Compound name
GSK-LSD1
Protein family
KDM
Target name
KDM1A/LSD1@Demethylase
Affinity biochemical (nM)
16
CG-Set
Other targets
Recommended Concentration
100 nM
Compound EUbOPEN ID
EUB0000213bCl
SMILES
Cl.Cl.c1ccc([C@@H]2C[C@H]2NC2CCNCC2)cc1
InChIKey
PJFZOGMSPBHPNS-WICJZZOFSA-N
NCBI gene ID
23028
UniProt ID
O60341
Synonyms
KIAA0601, BHC110, LSD1
Mode of action
Irreversible, mechanism based inhibitor
Affinity biochemical definition
IC50
Affinity biochemical assay type
Enzyme inhibition assay
Affinity Biochemical Source Knowledge
https://www.thesgc.org/chemical-probes/GSK-LSD1
Affinity biochemical relation
=
Selectivity platform
CEREP ExpressProfile selectivity/specificity profile
Selectivity platform number of targets
55
Selectivity remarks
Screened against 55 human recombinant receptors at 10 µM, closest targets as % inhibition: 5-HT1A (49%), 5-HAT (74%), dopamine transporter (39%); Screened against 45 other enzymes (GPCRs, kinases, transporters, ion channels, nuclear receptors), >1000-fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B)
Selectivity Source Knowledge
https://doi.org/10.1016/j.ccell.2015.06.002
https://www.thesgc.org/chemical-probes/GSK-LSD1
Selectivity Number of Off-targets
0