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

General Information of Drug (ID: DMDHZR1)

Drug Name

GSK1016790A Drug Info

Synonyms

GSK1016790A; 942206-85-1; GSK 1016790A; GSK-1016790A; GSK101; (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide; IVYQPSHHYIAUFO-VXKWHMMOSA-N; GTPL4205; SCHEMBL5007988; DTXSID30635248; CHEBI:140524; MolPort-044-560-329; EX-A1885; s8107; MFCD12912413; ZINC95571016; AKOS030527025; CS-5660; NCGC00250409-01

Indication

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

Cross-matching ID

PubChem CID: 23630211
ChEBI ID: CHEBI:140524
CAS Number: CAS 942206-85-1
TTD Drug ID: DMDHZR1

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Investigative Drug(s)

Download the Complete Related Drug List

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]
GSK2193874	DMY2XV3	Discovery agent	N.A.	Investigative	[10]
RN1734	DMA3ZXM	Discovery agent	N.A.	Investigative	[11]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Transient receptor potential cation channel V4 (TRPV4)	TTKP2SU	TRPV4_HUMAN	Activator	[2]

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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: 4205).
2	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.
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	An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure. Sci Transl Med. 2012 Nov 7;4(159):159ra148.
11	Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov 20;389(3):490-4.