Assay Detail
Binding
CHEMBL681249
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro-151788 from human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 stably expressed in L(tk-) cells
24
Total Activities
24
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
3-Heteroaryl-2-pyridones: benzodiazepine site ligands with functional delectivity for alpha 2/alpha 3-subtypes of human GABA(A) receptor-ion channels.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.08 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL264235 | — | — | 1 | 8.30 |
| CHEMBL56098 | — | — | 1 | 8.18 |
| CHEMBL55565 | — | — | 1 | 8.10 |
| CHEMBL17468 | — | — | 1 | 8.08 |
| CHEMBL294600 | — | — | 1 | 8.07 |
| CHEMBL55022 | — | — | 1 | 7.64 |
| CHEMBL54422 | — | — | 1 | 7.62 |
| CHEMBL59478 | — | — | 1 | 7.43 |
| CHEMBL56761 | — | — | 1 | 7.38 |
| CHEMBL59197 | — | — | 1 | 7.29 |
| CHEMBL291335 | — | — | 1 | 7.12 |
| CHEMBL53619 | — | — | 1 | 6.89 |
| CHEMBL55570 | — | — | 1 | 6.62 |
| CHEMBL413325 | — | — | 1 | 6.50 |
| CHEMBL301195 | — | — | 1 | 6.47 |
| CHEMBL299061 | — | — | 1 | 6.42 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.34 |
| CHEMBL298732 | — | — | 1 | 6.33 |
| CHEMBL56746 | — | — | 1 | 6.22 |
| CHEMBL55467 | — | — | 1 | 5.96 |
| CHEMBL301010 | — | — | 1 | 5.75 |
| CHEMBL54507 | — | — | 1 | - |
| CHEMBL291308 | — | — | 1 | - |
| CHEMBL55694 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL264235 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL56098 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL55565 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL17468 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL294600 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL55022 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL54422 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL59478 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL56761 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL59197 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL291335 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL53619 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL55570 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL413325 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL301195 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL299061 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL298732 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL56746 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL55467 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL301010 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL54507 | — | Ki | > | 667.0 | nM | - |
| CHEMBL291308 | — | Ki | > | 30000.0 | nM | - |
| CHEMBL55694 | — | Ki | > | 30000.0 | nM | - |