GSK-LSD1 |
GSK-LSD1 : Inhibitor of KDM1A
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| KDM1A |
|
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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