| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T39013 | ||||
| Target Name | Vanilloid receptor | ||||
| Target Type | Research |
||||
| Drug Potency against Target | IODORESINIFERATOXIN | Drug Info | Ki = 12.2 nM | [1] | |
| 6'-Iodononivamide | Drug Info | Ki = 127 nM | [2] | ||
| CAPSAZEPINE | Drug Info | IC50 = 887 nM | [3] | ||
| Pyrrolidin-1-yl-thiourea | Drug Info | IC50 = 3000 nM | [4] | ||
| 1,3-dibenzyl urea | Drug Info | IC50 = 10 nM | [5] | ||
| N-(4-tert-butylphenyl)-4-(pyridin-2-yl)benzamide | Drug Info | IC50 = 8 nM | [6] | ||
| 4-Pyridin-2-yl-piperazine-1-carboxylic acid amide | Drug Info | IC50 = 30 nM | [4] | ||
| AMG-628 | Drug Info | IC50 = 2 nM | [7] | ||
| A-795614 | Drug Info | IC50 = 30 nM | [8] | ||
| MK-056 | Drug Info | IC50 = 110 nM | [9] | ||
| ATC-120 | Drug Info | IC50 = 50 nM | [9] | ||
| JNJ-17203212 | Drug Info | IC50 = 16 nM | [3] | ||
| SC-0030 | Drug Info | IC50 = 40 nM | [9] | ||
| References | |||||
| REF 1 | J 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. | ||||
| REF 2 | Bioorg 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. | ||||
| REF 3 | J 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. | ||||
| REF 4 | Bioorg 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. | ||||
| REF 5 | Eur 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. | ||||
| REF 6 | Bioorg 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. | ||||
| REF 7 | J 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. | ||||
| REF 8 | Bioorg 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. | ||||
| REF 9 | Bioorg Med Chem. 2010 Jan 1;18(1):111-6. Epub 2009 Nov 10.Silicon switch approach in TRPV1 antagonist MK-056 and its analogues. | ||||
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