Assay Detail
Binding
CHEMBL853070
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H] Ro15-1788 from recombinant human GABAA alpha2 receptor plus beta-3-gamma-2 expressed in L(tk-) cells
12
Total Activities
12
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
Discovery of imidazo[1,2-b][1,2,4]triazines as GABA(A) alpha2/3 subtype selective agonists for the treatment of anxiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 8.57 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL199957 | — | — | 1 | 9.40 |
| CHEMBL369902 | — | — | 1 | 9.14 |
| CHEMBL427207 | — | — | 1 | 9.10 |
| CHEMBL202343 | — | — | 1 | 9.00 |
| CHEMBL204319 | — | — | 1 | 8.92 |
| CHEMBL204696 | — | — | 1 | 8.74 |
| CHEMBL204701 | — | — | 1 | 8.68 |
| CHEMBL199411 | — | — | 1 | 8.43 |
| CHEMBL201472 | — | — | 1 | 8.40 |
| CHEMBL381625 | — | — | 1 | 7.85 |
| CHEMBL202070 | — | — | 1 | 7.72 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL199957 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL369902 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL427207 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL202343 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL204319 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL204696 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL204701 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL199411 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL201472 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL381625 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL202070 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL12 | DIAZEPAM | Ki | = | 33.0 | nM | 7.48 |