Assay Detail
Binding
CHEMBL652650
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity to displace [3H]flunitrazepam from Benzodiazepine receptor in bovine brain membrane
21
Total Activities
21
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 (CHEMBL2094107) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Bos taurus |
Publication
Tricyclic heteroaromatic systems. [1]benzopyranopyrrol-4-ones and [1]benzopyrano-1,2,3-triazol-4-ones as benzodiazepine receptor ligands. Synthesis and structure-activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.01 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | 4.0 | 1 | 9.30 |
| CHEMBL328802 | — | — | 1 | 8.07 |
| CHEMBL90098 | — | — | 1 | 8.00 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.89 |
| CHEMBL453066 | BETA-CCM | — | 1 | 7.80 |
| CHEMBL316288 | — | — | 1 | 7.60 |
| CHEMBL313541 | — | — | 1 | 7.40 |
| CHEMBL88604 | — | — | 1 | 7.32 |
| CHEMBL330001 | — | — | 1 | 7.21 |
| CHEMBL91468 | — | — | 1 | 7.19 |
| CHEMBL297126 | — | — | 1 | 7.16 |
| CHEMBL49558 | — | — | 1 | 7.05 |
| CHEMBL313280 | — | — | 1 | 7.00 |
| CHEMBL88938 | — | — | 1 | 6.76 |
| CHEMBL330083 | — | — | 1 | 6.58 |
| CHEMBL90142 | — | — | 1 | 6.55 |
| CHEMBL412671 | — | — | 1 | 6.12 |
| CHEMBL91040 | — | — | 1 | 6.00 |
| CHEMBL90109 | — | — | 1 | 5.60 |
| CHEMBL313315 | — | — | 1 | 5.57 |
| CHEMBL90222 | — | — | 1 | 5.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL407 | FLUMAZENIL | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL328802 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL90098 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL453066 | BETA-CCM | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL316288 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL313541 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL88604 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL330001 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL91468 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL297126 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL49558 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL313280 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL88938 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL330083 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL90142 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL412671 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL91040 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL90109 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL313315 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL90222 | — | IC50 | = | 7500.0 | nM | 5.12 |