Target Validation Information
TTD ID	T73495
Target Name	Glutamate receptor ionotropic kainate 1 (GRIK1)
Type of Target	Successful
Drug Potency against Target	Topiramate	Drug Info	Ki = 0.87 nM	[10]
		Drug Info	Ki = 140 nM	[9]
		Drug Info	Ki = 1150 nM	[7]
	(2S,4R)-4-(3-Methoxy-3-oxopropyl)glutamic Acid	Drug Info	Ki = 42.8 nM	[6]
	2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid	Drug Info	IC50 = 4800 nM	[3]
	2-(3-bromobenzoylamino)-4-chlorobenzoic acid	Drug Info	IC50 = 19000 nM	[3]
	2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX)	Drug Info	Ki = 8100 nM	[9]
	2S,4R-4-METHYLGLUTAMATE	Drug Info	Ki = 0.663 nM	[6]
	DIHYDROKAINATE	Drug Info	Ki = 8180 nM	[5]
	Domoric acid	Drug Info	Ki = 1.11 nM	[6]
	LY293558	Drug Info	IC50 = 230 nM	[1]
	NBQX	Drug Info	IC50 = 31 nM	[1]
	S-ATPO	Drug Info	Ki = 2900 nM	[8]
	TQX-173	Drug Info	IC50 = 11600 nM	[2]
	UBP-302	Drug Info	IC50 = 15000 nM	[4]
	YM-90K	Drug Info	IC50 = 260 nM	[1]
	[3H]kainate	Drug Info	Ki = 75.9 nM	[6]
	[3H]quisqualate	Drug Info	Ki = 171 nM	[6]
References
REF 1	4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with... Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7.
REF 2	Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,... J Med Chem. 2001 Sep 13;44(19):3157-65.
REF 3	Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5. J Med Chem. 2004 Dec 30;47(27):6948-57.
REF 4	Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Syn... J Med Chem. 2006 Oct 5;49(20):6015-26.
REF 5	Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human exci... J Med Chem. 2008 Jul 24;51(14):4085-92.
REF 6	Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotr... J Med Chem. 2008 Jul 24;51(14):4093-103.
REF 7	1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of pot... J Med Chem. 2008 Oct 23;51(20):6614-8.
REF 8	3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands. Bioorg Med Chem. 2009 Sep 1;17(17):6390-401.
REF 9	4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological charact... J Med Chem. 2010 May 27;53(10):4110-8.
REF 10	Carbonic anhydrase inhibitors as anticonvulsant agents. Curr Top Med Chem. 2007;7(9):855-64.

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