Assay Detail
Binding
CHEMBL4138529
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Displacement of [3H]PK11195 from human TSPO A147T mutant expressed in HEK293T cell membranes after 90 mins by scintillation counting method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Determination and reduction of translocator protein (TSPO) ligand rs6971 discrimination.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 6.94 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513922 | EMAPUNIL | 2.0 | 1 | 7.50 |
| CHEMBL481537 | PK-11195 | — | 1 | 7.44 |
| CHEMBL4173816 | — | — | 1 | 7.03 |
| CHEMBL480041 | — | — | 1 | 7.00 |
| CHEMBL4169328 | — | — | 1 | 6.91 |
| CHEMBL4165898 | — | — | 1 | 6.86 |
| CHEMBL4177167 | — | — | 1 | 6.80 |
| CHEMBL4164932 | — | — | 1 | 6.79 |
| CHEMBL4173118 | — | — | 1 | 6.75 |
| CHEMBL4161842 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513922 | EMAPUNIL | Ki | = | 31.3 | nM | 7.50 |
| CHEMBL481537 | PK-11195 | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4173816 | — | Ki | = | 93.4 | nM | 7.03 |
| CHEMBL480041 | — | Ki | = | 98.8 | nM | 7.00 |
| CHEMBL4169328 | — | Ki | = | 123.4 | nM | 6.91 |
| CHEMBL4165898 | — | Ki | = | 137.3 | nM | 6.86 |
| CHEMBL4177167 | — | Ki | = | 159.8 | nM | 6.80 |
| CHEMBL4164932 | — | Ki | = | 160.9 | nM | 6.79 |
| CHEMBL4173118 | — | Ki | = | 176.6 | nM | 6.75 |
| CHEMBL4161842 | — | Ki | = | 459.6 | nM | 6.34 |