Assay Detail
Binding
CHEMBL651181
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-PK 11195 from peripheral-type benzodiazepine receptor of rat cerebral cortex membranes
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebral cortex |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Novel 2-phenylimidazo[1,2-a]pyridine derivatives as potent and selective ligands for peripheral benzodiazepine receptors: synthesis, binding affinity, and in vivo studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.75 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL450283 | — | — | 1 | 9.10 |
| CHEMBL432608 | ALPDEM | — | 1 | 9.00 |
| CHEMBL126262 | — | — | 1 | 8.85 |
| CHEMBL481537 | PK-11195 | — | 1 | 8.85 |
| CHEMBL321916 | — | — | 1 | 8.79 |
| CHEMBL104686 | — | — | 1 | 8.74 |
| CHEMBL321069 | — | — | 1 | 8.52 |
| CHEMBL128147 | — | — | 1 | 8.43 |
| CHEMBL128407 | — | — | 1 | 8.37 |
| CHEMBL340938 | — | — | 1 | 8.37 |
| CHEMBL339530 | — | — | 1 | 8.24 |
| CHEMBL340752 | — | — | 1 | 8.23 |
| CHEMBL339816 | — | — | 1 | 8.20 |
| CHEMBL106237 | — | — | 1 | 8.12 |
| CHEMBL340201 | — | — | 1 | 8.00 |
| CHEMBL341361 | — | — | 1 | 8.00 |
| CHEMBL129162 | — | — | 1 | 7.78 |
| CHEMBL337917 | — | — | 1 | 7.78 |
| CHEMBL129511 | — | — | 1 | 7.77 |
| CHEMBL129028 | — | — | 1 | 7.72 |
| CHEMBL338378 | — | — | 1 | 7.70 |
| CHEMBL127057 | — | — | 1 | 7.64 |
| CHEMBL338634 | — | — | 1 | 7.33 |
| CHEMBL338442 | — | — | 1 | 7.07 |
| CHEMBL320366 | — | — | 1 | 7.00 |
| CHEMBL126286 | — | — | 1 | 6.74 |
| CHEMBL128093 | — | — | 1 | 6.59 |
| CHEMBL126730 | — | — | 1 | 6.53 |
| CHEMBL128491 | — | — | 1 | 6.36 |
| CHEMBL127060 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL450283 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL432608 | ALPDEM | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL126262 | — | IC50 | = | 1.413 | nM | 8.85 |
| CHEMBL481537 | PK-11195 | IC50 | = | 1.413 | nM | 8.85 |
| CHEMBL321916 | — | IC50 | = | 1.622 | nM | 8.79 |
| CHEMBL104686 | — | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL321069 | — | IC50 | = | 3.02 | nM | 8.52 |
| CHEMBL128147 | — | IC50 | = | 3.715 | nM | 8.43 |
| CHEMBL128407 | — | IC50 | = | 4.266 | nM | 8.37 |
| CHEMBL340938 | — | IC50 | = | 4.266 | nM | 8.37 |
| CHEMBL339530 | — | IC50 | = | 5.754 | nM | 8.24 |
| CHEMBL340752 | — | IC50 | = | 5.888 | nM | 8.23 |
| CHEMBL339816 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL106237 | — | IC50 | = | 7.586 | nM | 8.12 |
| CHEMBL341361 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL340201 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL129162 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL337917 | — | IC50 | = | 16.6 | nM | 7.78 |
| CHEMBL129511 | — | IC50 | = | 16.98 | nM | 7.77 |
| CHEMBL129028 | — | IC50 | = | 19.05 | nM | 7.72 |
| CHEMBL338378 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL127057 | — | IC50 | = | 22.91 | nM | 7.64 |
| CHEMBL338634 | — | IC50 | = | 46.77 | nM | 7.33 |
| CHEMBL338442 | — | IC50 | = | 85.11 | nM | 7.07 |
| CHEMBL320366 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL126286 | — | IC50 | = | 181.97 | nM | 6.74 |
| CHEMBL128093 | — | IC50 | = | 257.04 | nM | 6.59 |
| CHEMBL126730 | — | IC50 | = | 295.12 | nM | 6.53 |
| CHEMBL128491 | — | IC50 | = | 436.52 | nM | 6.36 |
| CHEMBL127060 | — | IC50 | = | 457.09 | nM | 6.34 |
| CHEMBL129101 | — | IC50 | = | 588.84 | nM | 6.23 |
| CHEMBL338633 | — | IC50 | = | 1995.26 | nM | 5.70 |