General
Preferred name
GSK-2879552
Synonyms
GSK2879552 ()
GSK2879552 (dihydrochloride) ()
GSK2879552 2HCl ()
GSK2879552 2HCl (1401966-69-5(free base)) ()
P&D ID
PD016998
CAS
1401966-69-5
1902123-72-1
Tags
available
drug candidate
Drug indication
Small-cell lung cancer
Myelodysplastic syndrome
Drug Status
investigational
Max Phase
1.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1; officially known as lysine demethylase 1A, KDM1A). It was investigated for potential to modulate epigenetic regulation in cancer, but the programme was terminated due to serious adverse events becoming evident in early trials . GSK2879552-induced LDS1 inhibition causes expression of proteins indicative of a differentiated immunophenotype. GSK2879552 is Example 26 claimed in patent WO2012135113 .
(GtoPdb)
DESCRIPTION
GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A), with potential antineoplastic activity[1][2].
PRICE
820
DESCRIPTION
GSK2879552 is a selective, orally bioavailable, irreversible, mechanism-based inactivator of lysine-specific demethylase 1 (LSD1)/corepressor, with potential antineoplastic activity.
DESCRIPTION
GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity[1][2].
PRICE
166
DESCRIPTION
GSK2879552 has been found to be a LSD1 inhibitor that could have antineoplastic effect through restraining the growth of overexpressed tumor cells. It was just planed a Phase I/II trail by GSK against Myelodysplastic syndromes.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
GSK2879552 2HCl is a selective, orally bioavailable and irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
2
Organisms
0
Compound Sets
12
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
27
Molecular Weight
364.22
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
4
Aromatic Ring Count
2
cLogP
3.74
TPSA
52.57
Fraction CSP3
0.43
Chiral centers
2.0
Largest ring
6.0
QED
0.79
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
LSD1
KDM1A
Histone Demethylase,LSD1
MOA
Histone Demethylase
histone lysine demethylase inhibitor
Pathway
Epigenetics
Chromatin/Epigenetic
Solubility
Water: 44 mg/mL
DMSO: 29 mg/mL
DMSO: 31 mg/mL
Source data
