Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM7Z892)

• Drug Name: D-aspartic acid Drug Info
• Synonyms: D-Aspartic acid; 1783-96-6; (R)-2-aminosuccinic acid; D-Aspartate; H-D-Asp-OH; (-)-Aspartic acid; (R)-Aspartic acid; Aspartic acid D-form; (2R)-2-aminobutanedioic acid; Aspartic acid, D-; D-(-)-Aspartic acid; (R)-(-)-Aminosuccinic acid; D-Asp; D-Aminosuccinic acid; NSC 97922; D-Asparaginsaeure; UNII-4SR0Q8YD1X; BRN 1723529; Tocris-0213; EINECS 217-234-6; 4SR0Q8YD1X; (R)-2-aminobutanedioic acid; CHEMBL29757; CHEBI:17364; CKLJMWTZIZZHCS-UWTATZPHSA-N; MFCD00063081; NCGC00024498-02; (R)-2-Aminobutanedioate; D(-)-Aspartic acid, 99+%; D-aspartate; [3H]D-aspartic acid

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1] , [2]

• Cross-matching ID:
  PubChem CID: 83887
  ChEBI ID: CHEBI:17364
  CAS Number: CAS 1783-96-6
  TTD Drug ID: DM7Z892

Molecule-Related Drug Atlas

Drug(s) Targeting Glutamate receptor ionotropic NMDA 2A (NMDAR2A)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Glycine	DMIOZ29	Malnutrition	5B50-5B71	Approved	[13]
NBQX	DMPHZI5	Neurological disorder	6B60	Phase 1	[14]
YM-90K	DMWRT4L	Convulsion	8A68.Z	Discontinued in Phase 2	[15]
Spermine	DMD4BFY	N. A.	N. A.	Terminated	[16]
L-689560	DMCVY4U	Neurodegenerative disorder	8A20-8A23	Terminated	[9]
L-698544	DMLRBN1	Alzheimer disease	8A20	Terminated	[17]
Dizocilpine	DMMGYXR	Cerebrovascular ischaemia	8B1Z	Terminated	[18]
RPR-104632	DM9L50N	N. A.	N. A.	Terminated	[19]
L-698532	DMO9HM7	Neurological disorder	6B60	Terminated	[20]
L-695902	DMT1DNS	N. A.	N. A.	Terminated	[17]

Drug(s) Targeting Excitatory amino acid transporter 4 (SLC1A6)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
[3H]ETB-TBOA	DMWGY61	Discovery agent	N.A.	Investigative	[21]
DL-TBOA	DM2HGNU	Discovery agent	N.A.	Investigative	[22]
Threo-3-methylglutamate	DMOE3IJ	Discovery agent	N.A.	Investigative	[23]

Drug(s) Targeting Excitatory amino acid transporter 3 (SLC1A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
[3H]ETB-TBOA	DMWGY61	Discovery agent	N.A.	Investigative	[21]
DL-TBOA	DM2HGNU	Discovery agent	N.A.	Investigative	[24]
L-beta-BA	DMENM1B	Discovery agent	N.A.	Investigative	[25]
NBI-59159	DM7S5Y4	Discovery agent	N.A.	Investigative	[26]

Drug(s) Targeting Excitatory amino acid transporter 5 (SLC1A7)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
[3H]ETB-TBOA	DMWGY61	Discovery agent	N.A.	Investigative	[21]
DL-TBOA	DM2HGNU	Discovery agent	N.A.	Investigative	[22]

Drug(s) Targeting Glutamate receptor ionotropic NMDA 2D (GluN2D)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
L-689560	DMCVY4U	Neurodegenerative disorder	8A20-8A23	Terminated	[12]
[3H]CPP	DMR5UBF	Discovery agent	N.A.	Investigative	[12]
2-Methylamino-succinic acid(NMDA)	DMKP6BM	Discovery agent	N.A.	Investigative	[12]
[3H]MDL105519	DMPKGHB	Discovery agent	N.A.	Investigative	[12]
[3H]CGP39653	DMITR7A	Discovery agent	N.A.	Investigative	[12]
homoquinolinic acid	DMBW5DU	Discovery agent	N.A.	Investigative	[12]
[3H]dizocilpine	DMEC2PF	Discovery agent	N.A.	Investigative	[12]
CGP61594	DM8KFZH	Discovery agent	N.A.	Investigative	[12]
(RS)-(tetrazol-5-yl)glycine	DMYZCRF	Discovery agent	N.A.	Investigative	[12]
[3H]CGS19755	DM7H3JN	Discovery agent	N.A.	Investigative	[12]

Drug(s) Targeting Glutamate receptor ionotropic NMDA 1 (NMDAR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cycloserine	DMT1I52	Bacterial infection	1A00-1C4Z	Approved	[27]
D-Serine	DM3YH4I	N. A.	N. A.	Phase 4	[28]
ELIPRODIL	DMIOGZM	Multiple sclerosis	8A40	Phase 2	[29]
NBQX	DMPHZI5	Neurological disorder	6B60	Phase 1	[14]
YM-90K	DMWRT4L	Convulsion	8A68.Z	Discontinued in Phase 2	[15]
Spermine	DMD4BFY	N. A.	N. A.	Terminated	[16]
L-689560	DMCVY4U	Neurodegenerative disorder	8A20-8A23	Terminated	[8]
L-698544	DMLRBN1	Alzheimer disease	8A20	Terminated	[17]
Dizocilpine	DMMGYXR	Cerebrovascular ischaemia	8B1Z	Terminated	[18]
RPR-104632	DM9L50N	N. A.	N. A.	Terminated	[19]

Drug(s) Targeting Glutamate receptor ionotropic NMDA 2C (GluN2C)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
L-689560	DMCVY4U	Neurodegenerative disorder	8A20-8A23	Terminated	[11]
[3H]CPP	DMR5UBF	Discovery agent	N.A.	Investigative	[11]
2-Methylamino-succinic acid(NMDA)	DMKP6BM	Discovery agent	N.A.	Investigative	[11]
[3H]MDL105519	DMPKGHB	Discovery agent	N.A.	Investigative	[11]
[3H]CGP39653	DMITR7A	Discovery agent	N.A.	Investigative	[11]
homoquinolinic acid	DMBW5DU	Discovery agent	N.A.	Investigative	[11]
[3H]dizocilpine	DMEC2PF	Discovery agent	N.A.	Investigative	[11]
CGP61594	DM8KFZH	Discovery agent	N.A.	Investigative	[11]
(RS)-(tetrazol-5-yl)glycine	DMYZCRF	Discovery agent	N.A.	Investigative	[11]
[3H]CGS19755	DM7H3JN	Discovery agent	N.A.	Investigative	[11]

Drug(s) Targeting Glutamate receptor ionotropic NMDA 2B (NMDAR2B)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Alpha 1-PI	DMXC1K9	Alpha-1 antitrypsin deficiency	5C5A	Approved	[30]
ELIPRODIL	DMIOGZM	Multiple sclerosis	8A40	Phase 2	[29]
CP-101,606	DMIU19E	Parkinson disease	8A00.0	Phase 2	[31]
CERC-301	DMSABRI	Major depressive disorder	6A70.3	Phase 2	[32]
RGH-896	DMCHZAN	Peripheral neuropathy	8C0Z	Phase 2	[33]
MIJ821	DMN45RI	Major depressive disorder	6A70.3	Phase 2	[34]
NBQX	DMPHZI5	Neurological disorder	6B60	Phase 1	[14]
Neu-2000	DMNJTLC	Cardiac arrest	MC82	Phase 1	[35]
EVT100	DMAKWQD	Major depressive disorder	6A70.3	Phase 1	[36]
YM-90K	DMWRT4L	Convulsion	8A68.Z	Discontinued in Phase 2	[15]

Drug(s) Targeting Excitatory amino acid transporter 1 (SLC1A3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SYM2081	DM30WDL	Discovery agent	N.A.	Investigative	[3]
[3H]ETB-TBOA	DMWGY61	Discovery agent	N.A.	Investigative	[21]
DL-TBOA	DM2HGNU	Discovery agent	N.A.	Investigative	[37]
UCPH-101	DMTQEDA	Discovery agent	N.A.	Investigative	[38]

Drug(s) Targeting Excitatory amino acid transporter 2 (SLC1A2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SYM2081	DM30WDL	Discovery agent	N.A.	Investigative	[39]
[3H]ETB-TBOA	DMWGY61	Discovery agent	N.A.	Investigative	[21]
DL-TBOA	DM2HGNU	Discovery agent	N.A.	Investigative	[37]
Threo-3-methylglutamate	DMOE3IJ	Discovery agent	N.A.	Investigative	[39]
WAY-213613	DMMXL4E	Discovery agent	N.A.	Investigative	[40]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Excitatory amino acid transporter 1 (SLC1A3)	TT8WRDA	EAA1_HUMAN	Modulator	[3]
Excitatory amino acid transporter 2 (SLC1A2)	TT2F078	EAA2_HUMAN	Modulator	[4]
Excitatory amino acid transporter 3 (SLC1A1)	TTG2A6F	EAA3_HUMAN	Modulator	[5]
Excitatory amino acid transporter 4 (SLC1A6)	TT6KMPN	EAA4_HUMAN	Modulator	[6]
Excitatory amino acid transporter 5 (SLC1A7)	TTK41DM	EAA5_HUMAN	Modulator	[7]
Glutamate receptor ionotropic NMDA 1 (NMDAR1)	TTLD29N	NMDZ1_HUMAN	Agonist	[8]
Glutamate receptor ionotropic NMDA 2A (NMDAR2A)	TTKJEMQ	NMDE1_HUMAN	Agonist	[9]
Glutamate receptor ionotropic NMDA 2B (NMDAR2B)	TTN9D8E	NMDE2_HUMAN	Agonist	[10]
Glutamate receptor ionotropic NMDA 2C (GluN2C)	TT1M8OW	NMDE3_HUMAN	Agonist	[11]
Glutamate receptor ionotropic NMDA 2D (GluN2D)	TT5POTG	NMDE4_HUMAN	Agonist	[12]

References

• [1] 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: 4698).
• [2] 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: 6511).
• [3] 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: 868).
• [4] 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: 869).
• [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. (Target id: 870).
• [6] 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: 871).
• [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. (Target id: 872).
• [8] 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).
• [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. (Target id: 456).
• [10] 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: 457).
• [11] 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: 458).
• [12] 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: 459).
• [13] Glycine transport inhibitors for the treatment of schizophrenia: Symptom and disease modification. Curr Opin Drug Discov Devel. 2009 Jul;12(4):468-78.
• [14] 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.
• [15] 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.
• [16] Bivalent beta-carbolines as potential multitarget anti-Alzheimer agents. J Med Chem. 2010 May 13;53(9):3611-7.
• [17] 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).
• [18] 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.
• [19] 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.
• [20] 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.
• [21] Characterization of the tritium-labeled analog of L-threo-beta-benzyloxyaspartate binding to glutamate transporters. Mol Pharmacol. 2007 Jan;71(1):294-302.
• [22] Effects of threo-beta-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5). J Neurochem. 2001 Oct;79(2):297-302.
• [23] Pharmacological characterization of threo-3-methylglutamic acid with excitatory amino acid transporters in native and recombinant systems. J Neurochem. 2001 Apr;77(2):550-7.
• [24] Syntheses of optically pure beta-hydroxyaspartate derivatives as glutamate transporter blockers. Bioorg Med Chem Lett. 2000 Nov 6;10(21):2407-10.
• [25] The substituted aspartate analogue L-beta-threo-benzyl-aspartate preferentially inhibits the neuronal excitatory amino acid transporter EAAT3. Neuropharmacology. 2005 Nov;49(6):850-61.
• [26] Ligands targeting the excitatory amino acid transporters (EAATs). Curr Top Med Chem. 2006;6(17):1897-906.
• [27] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [28] Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
• [29] 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.
• [30] NMDA receptor stimulation induces reversible fission of the neuronal endoplasmic reticulum. PLoS One. 2009;4(4):e5250.
• [31] NMDA receptors as targets for drug action in neuropathic pain. Eur J Pharmacol. 2001 Oct 19;429(1-3):71-8.
• [32] Inhibition of in vivo [(3)H]MK-801 binding by NMDA receptor open channel blockers and GluN2B antagonists in rats and mice. Eur J Pharmacol. 2015 Nov 5;766:1-8.
• [33] Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
• [34] Clinical pipeline report, company report or official report of Cadent Therapeutics.
• [35] Neu2000, an NR2B-selective, moderate NMDA receptor antagonist and potent spin trapping molecule for stroke. Drug News Perspect. 2010 Nov;23(9):549-56.
• [36] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [37] DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. Mol Pharmacol. 1998 Feb;53(2):195-201.
• [38] Discovery of the first selective inhibitor of excitatory amino acid transporter subtype 1. J Med Chem. 2009 Feb 26;52(4):912-5.
• [39] Contrasting modes of action of methylglutamate derivatives on the excitatory amino acid transporters, EAAT1 and EAAT2. Mol Pharmacol. 1997 May;51(5):809-15.
• [40] Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinit... Mol Pharmacol. 2005 Oct;68(4):974-82.