Assay Detail
Binding
CHEMBL680878
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Binding affinity towards cloned human GluR5 subunit stably expressed in cultured HEK293 cells using [3]H-kainate as radioligand
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 1 (CHEMBL1918) ↗| 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 | 6.70 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63861 | — | — | 1 | 8.42 |
| CHEMBL67828 | — | — | 1 | 7.92 |
| CHEMBL13076 | — | — | 1 | 7.00 |
| CHEMBL416685 | — | — | 1 | 6.64 |
| CHEMBL12465 | — | — | 1 | 6.64 |
| CHEMBL429540 | — | — | 1 | 6.50 |
| CHEMBL303415 | — | — | 1 | 6.48 |
| CHEMBL63927 | — | — | 1 | 6.37 |
| CHEMBL268284 | — | — | 1 | 6.28 |
| CHEMBL293613 | — | — | 1 | 5.85 |
| CHEMBL305534 | — | — | 1 | 5.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63861 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL67828 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL13076 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL416685 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL12465 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL429540 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL303415 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL63927 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL268284 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL293613 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL305534 | — | Ki | = | 2400.0 | nM | 5.62 |