Assay Detail
Binding
CHEMBL839663
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Inhibition of [3H]KA binding to human iontropic glutamate receptors 5 and KA-2
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 4.74 | 5.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL189985 | — | — | 1 | 5.10 |
| CHEMBL191249 | — | — | 1 | 5.01 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 4.79 |
| CHEMBL222519 | NBQX | — | 1 | 4.58 |
| CHEMBL189721 | — | — | 1 | 4.21 |
| CHEMBL274226 | — | — | 1 | - |
| CHEMBL187941 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL189985 | — | Ki | = | 7890.0 | nM | 5.10 |
| CHEMBL191249 | — | Ki | = | 9860.0 | nM | 5.01 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | Ki | = | 16200.0 | nM | 4.79 |
| CHEMBL222519 | NBQX | Ki | = | 26600.0 | nM | 4.58 |
| CHEMBL189721 | — | Ki | = | 60900.0 | nM | 4.21 |
| CHEMBL274226 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL187941 | — | Ki | > | 100000.0 | nM | - |