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

General Information of Drug (ID: DM92RHP)

• Drug Name: KYS-05090 Drug Info
• Synonyms: KYS-05090; CHEMBL394956; CHEMBL1269457; SCHEMBL10019253; BDBM50222222; N-benzyl-2-(3-(biphenyl-4-yl)-2-((5-(dimethylamino)pentyl)(methyl)amino)-3,4-dihydroquinazolin-4-yl)acetamide; N-Benzyl-3-(4-biphenylyl)-2-[5-(dimethylamino)pentyl(methyl)amino]-3,4-dihydroquinazoline-4-acetamide

Indication

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

• Cross-matching ID:
  PubChem CID: 23661603
  TTD Drug ID: DM92RHP

Molecule-Related Drug Atlas

Drug(s) Targeting Voltage-gated calcium channel alpha Cav2.2 (CACNA1B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
LOMERIZINE	DME0TC8	Migraine	8A80	Approved	[3]
Ziconotide	DMSLJP4	Pain	MG30-MG3Z	Approved	[4]
Hesperidin	DMI5DW1	Vascular purpura	3B60	Approved	[5]
Cilnidipine	DM1975O	High blood pressure	BA00	Phase 3	[6]
Ralfinamide	DMUNMY0	Neuropathic pain	8E43.0	Phase 3	[7]
CNV-2197944	DMLT7JV	Pain	MG30-MG3Z	Phase 2	[8]
Ritanserin	DM0X36Y	Anxiety disorder	6B00-6B0Z	Discontinued in Phase 3	[9]
CNSB-004	DMHAI0M	Pain	MG30-MG3Z	Preclinical	[10]
TH-9229	DMG1MPD	Reperfusion injury	ND56.Z	Terminated	[11]
PD-157667	DM61NFD	N. A.	N. A.	Terminated	[12]

Drug(s) Targeting Voltage-gated calcium channel alpha Cav3.1 (CACNA1G)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[13]
Ethosuximide	DMDZ9LT	Epilepsy	8A60-8A68	Approved	[14]
Trimethadione	DM0Q8MZ	Absence epilepsy		Approved	[15]
Paramethadione	DMR5ZUP	Absence epilepsy		Approved	[15]
Methsuximide	DM6L5VO	Absence epilepsy		Approved	[16]
Penfluridol	DMG1DTE	Schizophrenia	6A20	Approved	[17]
PD-200390	DMPW28M	Insomnia	7A00-7A0Z	Phase 2	[18]
NGD 94-1	DMM1Y8F	Schizophrenia	6A20	Phase 1	[17]
ML218	DM3D21X	Discovery agent	N.A.	Investigative	[19]
KYS-05001	DM3MID9	Discovery agent	N.A.	Investigative	[2]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated calcium channel alpha Cav2.2 (CACNA1B)	TT4FDG6	CAC1B_HUMAN	Inhibitor	[2]
Voltage-gated calcium channel alpha Cav3.1 (CACNA1G)	TT729IR	CAC1G_HUMAN	Inhibitor	[1]

References

• [1] T-type Ca2+ channel blockers suppress the growth of human cancer cells. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3899-901.
• [2] Discovery of potent T-type calcium channel blocker. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3.
• [3] Synthesis and SAR of novel 2-arylthiazolidinones as selective analgesic N-type calcium channel blockers. Bioorg Med Chem Lett. 2007 Feb 1;17(3):662-7.
• [4] Emerging treatments for traumatic brain injury. Expert Opin Emerg Drugs. 2009 Mar;14(1):67-84.
• [5] In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
• [6] N- and L-type calcium channel antagonist improves glomerular dynamics, reverses severe nephrosclerosis, and inhibits apoptosis and proliferation in an l-NAME/SHR model. J Hypertens. 2002 May;20(5):993-1000.
• [7] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [8] Clinical pipeline report, company report or official report of Convergence Pharmaceuticals Ltd.
• [9] N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Mar 22;9(6):907-12.
• [10] CNSB004 (Leconotide) causes antihyperalgesia without side effects when given intravenously: a comparison with ziconotide in a rat model of diabetic neuropathic pain. Pain Med. 2010 Feb;11(2):262-73.
• [11] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008159)
• [12] Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers. Bioorg Med Chem Lett. 1999 Aug 16;9(16):2447-52.
• [13] Mechanism of tissue-selective drug action in the cardiovascular system. Mol Interv. 2005 Apr;5(2):84-93.
• [14] Maladaptive homeostatic plasticity in a rodent model of central pain syndrome: thalamic hyperexcitability after spinothalamic tract lesions. J Neurosci. 2008 Nov 12;28(46):11959-69.
• [15] Prophylactic and therapeutic functions of T-type calcium blockers against noise-induced hearing loss. Hear Res. 2007 Apr;226(1-2):52-60.
• [16] Block of cloned human T-type calcium channels by succinimide antiepileptic drugs. Mol Pharmacol. 2001 Nov;60(5):1121-32.
• [17] Differential inhibition of T-type calcium channels by neuroleptics. J Neurosci. 2002 Jan 15;22(2):396-403.
• [18] Pfizer. Product Development Pipeline. March 31 2009.
• [19] 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.