Assay Detail
Binding
CHEMBL3615166
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE3A using FAM-cAMP by fluorescence polarization assay
16
Total Activities
16
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
Design and discovery of 2-(4-(1H-tetrazol-5-yl)-1H-pyrazol-1-yl)-4-(4-phenyl)thiazole derivatives as cardiotonic agents via inhibition of PDE3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.30 | 6.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3614035 | — | — | 1 | 6.62 |
| CHEMBL3614036 | — | — | 1 | 5.84 |
| CHEMBL3614037 | — | — | 1 | 5.72 |
| CHEMBL3614033 | — | — | 1 | 5.61 |
| CHEMBL3614032 | — | — | 1 | 5.52 |
| CHEMBL3614034 | — | — | 1 | 5.44 |
| CHEMBL3614038 | — | — | 1 | 5.21 |
| CHEMBL3614039 | — | — | 1 | 5.16 |
| CHEMBL3614040 | — | — | 1 | 5.13 |
| CHEMBL3614031 | — | — | 1 | 5.09 |
| CHEMBL3614041 | — | — | 1 | 5.04 |
| CHEMBL3614042 | — | — | 1 | 5.00 |
| CHEMBL17423 | VESNARINONE | 2.0 | 1 | 4.95 |
| CHEMBL3614043 | — | — | 1 | 4.87 |
| CHEMBL3614044 | — | — | 1 | 4.83 |
| CHEMBL3614045 | — | — | 1 | 4.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3614035 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL3614036 | — | IC50 | = | 1450.0 | nM | 5.84 |
| CHEMBL3614037 | — | IC50 | = | 1890.0 | nM | 5.72 |
| CHEMBL3614033 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL3614032 | — | IC50 | = | 2990.0 | nM | 5.52 |
| CHEMBL3614034 | — | IC50 | = | 3620.0 | nM | 5.44 |
| CHEMBL3614038 | — | IC50 | = | 6230.0 | nM | 5.21 |
| CHEMBL3614039 | — | IC50 | = | 6890.0 | nM | 5.16 |
| CHEMBL3614040 | — | IC50 | = | 7430.0 | nM | 5.13 |
| CHEMBL3614031 | — | IC50 | = | 8150.0 | nM | 5.09 |
| CHEMBL3614041 | — | IC50 | = | 9120.0 | nM | 5.04 |
| CHEMBL3614042 | — | IC50 | = | 9890.0 | nM | 5.00 |
| CHEMBL17423 | VESNARINONE | IC50 | = | 11210.0 | nM | 4.95 |
| CHEMBL3614043 | — | IC50 | = | 13440.0 | nM | 4.87 |
| CHEMBL3614044 | — | IC50 | = | 14630.0 | nM | 4.83 |
| CHEMBL3614045 | — | IC50 | = | 16420.0 | nM | 4.79 |