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 525786 | Bioorg 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 529560 | J 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 529559 | J 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 527354 | J 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 530297 | Bioorg Med Chem. 2009 Sep 1;17(17):6390-401. Epub 2009 Jul 16.3-Substituted phenylalanines as selective AMPA- and kainate receptor ligands. | ||||
Ref 530863 | J 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 530863 | J 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 529560 | J 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 525786 | Bioorg 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 529560 | J 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 529560 | J 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 527354 | J 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 552703 | Carbonic anhydrase inhibitors as anticonvulsant agents. Curr Top Med Chem. 2007;7(9):855-64. | ||||
Ref 529714 | J 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 525786 | Bioorg 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 528453 | J 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 529560 | J 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 526134 | J 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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