Assay Detail
Functional
CHEMBL681267
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Gamma-aminobutyric acid A (GABA-A) receptor in vitro by whole-cell patch-clamp recording in cultured cerebral cortical neurones
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.71 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL32503 | GABAZINE | — | 1 | 6.62 |
| CHEMBL144718 | — | — | 1 | 6.43 |
| CHEMBL143979 | — | — | 1 | 6.05 |
| CHEMBL359417 | — | — | 1 | 5.89 |
| CHEMBL144364 | — | — | 1 | 5.40 |
| CHEMBL143993 | — | — | 1 | 4.99 |
| CHEMBL144416 | — | — | 1 | 4.58 |
| CHEMBL311761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL32503 | GABAZINE | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL144718 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL143979 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL359417 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL144364 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL143993 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL144416 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL311761 | — | IC50 | = | 110000.0 | nM | - |