Assay Detail
Binding
CHEMBL4042549
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human GABAA alpha3beta3gamma2 receptor expressed in HEK293 cells assessed as GABA-induced membrane potential change preincubated for 3 mins followed by addition of GABA measured after 3 mins by FLIPR assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-3/beta-3/gamma-2 (CHEMBL2094120) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 6.40 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4089504 | — | — | 1 | 7.96 |
| CHEMBL514974 | — | — | 1 | 7.54 |
| CHEMBL522055 | — | — | 1 | 6.84 |
| CHEMBL4090978 | — | — | 1 | 6.49 |
| CHEMBL2332214 | — | — | 1 | 6.33 |
| CHEMBL475022 | — | — | 1 | 6.07 |
| CHEMBL4062225 | — | — | 1 | 6.03 |
| CHEMBL4071696 | — | — | 1 | 5.93 |
| CHEMBL4063081 | — | — | 1 | 5.52 |
| CHEMBL4098713 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4089504 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL514974 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL522055 | — | EC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4090978 | — | EC50 | = | 321.0 | nM | 6.49 |
| CHEMBL2332214 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL475022 | — | EC50 | = | 844.0 | nM | 6.07 |
| CHEMBL4062225 | — | EC50 | = | 937.0 | nM | 6.03 |
| CHEMBL4071696 | — | EC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL4063081 | — | EC50 | = | 3020.0 | nM | 5.52 |
| CHEMBL4098713 | — | EC50 | = | 5150.0 | nM | 5.29 |