Assay Detail
Binding
CHEMBL999409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in HEK293 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| 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
A study of the structure-activity relationship of GABA(A)-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 6.41 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL286594 | — | — | 1 | 7.55 |
| CHEMBL449393 | — | — | 1 | 6.64 |
| CHEMBL505768 | — | — | 1 | 6.63 |
| CHEMBL522055 | — | — | 1 | 6.54 |
| CHEMBL499964 | — | — | 1 | 6.34 |
| CHEMBL443736 | — | — | 1 | 5.73 |
| CHEMBL505497 | — | — | 1 | 5.42 |
| CHEMBL35571 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL286594 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL449393 | — | Ki | = | 231.0 | nM | 6.64 |
| CHEMBL505768 | — | Ki | = | 236.0 | nM | 6.63 |
| CHEMBL522055 | — | Ki | = | 287.0 | nM | 6.54 |
| CHEMBL499964 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL443736 | — | Ki | = | 1852.0 | nM | 5.73 |
| CHEMBL505497 | — | Ki | = | 3795.0 | nM | 5.42 |
| CHEMBL35571 | — | Ki | > | 1000.0 | nM | - |