Assay Detail
Binding
CHEMBL1028971
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]SYM2081 from rat recombinant iGluR5(Q)1b expressed in Sf9 cells
17
Total Activities
17
Compounds Tested
2
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
1H-cyclopentapyrimidine-2,4(1H,3H)-dione-related ionotropic glutamate receptors ligands. structure-activity relationships and identification of potent and Selective iGluR5 modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 6.80 | 8.62 |
| IC50 | 2 | 8.28 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121915 | — | — | 1 | 8.62 |
| CHEMBL492630 | — | — | 1 | 8.28 |
| CHEMBL492469 | — | — | 1 | 8.28 |
| CHEMBL449296 | — | — | 1 | 7.83 |
| CHEMBL337577 | — | — | 1 | 7.36 |
| CHEMBL121388 | — | — | 1 | 7.33 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 7.12 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.85 |
| CHEMBL508818 | — | — | 1 | 6.31 |
| CHEMBL492629 | — | — | 1 | 6.01 |
| CHEMBL13378 | (R,S)-AMPA | — | 1 | 5.94 |
| CHEMBL123132 | — | — | 1 | 5.86 |
| CHEMBL493892 | — | — | 1 | 5.53 |
| CHEMBL492628 | — | — | 1 | - |
| CHEMBL493665 | — | — | 1 | - |
| CHEMBL366489 | — | — | 1 | - |
| CHEMBL493596 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121915 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL492630 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL492469 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL449296 | — | Ki | = | 14.8 | nM | 7.83 |
| CHEMBL337577 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL121388 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL508818 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL492629 | — | Ki | = | 976.0 | nM | 6.01 |
| CHEMBL13378 | (R,S)-AMPA | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL123132 | — | Ki | = | 1380.0 | nM | 5.86 |
| CHEMBL493892 | — | Ki | = | 2980.0 | nM | 5.53 |
| CHEMBL492628 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL493665 | — | Ki | > | 1000000.0 | nM | - |
| CHEMBL366489 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL493596 | — | Ki | - | — | - |