Assay Detail
Binding
CHEMBL652450
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against benzodiazepine receptor (BzR) in rat cortical membranes determined by competition experiments with radiolabeled [3H]flunitrazepam (Fnz)
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 53 | 7.65 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL339264 | — | — | 1 | 9.43 |
| CHEMBL123688 | — | — | 1 | 9.01 |
| CHEMBL125243 | — | — | 1 | 9.00 |
| CHEMBL127742 | — | — | 1 | 8.86 |
| CHEMBL333060 | — | — | 1 | 8.81 |
| CHEMBL279867 | PANADIPLON | 2.0 | 1 | 8.80 |
| CHEMBL419431 | — | — | 1 | 8.79 |
| CHEMBL445854 | — | — | 1 | 8.78 |
| CHEMBL421467 | — | — | 1 | 8.67 |
| CHEMBL124865 | — | — | 1 | 8.60 |
| CHEMBL339755 | — | — | 1 | 8.53 |
| CHEMBL126864 | — | — | 1 | 8.53 |
| CHEMBL124458 | — | — | 1 | 8.47 |
| CHEMBL338603 | — | — | 1 | 8.38 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.31 |
| CHEMBL127688 | — | — | 1 | 8.30 |
| CHEMBL339689 | — | — | 1 | 8.23 |
| CHEMBL338896 | — | — | 1 | 8.23 |
| CHEMBL340285 | — | — | 1 | 7.96 |
| CHEMBL339938 | — | — | 1 | 7.90 |
| CHEMBL124999 | — | — | 1 | 7.88 |
| CHEMBL339797 | — | — | 1 | 7.84 |
| CHEMBL441828 | — | — | 1 | 7.82 |
| CHEMBL126702 | — | — | 1 | 7.69 |
| CHEMBL127193 | — | — | 1 | 7.55 |
| CHEMBL124679 | — | — | 1 | 7.50 |
| CHEMBL127602 | — | — | 1 | 7.48 |
| CHEMBL339949 | — | — | 1 | 7.46 |
| CHEMBL339947 | — | — | 1 | 7.42 |
| CHEMBL124998 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL339264 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL123688 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL125243 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL127742 | — | Ki | = | 1.39 | nM | 8.86 |
| CHEMBL333060 | — | Ki | = | 1.54 | nM | 8.81 |
| CHEMBL279867 | PANADIPLON | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL419431 | — | Ki | = | 1.61 | nM | 8.79 |
| CHEMBL445854 | — | Ki | = | 1.65 | nM | 8.78 |
| CHEMBL421467 | — | Ki | = | 2.16 | nM | 8.67 |
| CHEMBL124865 | — | Ki | = | 2.49 | nM | 8.60 |
| CHEMBL339755 | — | Ki | = | 2.96 | nM | 8.53 |
| CHEMBL126864 | — | Ki | = | 2.97 | nM | 8.53 |
| CHEMBL124458 | — | Ki | = | 3.41 | nM | 8.47 |
| CHEMBL338603 | — | Ki | = | 4.16 | nM | 8.38 |
| CHEMBL12 | DIAZEPAM | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL127688 | — | Ki | = | 5.06 | nM | 8.30 |
| CHEMBL339689 | — | Ki | = | 5.91 | nM | 8.23 |
| CHEMBL338896 | — | Ki | = | 5.85 | nM | 8.23 |
| CHEMBL340285 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL339938 | — | Ki | = | 12.6 | nM | 7.90 |
| CHEMBL124999 | — | Ki | = | 13.2 | nM | 7.88 |
| CHEMBL339797 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL441828 | — | Ki | = | 15.2 | nM | 7.82 |
| CHEMBL126702 | — | Ki | = | 20.5 | nM | 7.69 |
| CHEMBL127193 | — | Ki | = | 27.9 | nM | 7.55 |
| CHEMBL124679 | — | Ki | = | 31.7 | nM | 7.50 |
| CHEMBL127602 | — | Ki | = | 33.4 | nM | 7.48 |
| CHEMBL339949 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL339947 | — | Ki | = | 38.5 | nM | 7.42 |
| CHEMBL124998 | — | Ki | = | 39.6 | nM | 7.40 |
| CHEMBL433673 | — | Ki | = | 42.4 | nM | 7.37 |
| CHEMBL124130 | — | Ki | = | 47.2 | nM | 7.33 |
| CHEMBL435813 | — | Ki | = | 47.4 | nM | 7.32 |
| CHEMBL125198 | — | Ki | = | 48.6 | nM | 7.31 |
| CHEMBL123851 | — | Ki | = | 49.7 | nM | 7.30 |
| CHEMBL421652 | — | Ki | = | 50.8 | nM | 7.29 |
| CHEMBL338147 | — | Ki | = | 59.4 | nM | 7.23 |
| CHEMBL127455 | — | Ki | = | 81.5 | nM | 7.09 |
| CHEMBL124932 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL126624 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL341492 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL333910 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL338672 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL340128 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL338208 | — | Ki | = | 216.0 | nM | 6.67 |
| CHEMBL125186 | — | Ki | = | 283.0 | nM | 6.55 |
| CHEMBL123674 | — | Ki | = | 334.0 | nM | 6.48 |
| CHEMBL126798 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL126539 | — | Ki | = | 478.0 | nM | 6.32 |
| CHEMBL339823 | — | Ki | = | 1692.0 | nM | 5.77 |