Assay Detail
Binding
CHEMBL760947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against phosphodiesterase 1/5 (PDE1/5) extracted from guinea pig trachea smooth muscle cells by using radioligands [3H]-cAMP or [3H]cGMP
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Trachea |
| 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 | 17 | 4.14 | 4.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL332853 | — | — | 1 | 4.40 |
| CHEMBL126581 | — | — | 1 | 4.18 |
| CHEMBL339749 | — | — | 1 | 4.14 |
| CHEMBL338657 | — | — | 1 | 4.00 |
| CHEMBL340860 | — | — | 1 | 4.00 |
| CHEMBL333585 | — | — | 1 | - |
| CHEMBL420335 | — | — | 1 | - |
| CHEMBL123266 | — | — | 1 | - |
| CHEMBL419791 | — | — | 1 | - |
| CHEMBL125123 | — | — | 1 | - |
| CHEMBL123782 | — | — | 1 | - |
| CHEMBL339408 | — | — | 1 | - |
| CHEMBL125828 | — | — | 1 | - |
| CHEMBL111925 | — | — | 1 | - |
| CHEMBL341304 | — | — | 1 | - |
| CHEMBL332854 | — | — | 1 | - |
| CHEMBL125671 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL332853 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL126581 | — | IC50 | = | 65300.0 | nM | 4.18 |
| CHEMBL339749 | — | IC50 | = | 71700.0 | nM | 4.14 |
| CHEMBL338657 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL340860 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL333585 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL420335 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL123266 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL419791 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125123 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL123782 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL339408 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125828 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL111925 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL341304 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL332854 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125671 | — | IC50 | > | 100000.0 | nM | - |