Assay Detail
Binding
CHEMBL696974
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Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 2 expressed in HEK293 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 6.77 | 7.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL331696 | — | — | 1 | 7.78 |
| CHEMBL331644 | — | — | 1 | 7.71 |
| CHEMBL123132 | — | — | 1 | 7.60 |
| CHEMBL121388 | — | — | 1 | 7.28 |
| CHEMBL121553 | — | — | 1 | 7.00 |
| CHEMBL333964 | — | — | 1 | 7.00 |
| CHEMBL276815 | (S)-AMPA | — | 1 | 6.97 |
| CHEMBL121191 | — | — | 1 | 6.94 |
| CHEMBL121915 | — | — | 1 | 6.75 |
| CHEMBL120808 | — | — | 1 | 6.43 |
| CHEMBL122656 | — | — | 1 | 6.34 |
| CHEMBL122005 | (S)-WILLARDIINE | — | 1 | 6.05 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.03 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL331696 | — | Ki | = | 16.7 | nM | 7.78 |
| CHEMBL331644 | — | Ki | = | 19.3 | nM | 7.71 |
| CHEMBL123132 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL121388 | — | Ki | = | 53.1 | nM | 7.28 |
| CHEMBL121553 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL333964 | — | Ki | = | 101.0 | nM | 7.00 |
| CHEMBL276815 | (S)-AMPA | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL121191 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL121915 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL120808 | — | Ki | = | 372.0 | nM | 6.43 |
| CHEMBL122656 | — | Ki | = | 461.0 | nM | 6.34 |
| CHEMBL122005 | (S)-WILLARDIINE | Ki | = | 898.0 | nM | 6.05 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 940.0 | nM | 6.03 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 12200.0 | nM | 4.91 |