Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T68876 | Target Info | |||
| Target Name | Glutamate receptor ionotropic kainate 3 (GluK3) | ||||
| Synonyms |
Glutamate receptor ionotropic, kainate 3; Glutamate receptor 7; GluR7; GluR-7; GluK3; Excitatory amino acid receptor 5; EAA5
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| Target Type | Literature-reported Target | ||||
| Gene Name | GRIK3 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 3 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
LY293558
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Phase 2 | Compound Info | ||
| Synonyms |
Tezampanel; 154652-83-2; LY-293558; LY293558; Ted-isoquinoline-3-cooh; LY 293558; UNII-GA36S2O9C2; CHEMBL14935; GA36S2O9C2; 150131-78-5; Decahydro-6-(2-(1H-tetrazol-5-yl)ethyl)-3-isoquinolinecarboxylic acid; 6-(2-(1H-Tetrazol-5-yl)ethyl)-1,2,3,4,4a,5,6,7,8,8a-decahydroisoquinoline-3-carboxylic acid; 3-Isoquinolinecarboxylic acid, decahydro-6-(2-(1H-tetrazol-5-yl)ethyl)-, (3S,4aR,6R,8aR)-; 3-Isoquinolinecarboxylic acid, decahydro-6-(2-(1H-tetrazol-5-yl)ethyl)-, (3S-(3alpha,4aalpha,6beta,8aalpha))-; Tezampanel [INN]
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| Activity |
Ki ~ 100000 nM
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[1] | |||
| Compound Name |
(2R,3S)-1-(9-Iodophenanthrene-3-carbonyl)piperazine-2,3-dicarboxylic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1950805; BDBM50364074
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| Activity |
IC50 = 81300 nM
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[2] | |||
| Compound Name |
(S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxythiophene-3-ylmethyl)pyrimidine-2,4-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL379442; BDBM50185318; ZINC13686112
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| Activity |
Ki = 111000 nM
|
[3] | |||
| Non Binders of This Target (in total, 1 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
2-[[3-(2-Amino-2-carboxyethyl)-2,6-dioxo-1-pyrimidinyl]methyl]benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
UBP 296; CHEMBL372631; (RS)-1-(2-amino-2-carboxyethyl)-3-(2-carboxybenzyl)pyrimidine-2,4-dione; 2-[[3-(2-amino-2-carboxyethyl)-2,6-dioxopyrimidin-1-yl]methyl]benzoic acid; SCHEMBL2265718; CTK8G3691; UBP-296; HMS3268J09; HMS3268J11; HMS3413E09; HMS3677E09; BDBM50178148; AKOS024456931; SR-01000597532; SR-01000597532-1; BRD-A45499626-001-01-0; BRD-A45499626-001-02-8; Q27163534
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| Activity |
Ki = 374000 nM
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[4] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. J Med Chem. 2010 Aug 12;53(15):5367-82. | ||||
| REF 2 | Piperazine-2,3-dicarboxylic acid derivatives as dual antagonists of NMDA and GluK1-containing kainate receptors. J Med Chem. 2012 Jan 12;55(1):327-41. | ||||
| REF 3 | Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists. J Med Chem. 2006 Apr 20;49(8):2579-92. | ||||
| REF 4 | Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. J Med Chem. 2005 Dec 1;48(24):7867-81. | ||||
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