Assay Detail
Binding
CHEMBL862728
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](S)-5-fluorowillardiine from AMPA receptor in rat brain membrane
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.34 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL276815 | (S)-AMPA | — | 1 | 6.89 |
| CHEMBL380804 | — | — | 1 | 5.30 |
| CHEMBL200737 | — | — | 1 | 4.89 |
| CHEMBL200337 | — | — | 1 | 4.87 |
| CHEMBL198511 | — | — | 1 | 4.75 |
| CHEMBL197437 | — | — | 1 | - |
| CHEMBL427186 | — | — | 1 | - |
| CHEMBL200271 | — | — | 1 | - |
| CHEMBL372797 | — | — | 1 | - |
| CHEMBL200309 | — | — | 1 | - |
| CHEMBL371944 | — | — | 1 | - |
| CHEMBL372631 | — | — | 1 | - |
| CHEMBL380805 | — | — | 1 | - |
| CHEMBL381221 | — | — | 1 | - |
| CHEMBL199233 | — | — | 1 | - |
| CHEMBL370793 | — | — | 1 | - |
| CHEMBL199232 | — | — | 1 | - |
| CHEMBL198632 | — | — | 1 | - |
| CHEMBL200237 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL276815 | (S)-AMPA | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL380804 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL200737 | — | Ki | = | 12900.0 | nM | 4.89 |
| CHEMBL200337 | — | Ki | = | 13400.0 | nM | 4.87 |
| CHEMBL198511 | — | Ki | = | 17800.0 | nM | 4.75 |
| CHEMBL197437 | — | Ki | - | — | - | |
| CHEMBL427186 | — | Ki | - | — | - | |
| CHEMBL200271 | — | Ki | - | — | - | |
| CHEMBL372797 | — | Ki | - | — | - | |
| CHEMBL200309 | — | Ki | = | 269000.0 | nM | - |
| CHEMBL371944 | — | Ki | - | — | - | |
| CHEMBL372631 | — | Ki | - | — | - | |
| CHEMBL380805 | — | Ki | - | — | - | |
| CHEMBL381221 | — | Ki | = | 166000.0 | nM | - |
| CHEMBL199233 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL370793 | — | Ki | - | — | - | |
| CHEMBL199232 | — | Ki | = | 195000.0 | nM | - |
| CHEMBL198632 | — | Ki | - | — | - | |
| CHEMBL200237 | — | Ki | = | 149000.0 | nM | - |