Assay Detail
Binding
CHEMBL1817066
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]SYM2081 from rat GluK3 expressed in Sf9 cells
11
Total Activities
11
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 3 (CHEMBL3744) ↗| 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 | 11 | 5.41 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL373428 | — | — | 1 | 7.64 |
| CHEMBL1812596 | — | — | 1 | 5.99 |
| CHEMBL492469 | — | — | 1 | 5.49 |
| CHEMBL492630 | — | — | 1 | 5.44 |
| CHEMBL1812598 | — | — | 1 | 5.32 |
| CHEMBL337577 | — | — | 1 | 5.29 |
| CHEMBL1738726 | — | — | 1 | 5.13 |
| CHEMBL1812599 | — | — | 1 | 4.27 |
| CHEMBL1812597 | — | — | 1 | 4.14 |
| CHEMBL1812601 | — | — | 1 | - |
| CHEMBL1812600 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL373428 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1812596 | — | Ki | = | 1022.0 | nM | 5.99 |
| CHEMBL492469 | — | Ki | = | 3250.0 | nM | 5.49 |
| CHEMBL492630 | — | Ki | = | 3650.0 | nM | 5.44 |
| CHEMBL1812598 | — | Ki | = | 4750.0 | nM | 5.32 |
| CHEMBL337577 | — | Ki | = | 5090.0 | nM | 5.29 |
| CHEMBL1738726 | — | Ki | = | 7450.0 | nM | 5.13 |
| CHEMBL1812599 | — | Ki | = | 53750.0 | nM | 4.27 |
| CHEMBL1812597 | — | Ki | = | 72300.0 | nM | 4.14 |
| CHEMBL1812601 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL1812600 | — | Ki | > | 1000000.0 | nM | - |