Assay Detail
Functional
CHEMBL740137
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Electrophysiology using Whole-cell patch-clamp recordings in mouse embryos
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 1 — Organism |
| Curated By | Expert |
Publication
Novel class of potent 4-arylalkyl substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.01 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL544544 | — | — | 1 | 7.70 |
| CHEMBL545008 | — | — | 1 | 7.30 |
| CHEMBL303580 | GABAZINE BROMIDE | — | 1 | 6.62 |
| CHEMBL538260 | — | — | 1 | 6.43 |
| CHEMBL555167 | — | — | 1 | 6.36 |
| CHEMBL544302 | — | — | 1 | 6.32 |
| CHEMBL540042 | — | — | 1 | 6.28 |
| CHEMBL544301 | — | — | 1 | 6.15 |
| CHEMBL555181 | — | — | 1 | 6.11 |
| CHEMBL553552 | — | — | 1 | 6.09 |
| CHEMBL544776 | — | — | 1 | 6.05 |
| CHEMBL552688 | — | — | 1 | 5.96 |
| CHEMBL543603 | — | — | 1 | 5.96 |
| CHEMBL543125 | — | — | 1 | 5.89 |
| CHEMBL545238 | — | — | 1 | 5.82 |
| CHEMBL541065 | — | — | 1 | 5.52 |
| CHEMBL542896 | — | — | 1 | 5.40 |
| CHEMBL541566 | — | — | 1 | 5.39 |
| CHEMBL542665 | — | — | 1 | 5.34 |
| CHEMBL543365 | — | — | 1 | 4.99 |
| CHEMBL553129 | — | — | 1 | 4.58 |
| CHEMBL311761 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL544544 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL545008 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL303580 | GABAZINE BROMIDE | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL538260 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL555167 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL544302 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL540042 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL544301 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL555181 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL553552 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL544776 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL552688 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL543603 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL543125 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL545238 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL541065 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL542896 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL541566 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL542665 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL543365 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL553129 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL311761 | — | IC50 | = | 110000.0 | nM | - |