Assay Detail
Binding
CHEMBL757892
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Inhibition of PDE4 in the cytosol of human neutrophils
27
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.60 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL421528 | — | — | 1 | 8.40 |
| CHEMBL315815 | PYRIDOPYRIDAZINONE | — | 1 | 8.30 |
| CHEMBL313170 | — | — | 1 | 8.10 |
| CHEMBL314722 | — | — | 1 | 7.90 |
| CHEMBL85278 | — | — | 1 | 7.60 |
| CHEMBL315981 | — | — | 1 | 7.30 |
| CHEMBL313111 | — | — | 1 | 7.10 |
| CHEMBL440878 | — | — | 1 | 7.00 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 7.00 |
| CHEMBL83484 | — | — | 1 | 6.90 |
| CHEMBL313842 | ZARDAVERINE | 2.0 | 1 | 6.80 |
| CHEMBL84702 | — | — | 1 | 6.80 |
| CHEMBL316413 | — | — | 2 | 6.70 |
| CHEMBL84861 | — | — | 1 | 6.50 |
| CHEMBL85617 | — | — | 1 | 6.50 |
| CHEMBL85424 | — | — | 1 | 6.40 |
| CHEMBL85556 | — | — | 1 | 6.40 |
| CHEMBL2367714 | — | — | 1 | 6.10 |
| CHEMBL84874 | — | — | 1 | 5.90 |
| CHEMBL275448 | — | — | 1 | 5.80 |
| CHEMBL84860 | — | — | 1 | 5.80 |
| CHEMBL314167 | — | — | 1 | 5.80 |
| CHEMBL316442 | — | — | 1 | 5.30 |
| CHEMBL314183 | — | — | 1 | 5.30 |
| CHEMBL81921 | — | — | 1 | 5.20 |
| CHEMBL2367717 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL421528 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL315815 | PYRIDOPYRIDAZINONE | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL313170 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL314722 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL85278 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL315981 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL313111 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL440878 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL83484 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL313842 | ZARDAVERINE | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL84702 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL316413 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL84861 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL85617 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL85424 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL85556 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL316413 | — | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL2367714 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL84874 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL275448 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL84860 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL314167 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL316442 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL314183 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL81921 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL2367717 | — | IC50 | = | 7943.28 | nM | 5.10 |