Assay Detail
Binding
CHEMBL1111451
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Displacement of [3H]flumazenil from GABAA alpha-3-beta-3-gamma-2 receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-3/beta-3/gamma-2 (CHEMBL2094120) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Imidazo[1,5-a][1,2,4]-triazolo[1,5-d][1,4]benzodiazepines as potent and highly selective GABAA alpha5 inverse agonists with potential for the treatment of cognitive dysfunction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.67 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL68684 | — | — | 1 | 8.82 |
| CHEMBL1080576 | — | — | 1 | 7.14 |
| CHEMBL1078580 | — | — | 1 | 6.88 |
| CHEMBL1081861 | — | — | 1 | 6.56 |
| CHEMBL1080398 | — | — | 1 | 6.39 |
| CHEMBL1080575 | — | — | 1 | 6.29 |
| CHEMBL1080397 | — | — | 1 | 6.23 |
| CHEMBL1080396 | — | — | 1 | 5.92 |
| CHEMBL1079272 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL68684 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1080576 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL1078580 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL1081861 | — | Ki | = | 277.0 | nM | 6.56 |
| CHEMBL1080398 | — | Ki | = | 407.0 | nM | 6.39 |
| CHEMBL1080575 | — | Ki | = | 515.0 | nM | 6.29 |
| CHEMBL1080397 | — | Ki | = | 592.0 | nM | 6.23 |
| CHEMBL1080396 | — | Ki | = | 1206.0 | nM | 5.92 |
| CHEMBL1079272 | — | Ki | = | 1624.0 | nM | 5.79 |