Assay Detail
Binding
CHEMBL681637
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Inhibition of [3H]Ro-151788 binding to human GABA A receptor (alpha-1-beta-3-gamma-2) stably expressed in L(tk-) cells.
22
Total Activities
22
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-1/beta-3/gamma-2 (CHEMBL2094121) ↗| 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 | 22 | 7.02 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17468 | — | — | 1 | 8.24 |
| CHEMBL55565 | — | — | 1 | 7.89 |
| CHEMBL264235 | — | — | 1 | 7.89 |
| CHEMBL56098 | — | — | 1 | 7.77 |
| CHEMBL294600 | — | — | 1 | 7.77 |
| CHEMBL55022 | — | — | 1 | 7.52 |
| CHEMBL54422 | — | — | 1 | 7.51 |
| CHEMBL59197 | — | — | 1 | 7.41 |
| CHEMBL54368 | — | — | 1 | 7.39 |
| CHEMBL59478 | — | — | 1 | 7.35 |
| CHEMBL53619 | — | — | 1 | 7.08 |
| CHEMBL56761 | — | — | 1 | 7.05 |
| CHEMBL55467 | — | — | 1 | 6.58 |
| CHEMBL55570 | — | — | 1 | 6.51 |
| CHEMBL299061 | — | — | 1 | 6.48 |
| CHEMBL58927 | — | — | 1 | 6.28 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.25 |
| CHEMBL298732 | — | — | 1 | 6.20 |
| CHEMBL413325 | — | — | 1 | 5.99 |
| CHEMBL301010 | — | — | 1 | 5.16 |
| CHEMBL54507 | — | — | 1 | - |
| CHEMBL55694 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17468 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL55565 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL264235 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL56098 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL294600 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL55022 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL54422 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL59197 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL54368 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL59478 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL53619 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL56761 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL55467 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL55570 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL299061 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL58927 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 560.0 | nM | 6.25 |
| CHEMBL298732 | — | Ki | = | 630.0 | nM | 6.20 |
| CHEMBL413325 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL301010 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL54507 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL55694 | — | Ki | > | 30000.0 | nM | - |