Assay Detail
Binding
CHEMBL3370251
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GABAAalpha1beta2gamma2S receptor expressed in tsA-201cells by FLIPR membrane potential blue assay
36
Total Activities
24
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-1/beta-2/gamma-2 (CHEMBL2095172) ↗| 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 | 36 | 5.48 | 6.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | 1.0 | 2 | 6.27 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 5.75 |
| CHEMBL3322882 | — | — | 2 | 5.58 |
| CHEMBL39071 | ISOGUVACINE | — | 2 | 4.96 |
| CHEMBL3322886 | — | — | 2 | 4.85 |
| CHEMBL3322871 | — | — | 2 | - |
| CHEMBL3322872 | — | — | 2 | - |
| CHEMBL3322873 | — | — | 1 | - |
| CHEMBL3322874 | — | — | 1 | - |
| CHEMBL3322875 | — | — | 2 | - |
| CHEMBL3322876 | — | — | 2 | - |
| CHEMBL3322877 | — | — | 2 | - |
| CHEMBL3322878 | — | — | 1 | - |
| CHEMBL3322870 | — | — | 1 | - |
| CHEMBL3322880 | — | — | 1 | - |
| CHEMBL3322881 | — | — | 1 | - |
| CHEMBL235168 | — | — | 1 | - |
| CHEMBL3322864 | — | — | 2 | - |
| CHEMBL3322883 | — | — | 2 | - |
| CHEMBL247316 | — | — | 1 | - |
| CHEMBL3322884 | — | — | 1 | - |
| CHEMBL3322885 | — | — | 1 | - |
| CHEMBL279998 | ISONIPECOTIC ACID | — | 1 | - |
| CHEMBL3322879 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273481 | MUSCIMOL | EC50 | = | 537.03 | nM | 6.27 |
| CHEMBL273481 | MUSCIMOL | EC50 | = | 540.0 | nM | 6.27 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 1778.28 | nM | 5.75 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL3322882 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3322882 | — | EC50 | = | 2630.27 | nM | 5.58 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL3322886 | — | EC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL3322886 | — | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3322883 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322872 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322870 | — | EC50 | - | — | - | |
| CHEMBL235168 | — | EC50 | - | — | - | |
| CHEMBL3322881 | — | EC50 | - | — | - | |
| CHEMBL3322880 | — | EC50 | - | — | - | |
| CHEMBL3322879 | — | EC50 | - | — | - | |
| CHEMBL3322878 | — | EC50 | - | — | - | |
| CHEMBL3322877 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322876 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322875 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322874 | — | EC50 | - | — | - | |
| CHEMBL3322873 | — | EC50 | - | — | - | |
| CHEMBL247316 | — | EC50 | - | — | - | |
| CHEMBL3322871 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322885 | — | EC50 | - | — | - | |
| CHEMBL3322864 | — | EC50 | > | 300000.0 | nM | - |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | - | — | - | |
| CHEMBL3322864 | — | EC50 | > | 316227.77 | nM | - |
| CHEMBL3322871 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322872 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322875 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322876 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322877 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322883 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322884 | — | EC50 | - | — | - |