Assay Detail
Binding
CHEMBL768653
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Inhibition of human platelet PDE by inhibiting cyclic Adenosine monophosphate (cAMP) hydrolysis
76
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 76 | 7.39 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL88108 | — | — | 1 | 9.52 |
| CHEMBL431799 | — | — | 1 | 9.40 |
| CHEMBL90804 | — | — | 1 | 9.30 |
| CHEMBL92264 | — | — | 1 | 9.00 |
| CHEMBL88245 | — | — | 1 | 9.00 |
| CHEMBL90237 | — | — | 1 | 8.70 |
| CHEMBL91368 | — | — | 1 | 8.70 |
| CHEMBL90677 | — | — | 1 | 8.70 |
| CHEMBL88444 | — | — | 1 | 8.70 |
| CHEMBL88835 | — | — | 1 | 8.52 |
| CHEMBL69139 | LIXAZINONE | 2.0 | 1 | 8.52 |
| CHEMBL91527 | — | — | 1 | 8.52 |
| CHEMBL89679 | — | — | 1 | 8.40 |
| CHEMBL91295 | — | — | 1 | 8.40 |
| CHEMBL91224 | — | — | 1 | 8.30 |
| CHEMBL313463 | — | — | 1 | 8.30 |
| CHEMBL328149 | — | — | 1 | 8.30 |
| CHEMBL88799 | — | — | 1 | 8.22 |
| CHEMBL91478 | — | — | 1 | 8.22 |
| CHEMBL92269 | — | — | 1 | 8.22 |
| CHEMBL90168 | — | — | 1 | 8.15 |
| CHEMBL330280 | — | — | 1 | 8.10 |
| CHEMBL330677 | — | — | 1 | 8.05 |
| CHEMBL93688 | — | — | 1 | 8.00 |
| CHEMBL88583 | — | — | 1 | 8.00 |
| CHEMBL90120 | — | — | 1 | 8.00 |
| CHEMBL314763 | — | — | 1 | 7.70 |
| CHEMBL88265 | — | — | 1 | 7.70 |
| CHEMBL90195 | — | — | 1 | 7.70 |
| CHEMBL91570 | — | — | 1 | 7.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL88108 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL431799 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL90804 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL92264 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL88245 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL90237 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL91368 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL90677 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL88444 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL88835 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL69139 | LIXAZINONE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL91527 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL91295 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL89679 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL328149 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL91224 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL313463 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL88799 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL91478 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL92269 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL90168 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL330280 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL330677 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL90120 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL93688 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL88583 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL314763 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL88265 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL90195 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL91570 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL90414 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL91259 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL423864 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL91843 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL88218 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL88955 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL89876 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL313609 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL88708 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL90958 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL89660 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL92158 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL91899 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL760 | ANAGRELIDE | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL88224 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL91204 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL91837 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL88525 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL90477 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL314093 | — | IC50 | = | 80.0 | nM | 7.10 |