Assay Detail
Binding
CHEMBL1028967
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR1 expressed in Sf9 cells
17
Total Activities
17
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
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 | 17 | 6.75 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL123132 | — | — | 1 | 8.54 |
| CHEMBL13378 | (R,S)-AMPA | — | 1 | 7.66 |
| CHEMBL449296 | — | — | 1 | 7.46 |
| CHEMBL121388 | — | — | 1 | 7.43 |
| CHEMBL492630 | — | — | 1 | 7.30 |
| CHEMBL492469 | — | — | 1 | 7.24 |
| CHEMBL121915 | — | — | 1 | 7.08 |
| CHEMBL492629 | — | — | 1 | 6.99 |
| CHEMBL337577 | — | — | 1 | 6.96 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.77 |
| CHEMBL366489 | — | — | 1 | 6.39 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 6.32 |
| CHEMBL508818 | — | — | 1 | 5.62 |
| CHEMBL493596 | — | — | 1 | 4.98 |
| CHEMBL493892 | — | — | 1 | 4.45 |
| CHEMBL493665 | — | — | 1 | - |
| CHEMBL492628 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL123132 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL13378 | (R,S)-AMPA | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL449296 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL121388 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL492630 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL492469 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL121915 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL492629 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL337577 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL366489 | — | Ki | = | 410.0 | nM | 6.39 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 477.0 | nM | 6.32 |
| CHEMBL508818 | — | Ki | = | 2390.0 | nM | 5.62 |
| CHEMBL493596 | — | Ki | = | 10400.0 | nM | 4.98 |
| CHEMBL493892 | — | Ki | = | 35200.0 | nM | 4.45 |
| CHEMBL493665 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL492628 | — | Ki | > | 100000.0 | nM | - |