Target Validation Information
TTD ID	T88185
Target Name	Nicotinic acid receptor (HCAR2)
Type of Target	Successful
Drug Potency against Target	INCB19602	Drug Info	IC50 = 1.2~13 nM	[6]
	1H-Pyrazole-3-carboxylic acid	Drug Info	Ki = 594 nM	[1]
	2-(2-(4-tert-butylphenoxy)acetamido)benzoic acid	Drug Info	IC50 = 1200 nM	[3]
	2-(3-(naphthalen-2-yl)propanamido)benzoic acid	Drug Info	IC50 = 140 nM	[3]
	2-(3-biphenyl-4-yl-propionylamino)-benzoic acid	Drug Info	IC50 = 94 nM	[2]
	2-(4-phenylbutyl)pyrido[2,3-d]pyrimidin-4(3H)-one	Drug Info	IC50 = 4400 nM	[5]
	2-(6-phenylhexyl)pyrido[2,3-d]pyrimidin-4(3H)-one	Drug Info	IC50 = 19000 nM	[5]
	2-(cinnamyloxy)pyrido[2,3-d]pyrimidin-4(3H)-one	Drug Info	IC50 = 370 nM	[5]
	4,5,6,7-Tetrahydro-1H-indazole-3-carboxylic acid	Drug Info	Ki = 3540 nM	[1]
	5-(3-Chloro-benzyl)-1H-pyrazole-3-carboxylic acid	Drug Info	Ki = 504 nM	[1]
	5-(3-Phenyl-propyl)-1H-pyrazole-3-carboxylic acid	Drug Info	Ki = 6300 nM	[1]
	5-(4-Chloro-benzyl)-1H-pyrazole-3-carboxylic acid	Drug Info	Ki = 3610 nM	[1]
	5-Benzyl-1H-pyrazole-3-carboxylic acid	Drug Info	Ki = 1250 nM	[1]
	5-Butyl-1H-pyrazole-3-carboxylic acid	Drug Info	Ki = 72 nM	[1]
	5-Isopropyl-1H-pyrazole-3-carboxylic acid	Drug Info	Ki = 683 nM	[1]
	5-Phenethyl-1H-pyrazole-3-carboxylic acid	Drug Info	Ki = 1570 nM	[1]
	5-Propyl-1H-pyrazole-3-carboxylic acid	Drug Info	Ki = 143 nM	[1]
	ISONICOTINIC ACID	Drug Info	Ki = 33 nM	[1]
	MK-0354	Drug Info	IC50 = 1200 nM	[4]
References
REF 1	Pyrazole derivatives as partial agonists for the nicotinic acid receptor. J Med Chem. 2003 Aug 28;46(18):3945-51.
REF 2	Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor. J Med Chem. 2007 Dec 13;50(25):6303-6.
REF 3	Molecular modeling aided design of nicotinic acid receptor GPR109A agonists. Bioorg Med Chem Lett. 2008 Sep 15;18(18):4963-7.
REF 4	GPR109a agonists. Part 2: pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4472-4.
REF 5	Pyrido pyrimidinones as selective agonists of the high affinity niacin receptor GPR109A: optimization of in vitro activity. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5426-30.
REF 6	Novel patent publications on high-affinity nicotinic acid receptor agonists. Expert Opin Ther Pat. 2009 Jul;19(7):957-67.

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