Assay Detail
Binding
CHEMBL4351326
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Displacement of (RS)-[3H]AMPA from recombinant rat GluA2(R) expressed in baculovirus infected Sf9 insect cell membranes
9
Total Activities
9
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
Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.49 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL94859 | — | — | 1 | 8.41 |
| CHEMBL276815 | (S)-AMPA | — | 1 | 7.77 |
| CHEMBL4529665 | — | — | 1 | 6.15 |
| CHEMBL3742451 | — | — | 1 | 5.73 |
| CHEMBL4556711 | — | — | 1 | 5.49 |
| CHEMBL3742450 | — | — | 1 | 5.36 |
| CHEMBL4448290 | — | — | 1 | - |
| CHEMBL4451018 | — | — | 1 | - |
| CHEMBL388746 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL94859 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL276815 | (S)-AMPA | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4529665 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL3742451 | — | Ki | = | 1870.0 | nM | 5.73 |
| CHEMBL4556711 | — | Ki | = | 3250.0 | nM | 5.49 |
| CHEMBL3742450 | — | Ki | = | 4380.0 | nM | 5.36 |
| CHEMBL4448290 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL4451018 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL388746 | — | Ki | = | 750.0 | nM | - |