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

General Information of Drug (ID: DMLQ71Y)

Drug Name
GR-159897 Drug Info
Synonyms
CHEMBL2110370; GR 159897; 158848-32-9; 5-FLUORO-3-[2-[4-METHOXY-4-[[(R)-PHENYLSULPHINYL]METHYL]-1-PIPERIDINYL]ETHYL]-1H-INDOLE; GR-159897; GR-159,897; GTPL2115; CHEBI:92912; MolPort-023-276-059; ZINC7999073; BDBM50212987; AKOS025147300; AKOS024456505; NCGC00381706-02; KB-309739; SR-01000597395; SR-01000597395-1; 5-fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]piperidin-1-yl]ethyl]-1H-indole; 5-Fluoro-3-[2-[4-methoxy-4-[[ -phenylsulphinyl]methyl]-1-piperidinyl]ethyl]-1H-indole
Indication
Disease Entry ICD 11 Status REF
Anxiety disorder 6B00-6B0Z Terminated [1]
Cross-matching ID
PubChem CID
9953599
ChEBI ID
CHEBI:92912
CAS Number
CAS 158848-32-9
TTD Drug ID
DMLQ71Y

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Substance-K receptor (TACR2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ibodutant DMT67EH Irritable bowel syndrome DD91.0 Phase 3 [3]
PMX-53 DMZUAJ4 Atopic dermatitis EA80 Phase 2 [4]
Rambazole DMP2DNS Psoriasis vulgaris EA90 Phase 2 [5]
Nepadutant DMPMF6L Infantile colics DD93.1 Phase 1/2 [6]
Saredutant DMSRJY3 Anxiety disorder 6B00-6B0Z Discontinued in Phase 3 [7]
CS-003 DM1AEVT Chronic obstructive pulmonary disease CA22 Discontinued in Phase 2 [8]
FK-224 DM1JUS0 Asthma CA23 Discontinued in Phase 2 [9]
DNK-333 DM4ZO01 Irritable bowel syndrome DD91.0 Discontinued in Phase 2 [10]
AVE-5883 DM3P84V Asthma CA23 Discontinued in Phase 1/2 [11]
UK-224671 DMDTRJB Urinary incontinence MF50.2 Discontinued in Phase 1 [12]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Substance-K receptor (TACR2) TTYO0A3 NK2R_HUMAN Modulator [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: 2115).
2 GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Eur J Pharmacol. 1995 Jan 16;272(2-3):241-8.
3 Antagonist profile of ibodutant at the tachykinin NK2 receptor in guinea pig isolated bronchi. Eur J Pharmacol. 2013 Nov 15;720(1-3):180-5.
4 Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
5 Pharmacology of an original and selective nonpeptide antagonist ligand for the human tachykinin NK2 receptor. Eur J Pharmacol. 2005 Jun 1;516(2):104-11.
6 Emerging drugs for postoperative ileus. Expert Opin Emerg Drugs. 2007 Nov;12(4):619-26.
7 Characterization of species-related differences in the pharmacology of tachykinin NK receptors 1, 2 and 3. Biochem Pharmacol. 2009 May 1;77(9):1522-30.
8 Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
9 Effects of FK224, a novel compound NK1 and NK2 receptor antagonist, on airway constriction and airway edema induced by neurokinins and sensory nerv... J Pharmacol Exp Ther. 1992 Jul;262(1):403-8.
10 Dual tachykinin NK1/NK2 antagonist DNK333 inhibits neurokinin A-induced bronchoconstriction in asthma patients. Eur Respir J. 2004 Jan;23(1):76-81.
11 Effect of an NK1/NK2 receptor antagonist on airway responses and inflammation to allergen in asthma. Am J Respir Crit Care Med. 2007 Mar 1;175(5):450-7.
12 Pharmacokinetics and metabolism of a sulphamide NK2 antagonist in rat, dog and human. Xenobiotica. 2000 Jun;30(6):627-42.