Search Ontology:
ChEBI

GSK126

Term ID
CHEBI:124921
Synonyms
  • (S)-1-(sec-butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide
  • 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-3-methyl-6-[6-(piperazin-1-yl)pyridin-3-yl]-1H-indole-4-carboxamide
  • GSK 126
  • GSK 2816126
  • GSK 2816126A
  • GSK-126
  • GSK-2816126
  • GSK-2816126A
  • GSK2816126
  • GSK2816126A
Definition
A member of the class of methylindoles that is 1H-indole substituted by (2S)-butan-2-yl, methyl, N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]acetamide, and 6-(piperazin-1-yl)pyridin-3-yl groups at positions 1, 3, 4, and 6, respectively. It is a potent and highly selective inhibitor of EZH2 methyltransferase (IC50 = 9.9 nM).
References
  • cas:1346574-57-9
  • lincs.smallmolecule:LSM-36365
  • pdb-ccd:A9G
  • pubmed:23051747
  • pubmed:26898301
  • pubmed:27868408
  • pubmed:27926488
  • pubmed:29070525
  • pubmed:29545866
  • pubmed:29654753
  • pubmed:29904056
  • pubmed:30737232
  • pubmed:31471312
  • pubmed:32298702
  • pubmed:32529327
  • pubmed:32606728
  • pubmed:32772228
  • pubmed:32805266
  • pubmed:32906688
  • pubmed:33085231
  • pubmed:33467134
  • pubmed:34149887
  • pubmed:35091962
  • pubmed:35864094
  • pubmed:36087682
  • pubmed:36469862
  • pubmed:36652457
  • pubmed:36734909
  • pubmed:37010741
  • pubmed:37558192
  • pubmed:37644332
  • pubmed:37989985
  • pubmed:38009194
  • pubmed:38362910
  • pubmed:38446700
  • pubmed:38530086
Ontology
ChEBI  ( EBI )
Relationships
Phenotype
Phenotype resulting from GSK126
Phenotype where environments contain GSK126
Phenotype modified by environments containing GSK126
Phenotype affecting GSK126
Human Disease Model