Assay Detail
Binding
CHEMBL784398
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Binding affinity against high affinity rolipram binding site (HARBS) was determined by displacing radioactive [3H]rolipram from brain membrane suspensions of Wistar rats
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.13 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 8.30 |
| CHEMBL125123 | — | — | 1 | 5.96 |
| CHEMBL332854 | — | — | 1 | - |
| CHEMBL419791 | — | — | 1 | - |
| CHEMBL339749 | — | — | 1 | - |
| CHEMBL332853 | — | — | 1 | - |
| CHEMBL125828 | — | — | 1 | - |
| CHEMBL126581 | — | — | 1 | - |
| CHEMBL111925 | — | — | 1 | - |
| CHEMBL338684 | — | — | 1 | - |
| CHEMBL341304 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63 | ROLIPRAM | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL125123 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL332854 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL419791 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL339749 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL332853 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL125828 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL126581 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL111925 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL338684 | — | IC50 | > | 3000.0 | nM | - |
| CHEMBL341304 | — | IC50 | > | 2000.0 | nM | - |