Assay Detail
Functional
CHEMBL861532
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity against GLUK5-containing kainate receptor by inhibition of kainate-induced depolarization of neonatal rat dorsal root fibers
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, kainate 5 (CHEMBL4041) ↗| Type | SINGLE PROTEIN |
| 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 |
|---|---|---|---|
| Kd | 14 | 5.32 | 6.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379442 | — | — | 1 | 6.98 |
| CHEMBL372797 | — | — | 1 | 6.40 |
| CHEMBL9790 | — | — | 1 | 5.78 |
| CHEMBL222519 | NBQX | — | 1 | 5.75 |
| CHEMBL206407 | — | — | 1 | 5.73 |
| CHEMBL446188 | — | — | 1 | 5.33 |
| CHEMBL382774 | — | — | 1 | 5.24 |
| CHEMBL200337 | — | — | 1 | 5.03 |
| CHEMBL438974 | — | — | 1 | 4.98 |
| CHEMBL208483 | — | — | 1 | 4.27 |
| CHEMBL207046 | — | — | 1 | 4.22 |
| CHEMBL200737 | — | — | 1 | 4.14 |
| CHEMBL382687 | — | — | 1 | - |
| CHEMBL383062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379442 | — | Kd | = | 105.0 | nM | 6.98 |
| CHEMBL372797 | — | Kd | = | 402.0 | nM | 6.40 |
| CHEMBL9790 | — | Kd | = | 1660.0 | nM | 5.78 |
| CHEMBL222519 | NBQX | Kd | = | 1780.0 | nM | 5.75 |
| CHEMBL206407 | — | Kd | = | 1880.0 | nM | 5.73 |
| CHEMBL446188 | — | Kd | = | 4680.0 | nM | 5.33 |
| CHEMBL382774 | — | Kd | = | 5800.0 | nM | 5.24 |
| CHEMBL200337 | — | Kd | = | 9250.0 | nM | 5.03 |
| CHEMBL438974 | — | Kd | = | 10500.0 | nM | 4.98 |
| CHEMBL208483 | — | Kd | = | 53700.0 | nM | 4.27 |
| CHEMBL207046 | — | Kd | = | 60200.0 | nM | 4.22 |
| CHEMBL200737 | — | Kd | = | 73100.0 | nM | 4.14 |
| CHEMBL382687 | — | Kd | - | — | - | |
| CHEMBL383062 | — | Kd | - | — | - |