Assay Detail
Binding
CHEMBL1111448
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Displacement of [3H]flumazenil from GABAA alpha-5-beta-3-gamma-2 receptor
15
Total Activities
15
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-5/beta-3/gamma-2 (CHEMBL2094122) ↗| 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 | 15 | 8.46 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1081862 | — | — | 1 | 9.22 |
| CHEMBL1080576 | — | — | 1 | 9.22 |
| CHEMBL1081140 | — | — | 1 | 9.10 |
| CHEMBL1081861 | — | — | 1 | 9.05 |
| CHEMBL1078209 | — | — | 1 | 8.92 |
| CHEMBL68684 | — | — | 1 | 8.82 |
| CHEMBL1077468 | — | — | 1 | 8.80 |
| CHEMBL1077518 | — | — | 1 | 8.66 |
| CHEMBL1080398 | — | — | 1 | 8.30 |
| CHEMBL1078580 | — | — | 1 | 8.22 |
| CHEMBL1080575 | — | — | 1 | 8.15 |
| CHEMBL1081139 | — | — | 1 | 7.96 |
| CHEMBL1080397 | — | — | 1 | 7.89 |
| CHEMBL1079272 | — | — | 1 | 7.70 |
| CHEMBL1080396 | — | — | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1081862 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1080576 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1081140 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL1081861 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1078209 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL68684 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1077468 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL1077518 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL1080398 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1078580 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL1080575 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL1081139 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1080397 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1079272 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL1080396 | — | Ki | = | 146.0 | nM | 6.84 |