Assay Detail
Binding
CHEMBL2433334
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Inhibition of PDE3A (unknown origin)
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A (CHEMBL241) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.77 | 6.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2431835 | — | — | 1 | 6.23 |
| CHEMBL2431834 | — | — | 1 | 5.90 |
| CHEMBL2431826 | — | — | 1 | 5.75 |
| CHEMBL2431822 | — | — | 1 | 5.54 |
| CHEMBL2431819 | — | — | 1 | 5.45 |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2431835 | — | IC50 | = | 589.0 | nM | 6.23 |
| CHEMBL2431834 | — | IC50 | = | 1250.0 | nM | 5.90 |
| CHEMBL2431826 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2431822 | — | IC50 | = | 2870.0 | nM | 5.54 |
| CHEMBL2431819 | — | IC50 | = | 3530.0 | nM | 5.45 |
| CHEMBL2001019 | PF-04217903 | IC50 | > | 10000.0 | nM | - |