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

General Information of Drug (ID: DMFC8Q4)

• Drug Name: 4-Pyridin-2-yl-piperazine-1-carboxylic acid amide Drug Info
• Synonyms: CHEMBL296963; SCHEMBL1270156; CTK7D3440; BDBM50224176; AKOS000158821; 4-(2-pyridyl)piperazine-1-carboxamide

Indication

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

• Cross-matching ID:
  PubChem CID: 22418783
  TTD Drug ID: DMFC8Q4

Molecule-Related Drug Atlas

Drug(s) Targeting Transient receptor potential cation channel V4 (TRPV4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
phorbol 12-myristate 13-acetate	DMJWD62	Acute myeloid leukaemia	2A60	Phase 2	[2]
GSK2798745	DM7V96W	Heart failure	BD10-BD13	Phase 2	[3]
citric acid	DM80YI7	Discovery agent	N.A.	Investigative	[4]
Pyrrolidin-1-yl-thiourea	DMYNZXC	Discovery agent	N.A.	Investigative	[1]
CAPSAZEPINE	DM4ATCI	Discovery agent	N.A.	Investigative	[5]
SC-0030	DMD2WEQ	Discovery agent	N.A.	Investigative	[6]
bisandrographolide	DMRSKGC	Discovery agent	N.A.	Investigative	[7]
GSK1016790A	DMDHZR1	Discovery agent	N.A.	Investigative	[8]
GSK2193874	DMY2XV3	Discovery agent	N.A.	Investigative	[9]
RN1734	DMA3ZXM	Discovery agent	N.A.	Investigative	[10]

Drug(s) Targeting Transient receptor potential cation channel V1 (TRPV1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[11]
CNTX-4975	DMB4JPG	Knee osteoarthritis	FA01	Phase 3	[12]
XEN-D0501	DMG7PDY	Overactive bladder	GC50.0	Phase 2	[13]
Resiniferatoxin	DMP62L5	Neuropathic pain	8E43.0	Phase 2	[14]
PAC-14028	DM3816P	Atopic dermatitis	EA80	Phase 2	[15]
GRC-15300	DMWXJSZ	Pain	MG30-MG3Z	Phase 2	[16]
DWP-05195	DMQKU2F	Neuropathic pain	8E43.0	Phase 2	[17]
SB-705498	DMRYHWI	Rhinitis	FA20	Phase 2	[18]
GRC-6211	DMZ0D3V	Asthma	CA23	Phase 1	[19]
ABT-102	DMJFWPR	Chronic pain	MG30	Phase 1	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Transient receptor potential cation channel V1 (TRPV1)	TTMI6F5	TRPV1_HUMAN	Inhibitor	[1]
Transient receptor potential cation channel V4 (TRPV4)	TTKP2SU	TRPV4_HUMAN	Inhibitor	[1]

References

• [1] N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1693-6.
• [2] Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives. J Biol Chem. 2002 Apr 19;277(16):13569-77.
• [3] Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
• [4] Impaired pressure sensation in mice lacking TRPV4. J Biol Chem. 2003 Jun 20;278(25):22664-8.
• [5] Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists. Bioorg Med Chem Lett. 2003 May 5;13(9):1549-52.
• [6] Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects. Bioorg Med Chem Lett. 2003 Dec 15;13(24):4389-93.
• [7] Bisandrographolide from Andrographis paniculata activates TRPV4 channels. J Biol Chem. 2006 Oct 6;281(40):29897-904.
• [8] N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42.
• [9] An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4(159):159ra148.
• [10] Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov 20;389(3):490-4.
• [11] Capsaicin receptor: TRPV1 a promiscuous TRP channel. Handb Exp Pharmacol. 2007;(179):155-71.
• [12] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [13] An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects. Br J Clin Pharmacol. 2011 Dec;72(6):921-31.
• [14] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [15] Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Arch Pharm Res. 2012 Mar;35(3):393-6.
• [16] The discovery and development of analgesics: new mechanisms, new modalities. J Clin Invest. 2010 November 1; 120(11): 3753-3759.
• [17] TRPV1 Antagonists as Analgesic Agents. The Open Pain Journal, 2013, 6, (Suppl 1: M11), 108-118 .
• [18] Analgesic potential of TRPV1 antagonists. Biochem Pharmacol. 2009 Aug 1;78(3):211-6.
• [19] GRC-6211, a new oral specific TRPV1 antagonist, decreases bladder overactivity and noxious bladder input in cystitis animal models. J Urol. 2009 Jan;181(1):379-86.