Assay Detail
Binding
CHEMBL2317652
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]KA from kainate receptor in rat brain cortex after 60 mins by Packard TopCount microplate scintillator counting
25
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 |
|---|---|---|---|
| IC50 | 25 | 4.82 | 7.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2312682 | — | — | 2 | 7.14 |
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.42 |
| CHEMBL2312403 | — | — | 2 | 4.94 |
| CHEMBL2312684 | — | — | 2 | 4.73 |
| CHEMBL2312686 | — | — | 2 | 4.61 |
| CHEMBL2312681 | — | — | 2 | 4.60 |
| CHEMBL2312399 | — | — | 2 | 4.54 |
| CHEMBL2312396 | — | — | 2 | 4.46 |
| CHEMBL2312400 | — | — | 2 | 4.30 |
| CHEMBL2312397 | — | — | 2 | 4.11 |
| CHEMBL2312685 | — | — | 2 | 4.05 |
| CHEMBL2312683 | — | — | 1 | - |
| CHEMBL2312680 | — | — | 1 | - |
| CHEMBL2312402 | — | — | 1 | - |
| CHEMBL2312401 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2312682 | — | IC50 | = | 72.44 | nM | 7.14 |
| CHEMBL2312682 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL575060 | GLUTAMIC ACID | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2312403 | — | IC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL2312403 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2312684 | — | IC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL2312684 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL2312686 | — | IC50 | = | 24547.09 | nM | 4.61 |
| CHEMBL2312686 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2312681 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL2312681 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL2312399 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL2312399 | — | IC50 | = | 28840.32 | nM | 4.54 |
| CHEMBL2312396 | — | IC50 | = | 34673.69 | nM | 4.46 |
| CHEMBL2312396 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL2312400 | — | IC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL2312400 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL2312397 | — | IC50 | = | 77624.71 | nM | 4.11 |
| CHEMBL2312397 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL2312685 | — | IC50 | = | 89125.09 | nM | 4.05 |
| CHEMBL2312685 | — | IC50 | = | 89000.0 | nM | 4.05 |
| CHEMBL2312680 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312402 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312401 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312683 | — | IC50 | > | 100000.0 | nM | - |