Assay Detail
Binding
CHEMBL680654
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against Diazepam insensitive (DI) Gamma-aminobutyric acid A receptor
33
Total Activities
31
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 of novel imidazobenzodiazepines as probes of the pharmacophore for "diazepam-insensitive" GABAA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.63 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415293 | — | — | 1 | 8.77 |
| CHEMBL3144617 | — | — | 1 | 8.72 |
| CHEMBL3144753 | — | — | 1 | 8.72 |
| CHEMBL269366 | RO-194603 | — | 1 | 8.59 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.51 |
| CHEMBL3144615 | — | — | 1 | 8.29 |
| CHEMBL3144739 | — | — | 1 | 8.03 |
| CHEMBL3144610 | — | — | 1 | 8.00 |
| CHEMBL415290 | Ro-151310 | — | 1 | 7.77 |
| CHEMBL46547 | SARMAZENIL | 2.0 | 1 | 7.70 |
| CHEMBL46482 | — | — | 1 | 7.62 |
| CHEMBL3144609 | — | — | 1 | 7.58 |
| CHEMBL6862 | — | — | 1 | 7.48 |
| CHEMBL416450 | — | — | 1 | 7.39 |
| CHEMBL19732 | CGS-8216 | — | 1 | 7.34 |
| CHEMBL3144841 | — | — | 1 | 7.33 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 7.24 |
| CHEMBL266943 | — | — | 1 | 6.91 |
| CHEMBL7069 | — | — | 1 | 6.91 |
| CHEMBL267665 | RO-147437 | — | 1 | 6.67 |
| CHEMBL44784 | — | — | 2 | 6.27 |
| CHEMBL43718 | — | — | 2 | 6.11 |
| CHEMBL45174 | — | — | 1 | - |
| CHEMBL295277 | — | — | 1 | - |
| CHEMBL6826 | — | — | 1 | - |
| CHEMBL46957 | — | — | 1 | - |
| CHEMBL43724 | — | — | 1 | - |
| CHEMBL45346 | — | — | 1 | - |
| CHEMBL295981 | — | — | 1 | - |
| CHEMBL43725 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415293 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL3144617 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3144753 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL269366 | RO-194603 | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL6597 | Ro-154513 | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3144615 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL3144739 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL3144610 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL415290 | Ro-151310 | Ki | = | 16.9 | nM | 7.77 |
| CHEMBL46547 | SARMAZENIL | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL46482 | — | Ki | = | 23.8 | nM | 7.62 |
| CHEMBL3144609 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL6862 | — | Ki | = | 33.3 | nM | 7.48 |
| CHEMBL416450 | — | Ki | = | 40.9 | nM | 7.39 |
| CHEMBL19732 | CGS-8216 | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3144841 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL7069 | — | Ki | = | 122.6 | nM | 6.91 |
| CHEMBL266943 | — | Ki | = | 123.5 | nM | 6.91 |
| CHEMBL267665 | RO-147437 | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL44784 | — | Ki | = | 540.0 | nM | 6.27 |
| CHEMBL43718 | — | Ki | = | 778.0 | nM | 6.11 |
| CHEMBL6826 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL45346 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL47853 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL295981 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL43724 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL46957 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL44784 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL43718 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL295277 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL45174 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL43725 | — | Ki | > | 1000.0 | nM | - |