Assay Detail
Binding
CHEMBL650829
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards Benzodiazepine receptor from bovine brain membrane using [3H]Ro-151788 as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2093872) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.64 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.05 |
| CHEMBL348367 | — | — | 1 | 9.00 |
| CHEMBL154342 | — | — | 1 | 8.77 |
| CHEMBL346677 | — | — | 1 | 8.20 |
| CHEMBL421983 | — | — | 1 | 8.17 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 8.00 |
| CHEMBL154754 | — | — | 1 | 7.94 |
| CHEMBL153980 | — | — | 1 | 7.88 |
| CHEMBL157109 | — | — | 1 | 7.61 |
| CHEMBL422158 | — | — | 1 | 7.36 |
| CHEMBL153979 | — | — | 1 | 6.86 |
| CHEMBL156846 | — | — | 1 | 6.77 |
| CHEMBL153195 | — | — | 1 | 6.57 |
| CHEMBL153252 | — | — | 1 | 6.31 |
| CHEMBL346379 | — | — | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL348367 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL154342 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL346677 | — | Ki | = | 6.26 | nM | 8.20 |
| CHEMBL421983 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL12 | DIAZEPAM | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL154754 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL153980 | — | Ki | = | 13.3 | nM | 7.88 |
| CHEMBL157109 | — | Ki | = | 24.4 | nM | 7.61 |
| CHEMBL422158 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL153979 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL156846 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL153195 | — | Ki | = | 272.0 | nM | 6.57 |
| CHEMBL153252 | — | Ki | = | 489.0 | nM | 6.31 |
| CHEMBL346379 | — | Ki | = | 680.0 | nM | 6.17 |