Assay Detail
Binding
CHEMBL680879
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Binding affinity for human GluR6 expressed in HEK293 cells using [3]H-kainate
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Glutamate receptor ionotropic, kainate 2 (CHEMBL3683) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 5.43 | 6.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13076 | — | — | 1 | 6.21 |
| CHEMBL305534 | — | — | 1 | 5.92 |
| CHEMBL67828 | — | — | 1 | 5.85 |
| CHEMBL12465 | — | — | 1 | 5.82 |
| CHEMBL416685 | — | — | 1 | 5.44 |
| CHEMBL268284 | — | — | 1 | 5.41 |
| CHEMBL63861 | — | — | 1 | 5.39 |
| CHEMBL293613 | — | — | 1 | 5.24 |
| CHEMBL429540 | — | — | 1 | 5.21 |
| CHEMBL63927 | — | — | 1 | 4.64 |
| CHEMBL303415 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13076 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL305534 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL67828 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL12465 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL416685 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL268284 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL63861 | — | Ki | = | 4100.0 | nM | 5.39 |
| CHEMBL293613 | — | Ki | = | 5800.0 | nM | 5.24 |
| CHEMBL429540 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL63927 | — | Ki | = | 23000.0 | nM | 4.64 |
| CHEMBL303415 | — | Ki | = | 28000.0 | nM | 4.55 |