Assay Detail
Binding
CHEMBL650179
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of binding of tritiated 3[H]diazepam radioligand to rat brain homogenates
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
Synthesis, benzodiazepine receptor binding, and anticonvulsant activity of 2,3-dihydro-3-oxo-5H-pyrido[3,4-b][1,4]benzothiazine-4-carbonitriles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.53 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL169612 | — | — | 1 | 6.50 |
| CHEMBL165820 | — | — | 1 | 6.50 |
| CHEMBL169918 | — | — | 1 | 6.40 |
| CHEMBL451 | CHLORDIAZEPOXIDE | 4.0 | 1 | 6.36 |
| CHEMBL168400 | — | — | 1 | 6.35 |
| CHEMBL169604 | — | — | 1 | 6.20 |
| CHEMBL169603 | — | — | 1 | 6.10 |
| CHEMBL169501 | — | — | 1 | 6.04 |
| CHEMBL169324 | — | — | 1 | 5.77 |
| CHEMBL169384 | — | — | 1 | 5.37 |
| CHEMBL169413 | — | — | 1 | 5.12 |
| CHEMBL169719 | — | — | 1 | 5.10 |
| CHEMBL169484 | — | — | 1 | 4.96 |
| CHEMBL166450 | — | — | 1 | 4.77 |
| CHEMBL413346 | — | — | 1 | 4.46 |
| CHEMBL451497 | — | — | 1 | 4.00 |
| CHEMBL166391 | — | — | 1 | 4.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL169612 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL165820 | — | IC50 | = | 314.0 | nM | 6.50 |
| CHEMBL169918 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL451 | CHLORDIAZEPOXIDE | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL168400 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL169604 | — | IC50 | = | 634.0 | nM | 6.20 |
| CHEMBL169603 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL169501 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL169324 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL169384 | — | IC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL169413 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL169719 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL169484 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL166450 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL413346 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL451497 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL166391 | — | IC50 | = | 100000.0 | nM | 4.00 |