Assay Detail
Binding
CHEMBL961474
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Displacement of [3H]PK11195 from PBR in rat kidney mitochondrial membrane
11
Total Activities
7
Compounds Tested
2
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
Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.62 | 9.59 |
| IC50 | 4 | 7.98 | 9.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483129 | — | — | 2 | 9.59 |
| CHEMBL483130 | — | — | 2 | 8.89 |
| CHEMBL481537 | PK-11195 | — | 1 | 7.54 |
| CHEMBL286346 | RO-54864 | — | 1 | 7.47 |
| CHEMBL483131 | — | — | 2 | 7.20 |
| CHEMBL504365 | — | — | 2 | 6.38 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483129 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL483129 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL483130 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL483130 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL481537 | PK-11195 | Ki | = | 28.8 | nM | 7.54 |
| CHEMBL286346 | RO-54864 | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL483131 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL483131 | — | IC50 | = | 66.5 | nM | 7.18 |
| CHEMBL504365 | — | Ki | = | 421.0 | nM | 6.38 |
| CHEMBL504365 | — | IC50 | = | 445.0 | nM | 6.35 |
| CHEMBL12 | DIAZEPAM | Ki | = | 574.0 | nM | 6.24 |