Target Validation Information
TTD ID T83193
Target Name Transient receptor potential cation channel V1 (TRPV1)
Type of Target
Successful
Drug Potency against Target A-425619 Drug Info IC50 = 4 nM [19]
ABT-102 Drug Info IC50 = 4 nM [19]
AMG-517 Drug Info IC50 = 0.8 nM [20]
BCTC Drug Info IC50 = 7 nM [19]
Drug Info IC50 = 110 nM [16]
(5E,8E,11E,14E)-Icosa-5,8,11,14-tetraenal Drug Info IC50 = 51 nM [4]
(E)-3-(4-tert-Butyl-phenyl)-N-phenyl-acrylamide Drug Info IC50 = 330 nM [2]
(E)-Octadec-9-enal Drug Info IC50 = 35 nM [4]
(R)-1-(1H-indazol-4-yl)-3-(1-p-tolylethyl)urea Drug Info IC50 = 73 nM [7]
(S)-1-(1H-indazol-4-yl)-3-(1-p-tolylethyl)urea Drug Info IC50 = 749 nM [7]
1,3-dibenzyl urea Drug Info IC50 = 10 nM [13]
1-(4-Bromo-benzyl)-3-quinazolin-8-yl-urea Drug Info IC50 = 170 nM [3]
1-(isoquinolin-5-yl)-3-(1-phenylpropyl)urea Drug Info IC50 = 2580 nM [7]
1-(isoquinolin-5-yl)-3-(4-morpholinobenzyl)urea Drug Info IC50 = 91 nM [8]
1-benzhydryl-3-(isoquinolin-5-yl)urea Drug Info IC50 = 600 nM [7]
2-(4-pentylphenyl)-N-(pyridin-3-yl)acetamide Drug Info Ki = 7260 nM [14]
4-(3-methylpyridin-2-yl)-N-p-tolylbenzamide Drug Info IC50 = 2585 nM [5]
4-(butyl(methyl)amino)-N-(quinolin-3-yl)benzamide Drug Info IC50 = 66 nM [14]
4-(cyclohexylamino)-N-(quinolin-3-yl)benzamide Drug Info IC50 = 10000 nM [14]
4-(hexyl(methyl)amino)-N-(quinolin-3-yl)benzamide Drug Info IC50 = 86 nM [14]
4-(methyl(nonyl)amino)-N-(quinolin-3-yl)benzamide Drug Info IC50 = 150 nM [14]
4-(methyl(octyl)amino)-N-(quinolin-3-yl)benzamide Drug Info IC50 = 190 nM [14]
4-butyl-N-(7-hydroxynaphthalen-1-yl)benzamide Drug Info IC50 = 42 nM [14]
4-butyl-N-(isoquinolin-5-yl)benzamide Drug Info IC50 = 2400 nM [14]
4-butyl-N-(pyridin-3-yl)benzamide Drug Info Ki = 626 nM [14]
4-butyl-N-(quinolin-3-yl)benzamide Drug Info IC50 = 230 nM [14]
4-butyl-N-phenylbenzamide Drug Info Ki = 6272 nM [14]
4-decyl-N-(pyridin-3-yl)benzamide Drug Info Ki = 607 nM [14]
4-heptyl-N-(pyridin-3-yl)benzamide Drug Info Ki = 1740 nM [14]
4-heptyl-N-(quinolin-3-yl)benzamide Drug Info Ki = 3520 nM [14]
4-hexyl-N-(quinolin-3-yl)benzamide Drug Info IC50 = 150 nM [14]
4-nonyl-N-(quinolin-3-yl)benzamide Drug Info Ki = 980 nM [14]
4-octyl-N-(pyridin-3-yl)benzamide Drug Info Ki = 546 nM [14]
4-octyl-N-(quinolin-3-yl)benzamide Drug Info Ki = 2080 nM [14]
4-pentyl-N-pyridin-3-yl benzamide Drug Info Ki = 421 nM [14]
4-propyl-N-(quinolin-3-yl)benzamide Drug Info IC50 = 130 nM [14]
4-Pyridin-2-yl-piperazine-1-carboxylic acid amide Drug Info IC50 = 30 nM [1]
4-tert-butyl-N-(quinolin-3-yl)benzamide Drug Info IC50 = 41 nM [14]
5'-iodoresiniferatoxin Drug Info Ki = 12.2 nM [11]
6'-Iodononivamide Drug Info Ki = 127 nM [17]
A-795614 Drug Info IC50 = 30 nM [15]
AMG-628 Drug Info IC50 = 2 nM [9]
ATC-120 Drug Info IC50 = 50 nM [16]
CAPSAZEPINE Drug Info IC50 = 887 nM [6]
JNJ-17203212 Drug Info IC50 = 16 nM [6]
N-(4-iodophenyl)-4-(trifluoromethoxy)benzamide Drug Info IC50 = 280 nM [12]
N-(4-iodophenyl)-4-(trifluoromethyl)benzamide Drug Info IC50 = 330 nM [12]
N-(4-tert-butylphenyl)-4-(pyridin-2-yl)benzamide Drug Info IC50 = 8 nM [5]
N-methyl-4-pentyl-N-(pyridin-3-yl)benzamide Drug Info Ki = 15000 nM [14]
N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]lauramide Drug Info IC50 = 740 nM [10]
N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]linoleamide Drug Info IC50 = 1820 nM [10]
N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]undecanamide Drug Info IC50 = 760 nM [10]
Pyrrolidin-1-yl-thiourea Drug Info IC50 = 3000 nM [1]
SC-0030 Drug Info IC50 = 40 nM [16]
Action against Disease Model SB-705498 Drug Info Using a Ca(2+)-based fluorometric imaging plate reader (FLIPR) assay, SB-705498 was shown to be a potent competitive antagonist of the capsaicin-mediated activation of the h uMan TRPV1 receptor (pK(i) = 7.6) with activity at rat (pK(i) = 7.5) and guinea pig (pK(i) = 7.3) orthologs. Whole-cell patch-clamp electrophysiology was used to confirm and extend these findings, demonstrating that SB-705498 can potently inhibit the multiple modes of receptor activation that may be relevant to the pathophysiological role of TRPV1 in vivo: SB-705498 caused rapid and reversible inhibition of the capsaicin (IC(50) = 3 nM)-, acid (pH 5.3)-, or heat (50 degrees C; IC(50) = 6 nM)-mediated activation of h uMan TRPV1 (at -70 mV). [18]
References
REF 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.
REF 2 Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J Med Chem. 2005 Jan 13;48(1):71-90.
REF 3 Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quin... J Med Chem. 2005 Feb 10;48(3):744-52.
REF 4 The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination. J Med Chem. 2005 Jul 14;48(14):4663-9.
REF 5 From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21.
REF 6 The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. J Med Chem. 2007 May 31;50(11):2589-96.
REF 7 Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher effic... Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9.
REF 8 In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 ... J Med Chem. 2007 Jul 26;50(15):3651-60.
REF 9 Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacok... J Med Chem. 2007 Jul 26;50(15):3528-39.
REF 10 New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. J Med Chem. 2007 Dec 27;50(26):6554-69.
REF 11 Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues. J Med Chem. 2008 Jan 10;51(1):57-67.
REF 12 Synthesis of benzamide derivatives as TRPV1 antagonists. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1072-8.
REF 13 Rare dipeptide and urea derivatives from roots of Moringa oleifera as potential anti-inflammatory and antinociceptive agents. Eur J Med Chem. 2009 Jan;44(1):432-6.
REF 14 N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1). Bioorg Med Chem Lett. 2008 Apr 15;18(8):2730-4.
REF 15 Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. Bioorg Med Chem. 2008 Sep 15;16(18):8516-25.
REF 16 Silicon switch approach in TRPV1 antagonist MK-056 and its analogues. Bioorg Med Chem. 2010 Jan 1;18(1):111-6.
REF 17 Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin. Bioorg Med Chem. 2010 Nov 15;18(22):8092-105.
REF 18 Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-med... J Pharmacol Exp Ther. 2007 Jun;321(3):1183-92.
REF 19 Recent progress in the development of selective TRPV1 antagonists for pain. Curr Top Med Chem. 2008;8(16):1431-41.
REF 20 Clinical development of TRPV1 antagonists: targeting a pivotal point in the pain pathway. Drug Discov Today. 2009 Jan;14(1-2):56-67.

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