Assay Detail
Binding
CHEMBL2212410
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Displacement of [11C]-PK-11195 from TPSO in Sprague-Dawley rat brain homogenate after 30 mins by gamma counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and evaluation of novel carbon-11 labeled oxopurine analogues for positron emission tomography imaging of translocator protein (18 kDa) in peripheral organs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 8.39 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL513922 | EMAPUNIL | 2.0 | 1 | 9.22 |
| CHEMBL416715 | (R)PK-11195 | — | 1 | 9.15 |
| CHEMBL2206282 | — | — | 1 | 8.29 |
| CHEMBL2206283 | — | — | 1 | 7.88 |
| CHEMBL2206284 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL513922 | EMAPUNIL | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL416715 | (R)PK-11195 | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2206282 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL2206283 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL2206284 | — | Ki | = | 40.0 | nM | 7.40 |