Assay Detail
Functional
CHEMBL904263
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at native GLUK5 kainate receptor assessed as antagonism of kainite-induced depolarization of neonatal anaesthetised rat dorsal root fibres
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Glutamate receptor ionotropic, kainate 1 (CHEMBL2919) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 14 | 7.03 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL220822 | — | — | 1 | 8.00 |
| CHEMBL373429 | — | — | 1 | 7.92 |
| CHEMBL373428 | — | — | 1 | 7.75 |
| CHEMBL222521 | — | — | 1 | 7.64 |
| CHEMBL221321 | — | — | 1 | 7.60 |
| CHEMBL375004 | — | — | 1 | 7.26 |
| CHEMBL220509 | — | — | 1 | 7.10 |
| CHEMBL374553 | — | — | 1 | 6.99 |
| CHEMBL379442 | — | — | 1 | 6.98 |
| CHEMBL427186 | — | — | 1 | 6.68 |
| CHEMBL223841 | — | — | 1 | 6.45 |
| CHEMBL372797 | — | — | 1 | 6.40 |
| CHEMBL9790 | — | — | 1 | 5.86 |
| CHEMBL206407 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL220822 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL373429 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL373428 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL222521 | — | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL221321 | — | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL375004 | — | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL220509 | — | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL374553 | — | Kd | = | 102.0 | nM | 6.99 |
| CHEMBL379442 | — | Kd | = | 105.0 | nM | 6.98 |
| CHEMBL427186 | — | Kd | = | 209.0 | nM | 6.68 |
| CHEMBL223841 | — | Kd | = | 358.0 | nM | 6.45 |
| CHEMBL372797 | — | Kd | = | 402.0 | nM | 6.40 |
| CHEMBL9790 | — | Kd | = | 1380.0 | nM | 5.86 |
| CHEMBL206407 | — | Kd | = | 1880.0 | nM | 5.73 |