Assay Detail
Functional
CHEMBL866387
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at human GABAA alpha-1-beta-3-gamma-2S expressed in Xenopus oocytes by voltage-clamp electrophysiology
19
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Oocyte |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-1/beta-3/gamma-2 (CHEMBL2094121) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.81 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL202028 | — | — | 2 | 8.92 |
| CHEMBL442789 | — | — | 2 | 8.53 |
| CHEMBL377925 | — | — | 1 | 7.70 |
| CHEMBL204017 | — | — | 2 | 7.66 |
| CHEMBL382791 | — | — | 2 | 6.64 |
| CHEMBL32503 | GABAZINE | — | 1 | 6.62 |
| CHEMBL144718 | — | — | 1 | 6.43 |
| CHEMBL203718 | — | — | 2 | 6.33 |
| CHEMBL204189 | — | — | 2 | 6.14 |
| CHEMBL204110 | — | — | 2 | 5.54 |
| CHEMBL109209 | — | — | 2 | 4.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL202028 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL202028 | — | Ki | = | 1.202 | nM | 8.92 |
| CHEMBL442789 | — | Ki | = | 2.951 | nM | 8.53 |
| CHEMBL442789 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL377925 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL204017 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL204017 | — | Ki | = | 21.88 | nM | 7.66 |
| CHEMBL382791 | — | Ki | = | 230.0 | nM | 6.64 |
| CHEMBL382791 | — | Ki | = | 229.09 | nM | 6.64 |
| CHEMBL32503 | GABAZINE | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL144718 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL203718 | — | Ki | = | 465.0 | nM | 6.33 |
| CHEMBL203718 | — | Ki | = | 467.74 | nM | 6.33 |
| CHEMBL204189 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL204189 | — | Ki | = | 724.44 | nM | 6.14 |
| CHEMBL204110 | — | Ki | = | 2880.0 | nM | 5.54 |
| CHEMBL204110 | — | Ki | = | 2884.03 | nM | 5.54 |
| CHEMBL109209 | — | Ki | = | 25703.96 | nM | 4.59 |
| CHEMBL109209 | — | Ki | = | 25704.0 | nM | 4.59 |