Aspartame
drug drugOn this page
Also known as APMAspartamAspartame (e951)AspartamoE-951EqualIns no.951Ins-951Methyl aspartylphenylalanateNSC-758953NutrasweetPal sweetSC-18862SladexZero-calSID17390037SID47193879SID26752906SID144204631
Summary
Aspartame (CHEMBL171679) is a phase-3 clinical-stage small molecule targeting TAS1R2.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (TAS1R2)
- Clinical trials: 13
- Chemistry: 294.3 Da · C14H18N2O5
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL171679 |
| Name | Aspartame |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 134601 |
| ChEBI | CHEBI:195544 |
| Molecular formula | C14H18N2O5 |
| Molecular weight | 294.3 |
| InChIKey | IAOZJIPTCAWIRG-QWRGUYRKSA-N |
SMILES: COC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC(=O)O)N
IUPAC name: (3S)-3-amino-4-[[(2S)-1-methoxy-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid
ChEBI definition: A dipeptide zwitterion resulting from transfer of a proton from the carboxy to the amino group of aspartame; major species at pH 7.3.
Also known as: APM, Aspartam, Aspartame, Aspartame (e951), Aspartamo, E-951, Equal, Ins no.951, Ins-951, Methyl aspartylphenylalanate, NSC-758953, Nutrasweet
Patent coverage: 53,265 distinct patent families (153,264 SureChEMBL compound mentions), from 1 matched compound structure(s). 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 |
|---|---|---|---|---|---|
| TAS1R2 | TAS1R2 | Agonist | 0.2% | Q8TE23 |
Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Thyrotropin receptor.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 2 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| TSHR | 5.8 | Potency | 1585 | nM | CHEMBL_ACT_3912522 |
| TSHR | 5.8 | Potency | 1585 | nM | CHEMBL_ACT_4722931 |
Target pathways
Aggregated over 1 target gene(s): TAS1R2.
Top Reactome pathways
3 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| G alpha (i) signalling events | 1 | TAS1R2 |
| Class C/3 (Metabotropic glutamate/pheromone receptors) | 1 | TAS1R2 |
| Sensory perception of sweet, bitter, and umami (glutamate) taste | 1 | TAS1R2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| detection of chemical stimulus involved in sensory perception of sweet taste | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| positive regulation of cytokinesis | 1 |
| sensory perception of sweet taste | 1 |
| signal transduction | 1 |
| sensory perception of taste | 1 |
Indications & clinical
Indications
0 indication records carry no mapped disease name (EFO/MeSH-only); none shown.
Clinical trials
Total trials: 13.
Phase distribution
| Phase | Trials |
|---|---|
| Not specified | 12 |
| PHASE1/PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01200940 | PHASE1/PHASE2 | COMPLETED | Metabolic Effects of Non-Nutritive Sweeteners |
| NCT05967741 | Not specified | RECRUITING | The Effects of Dietary Erythritol on Platelet Reactivity and Vascular Inflammation |
| NCT00731510 | Not specified | COMPLETED | MEDEX Hidden Valley 2008 |
| NCT01115088 | Not specified | COMPLETED | Effects of Stevia on Satiety and Eating Attitudes in Healthy, Overweight and Obese Adults |
| NCT01799096 | Not specified | COMPLETED | Effects of the Sugar Sucrose on Bodyweight and Energy Intake Over 28 Days in Obese Women |
| NCT02459535 | Not specified | COMPLETED | Immediate and Long-term Induction of Incretin Release by Artificial Sweeteners 1 |
| NCT02548767 | Not specified | COMPLETED | Adverse Metabolic Effects of Dietary Sugar |
| NCT02934321 | Not specified | COMPLETED | Assessment of Satiety Following Oral Administration of an Erythritol Sweetened Beverage |
| NCT02999321 | Not specified | COMPLETED | The Effects of Aspartame on Appetite, Body Composition and Oral Glucose Tolerance |
| NCT03353142 | Not specified | UNKNOWN | The Effects Of Equal Breathing On Pain Pressure Thresholds |
| NCT03708939 | Not specified | COMPLETED | Microbiome and Non-caloric Sweeteners in Humans |
| NCT04066569 | Not specified | COMPLETED | Reproducibility and Utility of OGTT in Acromegaly |
| NCT06057480 | Not specified | COMPLETED | APM in the Evoke SCS System to Program Patients With Chronic Pain of the Trunk and/or Limbs |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Genes: TAS1R2