Assay Detail
Binding
CHEMBL2443906
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Positive allosteric modulation of GluA2 receptor in rat embryonic cortex neuron assessed as increase of AMPA-induced membrane depolarization by fluorescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, pharmacological and structural characterization, and thermodynamic aspects of GluA2-positive allosteric modulators with a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 7 | 5.57 | 6.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2441067 | — | — | 1 | 6.05 |
| CHEMBL2441073 | — | — | 1 | 5.60 |
| CHEMBL2441068 | — | — | 1 | 5.50 |
| CHEMBL2441066 | — | — | 1 | 5.38 |
| CHEMBL2441069 | — | — | 1 | 5.32 |
| CHEMBL2441071 | — | — | 1 | - |
| CHEMBL2441070 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2441067 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2441073 | — | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL2441068 | — | EC50 | = | 3130.0 | nM | 5.50 |
| CHEMBL2441066 | — | EC50 | = | 4170.0 | nM | 5.38 |
| CHEMBL2441069 | — | EC50 | = | 4830.0 | nM | 5.32 |
| CHEMBL2441071 | — | EC50 | - | — | - | |
| CHEMBL2441070 | — | EC50 | - | — | - |