Assay Detail
Binding
CHEMBL1817063
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Displacement of [3H]AMPA from rat GluA2 expressed in Sf9 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Selective kainate receptor (GluK1) ligands structurally based upon 1H-cyclopentapyrimidin-2,4(1H,3H)-dione: synthesis, molecular modeling, and pharmacological and biostructural characterization.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.25 | 7.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL492469 | — | — | 1 | 7.10 |
| CHEMBL492630 | — | — | 1 | 6.95 |
| CHEMBL337577 | — | — | 1 | 6.65 |
| CHEMBL1812596 | — | — | 1 | 6.33 |
| CHEMBL1812598 | — | — | 1 | 6.30 |
| CHEMBL1738726 | — | — | 1 | 4.14 |
| CHEMBL1812601 | — | — | 1 | - |
| CHEMBL1812600 | — | — | 1 | - |
| CHEMBL1812599 | — | — | 1 | - |
| CHEMBL1812597 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL492469 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL492630 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL337577 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL1812596 | — | Ki | = | 465.0 | nM | 6.33 |
| CHEMBL1812598 | — | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL1738726 | — | Ki | = | 72900.0 | nM | 4.14 |
| CHEMBL1812601 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL1812600 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL1812599 | — | Ki | = | 107700.0 | nM | - |
| CHEMBL1812597 | — | Ki | > | 100000.0 | nM | - |