General Information of Drug (ID: DMEJMTR)

Drug Name
GSK1440115 Drug Info
Synonyms
UNII-GCT6G5G3C7; GCT6G5G3C7; GSK 1440115; SCHEMBL2957737; 4'-(1-(((6,7-Dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetyl)(methyl)amino)-2-(4-morpholinyl)ethyl)-4-diphenylcarboxylic acid; (1,1'-Biphenyl)-4-carboxylic acid, 4'-((1R)-1-((2-(6,7-dichloro-2,3-dihydro-3-oxo-4H-1,4-benzoxazin-4-yl)acetyl)methylamino)-2-(4-morpholinyl)ethyl)-
Indication
Disease Entry ICD 11 Status REF
Asthma CA23 Phase 1 [1]
Cross-matching ID
PubChem CID
24760693
CAS Number
CAS 1003878-16-7
TTD Drug ID
DMEJMTR

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
SB-436811 DMLPB0X Asthma CA23 Phase 1 [3]
PALOSURAN DMWCLZ6 Renal failure GB60-GB6Z Discontinued in Phase 2 [3]
SAR101099 DMIZ7Q4 Diabetic nephropathy GB61.Z Discontinued in Phase 1 [4]
ICI-199441 DMEWZ80 Discovery agent N.A. Investigative [5]
SB-328872 DMT1KFL Discovery agent N.A. Investigative [6]
Ac-[CFWKFC]-NH2 DM9IN4T Discovery agent N.A. Investigative [3]
Ac-FWKY-NH2 DM3XHIY Discovery agent N.A. Investigative [3]
Ac-[CFWkYC]-NH2 DMW24UH Discovery agent N.A. Investigative [3]
urotensin II-related peptide DMCE3PJ Discovery agent N.A. Investigative [7]
SB-611812 DMASQV4 Discovery agent N.A. Investigative [8]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Urotensin II receptor (UTS2R) TTW5UDX UR2R_HUMAN Antagonist [2]

References

1 ClinicalTrials.gov (NCT01424280) Single Dose Study of GSK1440115 in Patients With Asthma. U.S. National Institutes of Health.
2 Effects of Urotensin II Receptor Antagonist, GSK1440115, in Asthma. Front Pharmacol. 2013; 4: 54.
3 Urotensin-II receptor modulators as potential drugs. J Med Chem. 2010 Apr 8;53(7):2695-708.
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. (Target id: 365).
5 Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9.
6 Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3950-4.
7 Identification of urotensin II-related peptide as the urotensin II-immunoreactive molecule in the rat brain. Biochem Biophys Res Commun. 2003 Oct 24;310(3):860-8.
8 A role for urotensin II in restenosis following balloon angioplasty: use of a selective UT receptor blocker. J Mol Cell Cardiol. 2005 Nov;39(5):785-91.