Assay Detail
Binding
CHEMBL3370253
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human GABAA rho1 expressed in tsA-201cells by FLIPR membrane potential blue assay
29
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | tsA-201 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Gamma-aminobutyric acid receptor subunit rho-1 (CHEMBL3561) ↗| Type | SINGLE PROTEIN |
| 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 | 29 | 5.67 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | 1.0 | 2 | 6.57 |
| CHEMBL273481 | MUSCIMOL | 1.0 | 2 | 6.16 |
| CHEMBL3322882 | — | — | 2 | 5.91 |
| CHEMBL3322886 | — | — | 2 | 5.80 |
| CHEMBL39071 | ISOGUVACINE | — | 2 | 4.41 |
| CHEMBL279998 | ISONIPECOTIC ACID | — | 1 | - |
| CHEMBL235168 | — | — | 1 | - |
| CHEMBL3322881 | — | — | 1 | - |
| CHEMBL3322880 | — | — | 1 | - |
| CHEMBL3322879 | — | — | 1 | - |
| CHEMBL3322878 | — | — | 1 | - |
| CHEMBL3322877 | — | — | 2 | - |
| CHEMBL3322876 | — | — | 2 | - |
| CHEMBL3322875 | — | — | 1 | - |
| CHEMBL3322874 | — | — | 1 | - |
| CHEMBL3322873 | — | — | 1 | - |
| CHEMBL3322872 | — | — | 2 | - |
| CHEMBL3322871 | — | — | 2 | - |
| CHEMBL3322870 | — | — | 1 | - |
| CHEMBL3322864 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 269.15 | nM | 6.57 |
| CHEMBL96 | GAMMA-AMINOBUTYRIC ACID | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL273481 | MUSCIMOL | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL273481 | MUSCIMOL | EC50 | = | 691.83 | nM | 6.16 |
| CHEMBL3322882 | — | EC50 | = | 1230.27 | nM | 5.91 |
| CHEMBL3322886 | — | EC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL3322882 | — | EC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL3322886 | — | EC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 38904.51 | nM | 4.41 |
| CHEMBL39071 | ISOGUVACINE | EC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL3322872 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322873 | — | EC50 | - | — | - | |
| CHEMBL3322874 | — | EC50 | - | — | - | |
| CHEMBL3322875 | — | EC50 | - | — | - | |
| CHEMBL3322876 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322877 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322878 | — | EC50 | - | — | - | |
| CHEMBL3322879 | — | EC50 | - | — | - | |
| CHEMBL3322880 | — | EC50 | - | — | - | |
| CHEMBL3322881 | — | EC50 | - | — | - | |
| CHEMBL3322871 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322870 | — | EC50 | - | — | - | |
| CHEMBL3322864 | — | EC50 | - | — | - | |
| CHEMBL3322871 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322872 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322876 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL3322877 | — | EC50 | > | 1000000.0 | nM | - |
| CHEMBL279998 | ISONIPECOTIC ACID | EC50 | - | — | - | |
| CHEMBL235168 | — | EC50 | - | — | - |