Assay Detail
Binding
CHEMBL650466
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]diazepam binding to GABA-A central benzodiazepine receptor of rat brain homogenate
49
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
6-(Alkylamino)-3-aryl-1,2,4-triazolo[3,4-a]phthalazines. A new class of benzodiazepine receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 49 | 7.10 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL273456 | — | — | 1 | 8.59 |
| CHEMBL12 | DIAZEPAM | 4.0 | 3 | 8.54 |
| CHEMBL269449 | — | — | 1 | 8.41 |
| CHEMBL14645 | — | — | 1 | 8.39 |
| CHEMBL14202 | — | — | 1 | 8.27 |
| CHEMBL13897 | — | — | 1 | 7.96 |
| CHEMBL13408 | — | — | 1 | 7.85 |
| CHEMBL13621 | — | — | 1 | 7.84 |
| CHEMBL14248 | — | — | 1 | 7.81 |
| CHEMBL13994 | — | — | 1 | 7.80 |
| CHEMBL13942 | — | — | 1 | 7.77 |
| CHEMBL14214 | — | — | 1 | 7.77 |
| CHEMBL14006 | — | — | 1 | 7.70 |
| CHEMBL14105 | — | — | 1 | 7.68 |
| CHEMBL14234 | — | — | 1 | 7.44 |
| CHEMBL13663 | — | — | 1 | 7.42 |
| CHEMBL13860 | — | — | 1 | 7.42 |
| CHEMBL278449 | — | — | 1 | 7.39 |
| CHEMBL13869 | — | — | 1 | 7.36 |
| CHEMBL274600 | — | — | 1 | 7.33 |
| CHEMBL13794 | — | — | 1 | 7.18 |
| CHEMBL14018 | — | — | 1 | 6.99 |
| CHEMBL274549 | — | — | 1 | 6.95 |
| CHEMBL430276 | — | — | 1 | 6.85 |
| CHEMBL275121 | — | — | 1 | 6.74 |
| CHEMBL441218 | — | — | 1 | 6.61 |
| CHEMBL273680 | — | — | 1 | 6.61 |
| CHEMBL14175 | — | — | 1 | 6.61 |
| CHEMBL13898 | — | — | 1 | 6.51 |
| CHEMBL13909 | — | — | 1 | 6.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL273456 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL12 | DIAZEPAM | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL269449 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL14645 | — | Ki | = | 4.1 | nM | 8.39 |
| CHEMBL14202 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL13897 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL13408 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL13621 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL14248 | — | Ki | = | 15.6 | nM | 7.81 |
| CHEMBL13994 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL13942 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL14214 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL14006 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL14105 | — | Ki | = | 20.8 | nM | 7.68 |
| CHEMBL14234 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL13860 | — | Ki | = | 37.6 | nM | 7.42 |
| CHEMBL13663 | — | Ki | = | 37.7 | nM | 7.42 |
| CHEMBL278449 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL13869 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL274600 | — | Ki | = | 46.3 | nM | 7.33 |
| CHEMBL13794 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL14018 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL274549 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL430276 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL12 | DIAZEPAM | Ki | = | 144.0 | nM | 6.84 |
| CHEMBL275121 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL441218 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL273680 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL14175 | — | Ki | = | 243.0 | nM | 6.61 |
| CHEMBL13909 | — | Ki | = | 307.0 | nM | 6.51 |
| CHEMBL13898 | — | Ki | = | 306.0 | nM | 6.51 |
| CHEMBL12 | DIAZEPAM | Ki | = | 323.0 | nM | 6.49 |
| CHEMBL276260 | — | Ki | = | 393.0 | nM | 6.41 |
| CHEMBL275315 | — | Ki | = | 565.0 | nM | 6.25 |
| CHEMBL428336 | — | Ki | = | 760.0 | nM | 6.12 |
| CHEMBL409557 | — | Ki | = | 908.0 | nM | 6.04 |
| CHEMBL14237 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL430297 | — | Ki | = | 1820.0 | nM | 5.74 |
| CHEMBL14316 | — | Ki | = | 1970.0 | nM | 5.71 |
| CHEMBL14191 | — | Ki | = | 1930.0 | nM | 5.71 |
| CHEMBL279839 | — | Ki | = | 2650.0 | nM | 5.58 |
| CHEMBL275566 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL275800 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL264473 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL273906 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL416345 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL274461 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL13628 | — | Ki | > | 3000.0 | nM | - |
| CHEMBL268006 | — | Ki | > | 3000.0 | nM | - |