Aspartic Acid
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Also known as Acide aspartiqueAcido asparticoAspartatel-lDeamidated asparagineFEMA NO. 3656L-aspartic acidNSC-3973L-aspartateSID11113409SID26751648SID50104339SID90340967L-ASPARTIC-ACID(S)-aspartic acid
Summary
Aspartic Acid (CHEMBL274323) is a phase-3 clinical-stage small molecule targeting GRIN1, GRIN2A, and GRIN2B.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 5 (GRIN1, GRIN2A, GRIN2B…)
- Clinical trials: 14
- Chemistry: 133.1 Da · C4H7NO4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL274323 |
| Name | Aspartic Acid |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 5960 |
| ChEBI | CHEBI:17053 |
| Molecular formula | C4H7NO4 |
| Molecular weight | 133.1 |
| InChIKey | CKLJMWTZIZZHCS-REOHCLBHSA-N |
SMILES: C([C@@H](C(=O)O)N)C(=O)O
IUPAC name: (2S)-2-aminobutanedioic acid
ChEBI definition: The L-enantiomer of aspartic acid.
Other ChEBI roles (chemical / environmental): Escherichia coli metabolite, mouse metabolite.
Also known as: Acide aspartique, Acido aspartico, Aspartate, Aspartic acid, l-, l, Deamidated asparagine, FEMA NO. 3656, L-aspartic acid, NSC-3973, L-aspartate, L-Aspartic acid
Patent coverage: 241,902 distinct patent families (733,178 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 733,172 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| GRIN1 | GluN1 | Agonist | 0.1% | Q05586 | |
| GRIN2A | GluN2A | Agonist | 0.4% | Q12879 | |
| GRIN2B | GluN2B | Agonist | 0% | Q13224 | |
| GRIN2C | GluN2C | Agonist | 0.2% | Q14957 | |
| GRIN2D | GluN2D | Agonist | 0.2% | O15399 |
Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: Tyrosyl-DNA phosphodiesterase 1, Prelamin-A/C, RecQ-like DNA helicase BLM, 4’-phosphopantetheinyl transferase ffp, Ferritin light chain, Glutamate NMDA receptor, Menin/Histone-lysine N-methyltransferase MLL, Excitatory amino acid transporter 3, Excitatory amino acid transporter 1, Cytochrome P450 1A2.
Bioactivity
ChEMBL activities: 10 potent at pChembl ≥ 5 of 27 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| O59010 | 9 | Kd | 1 | nM | CHEMBL_ACT_2146809 |
| P15917 | 5.9 | Potency | 1259 | nM | CHEMBL_ACT_4663678 |
| P35439 | 5.79 | IC50 | 1638 | nM | CHEMBL_ACT_1012819 |
| BLM | 5.45 | Potency | 3548 | nM | CHEMBL_ACT_4745912 |
| BLM | 5.45 | Potency | 3548 | nM | CHEMBL_ACT_4921901 |
| Q9F4F7 | 5.25 | Potency | 5623 | nM | CHEMBL_ACT_4386733 |
| ALDH1A1 | 5.05 | Potency | 8912 | nM | CHEMBL_ACT_4135448 |
| SLC1A3 | 5.03 | IC50 | 9300 | nM | CHEMBL_ACT_18406080 |
| SLC1A3 | 5.03 | IC50 | 9333 | nM | CHEMBL_ACT_18406249 |
| P35439 | 5 | IC50 | 10000 | nM | CHEMBL_ACT_1128075 |
Target pathways
Aggregated over 5 target gene(s): GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D.
Top Reactome pathways
11 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Unblocking of NMDA receptors, glutamate binding and activation | 5 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| Neurexins and neuroligins | 5 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| Synaptic adhesion-like molecules | 5 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| Assembly and cell surface presentation of NMDA receptors | 5 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| Negative regulation of NMDA receptor-mediated neuronal transmission | 5 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| Long-term potentiation | 5 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| Ras activation upon Ca2+ influx through NMDA receptor | 3 | GRIN1, GRIN2B, GRIN2D |
| RAF/MAP kinase cascade | 3 | GRIN1, GRIN2B, GRIN2D |
| EPHB-mediated forward signaling | 2 | GRIN1, GRIN2B |
| MECP2 regulates neuronal receptors and channels | 2 | GRIN2A, GRIN2B |
| Activated NTRK2 signals through FYN | 1 | GRIN2B |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| brain development | 5 |
| ionotropic glutamate receptor signaling pathway | 5 |
| regulation of synaptic plasticity | 5 |
| regulation of neuronal synaptic plasticity | 5 |
| positive regulation of synaptic transmission, glutamatergic | 5 |
| excitatory postsynaptic potential | 5 |
| calcium ion transmembrane import into cytosol | 5 |
| monoatomic cation transmembrane transport | 5 |
| excitatory chemical synaptic transmission | 5 |
| regulation of monoatomic cation transmembrane transport | 5 |
| positive regulation of excitatory postsynaptic potential | 5 |
| monoatomic ion transport | 5 |
| monoatomic ion transmembrane transport | 5 |
| regulation of membrane potential | 4 |
| calcium-mediated signaling | 4 |
Indications & clinical
Indications
0 indications (0 at ChEMBL trial phase 4).
Clinical trials
Total trials: 14.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 4 |
| Not specified | 4 |
| PHASE2 | 2 |
| PHASE1/PHASE2 | 2 |
| PHASE3 | 1 |
| PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05737030 | PHASE4 | ACTIVE_NOT_RECRUITING | Effect of L-ornithine-L-aspertate (LOLA) on the Gut Microbiome |
| NCT01722578 | PHASE4 | COMPLETED | L-ornithine L-aspartate in Overt Hepatic Encephalopathy |
| NCT02158182 | PHASE4 | COMPLETED | Lactulose, L-ornithine L-aspartate, or Rifaximin Versus Placebo for Preventing Hepatic Encephalopathy in Variceal Bleeding |
| NCT05920213 | PHASE4 | UNKNOWN | Efficacy of L-Ornithine L-Aspartate and Polyethylene Glycol in Cirrhotic Patients With Overt Hepatic Encephalopathy |
| NCT00433368 | PHASE3 | COMPLETED | Efficacy of L-Ornithine-L-Aspartate in Cirrhotics With Hepatic Encephalopathy |
| NCT06506643 | PHASE1/PHASE2 | RECRUITING | Safety and Efficacy of KLS-1 Monotherapy in Malignant Neoplasms |
| NCT06592014 | PHASE1/PHASE2 | ENROLLING_BY_INVITATION | Lithium for Parkinson’s: an Extension Trial |
| NCT07117630 | PHASE2 | RECRUITING | An Open-Label, Bayesian Adaptive Phase II Clinical Study in HR+/HER2- Advanced Breast Cancer After Progression on Standard Therapy |
| NCT00470314 | PHASE2 | UNKNOWN | Therapeutic Efficacy of L-Ornithine L-Aspartate Infusion in Patients With Acute Liver Failure |
| NCT06099886 | PHASE1 | COMPLETED | Repurposing Lithium for Parkinson’s Disease |
| NCT06483737 | Not specified | RECRUITING | Human Albumin Infusion in Liver Cirrhosis and Overt Hepatic Encephalopathy (HACHE) |
| NCT00305591 | Not specified | COMPLETED | Brain Imaging in Patients With Chronic Liver Disease and Functional Impairment. |
| NCT02523703 | Not specified | COMPLETED | Excitotoxicity Markers and the Clinical-radiological Progression After a Demyelinating Event: a Prospective Pilot Study |
| NCT05778461 | Not specified | UNKNOWN | Efficacy of L-ornithine L-aspartate and Therapeutic Plasma Exchange Versus Plasma Exchange Alone in Lowering Ammonia and Improving Outcomes in Pediatric Acute Liver Failure. |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
41 molecules share ≥1 primary target. Top 41 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AMANTADINE | ChEMBL + PubChem | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| CHLORPROMAZINE | ChEMBL + PubChem | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| DEXTROMETHORPHAN | ChEMBL + PubChem | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| KETAMINE | ChEMBL + PubChem | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| LEVORPHANOL | ChEMBL + PubChem | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| MEMANTINE | ChEMBL + PubChem | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| ORPHENADRINE | ChEMBL + PubChem | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| CYCLOSERINE | ChEMBL | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| PROCYCLIDINE | ChEMBL | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| GLUTAMIC ACID | ChEMBL + PubChem | Phase 3 (approved) | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| DALZANEMDOR | ChEMBL | Phase 3 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| ESMETHADONE | ChEMBL | Phase 3 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| ALPHAMETHADOL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| BUDIPINE | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| DEXTRORPHAN | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| DIZOCILPINE | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| IFENPRODIL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| LANICEMINE | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| LEVOMETHADONE | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| LICOSTINEL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| PERZINFOTEL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| PHENCYCLIDINE | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| RACEMETHORPHAN | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| RADIPRODIL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| SELFOTEL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| TEZAMPANEL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| TRAXOPRODIL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2B, GRIN2C, GRIN2D |
| BETAMETHADOL | ChEMBL | Phase 2 | GRIN1, GRIN2A, GRIN2C, GRIN2D |
| TACRINE | ChEMBL | Phase 4 (approved) | GRIN1, GRIN2A, GRIN2B |
| LATREPIRDINE | ChEMBL | Phase 3 | GRIN1, GRIN2A, GRIN2B |
| ESKETAMINE | ChEMBL + PubChem | Phase 4 (approved) | GRIN1, GRIN2A |
| PENTAMIDINE | ChEMBL | Phase 4 (approved) | GRIN1, GRIN2A |
| DEXOXADROL | ChEMBL | Phase 2 | GRIN1, GRIN2A |
| DIMEMORFAN | ChEMBL | Phase 2 | GRIN1, GRIN2A |
| ELIPRODIL | ChEMBL | Phase 2 | GRIN1, GRIN2B |
| ETOXADROL | ChEMBL | Phase 2 | GRIN1, GRIN2A |
| ONFASPRODIL | ChEMBL | Phase 2 | GRIN1, GRIN2B |
| ZELQUISTINEL | ChEMBL | Phase 2 | GRIN2B, GRIN2C |
| Nimodipine | PubChem | Approved | GRIN2C, GRIN2D |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | GRIN2B |
| EVT-101 FREE BASE | ChEMBL | Phase 2 | GRIN2B |