Page last updated: 2024-08-05 15:39:50
AMPA receptor agonist
An agonist that selectively binds to and activates AMPA receptors.
ChEBI ID: 64102
Members (1)
| Member | Definition | Class |
|---|---|---|
| 5-fluorowillardiine | An alanine derivative that is L-alanine bearing a 5-fluorouracil-1-yl substituent at position 3. A more potent and selective AMPA receptor agonist (at hGluR1 and hGluR2) than AMPA itself (Ki = 14.7, 25.1, and 1820 nM for hGluR1, hGluR2 and hGluR5 respectively). | 3-(5-fluorouracil-1-yl)-L-alanine |
Research
Studies (29)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 11 (37.93) | 18.2507 |
| 2000's | 9 (31.03) | 29.6817 |
| 2010's | 6 (20.69) | 24.3611 |
| 2020's | 3 (10.34) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (3.45%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 28 (96.55%) | 84.16% |
Protein Targets (17)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 56.2341 | 1 | 1 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Chain A, glutamate receptor 2 | Rattus norvegicus (Norway rat) | IC50 | 0.0235 | 1 | 4 |
| Glutamate receptor 1 | Homo sapiens (human) | Ki | 0.0147 | 1 | 1 |
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | Ki | 0.0029 | 1 | 1 |
| Glutamate receptor 2 | Homo sapiens (human) | Ki | 0.0251 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Ki | 0.0040 | 1 | 1 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | Ki | 0.0700 | 1 | 1 |
| Glutamate receptor 4 | Homo sapiens (human) | Ki | 0.3050 | 1 | 1 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | Ki | 0.1230 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 1 | Rattus norvegicus (Norway rat) | Ki | 1.3800 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 2 | Rattus norvegicus (Norway rat) | Ki | 100.0000 | 1 | 1 |
| Glutamate receptor ionotropic, kainate 5 | Homo sapiens (human) | Ki | 1.8200 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Glutamate receptor 1 | Homo sapiens (human) | EC50 | 0.3810 | 2 | 2 |
| Glutamate receptor 1 | Rattus norvegicus (Norway rat) | EC50 | 0.3800 | 1 | 1 |
| Glutamate receptor 2 | Homo sapiens (human) | EC50 | 0.4630 | 1 | 1 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | EC50 | 0.4600 | 1 | 1 |
| Glutamate receptor 3 | Homo sapiens (human) | EC50 | 20.9000 | 2 | 2 |
| Glutamate receptor 3 | Rattus norvegicus (Norway rat) | EC50 | 20.9000 | 1 | 1 |
| Glutamate receptor 4 | Rattus norvegicus (Norway rat) | EC50 | 11.9000 | 1 | 1 |