Target Information
Target General Information | Top | |||||
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Target ID |
T62276
(Former ID: TTDR01259)
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Target Name |
Glutamate receptor ionotropic NMDA 1 (NMDAR1)
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Synonyms |
NmethylDaspartate receptor subunit NR1; NMDR1; NMD-R1; N-methyl-D-aspartate receptor subunit NR1; Glutamate receptor ionotropic, NMDA 1; Glutamate [NMDA] receptor subunit zeta1; Glutamate [NMDA] receptor subunit zeta-1; GluN1
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Gene Name |
GRIN1
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Bacterial infection [ICD-11: 1A00-1C4Z] | |||||
2 | HIV-infected patients with tuberculosis [ICD-11: 1B10-1B14] | |||||
Function |
Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+). Sensitivity to glutamate and channel kinetics depend on the subunit composition. Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium.
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BioChemical Class |
Glutamate-gated ion channel
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UniProt ID | ||||||
Sequence |
MSTMRLLTLALLFSCSVARAACDPKIVNIGAVLSTRKHEQMFREAVNQANKRHGSWKIQL
NATSVTHKPNAIQMALSVCEDLISSQVYAILVSHPPTPNDHFTPTPVSYTAGFYRIPVLG LTTRMSIYSDKSIHLSFLRTVPPYSHQSSVWFEMMRVYSWNHIILLVSDDHEGRAAQKRL ETLLEERESKAEKVLQFDPGTKNVTALLMEAKELEARVIILSASEDDAATVYRAAAMLNM TGSGYVWLVGEREISGNALRYAPDGILGLQLINGKNESAHISDAVGVVAQAVHELLEKEN ITDPPRGCVGNTNIWKTGPLFKRVLMSSKYADGVTGRVEFNEDGDRKFANYSIMNLQNRK LVQVGIYNGTHVIPNDRKIIWPGGETEKPRGYQMSTRLKIVTIHQEPFVYVKPTLSDGTC KEEFTVNGDPVKKVICTGPNDTSPGSPRHTVPQCCYGFCIDLLIKLARTMNFTYEVHLVA DGKFGTQERVNNSNKKEWNGMMGELLSGQADMIVAPLTINNERAQYIEFSKPFKYQGLTI LVKKEIPRSTLDSFMQPFQSTLWLLVGLSVHVVAVMLYLLDRFSPFGRFKVNSEEEEEDA LTLSSAMWFSWGVLLNSGIGEGAPRSFSARILGMVWAGFAMIIVASYTANLAAFLVLDRP EERITGINDPRLRNPSDKFIYATVKQSSVDIYFRRQVELSTMYRHMEKHNYESAAEAIQA VRDNKLHAFIWDSAVLEFEASQKCDLVTTGELFFRSGFGIGMRKDSPWKQNVSLSILKSH ENGFMEDLDKTWVRYQECDSRSNAPATLTFENMAGVFMLVAGGIVAGIFLIFIEIAYKRH KDARRKQMQLAFAAVNVWRKNLQDRKSGRAEPDPKKKATFRAITSTLASSFKRRRSSKDT STGGGRGALQNQKDTVLPRRAIEREEGQLQLCSRHRES Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
HIT2.0 ID | T86CQC |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
1 | Cycloserine | Drug Info | Approved | Tuberculosis | [2], [3] | |
Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
1 | ELIPRODIL | Drug Info | Phase 2 | Multiple sclerosis | [4] | |
2 | NBQX | Drug Info | Phase 1 | Neurological disorder | [5] | |
Discontinued Drug(s) | [+] 6 Discontinued Drugs | + | ||||
1 | YM-90K | Drug Info | Discontinued in Phase 2 | Convulsion | [6] | |
2 | DIZOCILPINE | Drug Info | Terminated | Cerebrovascular ischaemia | [7], [8] | |
3 | L-689560 | Drug Info | Terminated | Neurodegenerative disorder | [9], [10] | |
4 | L-698532 | Drug Info | Terminated | Neurological disorder | [11] | |
5 | L-698544 | Drug Info | Terminated | Alzheimer disease | [12] | |
6 | L-701324 | Drug Info | Terminated | Cerebrovascular ischaemia | [13], [14], [15] | |
Mode of Action | [+] 3 Modes of Action | + | ||||
Inhibitor | [+] 94 Inhibitor drugs | + | ||||
1 | Cycloserine | Drug Info | [1] | |||
2 | D-Serine | Drug Info | [16] | |||
3 | ELIPRODIL | Drug Info | [17] | |||
4 | NBQX | Drug Info | [18] | |||
5 | YM-90K | Drug Info | [19] | |||
6 | AM-92016 | Drug Info | [20] | |||
7 | DIZOCILPINE | Drug Info | [21] | |||
8 | L-687414 | Drug Info | [22] | |||
9 | L-695902 | Drug Info | [22] | |||
10 | L-698532 | Drug Info | [24] | |||
11 | L-698544 | Drug Info | [22] | |||
12 | L-701324 | Drug Info | [24] | |||
13 | MDL-105519 | Drug Info | [25] | |||
14 | RPR-104632 | Drug Info | [26] | |||
15 | SPERMINE | Drug Info | [27] | |||
16 | (D)-Ala-Pro-Glu | Drug Info | [28] | |||
17 | (R)-2-Amino-5-phosphono-pentanoic acid | Drug Info | [29] | |||
18 | (R)-2-Amino-7-phosphono-heptanoic acid | Drug Info | [29] | |||
19 | 1,3-ditolylguanidine | Drug Info | [30] | |||
20 | 2-(4-Phenoxy-benzyl)-1H-benzoimidazole | Drug Info | [31] | |||
21 | 2-(4-Phenoxy-benzyl)-3H-benzoimidazol-4-ol | Drug Info | [31] | |||
22 | 2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ol | Drug Info | [31] | |||
23 | 2-(4-Phenoxy-benzyl)-3H-benzoimidazol-5-ylamine | Drug Info | [31] | |||
24 | 2-Methylamino-succinic acid(NMDA) | Drug Info | [23], [32] | |||
25 | 2-Pyridin-4-yl-1,2,3,4-tetrahydro-isoquinoline | Drug Info | [33] | |||
26 | 3-Benzoyl-7-chloro-4-hydroxy-1H-quinolin-2-one | Drug Info | [22] | |||
27 | 3-Carbamoyl-6-chloro-1H-indole-2-carboxylic acid | Drug Info | [34] | |||
28 | 3-Hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [35] | |||
29 | 3-Hydroxy-6-methyl-1H-benzo[b]azepine-2,5-dione | Drug Info | [35] | |||
30 | 3-Hydroxy-7-nitro-1H-benzo[b]azepine-2,5-dione | Drug Info | [35] | |||
31 | 3-Hydroxy-8-methyl-1H-benzo[b]azepine-2,5-dione | Drug Info | [35] | |||
32 | 3-phenyl-4-hydroxyquinolin-2(1H)-one | Drug Info | [24] | |||
33 | 4,5,7-Trichloro-3-hydroxy-1H-quinolin-2-one | Drug Info | [36] | |||
34 | 4,6-Dichloro-1H-indole-2-carboxylic acid | Drug Info | [37] | |||
35 | 4-(3,4-Dihydro-1H-isoquinolin-2-yl)-quinoline | Drug Info | [33] | |||
36 | 4-Benzyl-1-(2-phenoxy-ethyl)-piperidine | Drug Info | [17] | |||
37 | 4-Benzyl-1-phenethyl-piperidine hydrochloride | Drug Info | [38] | |||
38 | 4-Bromo-3-hydroxy-1H-quinolin-2-one | Drug Info | [36] | |||
39 | 4-Bromo-5,7-dichloro-3-hydroxy-1H-quinolin-2-one | Drug Info | [36] | |||
40 | 4-Chloro-3-hydroxy-1H-quinolin-2-one | Drug Info | [36] | |||
41 | 4-hydroxy-5-phenylthieno[2,3-b]pyridin-6(7H)-one | Drug Info | [24] | |||
42 | 4-[2-(3-Phenyl-propylamino)-ethyl]-phenol | Drug Info | [38] | |||
43 | 4-[2-(4-Benzyl-piperidin-1-yl)-ethoxy]-phenol | Drug Info | [17] | |||
44 | 4-[2-(4-Phenyl-butoxy)-ethyl]-phenol | Drug Info | [38] | |||
45 | 4-[2-(4-Phenyl-butylamino)-ethyl]-phenol | Drug Info | [38] | |||
46 | 4-[2-(4-Phenyl-piperidin-1-yl)-ethoxy]-phenol | Drug Info | [17] | |||
47 | 4-[2-(5-Phenyl-pentylamino)-ethyl]-phenol | Drug Info | [38] | |||
48 | 4-[2-(6-Phenyl-hexylamino)-ethyl]-phenol | Drug Info | [38] | |||
49 | 4-[3-(4-Phenyl-butylamino)-propyl]-phenol | Drug Info | [39] | |||
50 | 4-[3-(5-Phenyl-pentylamino)-propyl]-phenol | Drug Info | [38] | |||
51 | 4-{2-[Ethyl-(4-phenyl-butyl)-amino]-ethyl}-phenol | Drug Info | [38] | |||
52 | 5,6,7-Trichloro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [40] | |||
53 | 5,7-Dibromo-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [40] | |||
54 | 5,7-Dichloro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [40] | |||
55 | 5,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione | Drug Info | [41] | |||
56 | 5,7-Dichloro-4-hydroxy-3-phenyl-1H-quinolin-2-one | Drug Info | [22] | |||
57 | 5,7-Dichlorokynurenic Acid | Drug Info | [42] | |||
58 | 5,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [22] | |||
59 | 6,7-Dichloro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [40] | |||
60 | 6,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione | Drug Info | [41] | |||
61 | 6-Chloro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [43] | |||
62 | 6-Methoxy-2-(4-phenoxy-benzyl)-1H-benzoimidazole | Drug Info | [31] | |||
63 | 6-Nitro-1,4-dihydro-quinoxaline-2,3-dione | Drug Info | [43] | |||
64 | 6-Nitro-2-(4-phenoxy-benzyl)-1H-benzoimidazole | Drug Info | [31] | |||
65 | 7-chloro-3-hydroxyquinazoline-2,4-dione | Drug Info | [44] | |||
66 | 8-Bromo-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [35] | |||
67 | 8-Chloro-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [35] | |||
68 | 8-Ethyl-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [35] | |||
69 | 8-Fluoro-3-hydroxy-1H-benzo[b]azepine-2,5-dione | Drug Info | [35] | |||
70 | Ala-Pro-Glu | Drug Info | [28] | |||
71 | AP-7 | Drug Info | [45] | |||
72 | Benzyl 4-aminobutyl(3-aminopropyl)carbamate | Drug Info | [46] | |||
73 | Cycloleucine | Drug Info | [47] | |||
74 | DNQX | Drug Info | [48] | |||
75 | Gly-Amp-Glu | Drug Info | [28] | |||
76 | Gly-b7Pro-Glu | Drug Info | [28] | |||
77 | Gly-Hyp-Glu | Drug Info | [28] | |||
78 | Gly-Pip-Glu | Drug Info | [28] | |||
79 | H-Gly-D-dmP-Glu-OH | Drug Info | [49] | |||
80 | H-Gly-dmP-Glu-OH | Drug Info | [49] | |||
81 | N,N'-Bis-(4-butoxy-phenyl)-guanidine | Drug Info | [30] | |||
82 | N,N'-Bis-(4-butyl-phenyl)-guanidine | Drug Info | [30] | |||
83 | N,N'-Bis-(4-ethyl-phenyl)-guanidine | Drug Info | [30] | |||
84 | N,N'-Bis-(4-hexyl-phenyl)-guanidine | Drug Info | [30] | |||
85 | N,N'-Bis-(4-isopropyl-phenyl)-guanidine | Drug Info | [30] | |||
86 | N,N'-Bis-(4-sec-butyl-phenyl)-guanidine | Drug Info | [30] | |||
87 | N-(2-methoxybenzyl)cinnamamidine | Drug Info | [50] | |||
88 | Nle-Pro-Glu | Drug Info | [28] | |||
89 | Phe-Pro-Glu | Drug Info | [28] | |||
90 | PHENCYCLIDINE | Drug Info | [51] | |||
91 | Phenethyl-(3-phenyl-propyl)-amine | Drug Info | [38] | |||
92 | Phenethyl-(4-phenyl-butyl)-amine | Drug Info | [38] | |||
93 | RPR-118723 | Drug Info | [26] | |||
94 | TRANSTORINE | Drug Info | [37] | |||
Antagonist | [+] 7 Antagonist drugs | + | ||||
1 | L-689560 | Drug Info | [23] | |||
2 | CGP61594 | Drug Info | [23] | |||
3 | [3H]CGP39653 | Drug Info | [23] | |||
4 | [3H]CGS19755 | Drug Info | [23] | |||
5 | [3H]CPP | Drug Info | [23] | |||
6 | [3H]dizocilpine | Drug Info | [23] | |||
7 | [3H]MDL105519 | Drug Info | [23] | |||
Agonist | [+] 5 Agonist drugs | + | ||||
1 | (+)-HA966 | Drug Info | [23] | |||
2 | (RS)-(tetrazol-5-yl)glycine | Drug Info | [23] | |||
3 | D-aspartic acid | Drug Info | [23] | |||
4 | homoquinolinic acid | Drug Info | [23] | |||
5 | L-aspartic acid | Drug Info | [23] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
REF 2 | Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8. | |||||
REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 4 | ClinicalTrials.gov (NCT00001929) Treatment of Parkinson's Disease With Eliprodil. U.S. National Institutes of Health. | |||||
REF 5 | URL: 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 6 | 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 7 | URL: 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 8 | 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 9 | URL: 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: 4239). | |||||
REF 10 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001828) | |||||
REF 11 | 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 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003218) | |||||
REF 13 | URL: 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 14 | 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 15 | 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 16 | Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. | |||||
REF 17 | 4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist. J Med Chem. 1999 Jul 29;42(15):2993-3000. | |||||
REF 18 | Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,... J Med Chem. 2001 Sep 13;44(19):3157-65. | |||||
REF 19 | 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... Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7. | |||||
REF 20 | Enantiomeric propanolamines as selective N-methyl-D-aspartate 2B receptor antagonists. J Med Chem. 2008 Sep 25;51(18):5506-21. | |||||
REF 21 | Synthesis and evaluation of 6,11-ethanohexahydrobenzo[b]quinolizidines: a new class of noncompetitive N-methyl-D-aspartate antagonists. J Med Chem. 1995 Jun 23;38(13):2483-9. | |||||
REF 22 | 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 23 | URL: 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 24 | 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. J Med Chem. 2006 Feb 9;49(3):864-71. | |||||
REF 25 | 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... J Med Chem. 2005 Feb 24;48(4):995-1018. | |||||
REF 26 | 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. J Med Chem. 2000 Jun 15;43(12):2371-81. | |||||
REF 27 | Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. J Med Chem. 2010 May 13;53(9):3611-7. | |||||
REF 28 | New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity. Bioorg Med Chem Lett. 2006 Mar 1;16(5):1392-6. | |||||
REF 29 | Synthesis and pharmacology of N1-substituted piperazine-2,3-dicarboxylic acid derivatives acting as NMDA receptor antagonists. J Med Chem. 2005 Apr 7;48(7):2627-37. | |||||
REF 30 | Synthesis and pharmacological evaluation of N,N'-diarylguanidines as potent sodium channel blockers and anticonvulsant agents. J Med Chem. 1998 Aug 13;41(17):3298-302. | |||||
REF 31 | NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. J Med Chem. 2004 Apr 8;47(8):2089-96. | |||||
REF 32 | 2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. J Med Chem. 1990 Oct;33(10):2772-7. | |||||
REF 33 | 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 an... Bioorg Med Chem Lett. 2003 May 19;13(10):1759-62. | |||||
REF 34 | 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 35 | Analogs of 3-hydroxy-1H-1-benzazepine-2,5-dione: structure-activity relationship at N-methyl-D-aspartate receptor glycine sites. J Med Chem. 1996 Nov 8;39(23):4643-53. | |||||
REF 36 | 3-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 37 | 3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspart... J Med Chem. 1990 Nov;33(11):2944-6. | |||||
REF 38 | Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors. J Med Chem. 1998 Aug 27;41(18):3499-506. | |||||
REF 39 | 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-... Bioorg Med Chem Lett. 1999 Jun 7;9(11):1619-24. | |||||
REF 40 | 1-Hydroxy-1,4-dihydroquinoxaline-2,3-diones: Novel antagonists at NMDA receptor glycine sites, Bioorg. Med. Chem. Lett. 6(4):439-440 (1996). | |||||
REF 41 | 3-hydroxy-quinazoline-2,4-dione as a useful scaffold to obtain selective Gly/NMDA and AMPA receptor antagonists. Bioorg Med Chem Lett. 2004 May 3;14(9):2345-9. | |||||
REF 42 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | |||||
REF 43 | 5-(N-oxyaza)-7-substituted-1,4-dihydroquinoxaline-2,3-diones: novel, systemically active and broad spectrum antagonists for NMDA/glycine, AMPA, and... J Med Chem. 1997 Oct 24;40(22):3679-86. | |||||
REF 44 | Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Syn... J Med Chem. 2006 Oct 5;49(20):6015-26. | |||||
REF 45 | Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobut... J Med Chem. 1992 Dec 11;35(25):4720-6. | |||||
REF 46 | Polyamines and the NMDA receptor: modifying intrinsic activities with aromatic substituents. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2837-41. | |||||
REF 47 | Effects of D-cycloserine and cycloleucine, ligands for the NMDA-associated strychnine-insensitive glycine site, on brain-stimulation reward and spontaneous locomotion. Pharmacol Biochem Behav. 1990 Aug;36(4):735-8. | |||||
REF 48 | Kynurenic acid derivatives. Structure-activity relationships for excitatory amino acid antagonism and identification of potent and selective antago... J Med Chem. 1991 Apr;34(4):1243-52. | |||||
REF 49 | The neuroprotective activity of GPE tripeptide analogues does not correlate with glutamate receptor binding affinity. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3396-400. | |||||
REF 50 | Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5439-41. | |||||
REF 51 | Synthesis and biological activity of conformationally restricted analogs of milnacipran: (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopro... J Med Chem. 1996 Nov 22;39(24):4844-52. |
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