Target Information

Target General Infomation
Target ID
T62276
Former ID
TTDR01259
Target Name
NMDA receptor subunit NR1
Gene Name
GRIN1
Synonyms
GluN1; Glutamate [NMDA] receptor subunit zeta1; Glutamate receptor ionotropic, NMDA 1; NMDR1; NmethylDaspartate receptor subunit NR1; GRIN1
Target Type
Clinical Trial
Disease Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Convulsions [ICD9: 780.3; ICD10: R56.0]
Multiple scierosis [ICD9: 340; ICD10: G35]
Neurological disease [ICD9: 338, 338.2, 410, 782.3,780; ICD10: I21, I22, R52, R52.1-R52.2, R60.9, G89]
Function
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors.
BioChemical Class
Glutamate-gated ion channel
Target Validation
T62276
UniProt ID
Q05586
Sequence
MSTMRLLTLALLFSCSVARAACDPKIVNIGAVLSTRKHEQMFREAVNQANKRHGSWKIQL
NATSVTHKPNAIQMALSVCEDLISSQVYAILVSHPPTPNDHFTPTPVSYTAGFYRIPVLG
LTTRMSIYSDKSIHLSFLRTVPPYSHQSSVWFEMMRVYSWNHIILLVSDDHEGRAAQKRL
ETLLEERESKAEKVLQFDPGTKNVTALLMEAKELEARVIILSASEDDAATVYRAAAMLNM
TGSGYVWLVGEREISGNALRYAPDGILGLQLINGKNESAHISDAVGVVAQAVHELLEKEN
ITDPPRGCVGNTNIWKTGPLFKRVLMSSKYADGVTGRVEFNEDGDRKFANYSIMNLQNRK
LVQVGIYNGTHVIPNDRKIIWPGGETEKPRGYQMSTRLKIVTIHQEPFVYVKPTLSDGTC
KEEFTVNGDPVKKVICTGPNDTSPGSPRHTVPQCCYGFCIDLLIKLARTMNFTYEVHLVA
DGKFGTQERVNNSNKKEWNGMMGELLSGQADMIVAPLTINNERAQYIEFSKPFKYQGLTI
LVKKEIPRSTLDSFMQPFQSTLWLLVGLSVHVVAVMLYLLDRFSPFGRFKVNSEEEEEDA
LTLSSAMWFSWGVLLNSGIGEGAPRSFSARILGMVWAGFAMIIVASYTANLAAFLVLDRP
EERITGINDPRLRNPSDKFIYATVKQSSVDIYFRRQVELSTMYRHMEKHNYESAAEAIQA
VRDNKLHAFIWDSAVLEFEASQKCDLVTTGELFFRSGFGIGMRKDSPWKQNVSLSILKSH
ENGFMEDLDKTWVRYQECDSRSNAPATLTFENMAGVFMLVAGGIVAGIFLIFIEIAYKRH
KDARRKQMQLAFAAVNVWRKNLQDRKSGRAEPDPKKKATFRAITSTLASSFKRRRSSKDT
STGGGRGALQNQKDTVLPRRAIEREEGQLQLCSRHRES
Structure
2HQW; 2NR1; 3BYA
Drugs and Mode of Action
Drug(s) D-Serine Drug Info Phase 4 Discovery agent [467510], [521721]
ELIPRODIL Drug Info Phase 2 Multiple scierosis [521427]
NBQX Drug Info Phase 1 Neurological disease [467600]
YM-90K Drug Info Discontinued in Phase 2 Convulsions [545107]
AM-92016 Drug Info Terminated Discovery agent [546232]
DIZOCILPINE Drug Info Terminated Cerebrovascular ischaemia [539532], [544717]
L-687414 Drug Info Terminated Discovery agent [544996]
L-695902 Drug Info Terminated Discovery agent [545371]
L-698532 Drug Info Terminated Neurological disease [546154]
L-701324 Drug Info Terminated Cerebrovascular ischaemia [467575], [525504], [534277]
MDL-105519 Drug Info Terminated Discovery agent [546254]
RPR-104632 Drug Info Terminated Discovery agent [545739]
SPERMINE Drug Info Terminated Discovery agent [542107], [546483]
Agonist (+)-HA966 Drug Info [543836]
(RS)-(tetrazol-5-yl)glycine Drug Info [543836]
D-aspartic acid Drug Info [543836]
homoquinolinic acid Drug Info [543836]
L-aspartic acid Drug Info [543836]
NMDA Drug Info [543836]
[3H]glycine Drug Info [543836]
Inhibitor (D)-Ala-Pro-Glu Drug Info [527903]
(R)-2-Amino-5-phosphono-pentanoic acid Drug Info [527496]
(R)-2-Amino-7-phosphono-heptanoic acid Drug Info [527496]
(R)-4-Amino-Isoxazolidin-3-One Drug Info [551393]
2-(4-Phenoxy-benzyl)-1H-benzoimidazole Drug Info [527020]
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-4-ol Drug Info [527020]
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ol Drug Info [527020]
2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ylamine Drug Info [527020]
2-Methylamino-succinic acid(NMDA) Drug Info [531531]
2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline Drug Info [526618]
3-Benzoyl-7-chloro-4-hydroxy-1H-quinolin-2-one Drug Info [551249]
3-Carbamoyl-6-chloro-1H-indole-2-carboxylic acid Drug Info [551231]
3-Hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info [534270]
3-Hydroxy-6-methyl-1H-benzo[b]azepine-2,5-dione Drug Info [534270]
3-Hydroxy-7-nitro-1H-benzo[b]azepine-2,5-dione Drug Info [534270]
3-Hydroxy-8-methyl-1H-benzo[b]azepine-2,5-dione Drug Info [534270]
3-phenyl-4-hydroxyquinolin-2(1H)-one Drug Info [527994]
4,5,7-Trichloro-3-hydroxy-1H-quinolin-2-one Drug Info [551312]
4,6-Dichloro-1H-indole-2-carboxylic acid Drug Info [531421]
4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline Drug Info [526618]
4-Benzyl-1-(2-phenoxy-ethyl)-piperidine Drug Info [525548]
4-Benzyl-1-phenethyl-piperidine hydrochloride Drug Info [534696]
4-Bromo-3-hydroxy-1H-quinolin-2-one Drug Info [551312]
4-Bromo-5,7-dichloro-3-hydroxy-1H-quinolin-2-one Drug Info [551312]
4-Chloro-3-hydroxy-1H-quinolin-2-one Drug Info [551312]
4-hydroxy-5-phenylthieno[2,3-b]pyridin-6(7H)-one Drug Info [527994]
4-Phosphonomethyl-piperidine-2-carboxylic acid Drug Info [533067]
4-[2-(3-Phenyl-propylamino)-ethyl]-phenol Drug Info [534696]
4-[2-(4-Benzyl-piperidin-1-yl)-ethoxy]-phenol Drug Info [525548]
4-[2-(4-Phenyl-butoxy)-ethyl]-phenol Drug Info [534696]
4-[2-(4-Phenyl-butylamino)-ethyl]-phenol Drug Info [534696]
4-[2-(4-Phenyl-piperidin-1-yl)-ethoxy]-phenol Drug Info [525548]
4-[2-(5-Phenyl-pentylamino)-ethyl]-phenol Drug Info [534696]
4-[2-(6-Phenyl-hexylamino)-ethyl]-phenol Drug Info [534696]
4-[3-(4-Phenyl-butylamino)-propyl]-phenol Drug Info [525527]
4-[3-(5-Phenyl-pentylamino)-propyl]-phenol Drug Info [534696]
4-{2-[Ethyl-(4-phenyl-butyl)-amino]-ethyl}-phenol Drug Info [534696]
5,6,7-Trichloro-1,4-dihydro-quinoxaline-2,3-dione Drug Info [551311]
5,7-Dibromo-1,4-dihydro-quinoxaline-2,3-dione Drug Info [551311]
5,7-Dichloro-1,4-dihydro-quinoxaline-2,3-dione Drug Info [551311]
5,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione Drug Info [527036]
5,7-Dichloro-4-hydroxy-3-phenyl-1H-quinolin-2-one Drug Info [551249]
5,7-Dichlorokynurenic Acid Drug Info [551374]
5,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione Drug Info [551249]
6,7-Dichloro-1,4-dihydro-quinoxaline-2,3-dione Drug Info [551311]
6,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione Drug Info [527036]
6-Chloro-1,4-dihydro-quinoxaline-2,3-dione Drug Info [534504]
6-Methoxy-2-(4-phenoxy-benzyl)-1H-benzoimidazole Drug Info [527020]
6-Nitro-1,4-dihydro-quinoxaline-2,3-dione Drug Info [534504]
6-Nitro-2-(4-phenoxy-benzyl)-1H-benzoimidazole Drug Info [527020]
7-chloro-3-hydroxyquinazoline-2,4-dione Drug Info [528453]
7-Chloro-3-nitro-3,4-dihydro-1H-quinolin-2-one Drug Info [551249]
8-Bromo-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info [534270]
8-Chloro-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info [534270]
8-Ethyl-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info [534270]
8-Fluoro-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info [534270]
Ala-Pro-Glu Drug Info [527903]
AM-92016 Drug Info [529698]
AP-7 Drug Info [526787]
Benzyl 4-aminobutyl(3-aminopropyl)carbamate Drug Info [528098]
Cycloleucine Drug Info [551384]
D-Serine Drug Info [551378]
DITOLYLGUANIDINE Drug Info [534685]
DIZOCILPINE Drug Info [533655]
DNQX Drug Info [529309]
ELIPRODIL Drug Info [525548]
GLUTAMATE Drug Info [526787]
Gly-Amp-Glu Drug Info [527903]
Gly-b7Pro-Glu Drug Info [527903]
Gly-Hyp-Glu Drug Info [527903]
Gly-Pip-Glu Drug Info [527903]
H-Gly-D-dmP-Glu-OH Drug Info [528176]
H-Gly-dmP-Glu-OH Drug Info [528176]
H-Gly-PMe-Glu-OH Drug Info [528176]
L-687414 Drug Info [551249]
L-695902 Drug Info [551249]
L-698532 Drug Info [527994]
L-701324 Drug Info [527994]
MDL-105519 Drug Info [527438]
N,N'-Bis-(4-butoxy-phenyl)-guanidine Drug Info [534685]
N,N'-Bis-(4-butyl-phenyl)-guanidine Drug Info [534685]
N,N'-Bis-(4-ethyl-phenyl)-guanidine Drug Info [534685]
N,N'-Bis-(4-hexyl-phenyl)-guanidine Drug Info [534685]
N,N'-Bis-(4-isopropyl-phenyl)-guanidine Drug Info [534685]
N,N'-Bis-(4-sec-butyl-phenyl)-guanidine Drug Info [534685]
N-(2-methoxybenzyl)cinnamamidine Drug Info [527787]
NBQX Drug Info [526134]
Nle-Pro-Glu Drug Info [527903]
Phe-Pro-Glu Drug Info [527903]
PHENCYCLIDINE Drug Info [534286]
Phenethyl-(3-phenyl-propyl)-amine Drug Info [534696]
Phenethyl-(4-phenyl-butyl)-amine Drug Info [534696]
RPR-104632 Drug Info [525816]
RPR-118723 Drug Info [525816]
SPERMINE Drug Info [530824]
TRANSTORINE Drug Info [531421]
YM-90K Drug Info [525786]
Antagonist [3H]CGP39653 Drug Info [543836]
[3H]CGP61594 Drug Info [543836]
[3H]CGS19755 Drug Info [543836]
[3H]CPP Drug Info [543836]
[3H]dizocilpine Drug Info [543836]
[3H]L689560 Drug Info [543836]
[3H]MDL105519 Drug Info [543836]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Ras signaling pathway
Rap1 signaling pathway
Calcium signaling pathway
cAMP signaling pathway
Neuroactive ligand-receptor interaction
Circadian entrainment
Long-term potentiation
Glutamatergic synapse
Alzheimer&#039
s disease
Amyotrophic lateral sclerosis (ALS)
Huntington&#039
Cocaine addiction
Amphetamine addiction
Nicotine addiction
Alcoholism
PANTHER Pathway Huntington disease
Ionotropic glutamate receptor pathway
Metabotropic glutamate receptor group III pathway
Metabotropic glutamate receptor group I pathway
Muscarinic acetylcholine receptor 1 and 3 signaling pathway
Reactome EPHB-mediated forward signaling
Unblocking of NMDA receptor, glutamate binding and activation
CREB phosphorylation through the activation of CaMKII
Ras activation uopn Ca2+ infux through NMDA receptor
RAF/MAP kinase cascade
WikiPathways SIDS Susceptibility Pathways
Hypothetical Network for Drug Addiction
Neurotransmitter Receptor Binding And Downstream Transmission In The Postsynaptic Cell
Spinal Cord Injury
BDNF signaling pathway
Alzheimers Disease
References
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Ref 467575(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4240).
Ref 467600(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4264).
Ref 521427ClinicalTrials.gov (NCT00001929) Treatment of Parkinson's Disease With Eliprodil. U.S. National Institutes of Health.
Ref 521721ClinicalTrials.gov (NCT00215904) D-serine Adjuvant Treatment for Parkinson's Disease. U.S. National Institutes of Health.
Ref 525504L-701,324, a selective antagonist at the glycine site of the NMDA receptor, counteracts haloperidol-induced muscle rigidity in rats. Psychopharmacology (Berl). 1999 Apr;143(3):235-43.
Ref 534277Anticonvulsant and behavioral profile of L-701,324, a potent, orally active antagonist at the glycine modulatory site on the N-methyl-D-aspartate receptor complex. J Pharmacol Exp Ther. 1996 Nov;279(2):492-501.
Ref 539532(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2403).
Ref 542107(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 710).
Ref 544717Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000713)
Ref 544996Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001829)
Ref 545107Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002155)
Ref 545371Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003055)
Ref 545739Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004459)
Ref 546154Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006620)
Ref 546232Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007035)
Ref 546254Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007135)
Ref 546483Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008464)
Ref 525527Bioorg 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 525548J 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 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 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 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 526618Bioorg 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 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 527020J Med Chem. 2004 Apr 8;47(8):2089-96.NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
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 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.
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 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 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 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 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 529309J 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 529698J Med Chem. 2008 Sep 25;51(18):5506-21.Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists.
Ref 530824J Med Chem. 2010 May 13;53(9):3611-7.Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents.
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 531531J Med Chem. 1990 Oct;33(10):2772-7.2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
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 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 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 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 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 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 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 543836(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 455).
Ref 5512312-carboxy indolines and indoles as potential glycine/NMDA antagonists: effect of five-membered ring conformation on affinity. Bioorg. Med. Chem. Lett. 2(12):1627-1630 (1992).
Ref 551249Amino acid bioisosteres: design of 2-quinolone derivatives as glycine-site N-methyl-D-aspartate receptor antagonists, Bioorg. Med. Chem. Lett. 3(2):299-304 (1993).
Ref 5513111-Hydroxy-1,4-dihydroquinoxaline-2,3-diones: Novel antagonists at NMDA receptor glycine sites, Bioorg. Med. Chem. Lett. 6(4):439-440 (1996).
Ref 5513123-Hydroxy-quinolin-2-ones: Inhibitors of [3H]-glycine binding to the site associated with the NMDA receptor, Bioorg. Med. Chem. Lett. 6(5):499-504 (1996).
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551378Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
Ref 551384Effects of D-cycloserine and cycloleucine, ligands for the <span class="caps">NMDA</span>-associated strychnine-insensitive glycine site, on brain-stimulation reward and spontaneous locomotion. Pharmacol Biochem Behav. 1990 Aug;36(4):735-8.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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