Assay Detail
Binding
CHEMBL768661
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Inhibitory activity against cGMP-phosphodiesterase from porcine aorta
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Cyclic GMP phosphodiesterase inhibitors. 2. Requirement of 6-substitution of quinazoline derivatives for potent and selective inhibitory activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.11 | 7.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL66620 | — | — | 1 | 7.72 |
| CHEMBL304927 | — | — | 1 | 7.51 |
| CHEMBL67243 | — | — | 1 | 7.05 |
| CHEMBL67276 | — | — | 1 | 7.00 |
| CHEMBL66323 | — | — | 1 | 6.64 |
| CHEMBL66855 | — | — | 1 | 6.46 |
| CHEMBL67061 | — | — | 1 | 6.42 |
| CHEMBL63259 | — | — | 1 | 6.42 |
| CHEMBL67239 | — | — | 1 | 6.28 |
| CHEMBL419806 | — | — | 1 | 6.21 |
| CHEMBL308657 | — | — | 1 | 6.14 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 6.14 |
| CHEMBL189 | MILRINONE | 4.0 | 1 | 6.13 |
| CHEMBL63428 | — | — | 1 | 6.11 |
| CHEMBL294731 | — | — | 1 | 6.09 |
| CHEMBL68072 | — | — | 1 | 6.09 |
| CHEMBL66913 | — | — | 1 | 6.08 |
| CHEMBL68337 | — | — | 1 | 6.03 |
| CHEMBL63637 | — | — | 1 | 6.00 |
| CHEMBL305771 | — | — | 1 | 5.96 |
| CHEMBL68448 | — | — | 1 | 5.85 |
| CHEMBL63416 | — | — | 1 | 5.80 |
| CHEMBL67736 | — | — | 1 | 5.64 |
| CHEMBL67892 | — | — | 1 | 5.64 |
| CHEMBL304277 | — | — | 1 | 5.57 |
| CHEMBL302588 | — | — | 1 | 5.44 |
| CHEMBL66732 | — | — | 1 | 5.38 |
| CHEMBL63379 | — | — | 1 | 5.23 |
| CHEMBL304275 | — | — | 1 | 5.12 |
| CHEMBL67418 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL66620 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL304927 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL67243 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL67276 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL66323 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL66855 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL67061 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL63259 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL67239 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL419806 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL308657 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL63 | ROLIPRAM | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL189 | MILRINONE | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL63428 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL294731 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL68072 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL66913 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL68337 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL63637 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL305771 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL68448 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL63416 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL67736 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL67892 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL304277 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL302588 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL66732 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL63379 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL304275 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL67418 | — | IC50 | = | 8700.0 | nM | 5.06 |