Assay Detail
Binding
CHEMBL768654
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human platelet PDE by inhibiting cyclic Guanosine monophosphate (cGMP) hydrolysis
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL2652) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
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 | 38 | 4.72 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL88444 | — | — | 1 | 5.52 |
| CHEMBL90237 | — | — | 1 | 5.30 |
| CHEMBL431799 | — | — | 1 | 5.30 |
| CHEMBL90804 | — | — | 1 | 5.26 |
| CHEMBL91368 | — | — | 1 | 5.22 |
| CHEMBL91422 | — | — | 1 | 5.16 |
| CHEMBL91295 | — | — | 1 | 5.16 |
| CHEMBL91527 | — | — | 1 | 5.16 |
| CHEMBL92363 | — | — | 1 | 5.10 |
| CHEMBL88764 | — | — | 1 | 5.00 |
| CHEMBL90601 | — | — | 1 | 5.00 |
| CHEMBL421885 | — | — | 1 | 5.00 |
| CHEMBL88265 | — | — | 1 | 5.00 |
| CHEMBL88583 | — | — | 1 | 4.70 |
| CHEMBL91478 | — | — | 1 | 4.70 |
| CHEMBL313463 | — | — | 1 | 4.52 |
| CHEMBL91224 | — | — | 1 | 4.52 |
| CHEMBL760 | ANAGRELIDE | 4.0 | 1 | 4.47 |
| CHEMBL89660 | — | — | 1 | 4.40 |
| CHEMBL330677 | — | — | 1 | 4.30 |
| CHEMBL88525 | — | — | 1 | 4.30 |
| CHEMBL313282 | — | — | 1 | 4.22 |
| CHEMBL91044 | — | — | 1 | 4.22 |
| CHEMBL92264 | — | — | 1 | 4.00 |
| CHEMBL91634 | — | — | 1 | 4.00 |
| CHEMBL328149 | — | — | 1 | 4.00 |
| CHEMBL88395 | — | — | 1 | 4.00 |
| CHEMBL90195 | — | — | 1 | - |
| CHEMBL88245 | — | — | 1 | - |
| CHEMBL90414 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL88444 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL90237 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL431799 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL90804 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL91368 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL91422 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL91295 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL91527 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL92363 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL421885 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL88265 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL90601 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL88764 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL88583 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL91478 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL313463 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL91224 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL760 | ANAGRELIDE | IC50 | = | 34000.0 | nM | 4.47 |
| CHEMBL89660 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL330677 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL88525 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL313282 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL91044 | — | IC50 | = | 60000.0 | nM | 4.22 |
| CHEMBL92264 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL91634 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL328149 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL88395 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL91837 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL88136 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL88218 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL91843 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL89679 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL91356 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL330280 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL90677 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL90414 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL88245 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL90195 | — | IC50 | > | 100000.0 | nM | - |