Assay Detail
Binding
CHEMBL1047622
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Inhibition of human recombinant PDE1C expressed in Sf9 cells by SPA
30
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C (CHEMBL4619) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.63 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL572934 | — | — | 2 | 8.68 |
| CHEMBL583914 | — | — | 2 | 7.30 |
| CHEMBL565667 | — | — | 2 | 7.14 |
| CHEMBL583064 | — | — | 2 | 6.96 |
| CHEMBL574449 | — | — | 2 | 6.72 |
| CHEMBL575791 | — | — | 2 | 6.71 |
| CHEMBL575790 | — | — | 2 | 6.68 |
| CHEMBL566300 | — | — | 2 | 6.66 |
| CHEMBL575775 | — | — | 2 | 6.57 |
| CHEMBL578033 | — | — | 2 | 6.40 |
| CHEMBL575745 | — | — | 2 | 6.25 |
| CHEMBL572747 | — | — | 2 | 6.01 |
| CHEMBL582856 | — | — | 2 | 5.89 |
| CHEMBL576952 | — | — | 2 | 5.83 |
| CHEMBL572517 | — | — | 2 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL572934 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL572934 | — | IC50 | = | 2.138 | nM | 8.67 |
| CHEMBL583914 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL583914 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL565667 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL565667 | — | IC50 | = | 72.44 | nM | 7.14 |
| CHEMBL583064 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL583064 | — | IC50 | = | 109.65 | nM | 6.96 |
| CHEMBL574449 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL575791 | — | IC50 | = | 194.98 | nM | 6.71 |
| CHEMBL574449 | — | IC50 | = | 194.98 | nM | 6.71 |
| CHEMBL575791 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL575790 | — | IC50 | = | 208.93 | nM | 6.68 |
| CHEMBL575790 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL566300 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL566300 | — | IC50 | = | 218.78 | nM | 6.66 |
| CHEMBL575775 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL575775 | — | IC50 | = | 269.15 | nM | 6.57 |
| CHEMBL578033 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL578033 | — | IC50 | = | 407.38 | nM | 6.39 |
| CHEMBL575745 | — | IC50 | = | 563.0 | nM | 6.25 |
| CHEMBL575745 | — | IC50 | = | 562.34 | nM | 6.25 |
| CHEMBL572747 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL572747 | — | IC50 | = | 977.24 | nM | 6.01 |
| CHEMBL582856 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL582856 | — | IC50 | = | 1318.26 | nM | 5.88 |
| CHEMBL576952 | — | IC50 | = | 1479.11 | nM | 5.83 |
| CHEMBL576952 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL572517 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL572517 | — | IC50 | = | 2137.96 | nM | 5.67 |