Assay Detail
Functional
CHEMBL862717
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity on AMPA receptor expressed on rat motoneurons by its ability to reduce the fast component dorsal root evoked ventral root potential (fDR-VRP)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| 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 |
|---|---|---|---|
| IC50 | 14 | 4.77 | 6.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 6.67 |
| CHEMBL200337 | — | — | 1 | 4.99 |
| CHEMBL380804 | — | — | 1 | 4.86 |
| CHEMBL200737 | — | — | 1 | 4.62 |
| CHEMBL427186 | — | — | 1 | 4.13 |
| CHEMBL380805 | — | — | 1 | 4.10 |
| CHEMBL372631 | — | — | 1 | 4.01 |
| CHEMBL198632 | — | — | 1 | - |
| CHEMBL197437 | — | — | 1 | - |
| CHEMBL200271 | — | — | 1 | - |
| CHEMBL372797 | — | — | 1 | - |
| CHEMBL200309 | — | — | 1 | - |
| CHEMBL198511 | — | — | 1 | - |
| CHEMBL199232 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL200337 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL380804 | — | IC50 | = | 13700.0 | nM | 4.86 |
| CHEMBL200737 | — | IC50 | = | 23800.0 | nM | 4.62 |
| CHEMBL427186 | — | IC50 | = | 74100.0 | nM | 4.13 |
| CHEMBL380805 | — | IC50 | = | 79900.0 | nM | 4.10 |
| CHEMBL372631 | — | IC50 | = | 97600.0 | nM | 4.01 |
| CHEMBL198632 | — | IC50 | - | — | - | |
| CHEMBL197437 | — | IC50 | > | 1000000.0 | nM | - |
| CHEMBL200271 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL372797 | — | IC50 | = | 106000.0 | nM | - |
| CHEMBL200309 | — | IC50 | = | 164000.0 | nM | - |
| CHEMBL198511 | — | IC50 | = | 136000.0 | nM | - |
| CHEMBL199232 | — | IC50 | = | 287000.0 | nM | - |