Assay Detail
Binding
CHEMBL680672
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Inhibition of [3H]-Ro- 15-1788 binding to human GABA-A receptor alpha-5-beta-3-gamma-2 subunits
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-5/beta-3/gamma-2 (CHEMBL2094122) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 8.42 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95746 | — | — | 1 | 9.30 |
| CHEMBL318873 | — | — | 1 | 9.00 |
| CHEMBL95443 | — | — | 1 | 9.00 |
| CHEMBL95541 | — | — | 1 | 8.72 |
| CHEMBL318370 | — | — | 1 | 8.68 |
| CHEMBL17468 | — | — | 1 | 8.66 |
| CHEMBL320395 | — | — | 1 | 8.59 |
| CHEMBL95760 | — | — | 1 | 8.59 |
| CHEMBL98649 | — | — | 1 | 8.49 |
| CHEMBL95724 | — | — | 1 | 8.12 |
| CHEMBL95188 | — | — | 1 | 7.72 |
| CHEMBL100469 | — | — | 1 | 7.60 |
| CHEMBL95268 | — | — | 1 | 6.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95746 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL318873 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL95443 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL95541 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL318370 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL17468 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL320395 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL95760 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL98649 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL95724 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL95188 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL100469 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL95268 | — | Ki | = | 103.0 | nM | 6.99 |