Assay Detail
Binding
CHEMBL648142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for Diazepam-Insensitive fraction of GABA-A benzodiazepine receptors
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.81 | 9.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6421 | — | — | 1 | 9.37 |
| CHEMBL6655 | — | — | 1 | 8.55 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.51 |
| CHEMBL7290 | — | — | 1 | 7.97 |
| CHEMBL415290 | Ro-151310 | — | 1 | 7.77 |
| CHEMBL7298 | — | — | 1 | 7.67 |
| CHEMBL268626 | — | — | 1 | 7.42 |
| CHEMBL6440 | — | — | 1 | 7.40 |
| CHEMBL173082 | — | — | 1 | 7.35 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 7.24 |
| CHEMBL267665 | RO-147437 | — | 1 | 6.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6421 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL6655 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL6597 | Ro-154513 | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL7290 | — | Ki | = | 10.8 | nM | 7.97 |
| CHEMBL415290 | Ro-151310 | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL7298 | — | Ki | = | 21.2 | nM | 7.67 |
| CHEMBL268626 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL6440 | — | Ki | = | 39.8 | nM | 7.40 |
| CHEMBL173082 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL267665 | RO-147437 | Ki | = | 214.0 | nM | 6.67 |