Assay Detail
Binding
CHEMBL769677
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of phosphodiesterase 4 extracted from human U937 cells by using radioligands [3H]-cAMP or [3H]cGMP.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | U-937 |
| 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 | 21 | 5.84 | 6.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL125671 | — | — | 1 | 6.48 |
| CHEMBL123266 | — | — | 1 | 6.39 |
| CHEMBL341304 | — | — | 1 | 6.20 |
| CHEMBL340860 | — | — | 1 | 6.19 |
| CHEMBL125123 | — | — | 1 | 6.15 |
| CHEMBL419791 | — | — | 1 | 6.12 |
| CHEMBL339749 | — | — | 1 | 6.12 |
| CHEMBL338684 | — | — | 1 | 6.02 |
| CHEMBL123782 | — | — | 1 | 5.94 |
| CHEMBL111925 | — | — | 1 | 5.94 |
| CHEMBL332854 | — | — | 1 | 5.90 |
| CHEMBL126581 | — | — | 1 | 5.79 |
| CHEMBL332853 | — | — | 1 | 5.75 |
| CHEMBL339408 | — | — | 1 | 5.58 |
| CHEMBL420335 | — | — | 1 | 5.40 |
| CHEMBL125828 | — | — | 1 | 5.38 |
| CHEMBL338657 | — | — | 1 | 4.00 |
| CHEMBL331051 | — | — | 1 | - |
| CHEMBL306760 | — | — | 1 | - |
| CHEMBL333994 | — | — | 1 | - |
| CHEMBL333585 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL125671 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL123266 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL341304 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL340860 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL125123 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL419791 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL339749 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL338684 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL123782 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL111925 | — | IC50 | = | 1140.0 | nM | 5.94 |
| CHEMBL332854 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL126581 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL332853 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL339408 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL420335 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL125828 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL338657 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL331051 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL306760 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL333994 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL333585 | — | IC50 | > | 100000.0 | nM | - |