Assay Detail
Binding
CHEMBL862572
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Displacement of [3H]Ro 15-1788 from recombinant human GABA-Aalpha5 receptor plus beta-3-gamma-2 expressed in L(tk-) cells
14
Total Activities
14
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-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 | 14 | 9.10 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL383677 | — | — | 1 | 9.85 |
| CHEMBL204003 | — | — | 1 | 9.51 |
| CHEMBL203455 | — | — | 1 | 9.49 |
| CHEMBL204004 | — | — | 1 | 9.38 |
| CHEMBL204156 | — | — | 1 | 9.30 |
| CHEMBL437877 | — | — | 1 | 9.30 |
| CHEMBL201472 | — | — | 1 | 9.28 |
| CHEMBL203437 | — | — | 1 | 9.17 |
| CHEMBL382005 | — | — | 1 | 8.95 |
| CHEMBL203732 | — | — | 1 | 8.91 |
| CHEMBL203315 | — | — | 1 | 8.91 |
| CHEMBL203781 | — | — | 1 | 8.80 |
| CHEMBL203897 | — | — | 1 | 8.57 |
| CHEMBL203785 | — | — | 1 | 8.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL383677 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL204003 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL203455 | — | Ki | = | 0.32 | nM | 9.49 |
| CHEMBL204004 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL204156 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL437877 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL201472 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL203437 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL382005 | — | Ki | = | 1.13 | nM | 8.95 |
| CHEMBL203732 | — | Ki | = | 1.24 | nM | 8.91 |
| CHEMBL203315 | — | Ki | = | 1.24 | nM | 8.91 |
| CHEMBL203781 | — | Ki | = | 1.57 | nM | 8.80 |
| CHEMBL203897 | — | Ki | = | 2.71 | nM | 8.57 |
| CHEMBL203785 | — | Ki | = | 9.34 | nM | 8.03 |