Assay Detail
Binding
CHEMBL685340
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Displacement of [3H]- Ro 15-1788 binding from human GABA-A receptor alpha-5-beta-3-gamma-2 subunits
12
Total Activities
12
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
6,7-Dihydro-2-benzothiophen-4(5H)-ones: a novel class of GABA-A alpha5 receptor inverse agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.64 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17547 | — | — | 1 | 9.30 |
| CHEMBL17424 | — | — | 1 | 8.85 |
| CHEMBL274281 | — | — | 1 | 8.80 |
| CHEMBL17603 | — | — | 1 | 8.80 |
| CHEMBL17698 | — | — | 1 | 8.77 |
| CHEMBL275645 | — | — | 1 | 8.70 |
| CHEMBL17468 | — | — | 1 | 8.66 |
| CHEMBL277504 | — | — | 1 | 8.66 |
| CHEMBL17466 | — | — | 1 | 8.54 |
| CHEMBL17354 | — | — | 1 | 8.28 |
| CHEMBL17574 | — | — | 1 | 8.24 |
| CHEMBL276508 | — | — | 1 | 8.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17547 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL17424 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL274281 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL17603 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL17698 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL275645 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL17468 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL277504 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL17466 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL17354 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL17574 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL276508 | — | Ki | = | 9.1 | nM | 8.04 |