Assay Detail
Binding
CHEMBL5146042
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from human recombinant alpha3beta2gamma2 GABAA receptor expressed in HEK cell membrane by competitive radioligand binding assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK |
| Subcellular | Cell membrane |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA A receptor alpha-3/beta-2/gamma-2 (CHEMBL2111339) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Rationalizing the binding and α subtype selectivity of synthesized imidazodiazepines and benzodiazepines at GABAA receptors by using molecular docking studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.09 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1709464 | PHENAZEPAM | — | 1 | 9.92 |
| CHEMBL3274851 | — | — | 1 | 9.55 |
| CHEMBL1451229 | — | — | 1 | 9.22 |
| CHEMBL661 | ALPRAZOLAM | 4.0 | 1 | 8.85 |
| CHEMBL475204 | — | — | 1 | 8.72 |
| CHEMBL5192472 | — | — | 1 | 8.47 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.35 |
| CHEMBL3246831 | — | — | 1 | 8.29 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.82 |
| CHEMBL5179487 | — | — | 1 | 7.72 |
| CHEMBL5189080 | — | — | 1 | 7.68 |
| CHEMBL368768 | — | — | 1 | 7.51 |
| CHEMBL174535 | — | — | 1 | 7.32 |
| CHEMBL5198159 | — | — | 1 | 6.98 |
| CHEMBL73096 | — | — | 1 | 6.50 |
| CHEMBL13458 | RO-052921 | — | 1 | 6.46 |
| CHEMBL5195108 | — | — | 1 | - |
| CHEMBL5170217 | — | — | 1 | - |
| CHEMBL3246832 | — | — | 1 | - |
| CHEMBL5205013 | — | — | 1 | - |
| CHEMBL5179977 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1709464 | PHENAZEPAM | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL3274851 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL1451229 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL661 | ALPRAZOLAM | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL475204 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL5192472 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL13280 | FLUNITRAZEPAM | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL3246831 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL12 | DIAZEPAM | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL5179487 | — | Ki | = | 19.1 | nM | 7.72 |
| CHEMBL5189080 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL368768 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL174535 | — | Ki | = | 47.4 | nM | 7.32 |
| CHEMBL5198159 | — | Ki | = | 103.9 | nM | 6.98 |
| CHEMBL73096 | — | Ki | = | 318.0 | nM | 6.50 |
| CHEMBL13458 | RO-052921 | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL5195108 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL5170217 | — | Ki | - | — | - | |
| CHEMBL3246832 | — | Ki | - | — | - | |
| CHEMBL5205013 | — | Ki | - | — | - | |
| CHEMBL5179977 | — | Ki | - | — | - |