Target Validation Information
TTD ID T22285
Target Name Glutamate receptor ionotropic NMDA 2A (NMDAR2A)
Type of Target
Successful
Drug Potency against Target Glycine Drug Info IC50 = 170 nM [26]
Drug Info IC50 = 452 nM [19]
Drug Info IC50 = 70 nM [4]
Drug Info Ki = 7960 nM [12]
(D)-Ala-Pro-Glu Drug Info Ki = 5400 nM [9]
(R)-2-Amino-5-phosphono-pentanoic acid Drug Info Ki = 170 nM [7]
(R)-2-Amino-7-phosphono-heptanoic acid Drug Info Ki = 76 nM [7]
1,3-ditolylguanidine Drug Info IC50 = 10200 nM [24]
2-Methylamino-succinic acid(NMDA) Drug Info IC50 = 6000 nM [18]
3-Benzoyl-7-chloro-4-hydroxy-1H-quinolin-2-one Drug Info IC50 = 3200 nM
3-Hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 830 nM [21]
3-Hydroxy-6-methyl-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 13000 nM [21]
3-Hydroxy-7-nitro-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 12000 nM [21]
3-Hydroxy-8-methyl-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 130 nM [21]
3-phenyl-4-hydroxyquinolin-2(1H)-one Drug Info Ki = 12200 nM [10]
4,5,7-Trichloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 4500 nM
4,6-Dichloro-1H-indole-2-carboxylic acid Drug Info IC50 = 6000 nM [17]
4-Bromo-5,7-dichloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 2800 nM
4-Chloro-3-hydroxy-1H-quinolin-2-one Drug Info IC50 = 1400 nM
4-hydroxy-5-phenylthieno[2,3-b]pyridin-6(7H)-one Drug Info Ki = 16400 nM [10]
4-[2-(4-Phenyl-butylamino)-ethyl]-phenol Drug Info IC50 = 15000 nM [25]
4-[2-(5-Phenyl-pentylamino)-ethyl]-phenol Drug Info IC50 = 12000 nM [25]
4-[2-(6-Phenyl-hexylamino)-ethyl]-phenol Drug Info IC50 = 17000 nM [25]
4-[3-(4-Phenyl-butylamino)-propyl]-phenol Drug Info IC50 = 18000 nM [25]
4-[3-(5-Phenyl-pentylamino)-propyl]-phenol Drug Info IC50 = 18000 nM [25]
5,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione Drug Info IC50 = 750 nM [5]
5,7-Dichloro-4-hydroxy-3-phenyl-1H-quinolin-2-one Drug Info IC50 = 97 nM
5,7-Dinitro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 170 nM
6,7-Dichloro-3-hydroxy-1H-quinazoline-2,4-dione Drug Info IC50 = 430 nM [5]
6-Chloro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 1800 nM [23]
6-Nitro-1,4-dihydro-quinoxaline-2,3-dione Drug Info IC50 = 3800 nM [23]
7-chloro-3-hydroxyquinazoline-2,4-dione Drug Info Ki = 240 nM [14]
8-Bromo-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 79 nM [21]
8-Chloro-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 13 nM [21]
8-Ethyl-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 5100 nM [21]
8-Fluoro-3-hydroxy-1H-benzo[b]azepine-2,5-dione Drug Info IC50 = 490 nM [21]
Ala-Pro-Glu Drug Info Ki = 2660 nM [9]
AP-7 Drug Info IC50 = 390 nM [4]
Benzyl 4-aminobutyl(3-aminopropyl)carbamate Drug Info IC50 = 17600 nM [11]
Besonprodil Drug Info IC50 = 6.6 nM [13]
Conantokin-R Drug Info IC50 = 1000 nM [15]
DIZOCILPINE Drug Info Ki = 2.2 nM [20]
DNQX Drug Info IC50 = 4500 nM [16]
Gly-Amp-Glu Drug Info Ki = 15540 nM [9]
Gly-b7Pro-Glu Drug Info Ki = 480 nM [9]
Gly-Hyp-Glu Drug Info Ki = 9240 nM [9]
Gly-Pip-Glu Drug Info Ki = 2390 nM [9]
H-Gly-D-dmP-Glu-OH Drug Info Ki = 330 nM [12]
H-Gly-dmP-Glu-OH Drug Info Ki = 3790 nM [12]
L-687414 Drug Info IC50 = 2700 nM
L-695902 Drug Info IC50 = 6500 nM
L-698532 Drug Info Ki = 151 nM [10]
L-698544 Drug Info IC50 = 410 nM
L-701324 Drug Info Ki = 1.4 nM [10]
MDL-105519 Drug Info IC50 = 157 nM [6]
N,N'-Bis-(4-butoxy-phenyl)-guanidine Drug Info IC50 = 3480 nM [24]
N,N'-Bis-(4-butyl-phenyl)-guanidine Drug Info IC50 = 3320 nM [24]
N,N'-Bis-(4-ethyl-phenyl)-guanidine Drug Info IC50 = 7910 nM [24]
N,N'-Bis-(4-hexyl-phenyl)-guanidine Drug Info IC50 = 7790 nM [24]
N,N'-Bis-(4-isopropyl-phenyl)-guanidine Drug Info IC50 = 17900 nM [24]
N,N'-Bis-(4-sec-butyl-phenyl)-guanidine Drug Info IC50 = 10100 nM [24]
N-(2-methoxybenzyl)cinnamamidine Drug Info IC50 = 6.6 nM [8]
NBQX Drug Info IC50 = 200 nM [3]
Nle-Pro-Glu Drug Info Ki = 19500 nM [9]
Phe-Pro-Glu Drug Info Ki = 4850 nM [9]
PHENCYCLIDINE Drug Info IC50 = 9.8 nM [22]
RPR-104632 Drug Info IC50 = 8.3 nM [2]
RPR-118723 Drug Info IC50 = 28 nM [2]
TRANSTORINE Drug Info IC50 = 16000 nM [17]
YM-90K Drug Info IC50 = 10400 nM [1]
References
REF 1 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 2 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 3 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 4 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 5 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 6 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 7 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 8 Indole-2-carboxamidines as novel NR2B selective NMDA receptor antagonists. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5439-41.
REF 9 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 10 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 11 Polyamines and the NMDA receptor: modifying intrinsic activities with aromatic substituents. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2837-41.
REF 12 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 13 Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4638-40.
REF 14 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 15 Novel conantokins from Conus parius venom are specific antagonists of N-methyl-D-aspartate receptors. J Biol Chem. 2007 Dec 21;282(51):36905-13.
REF 16 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 17 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 18 2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. J Med Chem. 1990 Oct;33(10):2772-7.
REF 19 4-(Phosphonoalkyl)- and 4-(phosphonoalkenyl)-2-piperidinecarboxylic acids: synthesis, activity at N-methyl-D-aspartic acid receptors, and anticonvu... J Med Chem. 1989 Sep;32(9):2171-8.
REF 20 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 21 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 22 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.
REF 23 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 24 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 25 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 26 Evidence for direct interactions between the NMDA and glycine recognition sites in brain. Eur J Pharmacol. 1990 Mar 13;188(2-3):175-9.

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