Assay Detail
Binding
CHEMBL682708
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Binding affinity evaluated by ability to displace [3H]-Ro-15-1788 from recombinant human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-)cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-2/beta-3/gamma-2 (CHEMBL2094130) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
N-(indol-3-ylglyoxylyl)piperidines: high affinity agonists of human GABA-A receptors containing the alpha1 subunit.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 6.86 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13280 | FLUNITRAZEPAM | 4.0 | 1 | 8.96 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.18 |
| CHEMBL28730 | — | — | 1 | 7.72 |
| CHEMBL285328 | — | — | 1 | 7.66 |
| CHEMBL27794 | — | — | 1 | 7.40 |
| CHEMBL282740 | — | — | 1 | 6.75 |
| CHEMBL284418 | — | — | 1 | 6.70 |
| CHEMBL28782 | — | — | 1 | 6.60 |
| CHEMBL281480 | — | — | 1 | 6.57 |
| CHEMBL286471 | — | — | 1 | 6.41 |
| CHEMBL282623 | — | — | 1 | 6.37 |
| CHEMBL29277 | — | — | 1 | 6.36 |
| CHEMBL29213 | — | — | 1 | 6.17 |
| CHEMBL283850 | — | — | 1 | 6.08 |
| CHEMBL287442 | — | — | 1 | 6.01 |
| CHEMBL31796 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13280 | FLUNITRAZEPAM | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL12 | DIAZEPAM | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL28730 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL285328 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL27794 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL282740 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL284418 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL28782 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL281480 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL286471 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL282623 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL29277 | — | Ki | = | 440.0 | nM | 6.36 |
| CHEMBL29213 | — | Ki | = | 680.0 | nM | 6.17 |
| CHEMBL283850 | — | Ki | = | 830.0 | nM | 6.08 |
| CHEMBL287442 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL31796 | — | Ki | = | 1300.0 | nM | 5.89 |