Assay Detail
Binding
CHEMBL4710744
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Displacement of [3H]-PK11195 from wild type TSPO (unknown origin) expressed in human HEK293T cells assessed as inhibitory constant incubated for 90 mins by microbeta scintillation counting method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Tricyclic heterocycles display diverse sensitivity to the A147T TSPO polymorphism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.30 | 8.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4789235 | — | — | 1 | 8.21 |
| CHEMBL4742003 | — | — | 1 | 8.03 |
| CHEMBL4742171 | — | — | 1 | 7.80 |
| CHEMBL480041 | — | — | 1 | 7.71 |
| CHEMBL4173118 | — | — | 1 | 7.52 |
| CHEMBL4758934 | — | — | 1 | 7.38 |
| CHEMBL4745926 | — | — | 1 | 7.38 |
| CHEMBL4447335 | — | — | 1 | 7.28 |
| CHEMBL4743573 | — | — | 1 | 7.12 |
| CHEMBL4161842 | — | — | 1 | 7.04 |
| CHEMBL4793373 | — | — | 1 | 6.70 |
| CHEMBL4753783 | — | — | 1 | 6.47 |
| CHEMBL4750743 | — | — | 1 | 6.31 |
| CHEMBL4451744 | — | — | 1 | - |
| CHEMBL4792527 | — | — | 1 | - |
| CHEMBL4761316 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4789235 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL4742003 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL4742171 | — | Ki | = | 15.8 | nM | 7.80 |
| CHEMBL480041 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL4173118 | — | Ki | = | 30.1 | nM | 7.52 |
| CHEMBL4758934 | — | Ki | = | 41.3 | nM | 7.38 |
| CHEMBL4745926 | — | Ki | = | 41.3 | nM | 7.38 |
| CHEMBL4447335 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4743573 | — | Ki | = | 76.8 | nM | 7.12 |
| CHEMBL4161842 | — | Ki | = | 91.6 | nM | 7.04 |
| CHEMBL4793373 | — | Ki | = | 200.5 | nM | 6.70 |
| CHEMBL4753783 | — | Ki | = | 337.9 | nM | 6.47 |
| CHEMBL4750743 | — | Ki | = | 493.0 | nM | 6.31 |
| CHEMBL4451744 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4792527 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4761316 | — | Ki | > | 10000.0 | nM | - |