Assay Detail
Binding
CHEMBL1817064
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]SYM2081 from rat GluK1 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 |
Target
Glutamate receptor ionotropic, kainate 1 (CHEMBL2919) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 6.88 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1812596 | — | — | 1 | 8.41 |
| CHEMBL492630 | — | — | 1 | 8.28 |
| CHEMBL492469 | — | — | 1 | 8.28 |
| CHEMBL1812598 | — | — | 1 | 8.23 |
| CHEMBL337577 | — | — | 1 | 7.36 |
| CHEMBL1738726 | — | — | 1 | 6.80 |
| CHEMBL1812599 | — | — | 1 | 6.25 |
| CHEMBL1812597 | — | — | 1 | 5.43 |
| CHEMBL1812601 | — | — | 1 | 4.92 |
| CHEMBL1812600 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1812596 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL492630 | — | Ki | = | 5.29 | nM | 8.28 |
| CHEMBL492469 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL1812598 | — | Ki | = | 5.89 | nM | 8.23 |
| CHEMBL337577 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL1738726 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL1812599 | — | Ki | = | 567.0 | nM | 6.25 |
| CHEMBL1812597 | — | Ki | = | 3673.0 | nM | 5.43 |
| CHEMBL1812601 | — | Ki | = | 11970.0 | nM | 4.92 |
| CHEMBL1812600 | — | Ki | = | 15090.0 | nM | 4.82 |