Assay Detail
Binding
CHEMBL4403717
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Binding affinity to GABA-A alpha2 (unknown origin)
28
Total Activities
26
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-2 (CHEMBL4956) ↗| 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 | 28 | 7.66 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783282 | AZD7325 | 2.0 | 2 | 9.52 |
| CHEMBL306422 | — | — | 1 | 9.24 |
| CHEMBL363211 | — | — | 1 | 9.07 |
| CHEMBL204696 | — | — | 1 | 8.70 |
| CHEMBL1783280 | — | — | 1 | 8.65 |
| CHEMBL1783256 | AZD6280 | 1.0 | 2 | 8.30 |
| CHEMBL1783247 | — | — | 1 | 8.26 |
| CHEMBL1783281 | — | — | 1 | 8.21 |
| CHEMBL1783279 | — | — | 1 | 8.13 |
| CHEMBL1783253 | — | — | 1 | 8.00 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.77 |
| CHEMBL52030 | — | — | 1 | 7.77 |
| CHEMBL1077391 | — | — | 1 | 7.62 |
| CHEMBL178942 | — | — | 1 | 7.58 |
| CHEMBL1783257 | — | — | 1 | 7.58 |
| CHEMBL1783258 | — | — | 1 | 7.53 |
| CHEMBL4581355 | — | — | 1 | 7.50 |
| CHEMBL1783259 | — | — | 1 | 7.25 |
| CHEMBL45346 | — | — | 1 | 6.75 |
| CHEMBL1080588 | — | — | 1 | 6.73 |
| CHEMBL4228824 | — | — | 1 | 6.44 |
| CHEMBL3681419 | BASMISANIL | 2.0 | 1 | 6.30 |
| CHEMBL4553352 | — | — | 1 | 6.10 |
| CHEMBL4537371 | — | — | 1 | 6.00 |
| CHEMBL4537552 | — | — | 1 | 4.52 |
| CHEMBL4441634 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783282 | AZD7325 | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1783282 | AZD7325 | Ki | = | 0.309 | nM | 9.51 |
| CHEMBL306422 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL363211 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL204696 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1783280 | — | Ki | = | 2.239 | nM | 8.65 |
| CHEMBL1783256 | AZD6280 | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1783247 | — | Ki | = | 5.495 | nM | 8.26 |
| CHEMBL1783281 | — | Ki | = | 6.166 | nM | 8.21 |
| CHEMBL1783279 | — | Ki | = | 7.413 | nM | 8.13 |
| CHEMBL1783253 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1783256 | AZD6280 | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL52030 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL12 | DIAZEPAM | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL1077391 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL178942 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL1783257 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL1783258 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL4581355 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL1783259 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL45346 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL1080588 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL4228824 | — | Ki | = | 360.0 | nM | 6.44 |
| CHEMBL3681419 | BASMISANIL | Ki | = | 502.0 | nM | 6.30 |
| CHEMBL4553352 | — | Ki | = | 789.0 | nM | 6.10 |
| CHEMBL4537371 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4537552 | — | Ki | = | 30000.0 | nM | 4.52 |
| CHEMBL4441634 | — | Ki | - | — | - |