Assay Detail
Binding
CHEMBL680430
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-3-beta-3-gamma-2 expressed in L(tk) cells by [3H]Ro-151788 displacement.
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-3/beta-3/gamma-2 (CHEMBL2094120) ↗| 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 | 19 | 8.48 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL44533 | — | — | 1 | 9.40 |
| CHEMBL295027 | — | — | 1 | 9.40 |
| CHEMBL45198 | — | — | 1 | 9.30 |
| CHEMBL45110 | — | — | 1 | 8.92 |
| CHEMBL43876 | — | — | 1 | 8.62 |
| CHEMBL46567 | — | — | 1 | 8.52 |
| CHEMBL47295 | — | — | 1 | 8.52 |
| CHEMBL44320 | — | — | 1 | 8.51 |
| CHEMBL44916 | — | — | 1 | 8.51 |
| CHEMBL296105 | — | — | 1 | 8.38 |
| CHEMBL44065 | — | — | 1 | 8.36 |
| CHEMBL44428 | — | — | 1 | 8.30 |
| CHEMBL44963 | — | — | 1 | 8.07 |
| CHEMBL297873 | — | — | 1 | 8.05 |
| CHEMBL44985 | — | — | 1 | 7.78 |
| CHEMBL297370 | — | — | 1 | 7.76 |
| CHEMBL48782 | — | — | 1 | 7.70 |
| CHEMBL416625 | — | — | 1 | - |
| CHEMBL294990 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL44533 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL295027 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL45198 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL45110 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL43876 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL46567 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL47295 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL44320 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL44916 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL296105 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL44065 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL44428 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL44963 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL297873 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL44985 | — | Ki | = | 16.8 | nM | 7.78 |
| CHEMBL297370 | — | Ki | = | 17.3 | nM | 7.76 |
| CHEMBL48782 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL416625 | — | Ki | > | 33.0 | nM | - |
| CHEMBL294990 | — | Ki | > | 33.0 | nM | - |