Assay Detail
Binding
CHEMBL919087
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in L(tk-) cells
10
Total Activities
10
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
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.69 | 9.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL375742 | — | — | 1 | 9.64 |
| CHEMBL200177 | MK-0777 | 2.0 | 1 | 9.57 |
| CHEMBL225631 | — | — | 1 | 9.44 |
| CHEMBL224561 | — | — | 1 | 9.42 |
| CHEMBL224175 | — | — | 1 | 9.11 |
| CHEMBL224134 | — | — | 1 | 8.96 |
| CHEMBL224608 | — | — | 1 | 8.21 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.85 |
| CHEMBL911 | ZOLPIDEM | 4.0 | 1 | 7.57 |
| CHEMBL178942 | — | — | 1 | 7.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL375742 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL200177 | MK-0777 | Ki | = | 0.27 | nM | 9.57 |
| CHEMBL225631 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL224561 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL224175 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL224134 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL224608 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL12 | DIAZEPAM | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL911 | ZOLPIDEM | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL178942 | — | Ki | = | 71.0 | nM | 7.15 |