General Information of Drug (ID: DM6SANW)

Drug Name
TD-5108 Drug Info
Synonyms
Velusetrag; TD-5108; UNII-J4VNV64ARB; J4VNV64ARB; Velusetrag [USAN:INN]; SCHEMBL2917361; GTPL8425; CHEMBL2087337; Serotonin 5-HT4 Receptor Agonists; BDBM50391069; ZINC15821733; TD 5108; DB12702; compound 15 [PMID 22959244]; N-((1R,3R,5S)-8-((2R)-2-hydroxy-3-(methyl(methylsulfonyl)amino)propyl)-8-azabicyclo(3.2.1)oct-3-yl)-1-(1-methylethyl)-2-oxo-1,2-dihydroquinoline-3-carboxamide; 3-Quinolinecarboxamide, 1,2-dihydro-N-((3-endo)-8-((2R)-2-hydroxy-3-(methyl(methylsulfonyl)amino)propyl)-8-azabicyclo(3.2.1)oct-3-yl)-1-(1-meth
Indication
Disease Entry ICD 11 Status REF
Gastroparesis DA41.00 Phase 2 [1] , [2]
Cross-matching ID
PubChem CID
11842633
CAS Number
CAS 866933-46-2
TTD Drug ID
DM6SANW
VARIDT Drug ID
DR00763

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 4 receptor (HTR4) TT07C3Y 5HT4R_HUMAN Agonist [3] , [4]

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

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
5-HT 4 receptor (HTR4) DTT HTR4 5.776 4.945 5.062 4.828
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 Gastroparesis
ICD Disease Classification DA41.00
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
5-HT 4 receptor (HTR4) DTT HTR4 6.16E-01 -0.03 -0.24
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: 8425).
2 ClinicalTrials.gov (NCT00391820) Evaluate the Safety and Efficacy of a 5-HT4 Agonist in Chronic Constipation (ACCORD Trial). U.S. National Institutes of Health.
3 The in vitro pharmacological profile of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):125-37.
4 The in vivo gastrointestinal activity of TD-5108, a selective 5-HT(4) receptor agonist with high intrinsic activity. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jul;378(1):139-47.