Assay Detail
Binding
CHEMBL680658
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Inhibition of [3H]flunitrazepam binding to GABA-A receptor of rat cortical membranes
47
Total Activities
47
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
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 47 | 8.63 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49471 | — | — | 1 | 9.37 |
| CHEMBL49778 | — | — | 1 | 9.35 |
| CHEMBL50763 | — | — | 1 | 9.32 |
| CHEMBL50957 | — | — | 1 | 9.25 |
| CHEMBL49278 | — | — | 1 | 9.21 |
| CHEMBL301789 | — | — | 1 | 9.19 |
| CHEMBL446141 | — | — | 1 | 9.19 |
| CHEMBL290036 | — | — | 1 | 9.17 |
| CHEMBL50122 | — | — | 1 | 9.15 |
| CHEMBL48485 | — | — | 1 | 9.14 |
| CHEMBL296952 | — | — | 1 | 9.09 |
| CHEMBL48759 | — | — | 1 | 9.07 |
| CHEMBL48377 | — | — | 1 | 9.05 |
| CHEMBL15093 | PNU-91571 | — | 1 | 9.00 |
| CHEMBL46013 | — | — | 1 | 8.96 |
| CHEMBL299072 | — | — | 1 | 8.96 |
| CHEMBL298365 | — | — | 1 | 8.96 |
| CHEMBL49160 | — | — | 1 | 8.96 |
| CHEMBL50059 | — | — | 1 | 8.89 |
| CHEMBL299133 | — | — | 1 | 8.82 |
| CHEMBL294916 | — | — | 1 | 8.82 |
| CHEMBL279867 | PANADIPLON | 2.0 | 1 | 8.80 |
| CHEMBL299326 | — | — | 1 | 8.74 |
| CHEMBL300633 | — | — | 1 | 8.72 |
| CHEMBL48839 | — | — | 1 | 8.68 |
| CHEMBL48403 | — | — | 1 | 8.64 |
| CHEMBL295216 | — | — | 1 | 8.55 |
| CHEMBL49538 | — | — | 1 | 8.54 |
| CHEMBL45807 | — | — | 1 | 8.51 |
| CHEMBL45734 | — | — | 1 | 8.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49471 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL49778 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL50763 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL50957 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL49278 | — | Ki | = | 0.61 | nM | 9.21 |
| CHEMBL301789 | — | Ki | = | 0.64 | nM | 9.19 |
| CHEMBL446141 | — | Ki | = | 0.65 | nM | 9.19 |
| CHEMBL290036 | — | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL50122 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL48485 | — | Ki | = | 0.73 | nM | 9.14 |
| CHEMBL296952 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL48759 | — | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL48377 | — | Ki | = | 0.89 | nM | 9.05 |
| CHEMBL15093 | PNU-91571 | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL49160 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL46013 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL298365 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL299072 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL50059 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL299133 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL294916 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL279867 | PANADIPLON | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL299326 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL300633 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL48839 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL48403 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL295216 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL49538 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL45807 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL45734 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL300059 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL50072 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL49388 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL298886 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL49888 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL48211 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL48924 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL12 | DIAZEPAM | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL299431 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL48418 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL45547 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL48209 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL296961 | — | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL48305 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL52097 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL295593 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL440478 | — | Ki | = | 143.0 | nM | 6.84 |