Assay Detail
Functional
CHEMBL917169
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human GABAA alpha-1-beta-3-gamma-2S expressed in Xenopus oocytes by two-electrode voltage-clamp electrophysiology
33
Total Activities
20
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
4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.05 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1202309 | — | — | 2 | 8.10 |
| CHEMBL1202310 | — | — | 2 | 8.05 |
| CHEMBL1204123 | — | — | 2 | 8.02 |
| CHEMBL373716 | — | — | 1 | 7.38 |
| CHEMBL1202300 | — | — | 2 | 7.32 |
| CHEMBL1202304 | — | — | 2 | 7.23 |
| CHEMBL1202302 | — | — | 2 | 7.17 |
| CHEMBL1202308 | — | — | 2 | 7.15 |
| CHEMBL1202306 | — | — | 2 | 7.12 |
| CHEMBL1202299 | — | — | 2 | 6.89 |
| CHEMBL1202303 | — | — | 2 | 6.86 |
| CHEMBL382320 | — | — | 1 | 6.85 |
| CHEMBL195164 | — | — | 1 | 6.80 |
| CHEMBL193370 | — | — | 1 | 6.70 |
| CHEMBL1202301 | — | — | 2 | 6.69 |
| CHEMBL1202307 | — | — | 2 | 6.59 |
| CHEMBL370714 | — | — | 1 | 6.48 |
| CHEMBL144718 | — | — | 1 | 6.43 |
| CHEMBL1202305 | — | — | 2 | 6.37 |
| CHEMBL311761 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1202309 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1202309 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1202310 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1202310 | — | Ki | = | 9.12 | nM | 8.04 |
| CHEMBL1204123 | — | Ki | = | 9.55 | nM | 8.02 |
| CHEMBL1204123 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL373716 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL1202300 | — | Ki | = | 47.86 | nM | 7.32 |
| CHEMBL1202300 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL1202304 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL1202304 | — | Ki | = | 58.88 | nM | 7.23 |
| CHEMBL1202302 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL1202302 | — | Ki | = | 67.61 | nM | 7.17 |
| CHEMBL1202308 | — | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL1202308 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL1202306 | — | Ki | = | 75.86 | nM | 7.12 |
| CHEMBL1202306 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL1202299 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL1202299 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL1202303 | — | Ki | = | 138.04 | nM | 6.86 |
| CHEMBL1202303 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL382320 | — | Ki | = | 141.0 | nM | 6.85 |
| CHEMBL195164 | — | Ki | = | 159.0 | nM | 6.80 |
| CHEMBL193370 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL1202301 | — | Ki | = | 204.17 | nM | 6.69 |
| CHEMBL1202301 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL1202307 | — | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL1202307 | — | Ki | = | 257.0 | nM | 6.59 |
| CHEMBL370714 | — | Ki | = | 334.0 | nM | 6.48 |
| CHEMBL144718 | — | Ki | = | 370.0 | nM | 6.43 |
| CHEMBL1202305 | — | Ki | = | 427.0 | nM | 6.37 |
| CHEMBL1202305 | — | Ki | = | 478.63 | nM | 6.32 |
| CHEMBL311761 | — | Ki | = | 11000.0 | nM | 4.96 |