Assay Detail
Binding
CHEMBL5228261
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]PK11195 from TSPO receptor in rat brain cortex membrane incubated for 120 mins by liquid scintillation spectrometer method
59
Total Activities
59
Compounds Tested
2
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
Exploring Translocator Protein (TSPO) Medicinal Chemistry: An Approach for Targeting Radionuclides and Boron Atoms to Mitochondria.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 58 | 6.90 | 9.30 |
| Ki | 1 | 8.41 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54349 | ALPIDEM | 4.0 | 1 | 9.30 |
| CHEMBL481537 | PK-11195 | — | 1 | 8.74 |
| CHEMBL15248 | — | — | 1 | 8.68 |
| CHEMBL276756 | — | — | 1 | 8.68 |
| CHEMBL15003 | — | — | 1 | 8.54 |
| CHEMBL280482 | — | — | 1 | 8.51 |
| CHEMBL15254 | — | — | 1 | 8.47 |
| CHEMBL97269 | — | — | 1 | 8.41 |
| CHEMBL6645 | — | — | 1 | 8.39 |
| CHEMBL275410 | — | — | 1 | 8.19 |
| CHEMBL14956 | — | — | 1 | 8.06 |
| CHEMBL15237 | — | — | 1 | 8.05 |
| CHEMBL276341 | — | — | 1 | 8.01 |
| CHEMBL5275613 | — | — | 1 | 8.00 |
| CHEMBL278011 | — | — | 1 | 7.96 |
| CHEMBL280035 | — | — | 1 | 7.89 |
| CHEMBL134590 | — | — | 1 | 7.40 |
| CHEMBL15714 | — | — | 1 | 7.35 |
| CHEMBL334887 | — | — | 1 | 6.82 |
| CHEMBL277586 | — | — | 1 | 6.77 |
| CHEMBL14920 | — | — | 1 | 6.64 |
| CHEMBL279346 | — | — | 1 | 6.64 |
| CHEMBL15584 | — | — | 1 | 6.57 |
| CHEMBL136030 | — | — | 1 | 6.54 |
| CHEMBL15659 | — | — | 1 | 6.43 |
| CHEMBL274244 | — | — | 1 | 6.34 |
| CHEMBL15315 | — | — | 1 | 6.32 |
| CHEMBL15630 | — | — | 1 | 6.31 |
| CHEMBL15652 | — | — | 1 | 6.27 |
| CHEMBL15239 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54349 | ALPIDEM | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL481537 | PK-11195 | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL276756 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL15248 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL15003 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL280482 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL15254 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL97269 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL6645 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL275410 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL14956 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL15237 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL276341 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5275613 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL278011 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL280035 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL134590 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL15714 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL334887 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL277586 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL14920 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL279346 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL15584 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL136030 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL15659 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL274244 | — | IC50 | = | 456.0 | nM | 6.34 |
| CHEMBL15315 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL15630 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL15652 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL15239 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL15316 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL278465 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL15255 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL429386 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL278279 | — | IC50 | = | 872.0 | nM | 6.06 |
| CHEMBL416162 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL15473 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL15741 | — | IC50 | = | 1317.0 | nM | 5.88 |
| CHEMBL135408 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL15709 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL15645 | — | IC50 | = | 2895.0 | nM | 5.54 |
| CHEMBL15683 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL15402 | — | IC50 | = | 8209.0 | nM | 5.09 |
| CHEMBL14948 | — | IC50 | = | 8867.0 | nM | 5.05 |
| CHEMBL137730 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL101823 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL14757 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL280483 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL279549 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5283306 | — | IC50 | > | 1000.0 | nM | - |