Assay Detail
Binding
CHEMBL644196
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In vitro binding affinity against AMPA receptor by [3H]AMPA displacement.
18
Total Activities
18
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 (CHEMBL2096670) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
Pyrrolylquinoxalinediones: Dicarboxylates as highly potent AMPA receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.14 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL84142 | — | — | 1 | 8.40 |
| CHEMBL82375 | — | — | 1 | 8.40 |
| CHEMBL309831 | — | — | 1 | 8.15 |
| CHEMBL12510 | — | — | 1 | 7.82 |
| CHEMBL310503 | — | — | 1 | 7.70 |
| CHEMBL293613 | — | — | 1 | 7.66 |
| CHEMBL79348 | — | — | 1 | 7.27 |
| CHEMBL79454 | — | — | 1 | 7.22 |
| CHEMBL314248 | — | — | 1 | 7.18 |
| CHEMBL222519 | NBQX | — | 1 | 7.16 |
| CHEMBL268284 | — | — | 1 | 7.16 |
| CHEMBL13260 | YM-90K | — | 1 | 6.87 |
| CHEMBL12448 | — | — | 1 | 6.75 |
| CHEMBL309300 | — | — | 1 | 6.67 |
| CHEMBL12730 | — | — | 1 | 6.40 |
| CHEMBL310814 | — | — | 1 | 6.35 |
| CHEMBL311344 | — | — | 1 | 5.82 |
| CHEMBL12820 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL84142 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL82375 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL309831 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL12510 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL310503 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL293613 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL79348 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL79454 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL314248 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL222519 | NBQX | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL268284 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL13260 | YM-90K | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL12448 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL309300 | — | Ki | = | 215.0 | nM | 6.67 |
| CHEMBL12730 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL310814 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL311344 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL12820 | — | Ki | = | 3000.0 | nM | 5.52 |