Assay Detail
Binding
CHEMBL4337304
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]PK11195 from wild-type human TSPO expressed in HEK293 cell membranes after 90 mins by scintillation counting method
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 6.64 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4459176 | — | — | 1 | 8.18 |
| CHEMBL416715 | (R)PK-11195 | — | 1 | 7.65 |
| CHEMBL4173118 | — | — | 1 | 7.52 |
| CHEMBL4447335 | — | — | 1 | 7.28 |
| CHEMBL4161842 | — | — | 1 | 7.16 |
| CHEMBL4439049 | — | — | 1 | 7.02 |
| CHEMBL4466212 | — | — | 1 | 6.74 |
| CHEMBL4535242 | — | — | 1 | 6.70 |
| CHEMBL4563441 | — | — | 1 | 6.64 |
| CHEMBL4560218 | — | — | 1 | 6.64 |
| CHEMBL4440106 | — | — | 1 | 6.61 |
| CHEMBL4461372 | — | — | 1 | 6.41 |
| CHEMBL4532562 | — | — | 1 | 6.35 |
| CHEMBL4475609 | — | — | 1 | 6.33 |
| CHEMBL4445371 | — | — | 1 | 6.25 |
| CHEMBL4551915 | — | — | 1 | 6.16 |
| CHEMBL4440548 | — | — | 1 | 5.82 |
| CHEMBL4536533 | — | — | 1 | 5.45 |
| CHEMBL4447625 | — | — | 1 | 5.32 |
| CHEMBL4451744 | — | — | 1 | - |
| CHEMBL4436847 | — | — | 1 | - |
| CHEMBL4571475 | — | — | 1 | - |
| CHEMBL4460152 | — | — | 1 | - |
| CHEMBL4587084 | — | — | 1 | - |
| CHEMBL4446805 | — | — | 1 | - |
| CHEMBL4518499 | — | — | 1 | - |
| CHEMBL4458416 | — | — | 1 | - |
| CHEMBL4585880 | — | — | 1 | - |
| CHEMBL4580702 | — | — | 1 | - |
| CHEMBL4554031 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4459176 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL416715 | (R)PK-11195 | Ki | = | 22.5 | nM | 7.65 |
| CHEMBL4173118 | — | Ki | = | 30.1 | nM | 7.52 |
| CHEMBL4447335 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL4161842 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL4439049 | — | Ki | = | 96.1 | nM | 7.02 |
| CHEMBL4466212 | — | Ki | = | 184.2 | nM | 6.74 |
| CHEMBL4535242 | — | Ki | = | 200.7 | nM | 6.70 |
| CHEMBL4563441 | — | Ki | = | 231.3 | nM | 6.64 |
| CHEMBL4560218 | — | Ki | = | 231.2 | nM | 6.64 |
| CHEMBL4440106 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL4461372 | — | Ki | = | 385.3 | nM | 6.41 |
| CHEMBL4532562 | — | Ki | = | 447.1 | nM | 6.35 |
| CHEMBL4475609 | — | Ki | = | 468.7 | nM | 6.33 |
| CHEMBL4445371 | — | Ki | = | 562.5 | nM | 6.25 |
| CHEMBL4551915 | — | Ki | = | 693.8 | nM | 6.16 |
| CHEMBL4440548 | — | Ki | = | 1531.3 | nM | 5.82 |
| CHEMBL4536533 | — | Ki | = | 3555.0 | nM | 5.45 |
| CHEMBL4447625 | — | Ki | = | 4737.3 | nM | 5.32 |
| CHEMBL4451744 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4436847 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4571475 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4460152 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4587084 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4446805 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4518499 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4458416 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4585880 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4580702 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4554031 | — | Ki | > | 10000.0 | nM | - |