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

General Information of Drug (ID: DMSDY2Z)

• Drug Name: [3H]A-585539 Drug Info
• Synonyms: [3H]A-585539; GTPL3974; SCHEMBL18833113

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 23643135
  TTD Drug ID: DMSDY2Z

Molecule-Related Drug Atlas

Drug(s) Targeting Neuronal acetylcholine receptor alpha-7 (CHRNA7)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ziprasidone	DMM58JY	Bipolar disorder	6A60	Approved	[3]
ALCURONIUM	DM2U4XQ	Anaesthesia	9A78.6	Approved	[4]
AMG 386	DMQJXL4	Breast cancer	2C60-2C65	Phase 3	[5]
CYTISINE	DMUF0BJ	Tobacco dependence	6C4A.2	Phase 3	[6]
EVP-6124	DMLQO7F	Alzheimer disease	8A20	Phase 3	[7]
GTS-21	DMEN5KA	Parkinson disease	8A00.0	Phase 2	[8]
JNJ-39393406	DMUOEKM	Depression	6A70-6A7Z	Phase 2	[9]
ABT-126	DM2OS51	Alzheimer disease	8A20	Phase 2	[10]
TC-6987	DMNFP21	Asthma	CA23	Phase 2	[11]
AQW-051	DMD2RFO	Alzheimer disease	8A20	Phase 2	[12]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Neuronal acetylcholine receptor alpha-7 (CHRNA7)	TTLA931	ACHA7_HUMAN	Agonist	[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: 3974).
• [2] [3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic... J Pharmacol Exp Ther. 2008 Jan;324(1):179-87.
• [3] The pipeline and future of drug development in schizophrenia. Mol Psychiatry. 2007 Oct;12(10):904-22.
• [4] Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine re... J Med Chem. 2007 Sep 20;50(19):4616-29.
• [5] Clinical pipeline report, company report or official report of Roche (2009).
• [6] 3,5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessation. Bioorg Med Chem Lett. 2005 Nov 15;15(22):4889-97.
• [7] Normalizing effects of EVP-6124, an alpha-7 nicotinic partial agonist, on event-related potentials and cognition: a proof of concept, randomized trial in patients with schizophrenia. J Psychiatr Pract. 2014 Jan;20(1):12-24.
• [8] The brain alpha7 nicotinic receptor may be an important therapeutic target for the treatment of Alzheimer's disease: studies with DMXBA (GTS-21). Behav Brain Res. 2000 Aug;113(1-2):169-81.
• [9] Allosteric alpha-7 nicotinic receptor modulation and P50 sensory gating in schizophrenia: a proof-of-mechanism study. Neuropharmacology. 2013 Jan;64:197-204.
• [10] A phase 2 randomized, controlled trial of the alpha7 agonist ABT-126 in mild-to-moderate Alzheimer's dementia. Alzheimer's & Dementia: Translational Research & Clinical Interventions Volume 1, Issue 1, June 2015, Pages 81-90.
• [11] ClinicalTrials.gov (NCT01293669) Glycemic Control, Safety and Tolerability of TC-6987 Monotherapy in Type 2 Diabetes Mellitus. U.S. National Institutes of Health.
• [12] AQW051, a novel and selective nicotinic acetylcholine receptor alpha7 partial agonist, reduces l-Dopa-induced dyskinesias and extends the duration of l-Dopa effects in parkinsonian monkeys. Parkinsonism Relat Disord. 2014 Nov;20(11):1119-23.