Assay Detail
Binding
CHEMBL2186540
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]Ro151788 from GABA(A)/BzR in bovine cerebral cortex membrane
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Development of ligands at γ-aminobutyrric acid type A (GABAA) receptor subtype as new agents for pain relief.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.44 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181572 | — | — | 1 | 9.96 |
| CHEMBL2177149 | — | — | 1 | 9.86 |
| CHEMBL2181573 | — | — | 1 | 9.15 |
| CHEMBL2181584 | — | — | 1 | 9.11 |
| CHEMBL2181576 | — | — | 1 | 8.99 |
| CHEMBL2181579 | — | — | 1 | 8.80 |
| CHEMBL2181574 | — | — | 1 | 8.61 |
| CHEMBL2181582 | — | — | 1 | 8.59 |
| CHEMBL2181583 | — | — | 1 | 8.56 |
| CHEMBL2181580 | — | — | 1 | 8.52 |
| CHEMBL2181578 | — | — | 1 | 8.33 |
| CHEMBL421983 | — | — | 1 | 8.17 |
| CHEMBL2181575 | — | — | 1 | 7.83 |
| CHEMBL2181571 | — | — | 1 | 7.64 |
| CHEMBL2181581 | — | — | 1 | 6.44 |
| CHEMBL2181577 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181572 | — | Ki | = | 0.109 | nM | 9.96 |
| CHEMBL2177149 | — | Ki | = | 0.138 | nM | 9.86 |
| CHEMBL2181573 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL2181584 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL2181576 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL2181579 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2181574 | — | Ki | = | 2.44 | nM | 8.61 |
| CHEMBL2181582 | — | Ki | = | 2.58 | nM | 8.59 |
| CHEMBL2181583 | — | Ki | = | 2.78 | nM | 8.56 |
| CHEMBL2181580 | — | Ki | = | 3.02 | nM | 8.52 |
| CHEMBL2181578 | — | Ki | = | 4.66 | nM | 8.33 |
| CHEMBL421983 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL2181575 | — | Ki | = | 14.72 | nM | 7.83 |
| CHEMBL2181571 | — | Ki | = | 22.8 | nM | 7.64 |
| CHEMBL2181581 | — | Ki | = | 361.2 | nM | 6.44 |
| CHEMBL2181577 | — | Ki | = | 400.0 | nM | 6.40 |