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

General Information of Drug (ID: DMT0CR5)

• Drug Name: KST-5468 Drug Info
• Synonyms: T-type calcium channel antagonist (pain); T-type calcium channel antagonist (pain), SNU/KIST

Indication

Disease Entry	ICD 11	Status	REF
Pain	MG30-MG3Z	Investigative	[1]

• Cross-matching ID: TTD Drug ID: DMT0CR5

Molecule-Related Drug Atlas

Drug(s) Targeting Voltage-gated calcium channel alpha Cav3.2 (CACNA1H)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sodium bicarbonate	DMMU6BJ	Metabolic acidosis	5C73	Approved	[2]
Flunarizine	DMZU5JP	Migraine	8A80	Approved	[3]
ABT-639	DMEWQ4X	Pain	MG30-MG3Z	Phase 2	[4]
Mibefradil	DMU9VDS	Glioblastoma multiforme	2A00.0	Phase 1	[5]
TTA-A8	DMWZCIF	Insomnia	7A00-7A0Z	Preclinical	[6]
U-92032	DMTYO3P	N. A.	N. A.	Terminated	[7]
ML218	DM3D21X	Discovery agent	N.A.	Investigative	[8]
KYS-05001	DM3MID9	Discovery agent	N.A.	Investigative	[9]
KYS-05077	DMHW40F	Discovery agent	N.A.	Investigative	[10]
KYS-05080	DM57BXZ	Discovery agent	N.A.	Investigative	[10]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated calcium channel alpha Cav3.2 (CACNA1H)	TTZPWGN	CAC1H_HUMAN	Antagonist	[1]

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. (Target id: 536).
• [2] Acute renal failure. Clin Evid (Online). 2008 Sep 3;2008. pii: 2001.
• [3] Positive allosteric interaction of structurally diverse T-type calcium channel antagonists. Cell Biochem Biophys. 2009;55(2):81-93.
• [4] Effects of a T-type calcium channel blocker, ABT-639, on spontaneous activity in C-nociceptors in patients with painful diabetic neuropathy: a randomized controlled trial. Pain. 2015 Nov;156(11):2175-83.
• [5] Mibefradil block of cloned T-type calcium channels. J Pharmacol Exp Ther. 2000 Oct;295(1):302-8.
• [6] Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents. ACS Med Chem Lett. 2010 Aug 24;1(9):504-9.
• [7] Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a ... J Med Chem. 2000 Sep 7;43(18):3372-6.
• [8] The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. ACS Chem Neurosci. 2011 Dec 21;2(12):730-742.
• [9] 3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84.
• [10] Synthesis and biological evaluation of novel T-type calcium channel blockers. Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5.