General Information of Drug (ID: DMGPRT7)

Drug Name
E339-3D6 Drug Info
Synonyms
E339-3D6; GTPL6187; 4-{[(1-{[2-(1-benzyl-3-methyl-1H-imidazol-3-ium-4-yl)-1-[(1-methylpiperidin-1-ium-4-yl)carbamoyl]ethyl]carbamoyl}-5-({[12-({4-[6-(diethylamino)-3-(diethyliminiumyl)-3H-xanthen-9-yl]-3-sulfobenzene}sulfonamido)dodecyl]carbamoyl}amino)pentyl)carbamoyl]methyl}-2-imino-3-methyl-2,3-dihydro-1,3-thiazol-3-ium tritrifluoroacetate
Indication
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [1]
Cross-matching ID
PubChem CID
73755182
TTD Drug ID
DMGPRT7

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Investigative Drug(s)
Drug(s) Targeting Apelin receptor (APLNR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AMG 986 DMZQ2DK Heart failure BD10-BD13 Phase 1 [3]
apelin-13 DM2CKUZ Discovery agent N.A. Investigative [4]
ML221 DM3OEP4 Discovery agent N.A. Investigative [5]
ML233 DM8CIE4 Discovery agent N.A. Investigative [6]

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Apelin receptor (APLNR) TTJ8E43 APJ_HUMAN Agonist [2]

References

1 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: 6187).
2 Identification and pharmacological properties of E339-3D6, the first nonpeptidic apelin receptor agonist. FASEB J. 2010 May;24(5):1506-17.
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Structural and functional study of the apelin-13 peptide, an endogenous ligand of the HIV-1 coreceptor, APJ. Biochemistry. 2003 Sep 2;42(34):10163-8.
5 Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60.
6 Functional Agonists of the Apelin (APJ) Receptor. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010.