Assay Detail
Binding
CHEMBL652362
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Displacement of [3H]-PK 11195 from rat peripheral (mitochondrial) benzodiazepine receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
A comparative molecular field analysis model for 6-arylpyrrolo[2,1-d] [1,5]benzothiazepines binding selectively to the mitochondrial benzodiazepine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.53 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL481537 | PK-11195 | — | 1 | 8.70 |
| CHEMBL117589 | — | — | 1 | 8.40 |
| CHEMBL335287 | — | — | 1 | 7.55 |
| CHEMBL116087 | — | — | 1 | 7.52 |
| CHEMBL133406 | — | — | 1 | 7.51 |
| CHEMBL133407 | — | — | 1 | 7.42 |
| CHEMBL324500 | — | — | 1 | 6.95 |
| CHEMBL326066 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL481537 | PK-11195 | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL117589 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL335287 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL116087 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL133406 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL133407 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL324500 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL326066 | — | IC50 | = | 675.0 | nM | 6.17 |