Assay Detail
Binding
CHEMBL3370257
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GABAAalpha2beta2gamma2S 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-2/beta-2/gamma-2 (CHEMBL2111413) ↗| 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 | 5.61 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | 1.0 | 2 | 6.39 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 6.19 |
| CHEMBL3322882 | — | — | 2 | 6.09 |
| CHEMBL39071 | ISOGUVACINE | — | 2 | 5.35 |
| CHEMBL3322886 | — | — | 2 | 5.03 |
| CHEMBL279998 | ISONIPECOTIC ACID | — | 2 | 4.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL273481 | MUSCIMOL | EC50 | = | 407.38 | nM | 6.39 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 660.69 | nM | 6.18 |
| CHEMBL3322882 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL3322882 | — | EC50 | = | 831.76 | nM | 6.08 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 4466.84 | nM | 5.35 |
| CHEMBL3322886 | — | EC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3322886 | — | EC50 | = | 9332.54 | nM | 5.03 |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | = | 23988.33 | nM | 4.62 |