Assay Detail
Functional
CHEMBL837196
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In vitro concentration required to inhibit peak currents in cerebral cortical neurones of rat
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.66 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL191991 | — | — | 1 | 7.38 |
| CHEMBL192050 | — | — | 1 | 7.21 |
| CHEMBL190925 | — | — | 1 | 6.95 |
| CHEMBL382320 | — | — | 1 | 6.94 |
| CHEMBL194544 | — | — | 1 | 6.90 |
| CHEMBL371775 | — | — | 1 | 6.85 |
| CHEMBL195164 | — | — | 1 | 6.80 |
| CHEMBL193370 | — | — | 1 | 6.70 |
| CHEMBL365174 | — | — | 1 | 6.67 |
| CHEMBL366160 | — | — | 1 | 6.65 |
| CHEMBL371854 | — | — | 1 | 6.62 |
| CHEMBL303580 | GABAZINE BROMIDE | — | 1 | 6.62 |
| CHEMBL370714 | — | — | 1 | 6.48 |
| CHEMBL144718 | — | — | 1 | 6.43 |
| CHEMBL191704 | — | — | 1 | 6.42 |
| CHEMBL311761 | — | — | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL191991 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL192050 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL190925 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL382320 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL194544 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL371775 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL195164 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL193370 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL365174 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL366160 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL371854 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL303580 | GABAZINE BROMIDE | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL370714 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL144718 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL191704 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL311761 | — | IC50 | = | 11000.0 | nM | 4.96 |