Assay Detail
Binding
CHEMBL680655
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Binding affinity against Diazepam sensitive (DS) Gamma-aminobutyric acid A receptor in rat cerebellum.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Cerebellum |
| 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 | 21 | 8.88 | 10.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3144615 | — | — | 1 | 10.30 |
| CHEMBL3144841 | — | — | 1 | 10.05 |
| CHEMBL3144609 | — | — | 1 | 9.92 |
| CHEMBL19732 | CGS-8216 | — | 1 | 9.89 |
| CHEMBL269366 | RO-194603 | — | 1 | 9.70 |
| CHEMBL3144739 | — | — | 1 | 9.68 |
| CHEMBL3144753 | — | — | 1 | 9.64 |
| CHEMBL3144610 | — | — | 1 | 9.40 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.10 |
| CHEMBL3144617 | — | — | 1 | 9.06 |
| CHEMBL267665 | RO-147437 | — | 1 | 8.89 |
| CHEMBL46547 | SARMAZENIL | 2.0 | 1 | 8.70 |
| CHEMBL415293 | — | — | 1 | 8.40 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.28 |
| CHEMBL415290 | Ro-151310 | — | 1 | 8.27 |
| CHEMBL6862 | — | — | 1 | 7.61 |
| CHEMBL7069 | — | — | 1 | 7.57 |
| CHEMBL266943 | — | — | 1 | 7.53 |
| CHEMBL6826 | — | — | 1 | 6.74 |
| CHEMBL45299 | — | — | 1 | - |
| CHEMBL298322 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3144615 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL3144841 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL3144609 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL19732 | CGS-8216 | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL269366 | RO-194603 | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3144739 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL3144753 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL3144610 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3144617 | — | Ki | = | 0.88 | nM | 9.06 |
| CHEMBL267665 | RO-147437 | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL46547 | SARMAZENIL | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL415293 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL6597 | Ro-154513 | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL415290 | Ro-151310 | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL6862 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL7069 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL266943 | — | Ki | = | 29.8 | nM | 7.53 |
| CHEMBL6826 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL45299 | — | Ki | - | nM | - | |
| CHEMBL298322 | — | Ki | - | nM | - |