Assay Detail
Binding
CHEMBL764832
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Inhibitory activity against phosphodiesterase 3 (PDE3) purified from bovine heart
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Potent tetracyclic guanine inhibitors of PDE1 and PDE5 cyclic guanosine monophosphate phosphodiesterases with oral antihypertensive activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 51 | 4.62 | 6.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL304389 | — | — | 1 | 6.00 |
| CHEMBL308249 | — | — | 1 | 5.46 |
| CHEMBL306666 | — | — | 1 | 5.22 |
| CHEMBL431377 | — | — | 1 | 5.16 |
| CHEMBL71204 | — | — | 1 | 4.96 |
| CHEMBL18745 | — | — | 1 | 4.92 |
| CHEMBL308828 | — | — | 1 | 4.92 |
| CHEMBL18744 | — | — | 1 | 4.82 |
| CHEMBL305237 | — | — | 1 | 4.77 |
| CHEMBL72812 | — | — | 1 | 4.60 |
| CHEMBL409425 | — | — | 1 | 4.60 |
| CHEMBL303154 | — | — | 1 | 4.58 |
| CHEMBL446663 | — | — | 1 | 4.52 |
| CHEMBL305988 | — | — | 1 | 4.52 |
| CHEMBL307640 | — | — | 1 | 4.50 |
| CHEMBL303385 | — | — | 1 | 4.46 |
| CHEMBL305989 | — | — | 1 | 4.44 |
| CHEMBL303917 | — | — | 1 | 4.35 |
| CHEMBL70837 | — | — | 1 | 4.30 |
| CHEMBL70295 | — | — | 1 | 4.30 |
| CHEMBL305617 | — | — | 1 | 4.24 |
| CHEMBL307379 | — | — | 1 | 4.14 |
| CHEMBL275204 | — | — | 1 | 4.10 |
| CHEMBL68152 | — | — | 1 | 4.10 |
| CHEMBL70471 | — | — | 1 | 4.07 |
| CHEMBL68706 | — | — | 1 | 4.05 |
| CHEMBL71300 | — | — | 1 | - |
| CHEMBL306426 | — | — | 1 | - |
| CHEMBL70569 | — | — | 1 | - |
| CHEMBL422235 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL304389 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL308249 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL306666 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL431377 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL71204 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL18745 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL308828 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL18744 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL305237 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL72812 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL409425 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL303154 | — | IC50 | = | 26000.0 | nM | 4.58 |
| CHEMBL446663 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL305988 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL307640 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL303385 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL305989 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL303917 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL70837 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL70295 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL305617 | — | IC50 | = | 57000.0 | nM | 4.24 |
| CHEMBL307379 | — | IC50 | = | 72000.0 | nM | 4.14 |
| CHEMBL275204 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL68152 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL70471 | — | IC50 | = | 85000.0 | nM | 4.07 |
| CHEMBL68706 | — | IC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL305618 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL308199 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL69324 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL430802 | — | IC50 | = | 130000.0 | nM | - |
| CHEMBL28079 | ZAPRINAST | IC50 | = | 122000.0 | nM | - |
| CHEMBL306417 | — | IC50 | = | 120000.0 | nM | - |
| CHEMBL70951 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL278644 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL71752 | VINPOCETINE | IC50 | > | 300000.0 | nM | - |
| CHEMBL303010 | — | IC50 | = | 110000.0 | nM | - |
| CHEMBL307232 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL308973 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL71300 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL431772 | — | IC50 | = | 111000.0 | nM | - |
| CHEMBL304161 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL419447 | — | IC50 | = | 175000.0 | nM | - |
| CHEMBL303671 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL307639 | — | IC50 | = | 240000.0 | nM | - |
| CHEMBL71874 | — | IC50 | = | 180000.0 | nM | - |
| CHEMBL71824 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL308747 | — | IC50 | = | 150000.0 | nM | - |
| CHEMBL422235 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL70569 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL306426 | — | IC50 | = | 110000.0 | nM | - |