Assay Detail
Binding
CHEMBL1687498
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flumazenil from GABAA receptor subunit alpha-2 expressed in CHO cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-2 (CHEMBL4956) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.84 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1681887 | — | — | 1 | 8.70 |
| CHEMBL20042 | CGS-9896 | — | 1 | 8.40 |
| CHEMBL1681897 | — | — | 1 | 7.24 |
| CHEMBL1681888 | — | — | 1 | 6.81 |
| CHEMBL1681895 | — | — | 1 | 6.81 |
| CHEMBL1681894 | — | — | 1 | 6.75 |
| CHEMBL1681900 | — | — | 1 | 6.73 |
| CHEMBL1681892 | — | — | 1 | 6.67 |
| CHEMBL1681886 | — | — | 1 | 6.58 |
| CHEMBL1681889 | — | — | 1 | 6.57 |
| CHEMBL1681891 | — | — | 1 | 6.34 |
| CHEMBL1681885 | — | — | 1 | 6.33 |
| CHEMBL1681890 | — | — | 1 | 6.22 |
| CHEMBL1681899 | — | — | 1 | 5.67 |
| CHEMBL1681896 | — | — | 1 | - |
| CHEMBL1681898 | — | — | 1 | - |
| CHEMBL1681893 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1681887 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL20042 | CGS-9896 | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1681897 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL1681888 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL1681895 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL1681894 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL1681900 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL1681892 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL1681886 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL1681889 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL1681891 | — | IC50 | = | 461.0 | nM | 6.34 |
| CHEMBL1681885 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL1681890 | — | IC50 | = | 605.0 | nM | 6.22 |
| CHEMBL1681899 | — | IC50 | = | 2114.0 | nM | 5.67 |
| CHEMBL1681896 | — | IC50 | - | — | - | |
| CHEMBL1681898 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL1681893 | — | IC50 | - | — | - |