Assay Detail
Binding
CHEMBL652658
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of [3H]- flumazenil binding to benzodiazepine receptor in bovine brain membranes
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Brain membranes |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL2094107) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Bos taurus |
Publication
Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 40 | 6.86 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL452 | CLONAZEPAM | 4.0 | 1 | 9.07 |
| CHEMBL74448 | — | — | 1 | 7.96 |
| CHEMBL308760 | — | — | 1 | 7.96 |
| CHEMBL75456 | — | — | 1 | 7.77 |
| CHEMBL74302 | — | — | 1 | 7.68 |
| CHEMBL521901 | — | — | 1 | 7.55 |
| CHEMBL75212 | — | — | 1 | 7.52 |
| CHEMBL74596 | — | — | 1 | 7.47 |
| CHEMBL306719 | — | — | 1 | 7.35 |
| CHEMBL75306 | — | — | 1 | 7.28 |
| CHEMBL75884 | — | — | 1 | 7.26 |
| CHEMBL73288 | — | — | 1 | 7.17 |
| CHEMBL75941 | — | — | 1 | 7.11 |
| CHEMBL2115163 | — | — | 1 | 7.10 |
| CHEMBL306370 | — | — | 1 | 7.03 |
| CHEMBL2114131 | — | — | 1 | 7.00 |
| CHEMBL74037 | — | — | 1 | 6.99 |
| CHEMBL73631 | — | — | 1 | 6.98 |
| CHEMBL74280 | — | — | 1 | 6.97 |
| CHEMBL74748 | — | — | 1 | 6.95 |
| CHEMBL75307 | — | — | 1 | 6.93 |
| CHEMBL75289 | — | — | 1 | 6.92 |
| CHEMBL31796 | — | — | 1 | 6.91 |
| CHEMBL74392 | — | — | 1 | 6.82 |
| CHEMBL306310 | — | — | 1 | 6.79 |
| CHEMBL72505 | — | — | 1 | 6.69 |
| CHEMBL306307 | — | — | 1 | 6.62 |
| CHEMBL74013 | — | — | 1 | 6.37 |
| CHEMBL75836 | — | — | 1 | 6.31 |
| CHEMBL74589 | — | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL452 | CLONAZEPAM | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL74448 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL308760 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL75456 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL74302 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL521901 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL75212 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL74596 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL306719 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL75306 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL75884 | — | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL73288 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL75941 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL2115163 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL306370 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL2114131 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL74037 | — | Ki | = | 103.0 | nM | 6.99 |
| CHEMBL73631 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL74280 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL74748 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL75307 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL75289 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL31796 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL74392 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL306310 | — | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL72505 | — | Ki | = | 203.0 | nM | 6.69 |
| CHEMBL306307 | — | Ki | = | 241.0 | nM | 6.62 |
| CHEMBL74013 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL75836 | — | Ki | = | 494.0 | nM | 6.31 |
| CHEMBL74589 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL307139 | — | Ki | = | 620.0 | nM | 6.21 |
| CHEMBL495592 | — | Ki | = | 675.0 | nM | 6.17 |
| CHEMBL73571 | — | Ki | = | 695.0 | nM | 6.16 |
| CHEMBL76102 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL75997 | — | Ki | = | 1150.0 | nM | 5.94 |
| CHEMBL74213 | — | Ki | = | 1168.0 | nM | 5.93 |
| CHEMBL75406 | — | Ki | = | 1307.0 | nM | 5.88 |
| CHEMBL74154 | — | Ki | = | 1370.0 | nM | 5.86 |
| CHEMBL307467 | — | Ki | = | 1950.0 | nM | 5.71 |
| CHEMBL75460 | — | Ki | = | 2700.0 | nM | 5.57 |