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Assay Detail

CHEMBL2060937

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

Binding
Inhibition of human recombinant MAO-B using kynuramine as substrate preincubated with compound for 15 mins measured after 20 mins by fluorometric analysis
ChEMBL ↗
51
Total Activities
51
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

Synthesis and evaluation of aplysinopsin analogs as inhibitors of human monoamine oxidase A and B.
Lewellyn K, Bialonska D, Chaurasiya ND, Tekwani BL, Zjawiony JK.
Bioorg Med Chem Lett (2012) 22 : 4926 -4929
PubMed 22781190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 5.13 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL972 SELEGILINE 4.0 1 7.35
CHEMBL2058428 — — 1 6.68
CHEMBL2058427 — — 1 6.43
CHEMBL2058694 — — 1 6.35
CHEMBL463249 — — 1 6.35
CHEMBL2058697 — — 1 5.91
CHEMBL2058700 — — 1 5.85
CHEMBL2058704 — — 1 5.70
CHEMBL2058701 — — 1 5.61
CHEMBL2058695 — — 1 5.59
CHEMBL2058696 — — 1 5.59
CHEMBL2058417 — — 1 5.57
CHEMBL1170237 — — 1 5.57
CHEMBL2058429 — — 1 5.55
CHEMBL2058420 — — 1 5.51
CHEMBL2058698 — — 1 5.43
CHEMBL2058413 — — 1 5.42
CHEMBL2058425 — — 1 5.37
CHEMBL2058412 — — 1 5.37
CHEMBL2058426 — — 1 5.28
CHEMBL2058702 — — 1 5.22
CHEMBL2058703 — — 1 5.15
CHEMBL2058699 — — 1 5.06
CHEMBL512332 METHYLAPLYSINOPSIN — 1 5.04
CHEMBL404232 APLYSINOPSIN — 1 5.00
CHEMBL2058152 — — 1 4.95
CHEMBL2058416 — — 1 4.93
CHEMBL2058418 — — 1 4.89
CHEMBL2058414 — — 1 4.85
CHEMBL2058423 — — 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL972 SELEGILINE IC50 = 45.0 nM 7.35
CHEMBL2058428 — IC50 = 207.0 nM 6.68
CHEMBL2058427 — IC50 = 370.0 nM 6.43
CHEMBL2058694 — IC50 = 450.0 nM 6.35
CHEMBL463249 — IC50 = 447.0 nM 6.35
CHEMBL2058697 — IC50 = 1237.0 nM 5.91
CHEMBL2058700 — IC50 = 1417.0 nM 5.85
CHEMBL2058704 — IC50 = 2000.0 nM 5.70
CHEMBL2058701 — IC50 = 2433.0 nM 5.61
CHEMBL2058695 — IC50 = 2567.0 nM 5.59
CHEMBL2058696 — IC50 = 2567.0 nM 5.59
CHEMBL2058417 — IC50 = 2667.0 nM 5.57
CHEMBL1170237 — IC50 = 2700.0 nM 5.57
CHEMBL2058429 — IC50 = 2817.0 nM 5.55
CHEMBL2058420 — IC50 = 3117.0 nM 5.51
CHEMBL2058698 — IC50 = 3733.0 nM 5.43
CHEMBL2058413 — IC50 = 3800.0 nM 5.42
CHEMBL2058425 — IC50 = 4260.0 nM 5.37
CHEMBL2058412 — IC50 = 4300.0 nM 5.37
CHEMBL2058426 — IC50 = 5217.0 nM 5.28
CHEMBL2058702 — IC50 = 6000.0 nM 5.22
CHEMBL2058703 — IC50 = 7033.0 nM 5.15
CHEMBL2058699 — IC50 = 8750.0 nM 5.06
CHEMBL512332 METHYLAPLYSINOPSIN IC50 = 9017.0 nM 5.04
CHEMBL404232 APLYSINOPSIN IC50 = 10017.0 nM 5.00
CHEMBL2058152 — IC50 = 11333.0 nM 4.95
CHEMBL2058416 — IC50 = 11633.0 nM 4.93
CHEMBL2058418 — IC50 = 12833.0 nM 4.89
CHEMBL2058414 — IC50 = 14267.0 nM 4.85
CHEMBL2058423 — IC50 = 16767.0 nM 4.78
CHEMBL2058705 — IC50 = 20700.0 nM 4.68
CHEMBL541474 — IC50 = 24333.0 nM 4.61
CHEMBL1173331 — IC50 = 24500.0 nM 4.61
CHEMBL2058153 — IC50 = 25333.0 nM 4.60
CHEMBL2058424 — IC50 = 25733.0 nM 4.59
CHEMBL2058415 — IC50 = 26333.0 nM 4.58
CHEMBL2058706 — IC50 = 26000.0 nM 4.58
CHEMBL2058422 — IC50 = 26833.0 nM 4.57
CHEMBL2058154 — IC50 = 27800.0 nM 4.56
CHEMBL2058151 — IC50 = 28333.0 nM 4.55
CHEMBL2058421 — IC50 = 30467.0 nM 4.52
CHEMBL2058150 — IC50 = 33000.0 nM 4.48
CHEMBL508657 ISOPLYSIN A IC50 = 33833.0 nM 4.47
CHEMBL2058410 — IC50 = 34333.0 nM 4.46
CHEMBL2058409 — IC50 = 34333.0 nM 4.46
CHEMBL2058408 — IC50 = 35667.0 nM 4.45
CHEMBL2058411 — IC50 = 37000.0 nM 4.43
CHEMBL1173525 — IC50 = 43167.0 nM 4.37
CHEMBL2058419 — IC50 = 51167.0 nM 4.29
CHEMBL1982267 — IC50 = 59333.0 nM 4.23