Assay Detail
Binding
CHEMBL3877924
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]PK11195 from TSPO in rat heart membranes after 15 mins by scintillation counting method
15
Total Activities
15
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 translocator protein 18 kDa ligand CfO-DPA-714.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 8.47 | 9.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3936390 | — | — | 1 | 9.60 |
| CHEMBL3979767 | — | — | 1 | 9.59 |
| CHEMBL3906952 | — | — | 1 | 9.52 |
| CHEMBL469682 | — | — | 1 | 9.43 |
| CHEMBL512306 | DPA-714 | 2.0 | 1 | 9.04 |
| CHEMBL3938340 | — | — | 1 | 8.96 |
| CHEMBL3960249 | — | — | 1 | 8.92 |
| CHEMBL3923539 | — | — | 1 | 8.66 |
| CHEMBL3929294 | — | — | 1 | 8.55 |
| CHEMBL3908452 | — | — | 1 | 7.82 |
| CHEMBL3909555 | — | — | 1 | 7.77 |
| CHEMBL3896806 | — | — | 1 | 7.58 |
| CHEMBL3981447 | — | — | 1 | 7.57 |
| CHEMBL3906707 | — | — | 1 | 7.50 |
| CHEMBL3920384 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3936390 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL3979767 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL3906952 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL469682 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL512306 | DPA-714 | Ki | = | 0.91 | nM | 9.04 |
| CHEMBL3938340 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL3960249 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3923539 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3929294 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3908452 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3909555 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL3896806 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3981447 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3906707 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL3920384 | — | Ki | = | 260.0 | nM | 6.58 |