Assay Detail
Binding
CHEMBL680293
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]- Ro 15-1788 binding from human GABA-A receptor alpha-1-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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| 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 | 7.63 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17547 | — | — | 1 | 8.44 |
| CHEMBL17424 | — | — | 1 | 8.37 |
| CHEMBL275645 | — | — | 1 | 8.30 |
| CHEMBL17468 | — | — | 1 | 8.00 |
| CHEMBL274281 | — | — | 1 | 7.92 |
| CHEMBL17603 | — | — | 1 | 7.70 |
| CHEMBL17466 | — | — | 1 | 7.51 |
| CHEMBL17698 | — | — | 1 | 7.35 |
| CHEMBL277504 | — | — | 1 | 7.21 |
| CHEMBL17354 | — | — | 1 | 7.18 |
| CHEMBL17574 | — | — | 1 | 6.78 |
| CHEMBL276508 | — | — | 1 | 6.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17547 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL17424 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL275645 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL17468 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL274281 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL17603 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL17466 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL17698 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL277504 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL17354 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL17574 | — | Ki | = | 165.0 | nM | 6.78 |
| CHEMBL276508 | — | Ki | = | 172.0 | nM | 6.76 |