Assay Detail
Binding
CHEMBL1041602
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PDE4D catalytic domain cloned from human HL60 cells assessed as inhibition of cAMP hydrolysis
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HL-60 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and biological evaluation of novel phthalazinone derivatives as topically active phosphodiesterase 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 8.49 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL593656 | — | — | 1 | 9.52 |
| CHEMBL594108 | — | — | 1 | 9.40 |
| CHEMBL594109 | — | — | 1 | 9.15 |
| CHEMBL595064 | — | — | 1 | 9.05 |
| CHEMBL593877 | — | — | 2 | 9.05 |
| CHEMBL595272 | — | — | 1 | 9.00 |
| CHEMBL596447 | — | — | 1 | 8.89 |
| CHEMBL592931 | — | — | 1 | 8.89 |
| CHEMBL596394 | — | — | 1 | 8.85 |
| CHEMBL595038 | — | — | 1 | 8.70 |
| CHEMBL605096 | — | — | 1 | 8.37 |
| CHEMBL595959 | — | — | 1 | 8.28 |
| CHEMBL603626 | — | — | 1 | 8.09 |
| CHEMBL595039 | — | — | 1 | 8.01 |
| CHEMBL605935 | — | — | 1 | 7.84 |
| CHEMBL603194 | — | — | 1 | 7.79 |
| CHEMBL592942 | — | — | 1 | 7.34 |
| CHEMBL440878 | — | — | 1 | 7.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL593656 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL594108 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL594109 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL595064 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL593877 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL595272 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL596447 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL592931 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL596394 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL595038 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL605096 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL595959 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL603626 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL593877 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL595039 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL605935 | — | IC50 | = | 14.3 | nM | 7.84 |
| CHEMBL603194 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL592942 | — | IC50 | = | 45.9 | nM | 7.34 |
| CHEMBL440878 | — | IC50 | = | 85.0 | nM | 7.07 |