Assay Detail
Binding
CHEMBL869459
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro-151788 from human recombinant GABA-Aalpha1 receptor plus beta3gamma2
9
Total Activities
9
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
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 9.03 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206380 | — | — | 1 | 9.80 |
| CHEMBL206587 | — | — | 1 | 9.55 |
| CHEMBL202696 | — | — | 1 | 9.28 |
| CHEMBL204696 | — | — | 1 | 9.22 |
| CHEMBL203211 | — | — | 1 | 9.15 |
| CHEMBL201472 | — | — | 1 | 8.85 |
| CHEMBL203877 | — | — | 1 | 8.62 |
| CHEMBL203186 | — | — | 1 | 8.60 |
| CHEMBL205205 | — | — | 1 | 8.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206380 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL206587 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL202696 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL204696 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL203211 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL201472 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL203877 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL203186 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL205205 | — | Ki | = | 6.5 | nM | 8.19 |