Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T76414 | ||||
Target Name | Glutamate [NMDA] receptor subunit epsilon 2 | ||||
Target Type | Clinical Trial |
||||
Drug Potency against Target | TRANSTORINE | Drug Info | IC50 = 16000 nM | [531421] | |
L-695902 | Drug Info | IC50 = 6500 nM | |||
4-Chloro-3-hydroxy-1H-quinolin-2-one | Drug Info | IC50 = 1400 nM | |||
4,5,7-Trichloro-3-hydroxy-1H-quinolin-2-one | Drug Info | IC50 = 4500 nM | |||
5,7-Dichloro-4-hydroxy-3-phenyl-1H-quinolin-2-one | Drug Info | IC50 = 97 nM | |||
RPR-104632 | Drug Info | IC50 = 8.3 nM | [525816] | ||
4-Phosphonomethyl-piperidine-2-carboxylic acid | Drug Info | IC50 = 452 nM | [533067] | ||
4-Bromo-5,7-dichloro-3-hydroxy-1H-quinolin-2-one | Drug Info | IC50 = 2800 nM | |||
7-chloro-3-hydroxyquinazoline-2,4-dione | Drug Info | Ki = 240 nM | [528453] | ||
Phe-Pro-Glu | Drug Info | Ki = 4850 nM | [527903] | ||
Nle-Pro-Glu | Drug Info | Ki = 19500 nM | [527903] | ||
N,N'-Bis-(4-hexyl-phenyl)-guanidine | Drug Info | IC50 = 7790 nM | [534685] | ||
L-701324 | Drug Info | Ki = 1.4 nM | [527994] | ||
(R)-2-Amino-5-phosphono-pentanoic acid | Drug Info | Ki = 280 nM | [527496] | ||
Phenethyl-(3-phenyl-propyl)-amine | Drug Info | IC50 = 7300 nM | [534696] | ||
Phenethyl-(4-phenyl-butyl)-amine | Drug Info | IC50 = 3500 nM | [534696] | ||
Conantokin-R | Drug Info | IC50 = 1000 nM | [529118] | ||
8-Fluoro-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | IC50 = 490 nM | [534270] | ||
6,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione | Drug Info | IC50 = 430 nM | [527036] | ||
8-Ethyl-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | IC50 = 5100 nM | [534270] | ||
6-Chloro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | IC50 = 1800 nM | [534504] | ||
Conantokin-G | Drug Info | IC50 = 100 nM | [529118] | ||
PHENCYCLIDINE | Drug Info | IC50 = 9.8 nM | [534286] | ||
5,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | IC50 = 170 nM | |||
Benzyl 4-aminobutyl(3-aminopropyl)carbamate | Drug Info | IC50 = 17600 nM | [528098] | ||
2-(4-Phenoxy-benzyl)-1H-benzoimidazole | Drug Info | Ki = 260 nM | [527020] | ||
6-Methoxy-2-(4-phenoxy-benzyl)-1H-benzoimidazole | Drug Info | Ki = 8400 nM | [527020] | ||
2-(4-benzyl-piperidin-1-ylmethyl)-1H-indol-6-ol | Drug Info | IC50 = 1158 nM | [528664] | ||
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline | Drug Info | Ki = 29 nM | [526618] | ||
N-(2-methoxybenzyl)cinnamamidine | Drug Info | IC50 = 6.6 nM | [527787] | ||
AP-7 | Drug Info | IC50 = 390 nM | [526787] | ||
7-Chloro-3-nitro-3,4-dihydro-1H-quinolin-2-one | Drug Info | IC50 = 410 nM | |||
2-Methylamino-succinic acid(NMDA) | Drug Info | IC50 = 6000 nM | [531531] | ||
N-(3-phenethoxybenzyl)-4-hydroxybenzamide | Drug Info | Ki = 5.6 nM | [529014] | ||
RPR-118723 | Drug Info | IC50 = 28 nM | [525816] | ||
N-(4-(benzyloxy)phenethyl)pyridin-4-amine | Drug Info | IC50 = 102 nM | [528635] | ||
N,N'-Bis-(4-sec-butyl-phenyl)-guanidine | Drug Info | IC50 = 10100 nM | [534685] | ||
GLUTAMATE | Drug Info | IC50 = 70 nM | [526787] | ||
Ala-Pro-Glu | Drug Info | Ki = 2660 nM | [527903] | ||
Gly-Hyp-Glu | Drug Info | Ki = 9240 nM | [527903] | ||
Gly-Pip-Glu | Drug Info | Ki = 2390 nM | [527903] | ||
N,N'-Bis-(4-isopropyl-phenyl)-guanidine | Drug Info | IC50 = 17900 nM | [534685] | ||
H-Gly-D-dmP-Glu-OH | Drug Info | Ki = 330 nM | [528176] | ||
L-687414 | Drug Info | IC50 = 2700 nM | |||
3-phenyl-4-hydroxyquinolin-2(1H)-one | Drug Info | Ki = 12200 nM | [527994] | ||
4-Benzyl-1-(2-phenoxy-ethyl)-piperidine | Drug Info | IC50 = 630 nM | [525548] | ||
N,N'-Bis-(4-butyl-phenyl)-guanidine | Drug Info | IC50 = 3320 nM | [534685] | ||
4-[2-(3-Phenyl-propylamino)-ethyl]-phenol | Drug Info | IC50 = 96 nM | [534696] | ||
4-[2-(6-Phenyl-hexylamino)-ethyl]-phenol | Drug Info | IC50 = 35 nM | [534696] | ||
4-[2-(5-Phenyl-pentylamino)-ethyl]-phenol | Drug Info | IC50 = 8 nM | [534696] | ||
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-4-ol | Drug Info | Ki = 140 nM | [527020] | ||
6-Nitro-2-(4-phenoxy-benzyl)-1H-benzoimidazole | Drug Info | Ki = 5400 nM | [527020] | ||
6-Nitro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | IC50 = 3800 nM | [534504] | ||
8-Chloro-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | IC50 = 13 nM | [534270] | ||
4-[3-(5-Phenyl-pentylamino)-propyl]-phenol | Drug Info | IC50 = 45 nM | [534696] | ||
5,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione | Drug Info | IC50 = 750 nM | [527036] | ||
3-Hydroxy-8-methyl-1H-benzo[b]azepine-2,5-dione | Drug Info | IC50 = 130 nM | [534270] | ||
4-[2-(4-Benzyl-piperidin-1-yl)-ethoxy]-phenol | Drug Info | IC50 = 25 nM | [525548] | ||
DNQX | Drug Info | IC50 = 4500 nM | [529309] | ||
4-[3-(4-Phenyl-butylamino)-propyl]-phenol | Drug Info | IC50 = 20 nM | [525527] | ||
Gly-b7Pro-Glu | Drug Info | Ki = 480 nM | [527903] | ||
Besonprodil | Drug Info | IC50 = 6.6 nM | [528259] | ||
L-698532 | Drug Info | Ki = 151 nM | [527994] | ||
4-hydroxy-5-phenylthieno[2,3-b]pyridin-6(7H)-one | Drug Info | Ki = 16400 nM | [527994] | ||
4-[2-(4-Phenyl-piperidin-1-yl)-ethoxy]-phenol | Drug Info | IC50 = 7700 nM | [525548] | ||
Gly-Amp-Glu | Drug Info | Ki = 15540 nM | [527903] | ||
(D)-Ala-Pro-Glu | Drug Info | Ki = 5400 nM | [527903] | ||
4,6-Dichloro-1H-indole-2-carboxylic acid | Drug Info | IC50 = 6000 nM | [531421] | ||
N,N'-Bis-(4-butoxy-phenyl)-guanidine | Drug Info | IC50 = 3480 nM | [534685] | ||
H-Gly-dmP-Glu-OH | Drug Info | Ki = 3790 nM | [528176] | ||
N,N'-Bis-(4-ethyl-phenyl)-guanidine | Drug Info | IC50 = 7910 nM | [534685] | ||
DITOLYLGUANIDINE | Drug Info | IC50 = 10200 nM | [534685] | ||
4-{2-[Ethyl-(4-phenyl-butyl)-amino]-ethyl}-phenol | Drug Info | IC50 = 300 nM | [534696] | ||
4-Benzyl-1-phenethyl-piperidine hydrochloride | Drug Info | IC50 = 1100 nM | [534696] | ||
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ylamine | Drug Info | Ki = 180 nM | [527020] | ||
4-[2-(4-Phenyl-butylamino)-ethyl]-phenol | Drug Info | IC50 = 43 nM | [534696] | ||
ELIPRODIL | Drug Info | IC50 = 1400 nM | [525548] | ||
3-Hydroxy-7-nitro-1H-benzo[b]azepine-2,5-dione | Drug Info | IC50 = 12000 nM | [534270] | ||
8-Bromo-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | IC50 = 79 nM | [534270] | ||
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ol | Drug Info | Ki = 3.2 nM | [527020] | ||
3-Benzoyl-7-chloro-4-hydroxy-1H-quinolin-2-one | Drug Info | IC50 = 3200 nM | |||
4-[2-(4-Phenyl-butoxy)-ethyl]-phenol | Drug Info | IC50 = 3700 nM | [534696] | ||
(R)-2-Amino-7-phosphono-heptanoic acid | Drug Info | Ki = 640 nM | [527496] | ||
YM-90K | Drug Info | IC50 = 10400 nM | [525786] | ||
DIZOCILPINE | Drug Info | Ki = 2.2 nM | [533655] | ||
3-Hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | IC50 = 830 nM | [534270] | ||
H-Gly-PMe-Glu-OH | Drug Info | Ki = 7960 nM | [528176] | ||
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | Ki = 8 nM | [526618] | ||
MDL-105519 | Drug Info | IC50 = 157 nM | [527438] | ||
3-Hydroxy-6-methyl-1H-benzo[b]azepine-2,5-dione | Drug Info | IC50 = 13000 nM | [534270] | ||
NBQX | Drug Info | IC50 = 200 nM | [526134] | ||
The Effect of Target Knockout, Knockdown or Genetic Variations | We investigated the effect of intrathecal (i.t.) injection of siRNAs targeting NMDA-R2B receptor subunit protein (NR2B) receptors, a subunit of NMDA receptor, for the modulationof pain. The results indicate that the use of siRNA targeting the NR2B subunit not only decreased the expression of NR2B mRNA and its associated protein, as demonstrated by real-time PCR and Western blotting, but also abolished formalin-induced pain behaviors in rat model. The peak effect occurred on day 3 for mRNA and day 7 for its protein, following i.t. injection of 5 microg of siRNA-NR2B. These data prove the feasibility of i.t. siRNAs in the investigation of functional gene expression in the context of whole animal behavior for the management of chronic pain. | [531421] | |||
References | |||||
Ref 531421 | J 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 525816 | J 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 533067 | J 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 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 527903 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. | ||||
Ref 527903 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. | ||||
Ref 534685 | J 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 527994 | J 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 527496 | J 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 534696 | J 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 534696 | J 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 529118 | J 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 534270 | J 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 527036 | Bioorg 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 534270 | J 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 534504 | J 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 529118 | J 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 534286 | J 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 528098 | Bioorg 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 527020 | J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. | ||||
Ref 527020 | J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. | ||||
Ref 528664 | J Med Chem. 2007 Mar 8;50(5):901-14. Epub 2007 Feb 10.Selective NR1/2B N-methyl-D-aspartate receptor antagonists among indole-2-carboxamides and benzimidazole-2-carboxamides. | ||||
Ref 526618 | Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists. | ||||
Ref 527787 | Bioorg 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 526787 | J 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 531531 | J Med Chem. 1990 Oct;33(10):2772-7.2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. | ||||
Ref 529014 | Bioorg Med Chem Lett. 2007 Oct 15;17(20):5537-42. Epub 2007 Aug 19.Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation. | ||||
Ref 525816 | J 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 528635 | J Med Chem. 2007 Feb 22;50(4):807-19. Epub 2007 Jan 24.Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist. | ||||
Ref 534685 | J 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 526787 | J 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 527903 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. | ||||
Ref 527903 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. | ||||
Ref 527903 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. | ||||
Ref 534685 | J 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 528176 | Bioorg 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 527994 | J 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 525548 | J Med Chem. 1999 Jul 29;42(15):2993-3000.4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist. | ||||
Ref 534685 | J 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 534696 | J 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 534696 | J 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 534696 | J 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 527020 | J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. | ||||
Ref 527020 | J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. | ||||
Ref 534504 | J 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 534270 | J 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 534696 | J 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 527036 | Bioorg 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 534270 | J 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 525548 | J Med Chem. 1999 Jul 29;42(15):2993-3000.4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist. | ||||
Ref 529309 | J Med Chem. 1991 Apr;34(4):1243-52.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. | ||||
Ref 525527 | Bioorg Med Chem Lett. 1999 Jun 7;9(11):1619-24.Structure-activity relationship for a series of 2-substituted 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indoles: potent subtype-selective inhibitors of N-methyl-D-aspartate (NMDA) receptors. | ||||
Ref 527903 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. | ||||
Ref 528259 | Bioorg Med Chem Lett. 2006 Sep 1;16(17):4638-40. Epub 2006 Jun 16.Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists. | ||||
Ref 527994 | J 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 527994 | J 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 525548 | J Med Chem. 1999 Jul 29;42(15):2993-3000.4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist. | ||||
Ref 527903 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. | ||||
Ref 527903 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6.New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. | ||||
Ref 531421 | J 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 534685 | J 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 528176 | Bioorg 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 534685 | J 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 534685 | J 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 534696 | J 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 534696 | J 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 527020 | J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. | ||||
Ref 534696 | J 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 525548 | J Med Chem. 1999 Jul 29;42(15):2993-3000.4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist. | ||||
Ref 534270 | J 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 534270 | J 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 527020 | J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. | ||||
Ref 534696 | J 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 527496 | J 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 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 533655 | J 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 534270 | J 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 528176 | Bioorg 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 526618 | Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62.4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists. | ||||
Ref 527438 | J 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. | ||||
Ref 534270 | J 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 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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