Assay Detail
Binding
CHEMBL1655209
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Displacement of [11C]PK11195 from TSPO in rat kidney mitochondrial membrane
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Kidney |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.15 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1651225 | — | — | 1 | 9.52 |
| CHEMBL1651226 | — | — | 1 | 9.52 |
| CHEMBL432608 | ALPDEM | — | 1 | 9.30 |
| CHEMBL1651234 | — | — | 1 | 8.97 |
| CHEMBL1651223 | — | — | 1 | 8.74 |
| CHEMBL1651228 | — | — | 1 | 8.54 |
| CHEMBL1651236 | — | — | 1 | 8.24 |
| CHEMBL1651235 | — | — | 1 | 8.17 |
| CHEMBL481537 | PK-11195 | — | 1 | 8.03 |
| CHEMBL1651222 | — | — | 1 | 7.92 |
| CHEMBL1651224 | — | — | 1 | 7.71 |
| CHEMBL1651233 | — | — | 1 | 7.70 |
| CHEMBL1651231 | — | — | 1 | 7.68 |
| CHEMBL286346 | RO-54864 | — | 1 | 7.64 |
| CHEMBL1651232 | — | — | 1 | 7.62 |
| CHEMBL1651230 | — | — | 1 | 7.42 |
| CHEMBL1651227 | — | — | 1 | 7.22 |
| CHEMBL1651229 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1651225 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL1651226 | — | Ki | = | 0.299 | nM | 9.52 |
| CHEMBL432608 | ALPDEM | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL1651234 | — | Ki | = | 1.07 | nM | 8.97 |
| CHEMBL1651223 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1651228 | — | Ki | = | 2.92 | nM | 8.54 |
| CHEMBL1651236 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL1651235 | — | Ki | = | 6.77 | nM | 8.17 |
| CHEMBL481537 | PK-11195 | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL1651222 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1651224 | — | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL1651233 | — | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL1651231 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL286346 | RO-54864 | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL1651232 | — | Ki | = | 23.7 | nM | 7.62 |
| CHEMBL1651230 | — | Ki | = | 38.2 | nM | 7.42 |
| CHEMBL1651227 | — | Ki | = | 60.2 | nM | 7.22 |
| CHEMBL1651229 | — | Ki | = | 190.0 | nM | 6.72 |