Assay Detail
Binding
CHEMBL648139
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for Diazepam sensitive (DS) isoform of the benzodiazepine (Bz) binding site on GABAA receptors
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthetic and computer-assisted analysis of the structural requirements for selective, high-affinity ligand binding to diazepam-insensitive benzodiazepine receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 48 | 8.28 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54338 | — | — | 1 | 10.00 |
| CHEMBL46547 | SARMAZENIL | 2.0 | 1 | 9.70 |
| CHEMBL269366 | RO-194603 | — | 1 | 9.70 |
| CHEMBL298777 | — | — | 1 | 9.70 |
| CHEMBL432891 | — | — | 1 | 9.70 |
| CHEMBL54069 | — | — | 1 | 9.40 |
| CHEMBL444045 | — | — | 1 | 9.30 |
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.10 |
| CHEMBL646 | TRIAZOLAM | 4.0 | 1 | 9.10 |
| CHEMBL294218 | — | — | 1 | 9.10 |
| CHEMBL173082 | — | — | 1 | 9.05 |
| CHEMBL6752 | — | — | 1 | 9.05 |
| CHEMBL301180 | — | — | 1 | 9.00 |
| CHEMBL51700 | — | — | 1 | 9.00 |
| CHEMBL7298 | — | — | 1 | 8.96 |
| CHEMBL54316 | — | — | 1 | 8.96 |
| CHEMBL267665 | RO-147437 | — | 1 | 8.89 |
| CHEMBL268626 | — | — | 1 | 8.85 |
| CHEMBL301513 | — | — | 1 | 8.82 |
| CHEMBL54884 | — | — | 1 | 8.74 |
| CHEMBL53072 | — | — | 1 | 8.72 |
| CHEMBL52668 | — | — | 1 | 8.66 |
| CHEMBL912 | FLUMAZENIL METHYLESTER | — | 1 | 8.51 |
| CHEMBL415293 | — | — | 1 | 8.40 |
| CHEMBL301931 | — | — | 1 | 8.29 |
| CHEMBL6597 | Ro-154513 | — | 1 | 8.28 |
| CHEMBL415290 | Ro-151310 | — | 1 | 8.27 |
| CHEMBL7009 | — | — | 1 | 8.20 |
| CHEMBL300027 | — | — | 1 | 8.12 |
| CHEMBL6440 | — | — | 1 | 8.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54338 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL46547 | SARMAZENIL | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL432891 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL269366 | RO-194603 | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL298777 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL54069 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL444045 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL407 | FLUMAZENIL | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL646 | TRIAZOLAM | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL294218 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL173082 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL6752 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL301180 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL51700 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL54316 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL7298 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL267665 | RO-147437 | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL268626 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL301513 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL54884 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL53072 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL52668 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL912 | FLUMAZENIL METHYLESTER | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL415293 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL301931 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL6597 | Ro-154513 | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL415290 | Ro-151310 | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL7009 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL300027 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL6440 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL6861 | — | Ki | = | 10.5 | nM | 7.98 |
| CHEMBL52934 | — | Ki | = | 13.7 | nM | 7.86 |
| CHEMBL6862 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL7069 | — | Ki | = | 26.9 | nM | 7.57 |
| CHEMBL266943 | — | Ki | = | 29.8 | nM | 7.53 |
| CHEMBL51740 | — | Ki | = | 39.2 | nM | 7.41 |
| CHEMBL416125 | — | Ki | = | 65.2 | nM | 7.19 |
| CHEMBL269705 | RO-145975 | Ki | = | 72.6 | nM | 7.14 |
| CHEMBL53425 | — | Ki | = | 88.4 | nM | 7.05 |
| CHEMBL6826 | — | Ki | = | 184.0 | nM | 6.74 |
| CHEMBL301369 | — | Ki | = | 378.0 | nM | 6.42 |
| CHEMBL53285 | — | Ki | = | 391.0 | nM | 6.41 |
| CHEMBL6793 | — | Ki | = | 499.3 | nM | 6.30 |
| CHEMBL53119 | — | Ki | = | 907.1 | nM | 6.04 |
| CHEMBL291473 | — | Ki | = | 1209.0 | nM | 5.92 |
| CHEMBL291497 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL301655 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL3350122 | — | Ki | > | 100.0 | nM | - |