Assay Detail
Binding
CHEMBL677036
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]-Ro- 15-1788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2
14
Total Activities
14
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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| 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 | 14 | 7.49 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95746 | — | — | 1 | 8.64 |
| CHEMBL95443 | — | — | 1 | 8.27 |
| CHEMBL17468 | — | — | 1 | 8.00 |
| CHEMBL318370 | — | — | 1 | 7.96 |
| CHEMBL95541 | — | — | 1 | 7.60 |
| CHEMBL320395 | — | — | 1 | 7.43 |
| CHEMBL318873 | — | — | 1 | 7.42 |
| CHEMBL98649 | — | — | 1 | 7.40 |
| CHEMBL95724 | — | — | 1 | 7.20 |
| CHEMBL95760 | — | — | 1 | 7.04 |
| CHEMBL95188 | — | — | 1 | 6.64 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.22 |
| CHEMBL100469 | — | — | 1 | - |
| CHEMBL95268 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95746 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL95443 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL17468 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL318370 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL95541 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL320395 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL318873 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL98649 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL95724 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL95760 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL95188 | — | Ki | = | 229.0 | nM | 6.64 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 605.0 | nM | 6.22 |
| CHEMBL100469 | — | Ki | > | 300.0 | nM | - |
| CHEMBL95268 | — | Ki | > | 300.0 | nM | - |