Assay Detail
Binding
CHEMBL697374
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Binding affinity at ionotropic glutamate receptor AMPA in rat cortical membranes [3H]AMPA displacement.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, AMPA (CHEMBL2093871) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis, ionotropic glutamate receptor binding affinity, and structure-activity relationships of a new set of 4,5-dihydro-8-heteroaryl-4-oxo-1,2,4-triazolo[1,5-a]quinoxaline-2-carboxylates analogues of TQX-173.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 5.47 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 7.16 |
| CHEMBL267276 | TQX-173 | — | 1 | 6.85 |
| CHEMBL110492 | — | — | 1 | 6.28 |
| CHEMBL314956 | — | — | 1 | 6.16 |
| CHEMBL110664 | — | — | 1 | 6.07 |
| CHEMBL320952 | — | — | 1 | 6.01 |
| CHEMBL310014 | — | — | 1 | 5.92 |
| CHEMBL110929 | — | — | 1 | 5.72 |
| CHEMBL105895 | — | — | 1 | 5.64 |
| CHEMBL322440 | — | — | 1 | 5.43 |
| CHEMBL322916 | — | — | 1 | 5.37 |
| CHEMBL105892 | — | — | 1 | 5.37 |
| CHEMBL432781 | — | — | 1 | 5.31 |
| CHEMBL106433 | — | — | 1 | 5.00 |
| CHEMBL311860 | — | — | 1 | 4.97 |
| CHEMBL324872 | — | — | 1 | 4.76 |
| CHEMBL326427 | — | — | 1 | 4.76 |
| CHEMBL110497 | — | — | 1 | 4.74 |
| CHEMBL106088 | — | — | 1 | 4.69 |
| CHEMBL321272 | — | — | 1 | 4.36 |
| CHEMBL325988 | — | — | 1 | 4.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL267276 | TQX-173 | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL110492 | — | Ki | = | 530.0 | nM | 6.28 |
| CHEMBL314956 | — | Ki | = | 700.0 | nM | 6.16 |
| CHEMBL110664 | — | Ki | = | 860.0 | nM | 6.07 |
| CHEMBL320952 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL310014 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL110929 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL105895 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL322440 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL322916 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL105892 | — | Ki | = | 4300.0 | nM | 5.37 |
| CHEMBL432781 | — | Ki | = | 4900.0 | nM | 5.31 |
| CHEMBL106433 | — | Ki | = | 10100.0 | nM | 5.00 |
| CHEMBL311860 | — | Ki | = | 10700.0 | nM | 4.97 |
| CHEMBL324872 | — | Ki | = | 17200.0 | nM | 4.76 |
| CHEMBL326427 | — | Ki | = | 17200.0 | nM | 4.76 |
| CHEMBL110497 | — | Ki | = | 18400.0 | nM | 4.74 |
| CHEMBL106088 | — | Ki | = | 20400.0 | nM | 4.69 |
| CHEMBL321272 | — | Ki | = | 44000.0 | nM | 4.36 |
| CHEMBL325988 | — | Ki | = | 47000.0 | nM | 4.33 |