Assay Detail
Binding
CHEMBL2317653
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Displacement of [3H]AMPA from AMPA receptor in rat brain cortex after 30 mins by Packard TopCount microplate scintillator counting
21
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 | 21 | 4.60 | 6.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575060 | GLUTAMIC ACID | 3.0 | 1 | 6.47 |
| CHEMBL2312682 | — | — | 2 | 5.19 |
| CHEMBL2312396 | — | — | 2 | 4.71 |
| CHEMBL2312400 | — | — | 2 | 4.26 |
| CHEMBL2312397 | — | — | 2 | 4.25 |
| CHEMBL2312399 | — | — | 2 | 4.18 |
| CHEMBL2312403 | — | — | 2 | 4.14 |
| CHEMBL2312686 | — | — | 1 | - |
| CHEMBL2312685 | — | — | 1 | - |
| CHEMBL2312684 | — | — | 1 | - |
| CHEMBL2312683 | — | — | 1 | - |
| CHEMBL2312681 | — | — | 1 | - |
| CHEMBL2312680 | — | — | 1 | - |
| CHEMBL2312402 | — | — | 1 | - |
| CHEMBL2312401 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575060 | GLUTAMIC ACID | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL2312682 | — | IC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL2312682 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL2312396 | — | IC50 | = | 19498.45 | nM | 4.71 |
| CHEMBL2312396 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL2312400 | — | IC50 | = | 54954.09 | nM | 4.26 |
| CHEMBL2312397 | — | IC50 | = | 56234.13 | nM | 4.25 |
| CHEMBL2312397 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL2312400 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL2312399 | — | IC50 | = | 66069.34 | nM | 4.18 |
| CHEMBL2312399 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL2312403 | — | IC50 | = | 72443.6 | nM | 4.14 |
| CHEMBL2312403 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL2312402 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312401 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312686 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312680 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312681 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312683 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312684 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2312685 | — | IC50 | > | 100000.0 | nM | - |