Assay Detail
Functional
CHEMBL862719
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonism on GLUK5 containing kainate induced depolarization of isolated neonatal rat dorsal root C-fibers
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, kainate 1 (CHEMBL2919) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 18 | 5.33 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL427186 | — | — | 1 | 6.68 |
| CHEMBL372797 | — | — | 1 | 6.40 |
| CHEMBL372631 | — | — | 1 | 5.96 |
| CHEMBL9790 | — | — | 1 | 5.78 |
| CHEMBL222519 | NBQX | — | 1 | 5.75 |
| CHEMBL200309 | — | — | 1 | 5.23 |
| CHEMBL380804 | — | — | 1 | 5.09 |
| CHEMBL200337 | — | — | 1 | 5.03 |
| CHEMBL371944 | — | — | 1 | 4.31 |
| CHEMBL198511 | — | — | 1 | 4.22 |
| CHEMBL200737 | — | — | 1 | 4.14 |
| CHEMBL200271 | — | — | 1 | - |
| CHEMBL197437 | — | — | 1 | - |
| CHEMBL380805 | — | — | 1 | - |
| CHEMBL198632 | — | — | 1 | - |
| CHEMBL199233 | — | — | 1 | - |
| CHEMBL370793 | — | — | 1 | - |
| CHEMBL199232 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL427186 | — | Kd | = | 209.0 | nM | 6.68 |
| CHEMBL372797 | — | Kd | = | 402.0 | nM | 6.40 |
| CHEMBL372631 | — | Kd | = | 1090.0 | nM | 5.96 |
| CHEMBL9790 | — | Kd | = | 1660.0 | nM | 5.78 |
| CHEMBL222519 | NBQX | Kd | = | 1780.0 | nM | 5.75 |
| CHEMBL200309 | — | Kd | = | 5940.0 | nM | 5.23 |
| CHEMBL380804 | — | Kd | = | 8170.0 | nM | 5.09 |
| CHEMBL200337 | — | Kd | = | 9250.0 | nM | 5.03 |
| CHEMBL371944 | — | Kd | = | 49100.0 | nM | 4.31 |
| CHEMBL198511 | — | Kd | = | 60500.0 | nM | 4.22 |
| CHEMBL200737 | — | Kd | = | 73100.0 | nM | 4.14 |
| CHEMBL200271 | — | Kd | > | 100000.0 | nM | - |
| CHEMBL197437 | — | Kd | - | — | - | |
| CHEMBL380805 | — | Kd | - | — | - | |
| CHEMBL198632 | — | Kd | - | — | - | |
| CHEMBL199233 | — | Kd | - | — | - | |
| CHEMBL370793 | — | Kd | - | — | - | |
| CHEMBL199232 | — | Kd | - | — | - |