Target Validation Information
TTD ID	T52790
Target Name	Substance-K receptor (TACR2)
Type of Target	Clinical trial
Drug Potency against Target	CS-003	Drug Info	Ki = 0.54 nM	[10]
	DNK-333	Drug Info	Ki = 5.5 nM	[7]
	Saredutant	Drug Info	Ki = 0.5 nM	[8]
	4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one	Drug Info	Ki < 1000 nM	[6]
	A-987306	Drug Info	IC50 = 5.7 nM	[3]
	Hoo-Phe-Orn-Pro-hle-Pff-Phe-NH2	Drug Info	IC50 = 710 nM	[2]
	L-732138	Drug Info	Ki = 134 nM	[5]
	PMX-53	Drug Info	IC50 = 87 nM	[2]
	Rambazole	Drug Info	Ki = 16 nM	[1]
	WAY-207024	Drug Info	Ki = 330 nM	[4]
Action against Disease Model	DNK-333	Drug Info	Male Brown Norway rats were imaged prior to and 10, 30 and 60 min after intra-tracheal challenge with capsaicin (30 microg kg(-1)) or vehicle (0.5% ethanol solution). Capsazepine (3.5 mg kg(-1)), DNK333 (10 mg kg(-1)) but not DSCG (10 mg kg(-1)) administered prophylactically were able to block the effect of capsaicin in the airways	[9]
References
REF 1	Generation of a new class of hNK(2) receptor ligands using the 'fragment approach'. Bioorg Med Chem Lett. 2005 Feb 1;15(3):585-8.
REF 2	Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: increased receptor specificity and in vivo activity. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5088-92.
REF 3	cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.
REF 4	Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the ... J Med Chem. 2009 Apr 9;52(7):2148-52.
REF 5	Biological and conformational evaluation of bifunctional compounds for opioid receptor agonists and neurokinin 1 receptor antagonists possessing tw... J Med Chem. 2010 Aug 12;53(15):5491-501.
REF 6	Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 7	Dual neurokinin NK(1)/NK(2) antagonists: N-[(R,R)-(E)-1-arylmethyl-3-(2-oxo-azepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamides and 3-[N'-3,5-bis(trifluoromethyl)benzoyl-N-arylmethyl-N'-methylhydrazino]-N-[(R)-2-oxo-azepan-3-yl]propionamides. Bioorg Med Chem Lett. 2001 Dec 3;11(23):3081-4.
REF 8	Recent developments in the medicinal chemistry of NK2 receptor antagonists. Curr Top Med Chem. 2003;3(12):1436-45.
REF 9	Capsaicin-induced mucus secretion in rat airways assessed in vivo and non-invasively by magnetic resonance imaging. Br J Pharmacol. 2007 Apr;150(8):1022-30.
REF 10	Novel triple neurokinin receptor antagonist CS-003 strongly inhibits neurokinin related responses. Eur J Pharmacol. 2008 May 31;586(1-3):306-12.

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