Assay Detail
Binding
CHEMBL840053
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Inhibition of [3H]KA binding to human iontropic glutamate receptors 5 and 6
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 | 5.40 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL189985 | — | — | 1 | 6.00 |
| CHEMBL191249 | — | — | 1 | 5.86 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | 2.0 | 1 | 5.68 |
| CHEMBL189721 | — | — | 1 | 5.22 |
| CHEMBL222519 | NBQX | — | 1 | 5.21 |
| CHEMBL274226 | — | — | 1 | 4.99 |
| CHEMBL187941 | — | — | 1 | 4.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL189985 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL191249 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL14935 | TEZAMPANEL ANHYDROUS | Ki | = | 2100.0 | nM | 5.68 |
| CHEMBL189721 | — | Ki | = | 5980.0 | nM | 5.22 |
| CHEMBL222519 | NBQX | Ki | = | 6120.0 | nM | 5.21 |
| CHEMBL274226 | — | Ki | = | 10170.0 | nM | 4.99 |
| CHEMBL187941 | — | Ki | = | 13710.0 | nM | 4.86 |