Assay Detail
Binding
CHEMBL681483
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Inhibition of [3H]Ro-151788 binding to human GABA A receptor (alpha-5-beta-3-gamma-2) stably expressed in L(tk-) cells.
19
Total Activities
19
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-5/beta-3/gamma-2 (CHEMBL2094122) ↗| 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 | 19 | 6.75 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL17468 | — | — | 1 | 9.00 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.50 |
| CHEMBL56098 | — | — | 1 | 6.48 |
| CHEMBL55022 | — | — | 1 | 6.46 |
| CHEMBL55565 | — | — | 1 | 6.42 |
| CHEMBL301195 | — | — | 1 | 6.41 |
| CHEMBL413325 | — | — | 1 | 6.41 |
| CHEMBL59197 | — | — | 1 | 6.35 |
| CHEMBL299061 | — | — | 1 | - |
| CHEMBL55694 | — | — | 1 | - |
| CHEMBL298732 | — | — | 1 | - |
| CHEMBL56761 | — | — | 1 | - |
| CHEMBL291308 | — | — | 1 | - |
| CHEMBL54507 | — | — | 1 | - |
| CHEMBL264235 | — | — | 1 | - |
| CHEMBL291335 | — | — | 1 | - |
| CHEMBL53619 | — | — | 1 | - |
| CHEMBL54422 | — | — | 1 | - |
| CHEMBL56746 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL17468 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL451 | CHLORDIAZEPOXIDE | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL56098 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL55022 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL55565 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL301195 | — | Ki | = | 393.0 | nM | 6.41 |
| CHEMBL413325 | — | Ki | = | 390.0 | nM | 6.41 |
| CHEMBL59197 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL299061 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL55694 | — | Ki | > | 667.0 | nM | - |
| CHEMBL298732 | — | Ki | > | 667.0 | nM | - |
| CHEMBL56761 | — | Ki | > | 667.0 | nM | - |
| CHEMBL291308 | — | Ki | > | 667.0 | nM | - |
| CHEMBL54507 | — | Ki | > | 667.0 | nM | - |
| CHEMBL264235 | — | Ki | > | 667.0 | nM | - |
| CHEMBL291335 | — | Ki | > | 667.0 | nM | - |
| CHEMBL53619 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL54422 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL56746 | — | Ki | > | 667.0 | nM | - |