 7.80
CHEMBL3094021 — — 1 7.77
CHEMBL3094024 — — 1 7.68
CHEMBL575931 — — 1 7.62
CHEMBL3091489 — — 1 7.57
CHEMBL3094008 — — 1 7.55
CHEMBL3094022 — — 1 7.54
CHEMBL575738 — — 1 7.52
CHEMBL3094018 — — 1 7.47
CHEMBL3093991 — — 1 7.44
CHEMBL3094011 — — 1 7.41
CHEMBL577616 — — 1 7.40
CHEMBL3094031 — — 1 7.40
CHEMBL3094025 — — 1 7.36
CHEMBL3094005 — — 1 7.34
CHEMBL3094030 — — 1 7.32
CHEMBL239508 — — 1 7.28
CHEMBL3094000 — — 1 7.21
CHEMBL3094001 — — 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3094016 — IC50 = 3.1 nM 8.51
CHEMBL3094016 — IC50 = 3.311 nM 8.48
CHEMBL3094037 — IC50 = 5.248 nM 8.28
CHEMBL3093993 — IC50 = 5.754 nM 8.24
CHEMBL575934 — IC50 = 7.413 nM 8.13
CHEMBL3093992 — IC50 = 7.762 nM 8.11
CHEMBL3094007 — IC50 = 8.71 nM 8.06
CHEMBL3094017 — IC50 = 8.913 nM 8.05
CHEMBL3094131 — IC50 = 10.96 nM 7.96
CHEMBL239507 — IC50 = 12.88 nM 7.89
CHEMBL3094038 — IC50 = 14.13 nM 7.85
CHEMBL572534 — IC50 = 15.14 nM 7.82
CHEMBL575093 — IC50 = 15.85 nM 7.80
CHEMBL3094021 — IC50 = 16.98 nM 7.77
CHEMBL3094024 — IC50 = 20.89 nM 7.68
CHEMBL575931 — IC50 = 23.99 nM 7.62
CHEMBL3091489 — IC50 = 26.92 nM 7.57
CHEMBL3094008 — IC50 = 28.18 nM 7.55
CHEMBL3094022 — IC50 = 28.84 nM 7.54
CHEMBL575738 — IC50 = 30.2 nM 7.52
CHEMBL3094018 — IC50 = 33.88 nM 7.47
CHEMBL3093991 — IC50 = 36.31 nM 7.44
CHEMBL3094011 — IC50 = 38.9 nM 7.41
CHEMBL577616 — IC50 = 39.81 nM 7.40
CHEMBL3094031 — IC50 = 39.81 nM 7.40
CHEMBL3094025 — IC50 = 43.65 nM 7.36
CHEMBL3094005 — IC50 = 45.71 nM 7.34
CHEMBL3094030 — IC50 = 47.86 nM 7.32
CHEMBL239508 — IC50 = 52.48 nM 7.28
CHEMBL3094000 — IC50 = 61.66 nM 7.21
CHEMBL3094001 — IC50 = 74.13 nM 7.13
CHEMBL3094039 — IC50 = 77.62 nM 7.11
CHEMBL3093990 — IC50 = 100.0 nM 7.00
CHEMBL3094003 — IC50 = 100.0 nM 7.00
CHEMBL3094035 — IC50 = 102.33 nM 6.99
CHEMBL3093996 — IC50 = 114.82 nM 6.94
CHEMBL3093997 — IC50 = 125.89 nM 6.90
CHEMBL3094132 — IC50 = 204.17 nM 6.69
CHEMBL3094026 — IC50 = 208.93 nM 6.68
CHEMBL3094036 — IC50 = 218.78 nM 6.66
CHEMBL3094034 — IC50 = 234.42 nM 6.63
CHEMBL3093995 — IC50 = 263.03 nM 6.58
CHEMBL3094004 — IC50 = 316.23 nM 6.50
CHEMBL3093999 — IC50 = 407.38 nM 6.39
CHEMBL3094033 — IC50 = 416.87 nM 6.38
CHEMBL3094133 — IC50 = 446.68 nM 6.35
CHEMBL3094028 — IC50 = 478.63 nM 6.32
CHEMBL3094029 — IC50 = 489.78 nM 6.31
CHEMBL3094019 — IC50 = 501.19 nM 6.30
CHEMBL3093998 — IC50 = 575.44 nM 6.24