Therapeutic Targets Database
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TTD Target ID: TTDC00049

Target Information
NameTransient receptor potential cation channel subfamily V member 1    
Type of targetClinical trial target    
SynonymsCapsaicin receptor    
OTRPC1    
Osm-9-like TRP channel 1    
TrpV1    
Vanilloid receptor 1    
DiseaseAcute migraine
[ICD9: 346   ICD10: G43]
[1][2]
Analgesics
[ICD9: 338   ICD10: R52]
[1]
Chronic pathological pain
[ICD9: 338,780   ICD10: R52, G89]
[1][2]
Osteoarthritis pain
[ICD9: 338, 715,780   ICD10: M15-M19, M47, R52, G89]
[1][2]
Pain, Acute or Chronic
[ICD9: 338,780   ICD10: R52, G89]
[1]
Urinary incontinence
[ICD9: 788.3   ICD10: N39.3, N39.4, R32]
[1]
Drug(s)AZD1386Phase II completedPain[3]
CapsaicinPhase II completedNeuropathic pain[4]
AZD1386Phase IISensitivity in Esophagus[3]
NGD-8243Phase IIAcute or Chronic Pain[1]
ResiniferatoxinPhase IINeuropathic pain[4]
SB-705498Phase IIAcute migraine[1][2]
SB-705498Phase IIAcute migraine, Non-allergic rhinitis[5]
ABT-102Phase IChronic pathological pain[1]
AMG-517Discontinued in Phase IChronic pathological pain[1][2]
GRC-6211Suspended in Phase IOsteoarthritis pain[1][2]
NGD-8243PreclinicalUrinary Incontinence[1]
A-425619Lead CompoundPain[1]
A-993610Lead CompoundPain[1]
AMG-8562Lead CompoundPain[1]
AMG-8563Lead CompoundPain[1]
BCTCLead CompoundPain[1]
PathwayNeuroactive ligand-receptor interaction
UniProt IDQ8NER1
SequenceMKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA DNTKFVTSMYNEILILGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (5E,8E,11E,14E)-Icosa-5,8,11,14-tetraenal[6]
(E)-3-[7]
(E)-Octadec-9-enal[6]
(R)-1-[8]
(S)-1-[8]
1,3-dibenzyl urea[9]
1- (4-Bromo-benzyl)-3-quinazolin-8-yl-urea[10]
1- (isoquinolin-5-yl)-3-[8]
1- (isoquinolin-5-yl)-3-[11]
1-benzhydryl-3- (isoquinolin-5-yl)urea[8]
2- (4-pentylphenyl)-N-[12]
4- (3-methylpyridin-2-yl)-N-p-tolylbenzamide[13]
4- (butyl[12]
4- (cyclohexylamino)-N-[12]
4- (hexyl[12]
4- (methyl[12]
4- (methyl[12]
4-Pyridin-2-yl-piperazine-1-carboxylic acid amide[14]
4-butyl-N- (7-hydroxynaphthalen-1-yl)benzamide[12]
4-butyl-N- (isoquinolin-5-yl)benzamide[12]
4-butyl-N- (pyridin-3-yl)benzamide[12]
4-butyl-N- (quinolin-3-yl)benzamide[12]
4-butyl-N-phenylbenzamide[12]
4-decyl-N- (pyridin-3-yl)benzamide[12]
4-heptyl-N- (pyridin-3-yl)benzamide[12]
4-heptyl-N- (quinolin-3-yl)benzamide[12]
4-hexyl-N- (quinolin-3-yl)benzamide[12]
4-nonyl-N- (quinolin-3-yl)benzamide[12]
4-octyl-N- (pyridin-3-yl)benzamide[12]
4-octyl-N- (quinolin-3-yl)benzamide[12]
4-pentyl-N-pyridin-3-yl benzamide[12]
4-propyl-N- (quinolin-3-yl)benzamide[12]
4-tert-butyl-N- (quinolin-3-yl)benzamide[12]
6'-Iodononivamide[15]
A-795614[16]
AMG-628[17]
ATC-120[18]
CAPSAZEPINE[19]
IODORESINIFERATOXIN[20]
JNJ-17203212[19]
MK-056[18]
N- (4-iodophenyl)-4-[21]
N- (4-iodophenyl)-4-[21]
N- (4-tert-butylphenyl)-4-[13]
N-[2- (5-hydroxy-1H-indol-3-yl)ethyl]lauramide[22]
N-[2- (5-hydroxy-1H-indol-3-yl)ethyl]linoleamide[22]
N-[2- (5-hydroxy-1H-indol-3-yl)ethyl]undecanamide[22]
N-methyl-4-pentyl-N- (pyridin-3-yl)benzamide[12]
Pyrrolidin-1-yl-thiourea[14]
SB-782443[23]
SC-0030,   SC0030[18]
BlockerA-425619[1]
A-993610[1]
ABT-102[1]
AMG-517[1][2]
AMG-8562[1]
AMG-8563[1]
AZD1386[3]
BCTC[1]
GRC-6211[1][2]
NGD-8243[1]
SB-705498[1][2]
SB-705498[5]
ActivatorCapsaicin[4]
Resiniferatoxin[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Analgesic potential of TRPV1 antagonists. Biochem Pharmacol. 2009 Aug 1;78(3):211-6. Epub 2009 Mar 5. To Reference
Ref 2The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat Rev Drug Discov. 2007 May;6(5):357-72. To Reference
Ref 3AstraZeneca. Product Development Pipeline. January 29 2009. To Reference
Ref 4Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 5GSK. Product Development Pipeline. February 2009. To Reference
Ref 6J Med Chem. 2005 Jul 14;48(14):4663-9.The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination. To Reference
Ref 7J Med Chem. 2005 Jan 13;48(1):71-90.Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. To Reference
Ref 8Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9. Epub 2007 May 3.Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model. To Reference
Ref 9Eur J Med Chem. 2009 Jan;44(1):432-6. Epub 2007 Dec 28.Rare dipeptide and urea derivatives from roots of Moringa oleifera as potential anti-inflammatory and antinociceptive agents. To Reference
Ref 10J Med Chem. 2005 Feb 10;48(3):744-52.Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties. To Reference
Ref 11J Med Chem. 2007 Jul 26;50(15):3651-60. Epub 2007 Jun 21.In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists. To Reference
Ref 12Bioorg Med Chem Lett. 2008 Apr 15;18(8):2730-4. Epub 2008 Mar 5.N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1). To Reference
Ref 13Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21. Epub 2006 Jul 25.From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist. To Reference
Ref 14Bioorg Med Chem Lett. 2004 Apr 5;14(7):1693-6.N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. To Reference
Ref 15Bioorg Med Chem. 2010 Nov 15;18(22):8092-105. Epub 2010 Sep 18.Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin. To Reference
Ref 16Bioorg Med Chem. 2008 Sep 15;16(18):8516-25. Epub 2008 Aug 7.Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. To Reference
Ref 17J Med Chem. 2007 Jul 26;50(15):3528-39. Epub 2007 Jun 22.Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. To Reference
Ref 18Bioorg Med Chem. 2010 Jan 1;18(1):111-6. Epub 2009 Nov 10.Silicon switch approach in TRPV1 antagonist MK-056 and its analogues. To Reference
Ref 19J Med Chem. 2007 May 31;50(11):2589-96. Epub 2007 May 10.The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. To Reference
Ref 20J Med Chem. 2008 Jan 10;51(1):57-67. Epub 2007 Dec 12.Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues. To Reference
Ref 21Bioorg Med Chem Lett. 2008 Feb 1;18(3):1072-8. Epub 2007 Dec 10.Synthesis of benzamide derivatives as TRPV1 antagonists. To Reference
Ref 22J Med Chem. 2007 Dec 27;50(26):6554-69. Epub 2007 Nov 21.New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. To Reference
Ref 23Bioorg Med Chem Lett. 2008 Oct 15;18(20):5609-13. Epub 2008 Aug 31.Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1. To Reference



 

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Professor in Department of Pharmacy
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