Assay Detail
Binding
CHEMBL2317647
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluK3 receptor expressed in sf9 cells by liquid scintillation counting
16
Total Activities
16
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 |
Target
Glutamate receptor ionotropic, kainate 3 (CHEMBL3744) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Chemoenzymatic synthesis of new 2,4-syn-functionalized (S)-glutamate analogues and structure-activity relationship studies at ionotropic glutamate receptors and excitatory amino acid transporters.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.89 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2312682 | — | — | 1 | 7.46 |
| CHEMBL2312403 | — | — | 1 | 6.91 |
| CHEMBL2312396 | — | — | 1 | 6.73 |
| CHEMBL2312681 | — | — | 1 | 6.66 |
| CHEMBL2312683 | — | — | 1 | 6.62 |
| CHEMBL2312684 | — | — | 1 | 6.47 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.31 |
| CHEMBL2312686 | — | — | 1 | 5.60 |
| CHEMBL2312402 | — | — | 1 | 5.55 |
| CHEMBL2312399 | — | — | 1 | 5.48 |
| CHEMBL2312397 | — | — | 1 | 5.33 |
| CHEMBL2312398 | — | — | 1 | 5.27 |
| CHEMBL2312680 | — | — | 1 | 5.25 |
| CHEMBL2312400 | — | — | 1 | 5.24 |
| CHEMBL2312685 | — | — | 1 | 4.99 |
| CHEMBL2312401 | — | — | 1 | 4.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2312682 | — | Ki | = | 34.5 | nM | 7.46 |
| CHEMBL2312403 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL2312396 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL2312681 | — | Ki | = | 217.0 | nM | 6.66 |
| CHEMBL2312683 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL2312684 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL575060 | GLUTAMIC ACID | Ki | = | 494.0 | nM | 6.31 |
| CHEMBL2312686 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL2312402 | — | Ki | = | 2810.0 | nM | 5.55 |
| CHEMBL2312399 | — | Ki | = | 3290.0 | nM | 5.48 |
| CHEMBL2312397 | — | Ki | = | 4660.0 | nM | 5.33 |
| CHEMBL2312398 | — | Ki | = | 5390.0 | nM | 5.27 |
| CHEMBL2312680 | — | Ki | = | 5660.0 | nM | 5.25 |
| CHEMBL2312400 | — | Ki | = | 5780.0 | nM | 5.24 |
| CHEMBL2312685 | — | Ki | = | 10200.0 | nM | 4.99 |
| CHEMBL2312401 | — | Ki | = | 44500.0 | nM | 4.35 |