Assay Detail
Binding
CHEMBL3616197
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Displacement of [3H]-PK11195 from rat heart membrane TSPO
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Heart |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.35 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3613363 | — | — | 1 | 9.52 |
| CHEMBL3613360 | — | — | 1 | 9.40 |
| CHEMBL3613361 | — | — | 1 | 9.38 |
| CHEMBL3613358 | — | — | 1 | 9.17 |
| CHEMBL517539 | — | — | 1 | 9.08 |
| CHEMBL3613362 | — | — | 1 | 9.02 |
| CHEMBL3613359 | — | — | 1 | 8.85 |
| CHEMBL3613365 | — | — | 1 | 8.82 |
| CHEMBL3613366 | — | — | 1 | 8.39 |
| CHEMBL3613370 | — | — | 1 | 8.38 |
| CHEMBL3613364 | — | — | 1 | 8.38 |
| CHEMBL3613369 | — | — | 1 | 8.09 |
| CHEMBL3613367 | — | — | 1 | 7.21 |
| CHEMBL3613368 | — | — | 1 | 6.92 |
| CHEMBL3613371 | — | — | 1 | 6.89 |
| CHEMBL3613372 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3613363 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3613360 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3613361 | — | Ki | = | 0.42 | nM | 9.38 |
| CHEMBL3613358 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL517539 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL3613362 | — | Ki | = | 0.96 | nM | 9.02 |
| CHEMBL3613359 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3613365 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL3613366 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL3613370 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3613364 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3613369 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL3613367 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL3613368 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL3613371 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL3613372 | — | Ki | = | 920.0 | nM | 6.04 |