Target Validation Information
Target ID T73495
Target Name Glutamate receptor, ionotropic kainate 1
Target Type
Successful
Drug Potency against Target NBQX Drug Info IC50 = 31 nM [525786]
KAINATE Drug Info Ki = 75.9 nM [529560]
DIHYDROKAINATE Drug Info Ki = 8180 nM [529559]
2-(3-bromobenzoylamino)-4-chlorobenzoic acid Drug Info IC50 = 19000 nM [527354]
S-ATPO Drug Info Ki = 2900 nM [530297]
2-AMINO-3-(4-HYDROXY-1,2,5-OXADIAZOL-3-YL)PROPIONIC ACID (STRUCTURAL MIX) Drug Info Ki = 8100 nM [530863]
GLUTAMATE Drug Info Ki = 140 nM [530863]
2S,4R-4-METHYLGLUTAMATE Drug Info Ki = 0.663 nM [529560]
LY293558 Drug Info IC50 = 230 nM [525786]
QUISQUALATE Drug Info Ki = 171 nM [529560]
(2S,4R)-4-(3-Methoxy-3-oxopropyl)glutamic Acid Drug Info Ki = 42.8 nM [529560]
2-(3-(3-bromophenyl)ureido)-4-chlorobenzoic acid Drug Info IC50 = 4800 nM [527354]
Topiramate Drug Info Ki = 0.87 nM [552703]
(R,S)-AMPA Drug Info Ki = 1150 nM [529714]
YM-90K Drug Info IC50 = 260 nM [525786]
UBP-302 Drug Info IC50 = 15000 nM [528453]
Domoric acid Drug Info Ki = 1.11 nM [529560]
TQX-173 Drug Info IC50 = 11600 nM [526134]
References
Ref 525786Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7.4,10-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 in vivo activity.
Ref 529560J Med Chem. 2008 Jul 24;51(14):4093-103. Epub 2008 Jun 25.Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation ofionotropic glutamate receptor subtypes 5, 6, and 7.
Ref 529559J Med Chem. 2008 Jul 24;51(14):4085-92. Epub 2008 Jun 25.Chemo-enzymatic synthesis of (2S,4R)-2-amino-4-(3-(2,2-diphenylethylamino)-3-oxopropyl)pentanedioic acid: a novel selective inhibitor of human excitatory amino acid transporter subtype 2.
Ref 527354J Med Chem. 2004 Dec 30;47(27):6948-57.Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.
Ref 530297Bioorg Med Chem. 2009 Sep 1;17(17):6390-401. Epub 2009 Jul 16.3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands.
Ref 530863J Med Chem. 2010 May 27;53(10):4110-8.4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
Ref 530863J Med Chem. 2010 May 27;53(10):4110-8.4-hydroxy-1,2,5-oxadiazol-3-yl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and molecular pharmacological characterization at ionotropic glutamate receptors of compounds related to glutamate and its homologues.
Ref 529560J Med Chem. 2008 Jul 24;51(14):4093-103. Epub 2008 Jun 25.Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation ofionotropic glutamate receptor subtypes 5, 6, and 7.
Ref 525786Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7.4,10-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 in vivo activity.
Ref 529560J Med Chem. 2008 Jul 24;51(14):4093-103. Epub 2008 Jun 25.Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation ofionotropic glutamate receptor subtypes 5, 6, and 7.
Ref 529560J Med Chem. 2008 Jul 24;51(14):4093-103. Epub 2008 Jun 25.Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation ofionotropic glutamate receptor subtypes 5, 6, and 7.
Ref 527354J Med Chem. 2004 Dec 30;47(27):6948-57.Bioisosteric modifications of 2-arylureidobenzoic acids: selective noncompetitive antagonists for the homomeric kainate receptor subtype GluR5.
Ref 552703Carbonic anhydrase inhibitors as anticonvulsant agents. Curr Top Med Chem. 2007;7(9):855-64.
Ref 529714J Med Chem. 2008 Oct 23;51(20):6614-8. Epub 2008 Sep 24.1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.
Ref 525786Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7.4,10-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 in vivo activity.
Ref 528453J Med Chem. 2006 Oct 5;49(20):6015-26.Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
Ref 529560J Med Chem. 2008 Jul 24;51(14):4093-103. Epub 2008 Jun 25.Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation ofionotropic glutamate receptor subtypes 5, 6, and 7.
Ref 526134J Med Chem. 2001 Sep 13;44(19):3157-65.Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.

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