Assay Detail
Binding
CHEMBL1028969
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Displacement of (R,S)-[5-methyl-3H]AMPA from rat recombinant flop iGluR3 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 | 5.99 | 7.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13378 | (R,S)-AMPA | — | 1 | 7.69 |
| CHEMBL123132 | — | — | 1 | 7.16 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.60 |
| CHEMBL492469 | — | — | 1 | 6.51 |
| CHEMBL449296 | — | — | 1 | 6.36 |
| CHEMBL121388 | — | — | 1 | 6.35 |
| CHEMBL492630 | — | — | 1 | 6.03 |
| CHEMBL121915 | — | — | 1 | 6.01 |
| CHEMBL492629 | — | — | 1 | 5.82 |
| CHEMBL337577 | — | — | 1 | 5.72 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 5.70 |
| CHEMBL508818 | — | — | 1 | 5.16 |
| CHEMBL366489 | — | — | 1 | 4.72 |
| CHEMBL493665 | — | — | 1 | 4.00 |
| CHEMBL493596 | — | — | 1 | - |
| CHEMBL492628 | — | — | 1 | - |
| CHEMBL493892 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13378 | (R,S)-AMPA | Ki | = | 20.6 | nM | 7.69 |
| CHEMBL123132 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL492469 | — | Ki | = | 311.0 | nM | 6.51 |
| CHEMBL449296 | — | Ki | = | 434.0 | nM | 6.36 |
| CHEMBL121388 | — | Ki | = | 451.0 | nM | 6.35 |
| CHEMBL492630 | — | Ki | = | 936.0 | nM | 6.03 |
| CHEMBL121915 | — | Ki | = | 976.0 | nM | 6.01 |
| CHEMBL492629 | — | Ki | = | 1510.0 | nM | 5.82 |
| CHEMBL337577 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 1980.0 | nM | 5.70 |
| CHEMBL508818 | — | Ki | = | 6910.0 | nM | 5.16 |
| CHEMBL366489 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL493665 | — | Ki | = | 100000.0 | nM | 4.00 |
| CHEMBL493596 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL492628 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL493892 | — | Ki | > | 100000.0 | nM | - |