Assay Detail
Binding
CHEMBL828279
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-KA binding to iontropic glutamate receptor 5
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, kainate 1 (CHEMBL1918) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 5.18 | 5.81 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191249 | — | — | 1 | 5.81 |
| CHEMBL189985 | — | — | 1 | 5.77 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 5.38 |
| CHEMBL189721 | — | — | 1 | 5.13 |
| CHEMBL222519 | NBQX | — | 1 | 4.93 |
| CHEMBL274226 | — | — | 1 | 4.77 |
| CHEMBL187941 | — | — | 1 | 4.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191249 | — | Ki | = | 1550.0 | nM | 5.81 |
| CHEMBL189985 | — | Ki | = | 1690.0 | nM | 5.77 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | Ki | = | 4160.0 | nM | 5.38 |
| CHEMBL189721 | — | Ki | = | 7370.0 | nM | 5.13 |
| CHEMBL222519 | NBQX | Ki | = | 11730.0 | nM | 4.93 |
| CHEMBL274226 | — | Ki | = | 17130.0 | nM | 4.77 |
| CHEMBL187941 | — | Ki | = | 31750.0 | nM | 4.50 |