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

General Information of Drug (ID: DMBJQU6)

• Drug Name: CGP-49823 Drug Info
• Synonyms: CGP-49823; CHEMBL290364; cgp49823; SCHEMBL6904655; BDBM50287397; {(R)-2-Benzyl-4-[(quinolin-4-ylmethyl)-amino]-piperidin-1-yl}-(3,5-dimethyl-phenyl)-methanone

Indication

Disease Entry	ICD 11	Status	REF
Pain	MG30-MG3Z	Discontinued in Phase 2	[1]

• Cross-matching ID:
  PubChem CID: 9869033
  CAS Number: CAS 150705-88-7
  TTD Drug ID: DMBJQU6

Molecule-Related Drug Atlas

Drug(s) Targeting Substance-P receptor (TACR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aprepitant	DM053KT	Depression	6A70-6A7Z	Approved	[3]
Selegiline	DM6034S	Major depressive disorder	6A70.3	Approved	[4]
Rolapitant	DM8XP26	Chemotherapy-induced nausea	MD90	Approved	[5]
Netupitant	DMEKAYI	Chemotherapy-induced nausea	MD90	Phase 3	[5]
Serlopitant	DM5VH6U	Prurigo nodularis	EC91.0	Phase 3	[6]
LY-686017	DM7WORZ	Atopic dermatitis	EA80	Phase 3	[7]
Elinzanetant	DMC6EFI	Hot flushes	GA30	Phase 3	[8]
CP-122721	DMSWLM5	Major depressive disorder	6A70.3	Phase 2	[9]
FR139317	DMEL5SV	Hypertension	BA00-BA04	Phase 2	[4]
VOFOPITANT HYDROCHLORIDE	DMQMYP5	Vomiting	MD90	Phase 2	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Substance-P receptor (TACR1)	TTZPO1L	NK1R_HUMAN	Antagonist	[2]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004456)
• [2] The potency of the novel tachykinin receptor antagonist CGP49823 at rat and gerbil motoneurones in vitro. Eur J Pharmacol. 1998 Jan 26;342(2-3):203-8.
• [3] Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46.
• [4] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [5] Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.
• [6] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [7] Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498.
• [8] Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3221-e3234.
• [9] A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
• [10] Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58.