Assay Detail
Binding
CHEMBL677033
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at human recombinant gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 expressed in L(tk) cells by [3H]Ro-151788 displacement.
17
Total Activities
17
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
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 17 | 8.28 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL44533 | — | — | 1 | 9.15 |
| CHEMBL45198 | — | — | 1 | 8.89 |
| CHEMBL45110 | — | — | 1 | 8.82 |
| CHEMBL44065 | — | — | 1 | 8.41 |
| CHEMBL47295 | — | — | 1 | 8.40 |
| CHEMBL44320 | — | — | 1 | 8.34 |
| CHEMBL46567 | — | — | 1 | 8.30 |
| CHEMBL43876 | — | — | 1 | 8.28 |
| CHEMBL44916 | — | — | 1 | 8.27 |
| CHEMBL296105 | — | — | 1 | 8.11 |
| CHEMBL44428 | — | — | 1 | 8.08 |
| CHEMBL48782 | — | — | 1 | 8.00 |
| CHEMBL44963 | — | — | 1 | 7.91 |
| CHEMBL297873 | — | — | 1 | 7.68 |
| CHEMBL297370 | — | — | 1 | 7.58 |
| CHEMBL416625 | — | — | 1 | - |
| CHEMBL294990 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL44533 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL45198 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL45110 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL44065 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL47295 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL44320 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL46567 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL43876 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL44916 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL296105 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL44428 | — | Ki | = | 8.3 | nM | 8.08 |
| CHEMBL48782 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL44963 | — | Ki | = | 12.2 | nM | 7.91 |
| CHEMBL297873 | — | Ki | = | 21.1 | nM | 7.68 |
| CHEMBL297370 | — | Ki | = | 26.1 | nM | 7.58 |
| CHEMBL416625 | — | Ki | > | 33.0 | nM | - |
| CHEMBL294990 | — | Ki | > | 33.0 | nM | - |