Assay Detail
Binding
CHEMBL863773
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro 15-1788 from recombinant human GABA-Aalpha2 receptor plus beta-3-gamma-2 expressed in mouse L(tk-) cells
6
Total Activities
6
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-2/beta-3/gamma-2 (CHEMBL2094130) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Imidazo[1,2-b][1,2,4]triazines as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.58 | 9.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL204156 | — | — | 1 | 9.04 |
| CHEMBL203455 | — | — | 1 | 8.81 |
| CHEMBL203732 | — | — | 1 | 8.64 |
| CHEMBL203897 | — | — | 1 | 8.46 |
| CHEMBL201472 | — | — | 1 | 8.43 |
| CHEMBL203785 | — | — | 1 | 8.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL204156 | — | Ki | = | 0.92 | nM | 9.04 |
| CHEMBL203455 | — | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL203732 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL203897 | — | Ki | = | 3.44 | nM | 8.46 |
| CHEMBL201472 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL203785 | — | Ki | = | 8.43 | nM | 8.07 |