Assay Detail
Binding
CHEMBL2071915
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Displacement of [3H]PK11195 from TSPO in Wistar rat heart incubated for 15 mins
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Exploration of the structure-activity relationship of the diaryl anilide class of ligands for translocator protein--potential novel positron emitting tomography imaging agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 31 | 8.31 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070800 | — | — | 1 | 10.30 |
| CHEMBL2070787 | — | — | 1 | 10.30 |
| CHEMBL2070786 | — | — | 1 | 9.72 |
| CHEMBL473435 | — | — | 1 | 9.55 |
| CHEMBL2070808 | — | — | 1 | 9.51 |
| CHEMBL63064 | — | — | 1 | 9.37 |
| CHEMBL2070788 | — | — | 1 | 9.34 |
| CHEMBL2070806 | — | — | 1 | 8.99 |
| CHEMBL2070785 | — | — | 1 | 8.94 |
| CHEMBL2070810 | — | — | 1 | 8.94 |
| CHEMBL481537 | PK-11195 | — | 1 | 8.91 |
| CHEMBL2070811 | — | — | 1 | 8.69 |
| CHEMBL2070799 | — | — | 1 | 8.66 |
| CHEMBL2070812 | — | — | 1 | 8.57 |
| CHEMBL2070809 | — | — | 1 | 8.45 |
| CHEMBL2070790 | — | — | 1 | 8.42 |
| CHEMBL2070802 | — | — | 1 | 8.42 |
| CHEMBL2070796 | — | — | 1 | 8.37 |
| CHEMBL2070793 | — | — | 1 | 8.35 |
| CHEMBL2070795 | — | — | 1 | 8.20 |
| CHEMBL2070789 | — | — | 1 | 8.18 |
| CHEMBL2070797 | — | — | 1 | 8.14 |
| CHEMBL2070791 | — | — | 1 | 8.01 |
| CHEMBL2070801 | — | — | 1 | 7.20 |
| CHEMBL2070803 | — | — | 1 | 7.14 |
| CHEMBL2070807 | — | — | 1 | 6.98 |
| CHEMBL2070798 | — | — | 1 | 6.90 |
| CHEMBL2070804 | — | — | 1 | 6.79 |
| CHEMBL2070792 | — | — | 1 | 6.66 |
| CHEMBL2070805 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070800 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL2070787 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL2070786 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL473435 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL2070808 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL63064 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL2070788 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL2070806 | — | Ki | = | 1.02 | nM | 8.99 |
| CHEMBL2070785 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL2070810 | — | Ki | = | 1.14 | nM | 8.94 |
| CHEMBL481537 | PK-11195 | Ki | = | 1.24 | nM | 8.91 |
| CHEMBL2070811 | — | Ki | = | 2.03 | nM | 8.69 |
| CHEMBL2070799 | — | Ki | = | 2.18 | nM | 8.66 |
| CHEMBL2070812 | — | Ki | = | 2.66 | nM | 8.57 |
| CHEMBL2070809 | — | Ki | = | 3.52 | nM | 8.45 |
| CHEMBL2070790 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL2070802 | — | Ki | = | 3.77 | nM | 8.42 |
| CHEMBL2070796 | — | Ki | = | 4.24 | nM | 8.37 |
| CHEMBL2070793 | — | Ki | = | 4.48 | nM | 8.35 |
| CHEMBL2070795 | — | Ki | = | 6.38 | nM | 8.20 |
| CHEMBL2070789 | — | Ki | = | 6.65 | nM | 8.18 |
| CHEMBL2070797 | — | Ki | = | 7.28 | nM | 8.14 |
| CHEMBL2070791 | — | Ki | = | 9.84 | nM | 8.01 |
| CHEMBL2070801 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL2070803 | — | Ki | = | 72.1 | nM | 7.14 |
| CHEMBL2070807 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL2070798 | — | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL2070804 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL2070792 | — | Ki | = | 219.0 | nM | 6.66 |
| CHEMBL2070805 | — | Ki | = | 497.0 | nM | 6.30 |
| CHEMBL2070794 | — | Ki | = | 3430.0 | nM | 5.46 |