Assay Detail
Functional
CHEMBL682418
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Effective agonist dose for human Gamma-aminobutyric acid A receptor alpha-6-beta-3-gamma-2
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-6/beta-3/gamma-2 (CHEMBL2095190) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Bioisosteric determinants for subtype selectivity of ligands for heteromeric GABA(A) receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 8 | 5.07 | 5.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 1 | 5.82 |
| CHEMBL39071 | ISOGUVACINE | — | 1 | 4.70 |
| CHEMBL34155 | — | — | 1 | 4.70 |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | — | 1 | - |
| CHEMBL279998 | ISONIPECOTIC ACID | — | 1 | - |
| CHEMBL290961 | — | — | 1 | - |
| CHEMBL291079 | — | — | 1 | - |
| CHEMBL41065 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL34155 | — | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL784 | IMIDAZOLE ACETIC ACID | EC50 | = | 460000.0 | nM | - |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | = | 160000.0 | nM | - |
| CHEMBL290961 | — | EC50 | = | 240000.0 | nM | - |
| CHEMBL291079 | — | EC50 | = | 140000.0 | nM | - |
| CHEMBL41065 | — | EC50 | = | 3000000.0 | nM | - |