Assay Detail
Binding
CHEMBL4403718
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Binding affinity to GABA-A alpha1 (unknown origin)
18
Total Activities
18
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-1 (CHEMBL1962) ↗| 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 | 18 | 7.44 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783282 | AZD7325 | 2.0 | 1 | 9.30 |
| CHEMBL1783256 | AZD6280 | 1.0 | 1 | 9.30 |
| CHEMBL204696 | — | — | 1 | 9.14 |
| CHEMBL363211 | — | — | 1 | 9.08 |
| CHEMBL306422 | — | — | 1 | 9.06 |
| CHEMBL1077391 | — | — | 1 | 7.82 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.80 |
| CHEMBL52030 | — | — | 1 | 7.77 |
| CHEMBL178942 | — | — | 1 | 7.15 |
| CHEMBL4581355 | — | — | 1 | 6.85 |
| CHEMBL1080588 | — | — | 1 | 6.76 |
| CHEMBL45346 | — | — | 1 | 6.44 |
| CHEMBL4553352 | — | — | 1 | 6.27 |
| CHEMBL4228824 | — | — | 1 | 6.07 |
| CHEMBL3681419 | BASMISANIL | 2.0 | 1 | 6.01 |
| CHEMBL4537552 | — | — | 1 | 4.26 |
| CHEMBL4537371 | — | — | 1 | - |
| CHEMBL4441634 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783282 | AZD7325 | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL1783256 | AZD6280 | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL204696 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL363211 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL306422 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL1077391 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL12 | DIAZEPAM | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL52030 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL178942 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL4581355 | — | Ki | = | 140.0 | nM | 6.85 |
| CHEMBL1080588 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL45346 | — | Ki | = | 362.0 | nM | 6.44 |
| CHEMBL4553352 | — | Ki | = | 542.0 | nM | 6.27 |
| CHEMBL4228824 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL3681419 | BASMISANIL | Ki | = | 985.0 | nM | 6.01 |
| CHEMBL4537552 | — | Ki | = | 55000.0 | nM | 4.26 |
| CHEMBL4537371 | — | Ki | - | — | - | |
| CHEMBL4441634 | — | Ki | - | — | - |