Assay Detail
Binding
CHEMBL5146041
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from human recombinant alpha2beta2gamma2 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-2/beta-2/gamma-2 (CHEMBL2111413) ↗| 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 | 8.33 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1709464 | PHENAZEPAM | — | 1 | 10.22 |
| CHEMBL3274851 | — | — | 1 | 9.82 |
| CHEMBL475204 | — | — | 1 | 9.22 |
| CHEMBL661 | ALPRAZOLAM | 4.0 | 1 | 9.22 |
| CHEMBL3246832 | — | — | 1 | 9.15 |
| CHEMBL1451229 | — | — | 1 | 9.00 |
| CHEMBL5170217 | — | — | 1 | 9.00 |
| CHEMBL5192472 | — | — | 1 | 8.92 |
| CHEMBL5179977 | — | — | 1 | 8.68 |
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.60 |
| CHEMBL3246831 | — | — | 1 | 8.21 |
| CHEMBL368768 | — | — | 1 | 8.03 |
| CHEMBL5179487 | — | — | 1 | 7.96 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.70 |
| CHEMBL5205013 | — | — | 1 | 7.59 |
| CHEMBL174535 | — | — | 1 | 7.38 |
| CHEMBL5189080 | — | — | 1 | 7.30 |
| CHEMBL5198159 | — | — | 1 | 7.09 |
| CHEMBL73096 | — | — | 1 | 6.86 |
| CHEMBL13458 | RO-052921 | — | 1 | 6.63 |
| CHEMBL5195108 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1709464 | PHENAZEPAM | Ki | = | 0.06 | nM | 10.22 |
| CHEMBL3274851 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL475204 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL661 | ALPRAZOLAM | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3246832 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL1451229 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL5170217 | — | Ki | = | 0.99 | nM | 9.00 |
| CHEMBL5192472 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL5179977 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL13280 | FLUNITRAZEPAM | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL3246831 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL368768 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL5179487 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL12 | DIAZEPAM | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL5205013 | — | Ki | = | 25.8 | nM | 7.59 |
| CHEMBL174535 | — | Ki | = | 42.1 | nM | 7.38 |
| CHEMBL5189080 | — | Ki | = | 50.1 | nM | 7.30 |
| CHEMBL5198159 | — | Ki | = | 81.3 | nM | 7.09 |
| CHEMBL73096 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL13458 | RO-052921 | Ki | = | 233.0 | nM | 6.63 |
| CHEMBL5195108 | — | Ki | > | 3000.0 | nM | - |