General Information of Drug (ID: DMX2U7G)

Drug Name
bromo-deaza-SAH Drug Info
Synonyms
CHEMBL2349526; bromo-deaza-SAH; (2s)-2-Amino-4-({[(2s,3s,4r,5r)-5-(4-Amino-5-Bromo-7h-Pyrrolo[2,3-D]pyrimidin-7-Yl)-3,4-Dihydroxytetrahydrofuran-2-Yl]methyl}sulfanyl)butanoic Acid (Non-Preferred Name); GTPL7018; BDBM50431676; (S)-2-Amino-4-[[(2S)-3beta,4beta-dihydroxy-5alpha-(4-amino-5-bromo-7H-pyrrolo[2,3-d]pyrimidine-7-yl)tetrahydrofuran-2alpha-yl]methylthio]butanoic acid; (2S)-2-amino-4-[[(2S,3S,4R,5R)-5-(4-amino-5-bromopyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxyoxolan-2-yl]methylsulfanyl]butanoic acid
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
53339032
TTD Drug ID
DMX2U7G

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
EPZ-5676 DMN2FS3 Acute myeloid leukaemia 2A60 Phase 1/2 [3]
EPZ-004777 DMLN4V5 leukaemia 2A60-2B33 Investigative [4]
SGC0946 DMP35VS Discovery agent N.A. Investigative [5]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histone-lysine N-methyltransferase (HLNM) TTSZ8T1 DOT1L_HUMAN Inhibitor [2]

References

1 DOT1L, the H3K79 methyltransferase, is required for MLL-AF9-mediated leukemogenesis. Blood. 2011 Jun 23;117(25):6912-22.
2 Bromo-deaza-SAH: a potent and selective DOT1L inhibitor. Bioorg Med Chem. 2013 Apr 1;21(7):1787-94.
3 Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Blood. 2013 August 8; 122(6): 1017-1025.
4 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7377).
5 Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors. Nat Commun. 2012;3:1288.