Assay Detail
Binding
CHEMBL863772
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro 15-1788 from recombinant human GABA-Aalpha1 receptor plus beta3gamma2 expressed in mouse L(tk-) cells
15
Total Activities
15
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-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 | 15 | 9.01 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL204156 | — | — | 1 | 9.26 |
| CHEMBL383677 | — | — | 1 | 9.22 |
| CHEMBL380730 | — | — | 1 | 9.17 |
| CHEMBL203897 | — | — | 1 | 9.17 |
| CHEMBL204003 | — | — | 1 | 9.17 |
| CHEMBL203455 | — | — | 1 | 9.12 |
| CHEMBL203315 | — | — | 1 | 9.10 |
| CHEMBL437877 | — | — | 1 | 9.09 |
| CHEMBL201472 | — | — | 1 | 9.07 |
| CHEMBL203785 | — | — | 1 | 8.89 |
| CHEMBL203437 | — | — | 1 | 8.85 |
| CHEMBL203732 | — | — | 1 | 8.84 |
| CHEMBL204004 | — | — | 1 | 8.80 |
| CHEMBL382005 | — | — | 1 | 8.75 |
| CHEMBL203781 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL204156 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL383677 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL380730 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL203897 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL204003 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL203455 | — | Ki | = | 0.76 | nM | 9.12 |
| CHEMBL203315 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL437877 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL201472 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL203785 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL203437 | — | Ki | = | 1.43 | nM | 8.85 |
| CHEMBL203732 | — | Ki | = | 1.45 | nM | 8.84 |
| CHEMBL204004 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL382005 | — | Ki | = | 1.79 | nM | 8.75 |
| CHEMBL203781 | — | Ki | = | 2.01 | nM | 8.70 |