Assay Detail
Binding
CHEMBL696375
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Inhibition of [3H]KA binding to kainate receptor of rat brain membranes
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Glutamate receptor ionotropic, kainate (CHEMBL2094119) ↗| 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 |
|---|---|---|---|
| IC50 | 11 | 4.55 | 5.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222519 | NBQX | — | 1 | 5.16 |
| CHEMBL110492 | — | — | 1 | 5.05 |
| CHEMBL267276 | TQX-173 | — | 1 | 4.94 |
| CHEMBL320952 | — | — | 1 | 4.78 |
| CHEMBL322916 | — | — | 1 | 4.70 |
| CHEMBL432781 | — | — | 1 | 4.65 |
| CHEMBL110664 | — | — | 1 | 4.44 |
| CHEMBL321272 | — | — | 1 | 4.09 |
| CHEMBL106088 | — | — | 1 | 4.08 |
| CHEMBL110929 | — | — | 1 | 4.06 |
| CHEMBL326427 | — | — | 1 | 4.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222519 | NBQX | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL110492 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL267276 | TQX-173 | IC50 | = | 11600.0 | nM | 4.94 |
| CHEMBL320952 | — | IC50 | = | 16800.0 | nM | 4.78 |
| CHEMBL322916 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL432781 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL110664 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL321272 | — | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL106088 | — | IC50 | = | 84000.0 | nM | 4.08 |
| CHEMBL110929 | — | IC50 | = | 88000.0 | nM | 4.06 |
| CHEMBL326427 | — | IC50 | = | 90000.0 | nM | 4.05 |