Assay Detail
Binding
CHEMBL651180
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity benzodiazepine receptor as ability to displace [3H]flunitrazepam from binding to membrane preparations from rat cerebral cortex.
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebral cortex |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
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 | 5.25 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL341361 | — | — | 1 | 7.19 |
| CHEMBL340752 | — | — | 1 | 7.04 |
| CHEMBL129101 | — | — | 1 | 6.93 |
| CHEMBL129511 | — | — | 1 | 6.30 |
| CHEMBL320366 | — | — | 1 | 6.28 |
| CHEMBL338633 | — | — | 1 | 6.09 |
| CHEMBL128491 | — | — | 1 | 5.68 |
| CHEMBL127060 | — | — | 1 | 5.58 |
| CHEMBL106237 | — | — | 1 | 5.47 |
| CHEMBL340938 | — | — | 1 | 5.27 |
| CHEMBL338634 | — | — | 1 | 5.27 |
| CHEMBL339816 | — | — | 1 | 5.07 |
| CHEMBL450283 | — | — | 1 | 5.00 |
| CHEMBL104686 | — | — | 1 | 5.00 |
| CHEMBL339530 | — | — | 1 | 5.00 |
| CHEMBL128093 | — | — | 1 | 4.96 |
| CHEMBL337917 | — | — | 1 | 4.92 |
| CHEMBL338378 | — | — | 1 | 4.85 |
| CHEMBL338442 | — | — | 1 | 4.80 |
| CHEMBL481537 | PK-11195 | — | 1 | 4.67 |
| CHEMBL127057 | — | — | 1 | 4.59 |
| CHEMBL321916 | — | — | 1 | 4.27 |
| CHEMBL129162 | — | — | 1 | 4.19 |
| CHEMBL340201 | — | — | 1 | 4.09 |
| CHEMBL126730 | — | — | 1 | 4.00 |
| CHEMBL128147 | — | — | 1 | 4.00 |
| CHEMBL432608 | ALPDEM | — | 1 | - |
| CHEMBL126286 | — | — | 1 | - |
| CHEMBL321069 | — | — | 1 | - |
| CHEMBL128407 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL341361 | — | IC50 | = | 64.57 | nM | 7.19 |
| CHEMBL340752 | — | IC50 | = | 91.2 | nM | 7.04 |
| CHEMBL129101 | — | IC50 | = | 117.49 | nM | 6.93 |
| CHEMBL129511 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL320366 | — | IC50 | = | 524.81 | nM | 6.28 |
| CHEMBL338633 | — | IC50 | = | 812.83 | nM | 6.09 |
| CHEMBL128491 | — | IC50 | = | 2089.3 | nM | 5.68 |
| CHEMBL127060 | — | IC50 | = | 2630.27 | nM | 5.58 |
| CHEMBL106237 | — | IC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL340938 | — | IC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL338634 | — | IC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL339816 | — | IC50 | = | 8511.38 | nM | 5.07 |
| CHEMBL450283 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL104686 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL339530 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL128093 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL337917 | — | IC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL338378 | — | IC50 | = | 14125.38 | nM | 4.85 |
| CHEMBL338442 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL481537 | PK-11195 | IC50 | = | 21379.62 | nM | 4.67 |
| CHEMBL127057 | — | IC50 | = | 25703.96 | nM | 4.59 |
| CHEMBL321916 | — | IC50 | = | 53703.18 | nM | 4.27 |
| CHEMBL129162 | — | IC50 | = | 64565.42 | nM | 4.19 |
| CHEMBL340201 | — | IC50 | = | 81283.05 | nM | 4.09 |
| CHEMBL126730 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL128147 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL432608 | ALPDEM | IC50 | = | 3981071.71 | nM | - |
| CHEMBL126286 | — | IC50 | = | 147910.84 | nM | - |
| CHEMBL321069 | — | IC50 | = | 3981071.71 | nM | - |
| CHEMBL128407 | — | IC50 | = | 3981071.71 | nM | - |
| CHEMBL129028 | — | IC50 | = | 117489.76 | nM | - |
| CHEMBL126262 | — | IC50 | = | 3981071.71 | nM | - |