Assay Detail
Binding
CHEMBL3370496
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GABAAalpha5beta2gamma2S 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 | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 6.43 | 7.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | 1.0 | 2 | 7.27 |
| CHEMBL3322882 | — | — | 2 | 7.04 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 6.97 |
| CHEMBL39071 | ISOGUVACINE | — | 2 | 6.11 |
| CHEMBL3322886 | — | — | 2 | 5.68 |
| CHEMBL279998 | ISONIPECOTIC ACID | — | 2 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL273481 | MUSCIMOL | EC50 | = | 53.7 | nM | 7.27 |
| CHEMBL3322882 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3322882 | — | EC50 | = | 91.2 | nM | 7.04 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 107.15 | nM | 6.97 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 780.0 | nM | 6.11 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 794.33 | nM | 6.10 |
| CHEMBL3322886 | — | EC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3322886 | — | EC50 | = | 2089.3 | nM | 5.68 |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | = | 2884.03 | nM | 5.54 |