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Found 612 Enz. Inhib. hit(s) with Target = 'Glutamate receptor ionotropic, kainate 1'
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50126761((S)-2-AMINO-3-(3-HYDROXY-5-TERT-BUTYLISOTHIAZOL-4-...)
Affinity DataEC50:  100nMAssay Description:Agonist activity at GluK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50126764((S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta...)
Affinity DataEC50:  130nMAssay Description:Agonist activity at ConA-treated rat GluR5(Q) RNA-edited isoform expressed in Xenopus laevis oocytes assessed as glutamic acid-induced maximal curren...Checked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50126764((S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta...)
Affinity DataEC50:  580nMAssay Description:Agonist activity at rat recombinant GluR5(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo...Checked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50295042((S)-2-Amino-3-((RS)-3-hydroxy-8-methyl-7,8-dihydro...)
Affinity DataEC50:  660nMAssay Description:Agonist activity at ConA-treated rat GluR5(Q) RNA-edited isoform expressed in Xenopus laevis oocytes assessed as glutamic acid-induced maximal curren...Checked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50126763((S)-2-amino-3-(3-hydroxy-5-tert-butyl-4-isoxazolyl...)
Affinity DataEC50:  660nMAssay Description:Agonist activity at ConA-treated rat GluR5(Q) RNA-edited isoform expressed in Xenopus laevis oocytes assessed as glutamic acid-induced maximal curren...Checked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50088222((2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pe...)
Affinity DataEC50:  800nMAssay Description:Compound was tested for agonistic activity on rat dorsal root ganglion neurons (thought to express GluR5 receptors)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50295042((S)-2-Amino-3-((RS)-3-hydroxy-8-methyl-7,8-dihydro...)
Affinity DataEC50:  860nMAssay Description:Agonist activity at rat recombinant GluR5(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo...Checked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50091477((S)-2-Amino-4-cyclopentylidene-pentanedioic acid |...)
Affinity DataEC50:  1.05E+3nMAssay Description:Compound was tested for agonistic activity on rat dorsal root ganglion neurons (thought to express GluR5 receptors)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088222((2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pe...)
Affinity DataEC50:  2.50E+3nMAssay Description:Agonist activity at GluK1 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088222((2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pe...)
Affinity DataEC50:  2.50E+3nMAssay Description:Compound was tested for agonistic activity at Glutamate receptor 6 using HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088222((2S,4R)-2-Amino-4-((E)-3-naphthalen-2-yl-allyl)-pe...)
Affinity DataEC50:  2.50E+3nMAssay Description:Effective concentration against GluR5 expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088197(CHEMBL58590 | E-2-Amino-4-[3-(4-chloro-phenyl)-all...)
Affinity DataEC50:  2.80E+3nMAssay Description:Effective concentration of the compound required for evoking response in HEK293 cellMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088216(CHEMBL59284 | E-2-Amino-4-[3-(2-methoxy-phenyl)-al...)
Affinity DataEC50:  3.30E+3nMAssay Description:Effective concentration against GluR5 expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088213((2S,4R)-4-allyl glutamate | 2-Allyl-4-amino-pentan...)
Affinity DataEC50:  4.40E+3nMAssay Description:Effective concentration of the compound required for evoking response in HEK293 cellMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50088212(2-Amino-4-but-2-enyl-pentanedioic acid(LY339180) |...)
Affinity DataEC50:  4.50E+3nMAssay Description:Effective concentration of the compound required for evoking response in HEK293 cellMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50091477((S)-2-Amino-4-cyclopentylidene-pentanedioic acid |...)
Affinity DataEC50:  6.20E+3nMAssay Description:Compound was tested for agonistic activity at Glutamate receptor 5 using HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50002369((2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methyleth...)
Affinity DataEC50:  1.20E+4nMAssay Description:Compound was tested for agonistic activity on rat dorsal root ganglion neurons (thought to express GluR5 receptors)More data for this Ligand-Target Pair
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50091481((S)-2-Amino-4-propylidene-pentanedioicacid | CHEMB...)
Affinity DataEC50:  1.42E+4nMAssay Description:Compound was tested for agonistic activity at Glutamate receptor 5 using HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50002369((2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methyleth...)
Affinity DataEC50:  1.62E+4nMAssay Description:Effective concentration against GluR5 expressed in HEK293 cellsMore data for this Ligand-Target Pair
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50002369((2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methyleth...)
Affinity DataEC50:  1.62E+4nMAssay Description:Compound was tested for agonistic activity at Glutamate receptor 5 using HEK293 cellsMore data for this Ligand-Target Pair
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM26431((2R)-2-aminopentanedioic acid | CHEMBL76232 | D-Gl...)
Affinity DataEC50:  2.20E+4nMAssay Description:Induction of calcium influx in HEK293 cells expressing human GLUK5 by FLIPR assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM17657((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)
Affinity DataEC50:  3.52E+4nMAssay Description:Compound was tested for agonistic activity on rat dorsal root ganglion neurons (thought to express GluR5 receptors)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50002369((2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methyleth...)
Affinity DataEC50:  3.70E+4nMAssay Description:Agonist activity at rat recombinant GluR5(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo...Checked by AuthorMore data for this Ligand-Target Pair
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM17657((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)
Affinity DataEC50:  7.50E+4nMAssay Description:Compound was tested for agonistic activity at Glutamate receptor 6 using HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM26431((2R)-2-aminopentanedioic acid | CHEMBL76232 | D-Gl...)
Affinity DataEC50:  7.50E+4nMAssay Description:Effective concentration against GluR5 expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM17657((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)
Affinity DataEC50:  1.30E+5nMAssay Description:Activity at rat cloned iGluR5 expressed in human HEK293 cells by calcium imaging assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM17657((2S)-2-aminopentanedioic acid | (S)-Glu | D-Glutam...)
Affinity DataEC50:  1.40E+5nMAssay Description:Agonist activity at rat recombinant GluR5(Q) RNA-edited isoform expressed in HEK293 cells assessed as increase in intracellular calcium level by Fluo...Checked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50373180(CHEMBL260328)
Affinity DataEC50:  2.80E+5nMAssay Description:Activity at rat cloned iGluR5 expressed in human HEK293 cells by calcium imaging assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50373179(CHEMBL260327)
Affinity DataEC50: >1.00E+6nMAssay Description:Activity at rat cloned iGluR5 expressed in human HEK293 cells by calcium imaging assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50373181(CHEMBL406621)
Affinity DataEC50: >1.00E+6nMAssay Description:Activity at rat cloned iGluR5 expressed in human HEK293 cells by calcium imaging assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50373182(CHEMBL260122)
Affinity DataEC50: >1.00E+6nMAssay Description:Activity at rat cloned iGluR5 expressed in human HEK293 cells by calcium imaging assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50034501((S)-Amino-(3-hydroxy-isoxazol-5-yl)-acetic acid | ...)
Affinity DataEC50: >1.00E+6nMAssay Description:Activity at rat cloned iGluR5 expressed in human HEK293 cells by calcium imaging assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50166288((S)-2-Amino-3-[3-hydroxy-5-(2-methyl-2H-tetrazol-5...)
Affinity DataKi:  0.0810nMAssay Description:Displacement of [3H]SYM 2081 from rat recombinant GluR5 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50031704((2S,4R)-2-Amino-4-methyl-pentanedioic acid | (2S,4...)
Affinity DataKi:  0.663nMAssay Description:Displacement of [3H]SYM2081 from rat recombinant iGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM85740(Dysiherbaine)
Affinity DataKi:  0.740nMAssay Description:Displacement of [3H]kianic acid from recombinant GluK1 kainate receptor (unknown origin) expressed in HEK293 cell membranes measured after 1 hrMore data for this Ligand-Target Pair
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50252103((2S,3S,4S)-2-CARBOXY-4-[(1Z,3E,5R)-5-CARBOXY-1-MET...)
Affinity DataKi:  1.11nMAssay Description:Displacement of [3H]SYM2081 from rat recombinant iGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50002370((R,S)-alpha-amino-3-hydroxy-5-methyl-4-isooxazole-...)
Affinity DataKi:  1.20nMAssay Description:Displacement of [3H]SYM 2081 from rat recombinant GluR5 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50126763((S)-2-amino-3-(3-hydroxy-5-tert-butyl-4-isoxazolyl...)
Affinity DataKi:  2.13nMAssay Description:Displacement of [3H]SYM from rat recombinant GluR5(Q) RNA-edited isoform expressed in baculovirus infected Sf9 cellsChecked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50002369((2S-(2alpha,3beta,4beta))-2-carboxy-4-(1-methyleth...)
Affinity DataKi:  2.20nMMore data for this Ligand-Target Pair
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50060627((S)-2-Amino-3-(5-iodo-2,4-dioxo-3,4-dihydro-2H-pyr...)
Affinity DataKi:  2.40nMAssay Description:Displacement of [3H]SYM2081 from rat recombinant iGluR5(Q)1b expressed in Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50126764((S)-2-amino-3-(3-hydroxy-7,8-dihydro-6H-cyclohepta...)
Affinity DataKi:  2.57nMAssay Description:Displacement of [3H]SYM from rat recombinant GluR5(Q) RNA-edited isoform expressed in baculovirus infected Sf9 cellsChecked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50166286((RS)-2-amino-3-[3-hydroxy-5-(2-ethyl-2H-5-tetrazol...)
Affinity DataKi:  2.90nMAssay Description:Displacement of [3H]SYM 2081 from rat recombinant GluR5 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50031704((2S,4R)-2-Amino-4-methyl-pentanedioic acid | (2S,4...)
Affinity DataKi:  3nMAssay Description:Binding affinity against human ionotropic glutamate receptor kainate 1 in HK293 cells using [3H]-kainate as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50426285(CHEMBL2312403)
Affinity DataKi:  3.40nMAssay Description:Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluKK1(Q)1b receptor expressed in sf9 cells by liquid scintillati...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50116042(CHEMBL63861 | {7-[3-(4-Benzyl-piperazin-1-ylmethyl...)
Affinity DataKi:  3.80nMAssay Description:Binding affinity towards cloned human GluR5 subunit stably expressed in cultured HEK-293 cells using [3]H-kainate as radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50252051((2S,4R)-2-amino-4-(3-(methylamino)-3-oxopropyl)pen...)
Affinity DataKi:  3.81nMAssay Description:Displacement of [3H]SYM2081 from rat recombinant iGluR5More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50349983(CHEMBL1812596)
Affinity DataKi:  3.90nMAssay Description:Displacement of [3H]SYM2081 from rat GluK1 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50295042((S)-2-Amino-3-((RS)-3-hydroxy-8-methyl-7,8-dihydro...)
Affinity DataKi:  5.08nMAssay Description:Displacement of [3H]SYM from rat recombinant GluR5(Q) RNA-edited isoform expressed in baculovirus infected Sf9 cellsChecked by AuthorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50252920((S)-1-[2'-Amino-2'-carboxyethyl]-5,7-dihydrothieno...)
Affinity DataKi:  5.20nMAssay Description:Displacement of [3H]SYM2081 from rat GluK1 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlutamate receptor ionotropic, kainate 1(RAT)
University Of Copenhagen

Curated by ChEMBL
LigandPNGBDBM50252922((S)-1-(2'-Amino-2'-carboxyethyl)thieno[3,2-d]pyrim...)
Affinity DataKi:  5.29nMAssay Description:Displacement of [3H]SYM2081 from rat GluK1 expressed in Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
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