Assay Detail
ADMET
CHEMBL4373381
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Inhibition of human GST-tagged PDE3A (484 to end residues) using cAMP as substrate measured after 60 mins
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.13 | 5.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4534373 | — | — | 1 | 5.96 |
| CHEMBL4569753 | — | — | 1 | 5.31 |
| CHEMBL4542237 | — | — | 1 | 5.15 |
| CHEMBL4535938 | — | — | 1 | 5.13 |
| CHEMBL4544877 | — | — | 1 | 5.11 |
| CHEMBL4542820 | — | — | 1 | 5.11 |
| CHEMBL4456157 | — | — | 1 | 5.07 |
| CHEMBL1086110 | — | — | 1 | 5.07 |
| CHEMBL4464637 | — | — | 1 | 4.78 |
| CHEMBL4556703 | — | — | 1 | 4.63 |
| CHEMBL4585428 | — | — | 1 | - |
| CHEMBL4580449 | — | — | 1 | - |
| CHEMBL4437406 | — | — | 1 | - |
| CHEMBL4472846 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4534373 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL4569753 | — | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL4542237 | — | IC50 | = | 7070.0 | nM | 5.15 |
| CHEMBL4535938 | — | IC50 | = | 7470.0 | nM | 5.13 |
| CHEMBL4544877 | — | IC50 | = | 7850.0 | nM | 5.11 |
| CHEMBL4542820 | — | IC50 | = | 7840.0 | nM | 5.11 |
| CHEMBL4456157 | — | IC50 | = | 8520.0 | nM | 5.07 |
| CHEMBL1086110 | — | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL4464637 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL4556703 | — | IC50 | = | 23600.0 | nM | 4.63 |
| CHEMBL4585428 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4580449 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4437406 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4472846 | — | IC50 | = | 111900.0 | nM | - |