Assay Detail
Binding
CHEMBL701549
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]AMPA from Ionotropic glutamate receptor AMPA in rat cortical membranes.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological evaluation of a new set of pyrazolo[1,5-c]quinazoline-2-carboxylates as novel excitatory amino acid antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 5.34 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL427734 | — | — | 1 | 6.85 |
| CHEMBL267276 | TQX-173 | — | 1 | 6.85 |
| CHEMBL276624 | — | — | 1 | 6.13 |
| CHEMBL268445 | — | — | 1 | 6.06 |
| CHEMBL274588 | — | — | 1 | 5.89 |
| CHEMBL9044 | — | — | 1 | 5.64 |
| CHEMBL9281 | — | — | 1 | 5.62 |
| CHEMBL8693 | — | — | 1 | 5.58 |
| CHEMBL275106 | — | — | 1 | 5.14 |
| CHEMBL9159 | — | — | 1 | 5.09 |
| CHEMBL267504 | — | — | 1 | 5.07 |
| CHEMBL267256 | — | — | 1 | 4.91 |
| CHEMBL9037 | — | — | 1 | 4.76 |
| CHEMBL8678 | — | — | 1 | 4.58 |
| CHEMBL267929 | — | — | 1 | 4.38 |
| CHEMBL267259 | — | — | 1 | 4.14 |
| CHEMBL8992 | — | — | 1 | 4.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL427734 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL267276 | TQX-173 | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL276624 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL268445 | — | Ki | = | 870.0 | nM | 6.06 |
| CHEMBL274588 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL9044 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL9281 | — | Ki | = | 2400.0 | nM | 5.62 |
| CHEMBL8693 | — | Ki | = | 2650.0 | nM | 5.58 |
| CHEMBL275106 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL9159 | — | Ki | = | 8200.0 | nM | 5.09 |
| CHEMBL267504 | — | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL267256 | — | Ki | = | 12400.0 | nM | 4.91 |
| CHEMBL9037 | — | Ki | = | 17300.0 | nM | 4.76 |
| CHEMBL8678 | — | Ki | = | 26000.0 | nM | 4.58 |
| CHEMBL267929 | — | Ki | = | 42000.0 | nM | 4.38 |
| CHEMBL267259 | — | Ki | = | 72000.0 | nM | 4.14 |
| CHEMBL8992 | — | Ki | = | 96000.0 | nM | 4.02 |