Assay Detail
Binding
CHEMBL653129
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In vitro binding affinity against benzodiazepine receptor using [3H]diazepam as radioligand
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Benzodiazepine receptor binding and anticonflict activity in a series of 3,6-disubstituted pyridazino[4,3-c]isoquinolines devoid of anticonvulsant properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 26 | 6.47 | 8.71 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 8.71 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.54 |
| CHEMBL25258 | — | — | 1 | 7.94 |
| CHEMBL24296 | — | — | 1 | 7.73 |
| CHEMBL278576 | — | — | 1 | 7.55 |
| CHEMBL278089 | — | — | 1 | 7.20 |
| CHEMBL24131 | — | — | 1 | 7.19 |
| CHEMBL25993 | — | — | 1 | 7.16 |
| CHEMBL282201 | — | — | 1 | 6.87 |
| CHEMBL283784 | — | — | 1 | 6.82 |
| CHEMBL13662 | CI-218872 | — | 1 | 6.70 |
| CHEMBL24676 | — | — | 1 | 6.66 |
| CHEMBL25683 | — | — | 1 | 6.61 |
| CHEMBL25538 | — | — | 1 | 6.40 |
| CHEMBL28333 | MEDAZEPAM | 2.0 | 1 | 6.28 |
| CHEMBL280930 | — | — | 1 | 6.18 |
| CHEMBL274757 | — | — | 1 | 5.93 |
| CHEMBL27330 | — | — | 1 | 5.82 |
| CHEMBL28204 | — | — | 1 | 5.77 |
| CHEMBL26642 | — | — | 1 | 5.72 |
| CHEMBL25281 | — | — | 1 | 5.46 |
| CHEMBL263718 | — | — | 1 | 5.40 |
| CHEMBL283090 | — | — | 1 | 5.21 |
| CHEMBL25696 | — | — | 1 | 5.03 |
| CHEMBL283507 | — | — | 1 | 4.75 |
| CHEMBL281405 | — | — | 1 | 4.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 1.94 | nM | 8.71 |
| CHEMBL12 | DIAZEPAM | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL25258 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL24296 | — | Ki | = | 18.7 | nM | 7.73 |
| CHEMBL278576 | — | Ki | = | 28.4 | nM | 7.55 |
| CHEMBL278089 | — | Ki | = | 63.3 | nM | 7.20 |
| CHEMBL24131 | — | Ki | = | 65.2 | nM | 7.19 |
| CHEMBL25993 | — | Ki | = | 69.6 | nM | 7.16 |
| CHEMBL282201 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL283784 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL13662 | CI-218872 | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL24676 | — | Ki | = | 221.0 | nM | 6.66 |
| CHEMBL25683 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL25538 | — | Ki | = | 402.0 | nM | 6.40 |
| CHEMBL28333 | MEDAZEPAM | Ki | = | 528.0 | nM | 6.28 |
| CHEMBL280930 | — | Ki | = | 658.0 | nM | 6.18 |
| CHEMBL274757 | — | Ki | = | 1180.0 | nM | 5.93 |
| CHEMBL27330 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL28204 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL26642 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL25281 | — | Ki | = | 3480.0 | nM | 5.46 |
| CHEMBL263718 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL283090 | — | Ki | = | 6200.0 | nM | 5.21 |
| CHEMBL25696 | — | Ki | = | 9300.0 | nM | 5.03 |
| CHEMBL283507 | — | Ki | = | 17800.0 | nM | 4.75 |
| CHEMBL281405 | — | Ki | = | 32500.0 | nM | 4.49 |