Assay Detail
Binding
CHEMBL4403720
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Binding affinity to GABA-A alpha5 (unknown origin)
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit alpha-5 (CHEMBL5112) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Subtype Selective γ-Aminobutyric Acid Type A Receptor (GABA<sub>A</sub>R) Modulators Acting at the Benzodiazepine Binding Site: An Update.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.76 | 9.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL306422 | — | — | 1 | 9.18 |
| CHEMBL204696 | — | — | 1 | 8.96 |
| CHEMBL363211 | — | — | 1 | 8.85 |
| CHEMBL1077391 | — | — | 1 | 8.70 |
| CHEMBL1080588 | — | — | 1 | 8.34 |
| CHEMBL3681419 | BASMISANIL | 2.0 | 1 | 8.33 |
| CHEMBL45346 | — | — | 1 | 8.22 |
| CHEMBL4581355 | — | — | 1 | 8.10 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.82 |
| CHEMBL4228824 | — | — | 1 | 7.26 |
| CHEMBL4553352 | — | — | 1 | 7.10 |
| CHEMBL1783282 | AZD7325 | 2.0 | 1 | 6.64 |
| CHEMBL1783256 | AZD6280 | 1.0 | 1 | 5.78 |
| CHEMBL4537552 | — | — | 1 | 5.30 |
| CHEMBL4441634 | — | — | 1 | - |
| CHEMBL4537371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL306422 | — | Ki | = | 0.66 | nM | 9.18 |
| CHEMBL204696 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL363211 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1077391 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1080588 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL3681419 | BASMISANIL | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL45346 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4581355 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL12 | DIAZEPAM | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4228824 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL4553352 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL1783282 | AZD7325 | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL1783256 | AZD6280 | Ki | = | 1680.0 | nM | 5.78 |
| CHEMBL4537552 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL4441634 | — | Ki | - | — | - | |
| CHEMBL4537371 | — | Ki | - | — | - |