Assay Detail
Binding
CHEMBL878454
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Displacement of [3H]AMPA from human Ionotropic glutamate receptor AMPA 4 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 | 6.69 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL331696 | — | — | 1 | 8.44 |
| CHEMBL331644 | — | — | 1 | 8.10 |
| CHEMBL121553 | — | — | 1 | 7.70 |
| CHEMBL120808 | — | — | 1 | 7.05 |
| CHEMBL276815 | (S)-AMPA | — | 1 | 6.81 |
| CHEMBL122656 | — | — | 1 | 6.72 |
| CHEMBL121191 | — | — | 1 | 6.68 |
| CHEMBL123132 | — | — | 1 | 6.52 |
| CHEMBL121388 | — | — | 1 | 6.35 |
| CHEMBL333964 | — | — | 1 | 6.34 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.06 |
| CHEMBL121915 | — | — | 1 | 6.01 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 5.77 |
| CHEMBL122005 | (S)-WILLARDIINE | — | 1 | 5.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL331696 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL331644 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL121553 | — | Ki | = | 19.9 | nM | 7.70 |
| CHEMBL120808 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL276815 | (S)-AMPA | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL122656 | — | Ki | = | 189.0 | nM | 6.72 |
| CHEMBL121191 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL123132 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL121388 | — | Ki | = | 451.0 | nM | 6.35 |
| CHEMBL333964 | — | Ki | = | 457.0 | nM | 6.34 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 868.0 | nM | 6.06 |
| CHEMBL121915 | — | Ki | = | 972.0 | nM | 6.01 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 1710.0 | nM | 5.77 |
| CHEMBL122005 | (S)-WILLARDIINE | Ki | = | 8850.0 | nM | 5.05 |