Target Validation Information
Target ID T22285
Target Name Glutamate [NMDA] receptor subunit epsilon 1
Target Type
Successful
Drug Potency against Target DNQX Drug Info IC50 = 4500 nM [529309]
Besonprodil Drug Info IC50 = 6.6 nM [528259]
(D)-Ala-Pro-Glu Drug Info Ki = 5400 nM [527903]
Gly-Pip-Glu Drug Info Ki = 2390 nM [527903]
Ala-Pro-Glu Drug Info Ki = 2660 nM [527903]
3-Hydroxy-8-methyl-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 130 nM [534270]
4-[2-(5-Phenyl-pentylamino)-ethyl]-phenol Drug Info IC50 = 12000 nM [534696]
4-[2-(4-Phenyl-butylamino)-ethyl]-phenol Drug Info IC50 = 15000 nM [534696]
8-Bromo-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 79 nM [534270]
5,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione Drug Info IC50 = 750 nM [527036]
N,N'-Bis-(4-ethyl-phenyl)-guanidine Drug Info IC50 = 7910 nM [534685]
Conantokin-R Drug Info IC50 = 1000 nM [529118]
(R)-2-Amino-7-phosphono-heptanoic acid Drug Info Ki = 76 nM [527496]
N-(2-methoxybenzyl)cinnamamidine Drug Info IC50 = 6.6 nM [527787]
L-695902 Drug Info IC50 = 6500 nM
4-Bromo-5,7-dichloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 2800 nM
Gly-Amp-Glu Drug Info Ki = 15540 nM [527903]
N,N'-Bis-(4-sec-butyl-phenyl)-guanidine Drug Info IC50 = 10100 nM [534685]
AP-7 Drug Info IC50 = 390 nM [526787]
4-hydroxy-5-phenylthieno[2,3-b]pyridin-6(7H)-one Drug Info Ki = 16400 nM [527994]
8-Ethyl-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 5100 nM [534270]
3-phenyl-4-hydroxyquinolin-2(1H)-one Drug Info Ki = 12200 nM [527994]
2-Methylamino-succinic acid(NMDA) Drug Info IC50 = 6000 nM [531531]
7-Chloro-3-nitro-3,4-dihydro-1H-quinolin-2-one Drug Info IC50 = 410 nM
NBQX Drug Info IC50 = 200 nM [526134]
L-701324 Drug Info Ki = 1.4 nM [527994]
Nle-Pro-Glu Drug Info Ki = 19500 nM [527903]
4,6-Dichloro-1H-indole-2-carboxylic acid Drug Info IC50 = 6000 nM [531421]
Phe-Pro-Glu Drug Info Ki = 4850 nM [527903]
H-Gly-dmP-Glu-OH Drug Info Ki = 3790 nM [528176]
4-[2-(6-Phenyl-hexylamino)-ethyl]-phenol Drug Info IC50 = 17000 nM [534696]
DITOLYLGUANIDINE Drug Info IC50 = 10200 nM [534685]
N,N'-Bis-(4-isopropyl-phenyl)-guanidine Drug Info IC50 = 17900 nM [534685]
N,N'-Bis-(4-butyl-phenyl)-guanidine Drug Info IC50 = 3320 nM [534685]
8-Fluoro-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 490 nM [534270]
7-chloro-3-hydroxyquinazoline-2,4-dione Drug Info Ki = 240 nM [528453]
4-[3-(4-Phenyl-butylamino)-propyl]-phenol Drug Info IC50 = 18000 nM [534696]
TRANSTORINE Drug Info IC50 = 16000 nM [531421]
3-Hydroxy-6-methyl-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 13000 nM [534270]
6,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione Drug Info IC50 = 430 nM [527036]
5,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 170 nM
4-Phosphonomethyl-piperidine-2-carboxylic acid Drug Info IC50 = 452 nM [533067]
5,7-Dichloro-4-hydroxy-3-phenyl-1H-quinolin-2-one Drug Info IC50 = 97 nM
Glycine Drug Info IC50 = 170 nM [553100]
L-687414 Drug Info IC50 = 2700 nM
6-Nitro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 3800 nM [534504]
4,5,7-Trichloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 4500 nM
GLUTAMATE Drug Info IC50 = 70 nM [526787]
RPR-104632 Drug Info IC50 = 8.3 nM [525816]
RPR-118723 Drug Info IC50 = 28 nM [525816]
Gly-b7Pro-Glu Drug Info Ki = 480 nM [527903]
Gly-Hyp-Glu Drug Info Ki = 9240 nM [527903]
H-Gly-D-dmP-Glu-OH Drug Info Ki = 330 nM [528176]
4-[3-(5-Phenyl-pentylamino)-propyl]-phenol Drug Info IC50 = 18000 nM [534696]
N,N'-Bis-(4-hexyl-phenyl)-guanidine Drug Info IC50 = 7790 nM [534685]
L-698532 Drug Info Ki = 151 nM [527994]
3-Hydroxy-7-nitro-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 12000 nM [534270]
(R)-2-Amino-5-phosphono-pentanoic acid Drug Info Ki = 170 nM [527496]
N,N'-Bis-(4-butoxy-phenyl)-guanidine Drug Info IC50 = 3480 nM [534685]
6-Chloro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 1800 nM [534504]
8-Chloro-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 13 nM [534270]
3-Hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 830 nM [534270]
YM-90K Drug Info IC50 = 10400 nM [525786]
4-Chloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 1400 nM
Benzyl 4-aminobutyl(3-aminopropyl)carbamate Drug Info IC50 = 17600 nM [528098]
PHENCYCLIDINE Drug Info IC50 = 9.8 nM [534286]
3-Benzoyl-7-chloro-4-hydroxy-1H-quinolin-2-one Drug Info IC50 = 3200 nM
H-Gly-PMe-Glu-OH Drug Info Ki = 7960 nM [528176]
DIZOCILPINE Drug Info Ki = 2.2 nM [533655]
MDL-105519 Drug Info IC50 = 157 nM [527438]
References
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Ref 528259Bioorg Med Chem Lett. 2006 Sep 1;16(17):4638-40. Epub 2006 Jun 16.Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
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Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 527036Bioorg Med Chem Lett. 2004 May 3;14(9):2345-9.3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 529118J Biol Chem. 2007 Dec 21;282(51):36905-13. Epub 2007 Oct 25.Novel conantokins from Conus parius venom are specific antagonists of N-methyl-D-aspartate receptors.
Ref 527496J Med Chem. 2005 Apr 7;48(7):2627-37.Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
Ref 527787Bioorg Med Chem Lett. 2005 Dec 15;15(24):5439-41. Epub 2005 Oct 5.Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 526787J Med Chem. 1992 Dec 11;35(25):4720-6.Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
Ref 527994J Med Chem. 2006 Feb 9;49(3):864-71.Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 527994J Med Chem. 2006 Feb 9;49(3):864-71.Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
Ref 531531J Med Chem. 1990 Oct;33(10):2772-7.2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
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.
Ref 527994J Med Chem. 2006 Feb 9;49(3):864-71.Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 531421J Med Chem. 1990 Nov;33(11):2944-6.3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 528176Bioorg Med Chem Lett. 2006 Jul 1;16(13):3396-400. Epub 2006 May 2.The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
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 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 531421J Med Chem. 1990 Nov;33(11):2944-6.3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 527036Bioorg Med Chem Lett. 2004 May 3;14(9):2345-9.3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists.
Ref 533067J Med Chem. 1989 Sep;32(9):2171-8.4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvulsant activity.
Ref 553100Evidence for direct interactions between the NMDA and glycine recognition sites in brain. Eur J Pharmacol. 1990 Mar 13;188(2-3):175-9.
Ref 534504J Med Chem. 1997 Oct 24;40(22):3679-86.5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
Ref 526787J Med Chem. 1992 Dec 11;35(25):4720-6.Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
Ref 525816J Med Chem. 2000 Jun 15;43(12):2371-81.Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
Ref 525816J Med Chem. 2000 Jun 15;43(12):2371-81.Indeno[1,2-b]pyrazin-2,3-diones: a new class of antagonists at the glycine site of the NMDA receptor with potent in vivo activity.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 527903Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Ref 528176Bioorg Med Chem Lett. 2006 Jul 1;16(13):3396-400. Epub 2006 May 2.The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity.
Ref 534696J Med Chem. 1998 Aug 27;41(18):3499-506.Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 527994J Med Chem. 2006 Feb 9;49(3):864-71.Synthesis of thieno[2,3-b]pyridinones acting as cytoprotectants and as inhibitors of [3H]glycine binding to the N-methyl-D-aspartate (NMDA) receptor.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 527496J Med Chem. 2005 Apr 7;48(7):2627-37.Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists.
Ref 534685J Med Chem. 1998 Aug 13;41(17):3298-302.Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents.
Ref 534504J Med Chem. 1997 Oct 24;40(22):3679-86.5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and kainate receptors.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
Ref 534270J Med Chem. 1996 Nov 8;39(23):4643-53.Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites.
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 528098Bioorg Med Chem Lett. 2006 Jun 1;16(11):2837-41. Epub 2006 Mar 24.Polyamines and the NMDA receptor: modifying intrinsic activities with aromatic substituents.
Ref 534286J Med Chem. 1996 Nov 22;39(24):4844-52.Synthesis and biological activity of conformationally restricted analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxamide, an efficient noncompetitive N-methyl-D-aspartic acid receptor antagonist.
Ref 528176Bioorg Med Chem Lett. 2006 Jul 1;16(13):3396-400. Epub 2006 May 2.The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity.
Ref 533655J Med Chem. 1995 Jun 23;38(13):2483-9.Synthesis and evaluation of 6,11-ethanohexahydrobenzo[b]quinolizidines: a new class of noncompetitive N-methyl-D-aspartate antagonists.
Ref 527438J Med Chem. 2005 Feb 24;48(4):995-1018.CoMFA, synthesis, and pharmacological evaluation of (E)-3-(2-carboxy-2-arylvinyl)-4,6-dichloro-1H-indole-2-carboxylic acids: 3-[2-(3-aminophenyl)-2-carboxyvinyl]-4,6-dichloro-1H-indole-2-carboxylic acid, a potent selective glycine-site NMDA receptor antagonist.

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