Assay Detail
Binding
CHEMBL904137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095167) ↗| Type | PROTEIN COMPLEX |
| Organism | Rattus norvegicus |
Publication
Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.19 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL229145 | — | — | 1 | 8.59 |
| CHEMBL229144 | — | — | 1 | 8.39 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.92 |
| CHEMBL388601 | — | — | 1 | 7.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL229145 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL229144 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL12 | DIAZEPAM | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL388601 | — | Ki | = | 13.8 | nM | 7.86 |