Assay Detail
Binding
CHEMBL863774
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro 15-1788 from recombinant human GABA-Aalpha3 receptor plus beta-3-gamma-2 expressed in 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-3/beta-3/gamma-2 (CHEMBL2094120) ↗| 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 | 8.70 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383677 | — | — | 1 | 9.55 |
| CHEMBL203315 | — | — | 1 | 9.38 |
| CHEMBL204156 | — | — | 1 | 9.28 |
| CHEMBL203455 | — | — | 1 | 8.97 |
| CHEMBL437877 | — | — | 1 | 8.79 |
| CHEMBL204004 | — | — | 1 | 8.71 |
| CHEMBL204003 | — | — | 1 | 8.65 |
| CHEMBL203732 | — | — | 1 | 8.56 |
| CHEMBL380730 | — | — | 1 | 8.48 |
| CHEMBL203781 | — | — | 1 | 8.47 |
| CHEMBL203437 | — | — | 1 | 8.44 |
| CHEMBL382005 | — | — | 1 | 8.43 |
| CHEMBL201472 | — | — | 1 | 8.40 |
| CHEMBL203897 | — | — | 1 | 8.35 |
| CHEMBL203785 | — | — | 1 | 8.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383677 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL203315 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL204156 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL203455 | — | Ki | = | 1.06 | nM | 8.97 |
| CHEMBL437877 | — | Ki | = | 1.63 | nM | 8.79 |
| CHEMBL204004 | — | Ki | = | 1.94 | nM | 8.71 |
| CHEMBL204003 | — | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL203732 | — | Ki | = | 2.77 | nM | 8.56 |
| CHEMBL380730 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL203781 | — | Ki | = | 3.42 | nM | 8.47 |
| CHEMBL203437 | — | Ki | = | 3.64 | nM | 8.44 |
| CHEMBL382005 | — | Ki | = | 3.76 | nM | 8.43 |
| CHEMBL201472 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL203897 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL203785 | — | Ki | = | 9.53 | nM | 8.02 |