Assay Detail
Binding
CHEMBL681481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro-151788 from human GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in L(tk-) cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| 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 | 4 | 6.20 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL294600 | — | — | 1 | 6.50 |
| CHEMBL55467 | — | — | 1 | 5.89 |
| CHEMBL55777 | — | — | 1 | - |
| CHEMBL59478 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL294600 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL55467 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL55777 | — | Ki | > | 667.0 | nM | - |
| CHEMBL59478 | — | Ki | > | 1000.0 | nM | - |