Details of the Drug-Related molecule(s) Interaction Atlas

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 Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Discontinued Drug(s)

Investigative Drug(s)

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Drug(s) Targeting Urotensin II receptor (UTS2R)

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]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

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

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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.