Assay Detail
Binding
CHEMBL990634
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Displacement of [3H]flunitrazepam from GABAA benzodiazepine receptor in rat brain membrane
11
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.47 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL483385 | — | — | 3 | 8.82 |
| CHEMBL646 | TRIAZOLAM | 4.0 | 1 | 8.81 |
| CHEMBL12 | DIAZEPAM | 4.0 | 1 | 7.67 |
| CHEMBL519656 | — | — | 3 | 7.34 |
| CHEMBL285674 | ESTAZOLAM | 4.0 | 1 | 7.33 |
| CHEMBL483384 | — | — | 2 | 7.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL483385 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL646 | TRIAZOLAM | IC50 | = | 1.54 | nM | 8.81 |
| CHEMBL483385 | — | IC50 | = | 4.35 | nM | 8.36 |
| CHEMBL483385 | — | IC50 | = | 8.77 | nM | 8.06 |
| CHEMBL12 | DIAZEPAM | IC50 | = | 21.2 | nM | 7.67 |
| CHEMBL519656 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL285674 | ESTAZOLAM | IC50 | = | 46.6 | nM | 7.33 |
| CHEMBL483384 | — | IC50 | = | 93.6 | nM | 7.03 |
| CHEMBL519656 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL483384 | — | IC50 | = | 394.0 | nM | 6.41 |
| CHEMBL519656 | — | IC50 | = | 2320.0 | nM | 5.63 |