Assay Detail
Binding
CHEMBL1687497
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flumazenil from GABAA receptor subunit alpha-1 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-1 (CHEMBL1962) ↗| 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 | 7.38 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL20042 | CGS-9896 | — | 1 | 9.00 |
| CHEMBL1681887 | — | — | 1 | 9.00 |
| CHEMBL1681889 | — | — | 1 | 7.34 |
| CHEMBL1681888 | — | — | 1 | 7.30 |
| CHEMBL1681897 | — | — | 1 | 7.30 |
| CHEMBL1681886 | — | — | 1 | 7.19 |
| CHEMBL1681895 | — | — | 1 | 7.19 |
| CHEMBL1681892 | — | — | 1 | 7.17 |
| CHEMBL1681885 | — | — | 1 | 7.13 |
| CHEMBL1681900 | — | — | 1 | 7.03 |
| CHEMBL1681899 | — | — | 1 | 6.87 |
| CHEMBL1681894 | — | — | 1 | 6.80 |
| CHEMBL1681890 | — | — | 1 | 6.62 |
| CHEMBL1681896 | — | — | 1 | - |
| CHEMBL1681893 | — | — | 1 | - |
| CHEMBL1681891 | — | — | 1 | - |
| CHEMBL1681898 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL20042 | CGS-9896 | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1681887 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1681889 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL1681888 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1681897 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1681886 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1681895 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL1681892 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1681885 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL1681900 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1681899 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL1681894 | — | IC50 | = | 157.0 | nM | 6.80 |
| CHEMBL1681890 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL1681896 | — | IC50 | - | — | - | |
| CHEMBL1681893 | — | IC50 | - | — | - | |
| CHEMBL1681891 | — | IC50 | - | — | - | |
| CHEMBL1681898 | — | IC50 | > | 3000.0 | nM | - |