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

General Information of Drug (ID: DMY2XV3)

• Drug Name: GSK2193874 Drug Info
• Synonyms: GSK 2193874; GSK-2193874

Indication

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

• Cross-matching ID:
  PubChem CID: 53464483
  TTD Drug ID: DMY2XV3

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	[3]
GSK2798745	DM7V96W	Heart failure	BD10-BD13	Phase 2	[4]
citric acid	DM80YI7	Discovery agent	N.A.	Investigative	[5]
4-Pyridin-2-yl-piperazine-1-carboxylic acid amide	DMFC8Q4	Discovery agent	N.A.	Investigative	[6]
Pyrrolidin-1-yl-thiourea	DMYNZXC	Discovery agent	N.A.	Investigative	[6]
CAPSAZEPINE	DM4ATCI	Discovery agent	N.A.	Investigative	[7]
SC-0030	DMD2WEQ	Discovery agent	N.A.	Investigative	[8]
bisandrographolide	DMRSKGC	Discovery agent	N.A.	Investigative	[9]
GSK1016790A	DMDHZR1	Discovery agent	N.A.	Investigative	[10]
RN1734	DMA3ZXM	Discovery agent	N.A.	Investigative	[11]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Transient receptor potential cation channel V4 (TRPV4)	TTKP2SU	TRPV4_HUMAN	Blocker (channel blocker)	[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: 6465).
• [2] An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4(159):159ra148.
• [3] Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives. J Biol Chem. 2002 Apr 19;277(16):13569-77.
• [4] Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
• [5] Impaired pressure sensation in mice lacking TRPV4. J Biol Chem. 2003 Jun 20;278(25):22664-8.
• [6] 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.
• [7] Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists. Bioorg Med Chem Lett. 2003 May 5;13(9):1549-52.
• [8] 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.
• [9] Bisandrographolide from Andrographis paniculata activates TRPV4 channels. J Biol Chem. 2006 Oct 6;281(40):29897-904.
• [10] 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.
• [11] Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov 20;389(3):490-4.