Assay Detail
Binding
CHEMBL5388308
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Positive allosteric modulation at AMPAR in HEK293 cells expressing GluA2Q assessed as glutamate induced calcium influx
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic AMPA (CHEMBL2096670) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
New insights in the development of positive allosteric modulators of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors belonging to 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides: Introduction of (mono/difluoro)methyl groups at the 2-position of the thiadiazine ring.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 5.28 | 6.56 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2441067 | — | — | 1 | 6.56 |
| CHEMBL5396768 | — | — | 1 | 6.55 |
| CHEMBL2441068 | — | — | 1 | 6.10 |
| CHEMBL5400708 | — | — | 1 | 5.67 |
| CHEMBL5419553 | — | — | 1 | 5.66 |
| CHEMBL5397532 | — | — | 1 | 5.06 |
| CHEMBL5403565 | — | — | 1 | 4.82 |
| CHEMBL5410137 | — | — | 1 | 4.78 |
| CHEMBL5427188 | — | — | 1 | 4.50 |
| CHEMBL5416254 | — | — | 1 | 4.24 |
| CHEMBL4073431 | — | — | 1 | 4.09 |
| CHEMBL5431136 | — | — | 1 | - |
| CHEMBL5400980 | — | — | 1 | - |
| CHEMBL5408760 | — | — | 1 | - |
| CHEMBL5404910 | — | — | 1 | - |
| CHEMBL5409424 | — | — | 1 | - |
| CHEMBL5397405 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2441067 | — | EC50 | = | 275.42 | nM | 6.56 |
| CHEMBL5396768 | — | EC50 | = | 281.84 | nM | 6.55 |
| CHEMBL2441068 | — | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL5400708 | — | EC50 | = | 2137.96 | nM | 5.67 |
| CHEMBL5419553 | — | EC50 | = | 2187.76 | nM | 5.66 |
| CHEMBL5397532 | — | EC50 | = | 8709.64 | nM | 5.06 |
| CHEMBL5403565 | — | EC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL5410137 | — | EC50 | = | 16595.87 | nM | 4.78 |
| CHEMBL5427188 | — | EC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL5416254 | — | EC50 | = | 57543.99 | nM | 4.24 |
| CHEMBL4073431 | — | EC50 | = | 81283.05 | nM | 4.09 |
| CHEMBL5431136 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5400980 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5408760 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5404910 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5409424 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5397405 | — | EC50 | > | 100000.0 | nM | - |