Assay Detail
Binding
CHEMBL759867
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Inhibition of dual cGMP-inhibited phosphodiesterase 3 (PDE3) was determined in homogenates from human platelets.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.60 | 7.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38017 | — | — | 1 | 7.90 |
| CHEMBL61116 | — | — | 1 | 7.50 |
| CHEMBL61699 | — | — | 1 | 7.10 |
| CHEMBL61667 | — | — | 1 | 7.10 |
| CHEMBL64052 | — | — | 1 | 7.00 |
| CHEMBL432717 | — | — | 1 | 6.90 |
| CHEMBL62131 | — | — | 1 | 6.70 |
| CHEMBL304715 | — | — | 1 | 6.70 |
| CHEMBL64824 | — | — | 1 | 6.70 |
| CHEMBL293589 | — | — | 1 | 6.60 |
| CHEMBL282765 | TETRAHYDROBENXIMIDAZOLE | — | 1 | 6.30 |
| CHEMBL61822 | — | — | 1 | 6.30 |
| CHEMBL313842 | ZARDAVERINE | 2.0 | 1 | 6.20 |
| CHEMBL64544 | — | — | 1 | 6.10 |
| CHEMBL59953 | — | — | 1 | 5.90 |
| CHEMBL60026 | — | — | 1 | 5.80 |
| CHEMBL294327 | — | — | 1 | 5.40 |
| CHEMBL303550 | — | — | 1 | - |
| CHEMBL60999 | — | — | 1 | - |
| CHEMBL60839 | — | — | 1 | - |
| CHEMBL59996 | — | — | 1 | - |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38017 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL61116 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL61699 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL61667 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL64052 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL432717 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL62131 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL304715 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL64824 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL293589 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL282765 | TETRAHYDROBENXIMIDAZOLE | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL61822 | — | IC50 | = | 501.19 | nM | 6.30 |
| CHEMBL313842 | ZARDAVERINE | IC50 | = | 630.96 | nM | 6.20 |
| CHEMBL64544 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL59953 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL60026 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL294327 | — | IC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL303550 | — | IC50 | < | 10000.0 | nM | - |
| CHEMBL60999 | — | IC50 | < | 10000.0 | nM | - |
| CHEMBL60839 | — | IC50 | < | 10000.0 | nM | - |
| CHEMBL59996 | — | IC50 | < | 10000.0 | nM | - |
| CHEMBL511115 | CILOMILAST | IC50 | < | 10000.0 | nM | - |