Assay Detail
Binding
CHEMBL4135334
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Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat cerebral cortex membranes after 60 mins by liquid scintillation counting analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of thienopyrrolotriazine derivatives to protect mitochondrial function against Aβ-induced neurotoxicity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.09 | 8.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL481537 | PK-11195 | — | 1 | 8.12 |
| CHEMBL286346 | RO-54864 | — | 1 | 7.96 |
| CHEMBL1315992 | — | — | 1 | 7.61 |
| CHEMBL4174207 | — | — | 1 | 7.40 |
| CHEMBL4170783 | — | — | 1 | 7.26 |
| CHEMBL4175877 | — | — | 1 | 6.91 |
| CHEMBL4166954 | — | — | 1 | 5.78 |
| CHEMBL4160135 | — | — | 1 | 5.65 |
| CHEMBL4159052 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL481537 | PK-11195 | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL286346 | RO-54864 | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL1315992 | — | IC50 | = | 24.8 | nM | 7.61 |
| CHEMBL4174207 | — | IC50 | = | 39.9 | nM | 7.40 |
| CHEMBL4170783 | — | IC50 | = | 55.1 | nM | 7.26 |
| CHEMBL4175877 | — | IC50 | = | 122.5 | nM | 6.91 |
| CHEMBL4166954 | — | IC50 | = | 1667.0 | nM | 5.78 |
| CHEMBL4160135 | — | IC50 | = | 2225.0 | nM | 5.65 |
| CHEMBL4159052 | — | IC50 | > | 10000.0 | nM | - |