Assay Detail
Binding
CHEMBL651179
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes
64
Total Activities
64
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 64 | 8.03 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL15093 | PNU-91571 | — | 1 | 9.00 |
| CHEMBL15102 | — | — | 1 | 8.98 |
| CHEMBL15079 | — | — | 1 | 8.87 |
| CHEMBL279867 | PANADIPLON | 2.0 | 1 | 8.80 |
| CHEMBL15143 | — | — | 1 | 8.63 |
| CHEMBL2079553 | — | — | 1 | 8.63 |
| CHEMBL416897 | — | — | 1 | 8.61 |
| CHEMBL14805 | — | — | 1 | 8.59 |
| CHEMBL263211 | — | — | 1 | 8.57 |
| CHEMBL14716 | — | — | 1 | 8.52 |
| CHEMBL277383 | — | — | 1 | 8.52 |
| CHEMBL274915 | — | — | 1 | 8.49 |
| CHEMBL276144 | — | — | 1 | 8.48 |
| CHEMBL15276 | — | — | 1 | 8.46 |
| CHEMBL277832 | — | — | 1 | 8.40 |
| CHEMBL555381 | — | — | 1 | 8.39 |
| CHEMBL2079608 | — | — | 1 | 8.39 |
| CHEMBL15064 | — | — | 1 | 8.38 |
| CHEMBL279382 | — | — | 1 | 8.36 |
| CHEMBL15180 | — | — | 1 | 8.35 |
| CHEMBL276143 | — | — | 1 | 8.35 |
| CHEMBL279165 | — | — | 1 | 8.33 |
| CHEMBL278439 | — | — | 1 | 8.33 |
| CHEMBL14865 | — | — | 1 | 8.31 |
| CHEMBL14914 | — | — | 1 | 8.29 |
| CHEMBL15319 | — | — | 1 | 8.29 |
| CHEMBL277136 | — | — | 1 | 8.29 |
| CHEMBL14983 | — | — | 1 | 8.28 |
| CHEMBL15107 | — | — | 1 | 8.27 |
| CHEMBL274982 | — | — | 1 | 8.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL15093 | PNU-91571 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL15102 | — | Ki | = | 1.04 | nM | 8.98 |
| CHEMBL15079 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL279867 | PANADIPLON | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL15143 | — | Ki | = | 2.35 | nM | 8.63 |
| CHEMBL2079553 | — | Ki | = | 2.34 | nM | 8.63 |
| CHEMBL416897 | — | Ki | = | 2.47 | nM | 8.61 |
| CHEMBL14805 | — | Ki | = | 2.56 | nM | 8.59 |
| CHEMBL263211 | — | Ki | = | 2.69 | nM | 8.57 |
| CHEMBL14716 | — | Ki | = | 3.04 | nM | 8.52 |
| CHEMBL277383 | — | Ki | = | 3.03 | nM | 8.52 |
| CHEMBL274915 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL276144 | — | Ki | = | 3.27 | nM | 8.48 |
| CHEMBL15276 | — | Ki | = | 3.45 | nM | 8.46 |
| CHEMBL277832 | — | Ki | = | 3.99 | nM | 8.40 |
| CHEMBL555381 | — | Ki | = | 4.11 | nM | 8.39 |
| CHEMBL2079608 | — | Ki | = | 4.03 | nM | 8.39 |
| CHEMBL15064 | — | Ki | = | 4.18 | nM | 8.38 |
| CHEMBL279382 | — | Ki | = | 4.35 | nM | 8.36 |
| CHEMBL15180 | — | Ki | = | 4.48 | nM | 8.35 |
| CHEMBL276143 | — | Ki | = | 4.48 | nM | 8.35 |
| CHEMBL279165 | — | Ki | = | 4.66 | nM | 8.33 |
| CHEMBL278439 | — | Ki | = | 4.66 | nM | 8.33 |
| CHEMBL14865 | — | Ki | = | 4.89 | nM | 8.31 |
| CHEMBL277136 | — | Ki | = | 5.17 | nM | 8.29 |
| CHEMBL15319 | — | Ki | = | 5.16 | nM | 8.29 |
| CHEMBL14914 | — | Ki | = | 5.13 | nM | 8.29 |
| CHEMBL14983 | — | Ki | = | 5.25 | nM | 8.28 |
| CHEMBL15107 | — | Ki | = | 5.39 | nM | 8.27 |
| CHEMBL274982 | — | Ki | = | 5.45 | nM | 8.26 |
| CHEMBL274685 | — | Ki | = | 5.47 | nM | 8.26 |
| CHEMBL277110 | — | Ki | = | 5.56 | nM | 8.26 |
| CHEMBL14891 | — | Ki | = | 5.96 | nM | 8.22 |
| CHEMBL14847 | — | Ki | = | 6.67 | nM | 8.18 |
| CHEMBL278968 | — | Ki | = | 6.71 | nM | 8.17 |
| CHEMBL15140 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL277782 | — | Ki | = | 9.15 | nM | 8.04 |
| CHEMBL277558 | — | Ki | = | 9.5 | nM | 8.02 |
| CHEMBL274465 | — | Ki | = | 10.47 | nM | 7.98 |
| CHEMBL278182 | — | Ki | = | 10.87 | nM | 7.96 |
| CHEMBL279575 | — | Ki | = | 10.86 | nM | 7.96 |
| CHEMBL262970 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL278414 | — | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL15155 | — | Ki | = | 15.1 | nM | 7.82 |
| CHEMBL430324 | — | Ki | = | 16.7 | nM | 7.78 |
| CHEMBL274914 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL277584 | — | Ki | = | 19.93 | nM | 7.70 |
| CHEMBL277781 | — | Ki | = | 20.91 | nM | 7.68 |
| CHEMBL15022 | — | Ki | = | 23.21 | nM | 7.63 |
| CHEMBL14997 | — | Ki | = | 25.6 | nM | 7.59 |