Assay Detail
Binding
CHEMBL3375790
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE7A1 expressed in insect cells assessed as inhibition of [3H]cAMP to [3H]AMP hydrolysis after 30 mins by scintillation counting
28
Total Activities
28
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
High affinity 3',5'-cyclic-AMP phosphodiesterase 7A (CHEMBL3012) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of 2-(cyclopentylamino)thieno[3,2-d]pyrimidin-4(3H)-one derivatives as a new series of potent phosphodiesterase 7 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 7.11 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3354181 | — | — | 1 | 9.00 |
| CHEMBL3354179 | — | — | 1 | 8.70 |
| CHEMBL3354180 | — | — | 1 | 8.64 |
| CHEMBL3354171 | — | — | 1 | 8.38 |
| CHEMBL3354178 | — | — | 1 | 8.31 |
| CHEMBL3354177 | — | — | 1 | 8.30 |
| CHEMBL3354175 | — | — | 1 | 8.25 |
| CHEMBL3354173 | — | — | 1 | 8.14 |
| CHEMBL3354182 | — | — | 1 | 7.92 |
| CHEMBL3354172 | — | — | 1 | 7.72 |
| CHEMBL3354168 | — | — | 1 | 7.52 |
| CHEMBL3354174 | — | — | 1 | 7.41 |
| CHEMBL3354167 | — | — | 1 | 7.38 |
| CHEMBL3354169 | — | — | 1 | 7.35 |
| CHEMBL3354170 | — | — | 1 | 7.17 |
| CHEMBL3354166 | — | — | 1 | 7.01 |
| CHEMBL3354160 | — | — | 1 | 6.82 |
| CHEMBL3354155 | — | — | 1 | 6.80 |
| CHEMBL3354157 | — | — | 1 | 6.51 |
| CHEMBL3354176 | — | — | 1 | 6.42 |
| CHEMBL3354161 | — | — | 1 | 6.13 |
| CHEMBL3354156 | — | — | 1 | 5.96 |
| CHEMBL3354165 | — | — | 1 | 5.58 |
| CHEMBL3354159 | — | — | 1 | 5.30 |
| CHEMBL3354163 | — | — | 1 | 5.19 |
| CHEMBL3354158 | — | — | 1 | 5.17 |
| CHEMBL3354162 | — | — | 1 | 4.96 |
| CHEMBL3354164 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3354181 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3354179 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3354180 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3354171 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3354178 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3354177 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3354175 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3354173 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL3354182 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3354172 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3354168 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3354174 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3354167 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL3354169 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3354170 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3354166 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3354160 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3354155 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3354157 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3354176 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3354161 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL3354156 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3354165 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL3354159 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3354163 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL3354158 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL3354162 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3354164 | — | IC50 | > | 1000.0 | nM | - |