Assay Detail
Binding
CHEMBL698076
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]kainate from human Ionotropic glutamate receptor ionotropic kainate 1 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 |
Target
Glutamate receptor ionotropic, kainate 5 (CHEMBL2675) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 6.83 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL121915 | — | — | 1 | 9.62 |
| CHEMBL331644 | — | — | 1 | 8.54 |
| CHEMBL333964 | — | — | 1 | 8.04 |
| CHEMBL121553 | — | — | 1 | 7.70 |
| CHEMBL331696 | — | — | 1 | 7.51 |
| CHEMBL121388 | — | — | 1 | 7.24 |
| CHEMBL275040 | KAINIC ACID | 2.0 | 1 | 6.75 |
| CHEMBL121191 | — | — | 1 | 6.41 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.15 |
| CHEMBL120808 | — | — | 1 | 5.94 |
| CHEMBL123132 | — | — | 1 | 5.74 |
| CHEMBL122656 | — | — | 1 | 5.70 |
| CHEMBL276815 | (S)-AMPA | — | 1 | 5.67 |
| CHEMBL122005 | (S)-WILLARDIINE | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL121915 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL331644 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL333964 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL121553 | — | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL331696 | — | Ki | = | 30.9 | nM | 7.51 |
| CHEMBL121388 | — | Ki | = | 57.1 | nM | 7.24 |
| CHEMBL275040 | KAINIC ACID | Ki | = | 177.0 | nM | 6.75 |
| CHEMBL121191 | — | Ki | = | 393.0 | nM | 6.41 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 701.0 | nM | 6.15 |
| CHEMBL120808 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL123132 | — | Ki | = | 1820.0 | nM | 5.74 |
| CHEMBL122656 | — | Ki | = | 1980.0 | nM | 5.70 |
| CHEMBL276815 | (S)-AMPA | Ki | = | 2144.0 | nM | 5.67 |
| CHEMBL122005 | (S)-WILLARDIINE | Ki | = | 28900.0 | nM | 4.54 |