Target Information
Target General Infomation | |||||
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Target ID |
T62276
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Former ID |
TTDR01259
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Target Name |
NMDA receptor subunit NR1
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Gene Name |
GRIN1
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Synonyms |
GluN1; Glutamate [NMDA] receptor subunit zeta1; Glutamate receptor ionotropic, NMDA 1; NMDR1; NmethylDaspartate receptor subunit NR1; GRIN1
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Target Type |
Clinical Trial
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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.
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BioChemical Class |
Glutamate-gated ion channel
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Target Validation |
T62276
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UniProt ID | |||||
Sequence |
MSTMRLLTLALLFSCSVARAACDPKIVNIGAVLSTRKHEQMFREAVNQANKRHGSWKIQL
NATSVTHKPNAIQMALSVCEDLISSQVYAILVSHPPTPNDHFTPTPVSYTAGFYRIPVLG LTTRMSIYSDKSIHLSFLRTVPPYSHQSSVWFEMMRVYSWNHIILLVSDDHEGRAAQKRL ETLLEERESKAEKVLQFDPGTKNVTALLMEAKELEARVIILSASEDDAATVYRAAAMLNM TGSGYVWLVGEREISGNALRYAPDGILGLQLINGKNESAHISDAVGVVAQAVHELLEKEN ITDPPRGCVGNTNIWKTGPLFKRVLMSSKYADGVTGRVEFNEDGDRKFANYSIMNLQNRK LVQVGIYNGTHVIPNDRKIIWPGGETEKPRGYQMSTRLKIVTIHQEPFVYVKPTLSDGTC KEEFTVNGDPVKKVICTGPNDTSPGSPRHTVPQCCYGFCIDLLIKLARTMNFTYEVHLVA DGKFGTQERVNNSNKKEWNGMMGELLSGQADMIVAPLTINNERAQYIEFSKPFKYQGLTI LVKKEIPRSTLDSFMQPFQSTLWLLVGLSVHVVAVMLYLLDRFSPFGRFKVNSEEEEEDA LTLSSAMWFSWGVLLNSGIGEGAPRSFSARILGMVWAGFAMIIVASYTANLAAFLVLDRP EERITGINDPRLRNPSDKFIYATVKQSSVDIYFRRQVELSTMYRHMEKHNYESAAEAIQA VRDNKLHAFIWDSAVLEFEASQKCDLVTTGELFFRSGFGIGMRKDSPWKQNVSLSILKSH ENGFMEDLDKTWVRYQECDSRSNAPATLTFENMAGVFMLVAGGIVAGIFLIFIEIAYKRH KDARRKQMQLAFAAVNVWRKNLQDRKSGRAEPDPKKKATFRAITSTLASSFKRRRSSKDT STGGGRGALQNQKDTVLPRRAIEREEGQLQLCSRHRES |
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Structure |
2HQW; 2NR1; 3BYA
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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' | |||||
s disease | |||||
Amyotrophic lateral sclerosis (ALS) | |||||
Huntington' | |||||
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 | |||||
Ref 467510 | (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: 4171). | ||||
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 521427 | ClinicalTrials.gov (NCT00001929) Treatment of Parkinson's Disease With Eliprodil. U.S. National Institutes of Health. | ||||
Ref 521721 | ClinicalTrials.gov (NCT00215904) D-serine Adjuvant Treatment for Parkinson's Disease. U.S. National Institutes of Health. | ||||
Ref 525504 | L-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 534277 | Anticonvulsant 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 544717 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000713) | ||||
Ref 544996 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001829) | ||||
Ref 545107 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002155) | ||||
Ref 545371 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003055) | ||||
Ref 545739 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004459) | ||||
Ref 546154 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006620) | ||||
Ref 546232 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007035) | ||||
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 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 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 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 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. | ||||
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 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 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 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 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 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 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 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 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 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 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 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 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 529698 | J Med Chem. 2008 Sep 25;51(18):5506-21.Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists. | ||||
Ref 530824 | J Med Chem. 2010 May 13;53(9):3611-7.Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. | ||||
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 531531 | J Med Chem. 1990 Oct;33(10):2772-7.2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. | ||||
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 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 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 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 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 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 551231 | 2-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 551249 | Amino 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 551311 | 1-Hydroxy-1,4-dihydroquinoxaline-2,3-diones: Novel antagonists at NMDA receptor glycine sites, Bioorg. Med. Chem. Lett. 6(4):439-440 (1996). | ||||
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