Assay Detail
Functional
CHEMBL866869
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against AMPA receptor expressed in motoneurones by inhibition of fDR-VRP in the neonatal rat spinal cord
17
Total Activities
16
Compounds Tested
2
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
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.22 | 6.67 |
| Kd | 1 | 4.15 | 4.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 6.67 |
| CHEMBL9790 | — | — | 1 | 6.67 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.67 |
| CHEMBL382687 | — | — | 1 | 5.43 |
| CHEMBL208483 | — | — | 1 | 5.16 |
| CHEMBL200337 | — | — | 1 | 4.99 |
| CHEMBL206407 | — | — | 1 | 4.93 |
| CHEMBL200737 | — | — | 1 | 4.62 |
| CHEMBL379442 | — | — | 2 | 4.51 |
| CHEMBL207046 | — | — | 1 | 4.34 |
| CHEMBL446188 | — | — | 1 | 4.31 |
| CHEMBL383062 | — | — | 1 | 4.29 |
| CHEMBL202786 | — | — | 1 | - |
| CHEMBL438974 | — | — | 1 | - |
| CHEMBL382774 | — | — | 1 | - |
| CHEMBL372797 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9790 | — | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL222519 | NBQX | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL575060 | GLUTAMIC ACID | IC50 | = | 214.0 | nM | 6.67 |
| CHEMBL382687 | — | IC50 | = | 3730.0 | nM | 5.43 |
| CHEMBL208483 | — | IC50 | = | 6870.0 | nM | 5.16 |
| CHEMBL200337 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL206407 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL200737 | — | IC50 | = | 23800.0 | nM | 4.62 |
| CHEMBL379442 | — | IC50 | = | 31200.0 | nM | 4.51 |
| CHEMBL207046 | — | IC50 | = | 45400.0 | nM | 4.34 |
| CHEMBL446188 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL383062 | — | IC50 | = | 50900.0 | nM | 4.29 |
| CHEMBL379442 | — | Kd | = | 71400.0 | nM | 4.15 |
| CHEMBL372797 | — | IC50 | = | 106000.0 | nM | - |
| CHEMBL382774 | — | IC50 | = | 107000.0 | nM | - |
| CHEMBL438974 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL202786 | — | IC50 | > | 100000.0 | nM | - |