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

General Information of Drug (ID: DMEL5SV)

Drug Name

FR139317 Drug Info

Synonyms

D-Alanine, N-((hexahydro-1H-azepin-1-yl)carbonyl)-L-leucyl-1-methyl-D-tryptophyl-3-(2-pyridinyl)-; FR 139317; 142375-60-8; CHEMBL352396; 2-((1-(Hexahydro-1H-azepinyl)carbonyl)amino-4-methylpentanoyl)-3-(-(1-methyl-1H-indolyl)propionyl)amino-3-(2-pyridyl)propionic acid; D-Alanine, N-(N-(N-((hexahydro-1H-azepin-1-yl)carbonyl)-L-leucyl)-1-methyl-D-tryptophyl)-3-(2-pyridinyl)-; GSK424887

Indication

Disease Entry	ICD 11	Status	REF
Hypertension	BA00-BA04	Phase 2	[1]
Anxiety disorder	6B00-6B0Z	Discontinued in Phase 1	[2]
Depression	6A70-6A7Z	Discontinued in Phase 1	[2]

Cross-matching ID

PubChem CID: 107810
CAS Number: CAS 142375-60-8
TTD Drug ID: DMEL5SV

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Endothelin A receptor (EDNRA)	TTKRD0G	EDNRA_HUMAN	Antagonist	[3]
Substance-P receptor (TACR1)	TTZPO1L	NK1R_HUMAN	Antagonist	[4]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Substance-P receptor (TACR1)	DTT	TACR1	3.597	4.186	4.271	5.113
Endothelin A receptor (EDNRA)	DTT	EDNRA	3.776	4.505	5.121	3.536

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease

Hypertension

ICD Disease Classification

BA00-BA04

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Substance-P receptor (TACR1)	DTT	TACR1	7.40E-01	0.02	0.07
Substance-P receptor (TACR1)	DTT	TACR1	8.57E-01	-0.02	-0.18

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

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: 998).
2	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027682)
3	Reduction of bFGF-induced smooth muscle cell proliferation and endothelin receptor mRNA expression by mevastatin and atorvastatin. Biochem Pharmacol. 2002 Aug 1;64(3):497-505.
4	Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).