GSK-LSD1 | GSK-LSD1 : Inhibitor of KDM1A
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Control Compounds

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KDM1A
  • EC50:0.1-10 nM
Inhibitor
100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
> 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B).
Selectivity Assessment Description:
LSD-1 at 10 µM showed no activity against 55 human recombinant receptors in the CEREP ExpresSProfi ...

Potency
Cellular
In Vitro

KDM1A

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1016/j.ccell.2015.06.002

In Vivo Validations

Mouse
Dose: 5 mg/kg
Route of delivery: Intraperitoneal
Plasma half life: 3.6 hr

DOI Reference: 10.1016/j.ccell.2015.06.002

Chemical Information

Molecular Formula C14H20N2
SMILEs c1ccc([C@@H]2C[C@H]2NC2CCNCC2)cc1
InChI InChI=1S/C14H20N2/c1-2-4-11(5-3-1)13-10-14(13)16-12-6-8-15-9-7-12/h1-5,12-16H,6-10H2/t13-,14+/m0/s1
Molecular weight 216.16 Da
AlogP 1.8841
HBond acceptors 2
HBond donors 2
Atoms 36

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Expert Reviews


(on 7 Mar 2026 )
Cellular Use Rating
In Model Organisms
There is a broad range of LSD1 inhibitors reported in the literature. GSK-LSD1 is the prototype of the most common covalent inhibitors and is widely used in cellular systems. While catalytic inhibitors...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria