Assay Detail
Binding
CHEMBL3370259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GABAAalpha3beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay
12
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | tsA-201 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA A receptor alpha-3/beta-2/gamma-2 (CHEMBL2111339) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.57 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | 1.0 | 2 | 6.68 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 6.04 |
| CHEMBL3322882 | — | — | 2 | 5.98 |
| CHEMBL39071 | ISOGUVACINE | — | 2 | 5.25 |
| CHEMBL279998 | ISONIPECOTIC ACID | — | 2 | 4.77 |
| CHEMBL3322886 | — | — | 2 | 4.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL273481 | MUSCIMOL | EC50 | = | 213.8 | nM | 6.67 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 912.01 | nM | 6.04 |
| CHEMBL3322882 | — | EC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL3322882 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 5623.41 | nM | 5.25 |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | = | 16982.44 | nM | 4.77 |
| CHEMBL3322886 | — | EC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL3322886 | — | EC50 | = | 19498.45 | nM | 4.71 |