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Assay Detail

CHEMBL3388873

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

Binding
Inhibition of human recombinant MAOA expressed in Pichia pastoris incubated for 20 mins by bioluminescent-coupled assay
19
Total Activities
19
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] A (CHEMBL1951)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological activity and mechanistic insights of 1-substituted cyclopropylamine derivatives: a novel class of irreversible inhibitors of histone demethylase KDM1A.
Vianello P, Botrugno OA, Cappa A, Ciossani G, Dessanti P, Mai A, Mattevi A, Meroni G, Minucci S, Thaler F, Tortorici M, Trifiró P, Valente S, Villa M, Varasi M, Mercurio C.
Eur J Med Chem (2014) 86 : 352 -363
PubMed 25173853 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.20 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3330334 1 7.67
CHEMBL3330339 1 7.16
CHEMBL3330331 1 7.08
CHEMBL3330341 1 7.03
CHEMBL3330328 1 6.77
CHEMBL3330337 1 6.63
CHEMBL3330330 1 6.28
CHEMBL3989843 TRANYLCYPROMINE 4.0 1 5.92
CHEMBL3330333 1 5.89
CHEMBL3330335 1 5.89
CHEMBL3330340 1 5.84
CHEMBL3330329 1 5.72
CHEMBL3330338 1 5.59
CHEMBL3330332 1 5.46
CHEMBL3330336 1 5.17
CHEMBL3330342 1 5.08
CHEMBL3330343 1 -
CHEMBL3330344 1 -
CHEMBL3330345 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3330334 IC50 = 21.4 nM 7.67
CHEMBL3330339 IC50 = 70.0 nM 7.16
CHEMBL3330331 IC50 = 82.8 nM 7.08
CHEMBL3330341 IC50 = 94.0 nM 7.03
CHEMBL3330328 IC50 = 170.0 nM 6.77
CHEMBL3330337 IC50 = 235.0 nM 6.63
CHEMBL3330330 IC50 = 527.0 nM 6.28
CHEMBL3989843 TRANYLCYPROMINE IC50 = 1190.0 nM 5.92
CHEMBL3330333 IC50 = 1300.0 nM 5.89
CHEMBL3330335 IC50 = 1280.0 nM 5.89
CHEMBL3330340 IC50 = 1430.0 nM 5.84
CHEMBL3330329 IC50 = 1920.0 nM 5.72
CHEMBL3330338 IC50 = 2590.0 nM 5.59
CHEMBL3330332 IC50 = 3510.0 nM 5.46
CHEMBL3330336 IC50 = 6800.0 nM 5.17
CHEMBL3330342 IC50 = 8310.0 nM 5.08
CHEMBL3330343 IC50 - -
CHEMBL3330344 IC50 - -
CHEMBL3330345 IC50 - -