Assay Detail
Binding
CHEMBL865634
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Displacement of [3H]kainate from rat GLUK6 expressed in HEK293 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, kainate 2 (CHEMBL3607) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Structure-activity relationship studies on N3-substituted willardiine derivatives acting as AMPA or kainate receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 5.73 | 5.98 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9790 | — | — | 1 | 5.98 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 5.48 |
| CHEMBL200737 | — | — | 1 | - |
| CHEMBL206407 | — | — | 1 | - |
| CHEMBL202786 | — | — | 1 | - |
| CHEMBL379442 | — | — | 1 | - |
| CHEMBL438974 | — | — | 1 | - |
| CHEMBL446188 | — | — | 1 | - |
| CHEMBL382774 | — | — | 1 | - |
| CHEMBL382687 | — | — | 1 | - |
| CHEMBL208483 | — | — | 1 | - |
| CHEMBL207046 | — | — | 1 | - |
| CHEMBL383062 | — | — | 1 | - |
| CHEMBL372797 | — | — | 1 | - |
| CHEMBL200337 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9790 | — | Ki | = | 1050.0 | nM | 5.98 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 3280.0 | nM | 5.48 |
| CHEMBL200737 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL206407 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL202786 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL379442 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL438974 | — | Ki | - | — | - | |
| CHEMBL446188 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL382774 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL382687 | — | Ki | - | — | - | |
| CHEMBL208483 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL207046 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL383062 | — | Ki | - | — | - | |
| CHEMBL372797 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL200337 | — | Ki | > | 100000.0 | nM | - |