Assay Detail
Binding
CHEMBL869461
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro-151788 from human recombinant GABA-Aalpha5 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-5/beta-3/gamma-2 (CHEMBL2094122) ↗| 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 | 9.25 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL202696 | — | — | 1 | 10.00 |
| CHEMBL206587 | — | — | 1 | 9.82 |
| CHEMBL206380 | — | — | 1 | 9.72 |
| CHEMBL203211 | — | — | 1 | 9.41 |
| CHEMBL201472 | — | — | 1 | 9.28 |
| CHEMBL204696 | — | — | 1 | 9.05 |
| CHEMBL203877 | — | — | 1 | 9.02 |
| CHEMBL205205 | — | — | 1 | 8.64 |
| CHEMBL203186 | — | — | 1 | 8.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL202696 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL206587 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL206380 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL203211 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL201472 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL204696 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL203877 | — | Ki | = | 0.95 | nM | 9.02 |
| CHEMBL205205 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL203186 | — | Ki | = | 4.8 | nM | 8.32 |