Proteins > Glutamate receptor ionotropic, kainate 5
Page last updated: 2024-08-07 17:14:19
Glutamate receptor ionotropic, kainate 5
A glutamate receptor ionotropic, kainate 5 that is encoded in the genome of rat. [OMA:Q63273, PRO:DNx]
Synonyms
GluK5;
Glutamate receptor KA-2;
KA2
Research
Bioassay Publications (35)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 2 (5.71) | 18.7374 |
| 1990's | 21 (60.00) | 18.2507 |
| 2000's | 12 (34.29) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (41)
Drugs with Potency Measurements
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | IC50 | 80.0400 | 4 | 5 |
| ibotenic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| 5,7-dichlorokynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 300.0000 | 1 | 2 |
| 7-chlorokynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 2 |
| alpha-amino-3-hydroxy-5-tert-butyl-4-isoxazolepropionate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| kynurenic acid | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 2 |
| kainic acid | Rattus norvegicus (Norway rat) | IC50 | 0.0126 | 8 | 10 |
| kainic acid | Rattus norvegicus (Norway rat) | Ki | 0.0150 | 1 | 1 |
| n-methylaspartate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| glutamic acid | Rattus norvegicus (Norway rat) | IC50 | 0.3800 | 3 | 5 |
| glutamic acid | Rattus norvegicus (Norway rat) | Ki | 0.0630 | 1 | 1 |
| quisqualic acid | Rattus norvegicus (Norway rat) | IC50 | 0.1500 | 1 | 1 |
| n,n'-bis(salicyl)hydrazine | Rattus norvegicus (Norway rat) | IC50 | 1,000.0000 | 1 | 1 |
| 6,7-dichloroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | IC50 | 52,000.0000 | 1 | 1 |
| sym 2081 | Rattus norvegicus (Norway rat) | IC50 | 0.0350 | 1 | 1 |
| 1-amino-1,3-dicarboxycyclopentane | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| 2-amino-3-(3-(carboxymethoxy)-5-methylisoxazol-4-yl)propionic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| 2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| ly 293558 | Rattus norvegicus (Norway rat) | IC50 | 107.6038 | 5 | 8 |
| alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 5 | 5 |
| alpha-amino-3-(hydroxy)-5-methyl-4-isoxazoleacetic acid | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 2 | 2 |
| eglumetad | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| mdl29,951 | Rattus norvegicus (Norway rat) | IC50 | 418.0000 | 1 | 1 |
| (S)-ATPA | Rattus norvegicus (Norway rat) | IC50 | 23.0000 | 1 | 1 |
| 4-methylglutamic acid, threo-(l)-isomer | Rattus norvegicus (Norway rat) | IC50 | 0.3100 | 1 | 1 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Rattus norvegicus (Norway rat) | IC50 | 2.9090 | 8 | 9 |
| 2,3-dioxo-6-nitro-7-sulfamoylbenzo(f)quinoxaline | Rattus norvegicus (Norway rat) | Ki | 4.1000 | 1 | 1 |
| 6-nitro-1,4-dihydroquinoxaline-2,3-dione | Rattus norvegicus (Norway rat) | IC50 | 15,000.0000 | 1 | 1 |
| 2r,4r-4-aminopyrrolidine-2,4-dicarboxylate | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| lofepramine hydrochloride | Rattus norvegicus (Norway rat) | IC50 | 0.2800 | 2 | 2 |
| lofepramine hydrochloride | Rattus norvegicus (Norway rat) | Ki | 2.2000 | 1 | 1 |
| gavestinel | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| ampa, (r)-isomer | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| tqx 173 | Rattus norvegicus (Norway rat) | IC50 | 11.5250 | 4 | 4 |
| naveglitazar | Rattus norvegicus (Norway rat) | IC50 | 1.9160 | 1 | 1 |
| ly 379268 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Novel 1-hydroxyazole bioisosteres of glutamic acid. Synthesis, protolytic properties, and pharmacology.Journal of medicinal chemistry, , Jan-03, Volume: 45, Issue:1, 2002
Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R,S)-APPA].Journal of medicinal chemistry, , Apr-01, Volume: 37, Issue:7, 1994
Excitatory amino acid receptor ligands. Synthesis and biological activity of 3-isoxazolol amino acids structurally related to homoibotenic acid.Journal of medicinal chemistry, , Sep-18, Volume: 35, Issue:19, 1992
Heterocyclic excitatory amino acids. Synthesis and biological activity of novel analogues of AMPA.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Synthesis and pharmacology of a new AMPA-kainate receptor agonist with potent convulsant activity.Journal of medicinal chemistry, , Sep-24, Volume: 41, Issue:20, 1998
Synthesis and pharmacology of highly selective carboxy and phosphono isoxazole amino acid AMPA receptor antagonists.Journal of medicinal chemistry, , Apr-12, Volume: 39, Issue:8, 1996
Synthesis, resolution, and biological evaluation of the four stereoisomers of 4-methylglutamic acid: selective probes of kainate receptors.Journal of medicinal chemistry, , Jul-07, Volume: 38, Issue:14, 1995
Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R,S)-APPA].Journal of medicinal chemistry, , Apr-01, Volume: 37, Issue:7, 1994
Heterocyclic excitatory amino acids. Synthesis and biological activity of novel analogues of AMPA.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Synthesis and structure-activity studies on excitatory amino acids structurally related to ibotenic acid.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Ibotenic acid analogues. Synthesis and biological and in vitro activity of conformationally restricted agonists at central excitatory amino acid receptors.Journal of medicinal chemistry, , Volume: 27, Issue:5, 1984
A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). new glutamate and aspartate analogues as potential neuroprotective agents.Journal of medicinal chemistry, , Aug-02, Volume: 44, Issue:16, 2001
Heterocyclic excitatory amino acids. Synthesis and biological activity of novel analogues of AMPA.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Synthesis and structure-activity studies on excitatory amino acids structurally related to ibotenic acid.Journal of medicinal chemistry, , Volume: 28, Issue:5, 1985
Ibotenic acid analogues. Synthesis and biological and in vitro activity of conformationally restricted agonists at central excitatory amino acid receptors.Journal of medicinal chemistry, , Volume: 27, Issue:5, 1984
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
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.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Structure-activity studies of 6-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 2. Effects of distal acid bioisosteric substitution, absolute stereochemical preferences, and in vivo activity.Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
Structure-activity studies of 6-(tetrazolylalkyl)-substituted decahydroisoquinoline-3-carboxylic acid AMPA receptor antagonists. 1. Effects of stereochemistry, chain length, and chain substitution.Journal of medicinal chemistry, , May-24, Volume: 39, Issue:11, 1996
(S)-2-Amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta[d]isoxazol-4-yl)propionic acid, a potent and selective agonist at the GluR5 subtype of ionotropic glutamate receptors. Synthesis, modeling, and molecular pharmacology.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists.Journal of medicinal chemistry, , Oct-07, Volume: 42, Issue:20, 1999
Synthesis and pharmacology of a new AMPA-kainate receptor agonist with potent convulsant activity.Journal of medicinal chemistry, , Sep-24, Volume: 41, Issue:20, 1998
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
N-methyl-D-aspartic acid receptor agonists: resolution, absolute stereochemistry, and pharmacology of the enantiomers of 2-amino-2-(3-hydroxy-5-methyl-4-isoxazolyl)acetic acid.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
A new highly selective metabotropic excitatory amino acid agonist: 2-amino-4-(3-hydroxy-5-methylisoxazol-4-yl)butyric acid.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.Journal of medicinal chemistry, , Apr-20, Volume: 49, Issue:8, 2006
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
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.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
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.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Structure-activity relationships in a series of 2(1H)-quinolones bearing different acidic function in the 3-position: 6,7-dichloro-2(1H)-oxoquinoline-3-phosphonic acid, a new potent and selective AMPA/kainate antagonist with neuroprotective properties.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Novel AMPA receptor antagonists: synthesis and structure-activity relationships of 1-hydroxy-7-(1H-imidazol-1-yl)-6-nitro-2,3(1H,4H)- quinoxalinedione and related compounds.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Synthesis of 1,4,7,8,9,10-hexahydro-9-methyl-6-nitropyrido[3,4-f]- quinoxaline-2,3-dione and related quinoxalinediones: characterization of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (and N-methyl-D-aspartate) receptor and anticonvulsant actJournal of medicinal chemistry, , Sep-15, Volume: 38, Issue:19, 1995
5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.Journal of medicinal chemistry, , Oct-24, Volume: 40, Issue:22, 1997
Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antagonists at the glycine site on the N-methyl-D-aspartate receptor.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
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.Bioorganic & medicinal chemistry letters, , May-15, Volume: 10, Issue:10, 2000
Structure-activity relationships in a series of 2(1H)-quinolones bearing different acidic function in the 3-position: 6,7-dichloro-2(1H)-oxoquinoline-3-phosphonic acid, a new potent and selective AMPA/kainate antagonist with neuroprotective properties.Journal of medicinal chemistry, , Jan-05, Volume: 39, Issue:1, 1996
Novel AMPA receptor antagonists: synthesis and structure-activity relationships of 1-hydroxy-7-(1H-imidazol-1-yl)-6-nitro-2,3(1H,4H)- quinoxalinedione and related compounds.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Synthesis and biological evaluation of analogues of 7-chloro-4,5-dihydro-4- oxo-8-(1,2,4-triazol-4-yl)-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylic acid (TQX-173) as novel selective AMPA receptor antagonists.Journal of medicinal chemistry, , Jan-01, Volume: 47, Issue:1, 2004
Synthesis and biological evaluation of a new set of pyrazolo[1,5-c]quinazoline-2-carboxylates as novel excitatory amino acid antagonists.Journal of medicinal chemistry, , Feb-28, Volume: 45, Issue:5, 2002
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.Journal of medicinal chemistry, , Sep-13, Volume: 44, Issue:19, 2001
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.Journal of medicinal chemistry, , Oct-19, Volume: 43, Issue:21, 2000
Synthesis, pharmacological characterization, and molecular modeling of heterobicyclic amino acids related to (+)-2-aminobicyclo[3.1.0] hexane-2,6-dicarboxylic acid (LY354740): identification of two new potent, selective, and systemically active agonists fJournal of medicinal chemistry, , Mar-25, Volume: 42, Issue:6, 1999