Assay Detail
Binding
CHEMBL2185812
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PDE1C expressed in Sf9 cells using [3H]cAMP as substrate after 30 mins by scintillation proximity assay
15
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 | Autocuration |
Target
Dual specificity calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1C (CHEMBL4619) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.34 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL572934 | — | — | 1 | 9.40 |
| CHEMBL2179093 | — | — | 1 | 7.85 |
| CHEMBL2179099 | — | — | 1 | 6.78 |
| CHEMBL2179096 | — | — | 1 | 6.37 |
| CHEMBL2179100 | — | — | 1 | 6.33 |
| CHEMBL2177125 | — | — | 1 | 6.16 |
| CHEMBL2179098 | — | — | 1 | 6.05 |
| CHEMBL2179102 | — | — | 1 | 6.01 |
| CHEMBL2179105 | EDELINONTRINE | 2.0 | 1 | 5.86 |
| CHEMBL2179103 | — | — | 1 | 5.79 |
| CHEMBL2179104 | — | — | 1 | 5.73 |
| CHEMBL2179101 | — | — | 1 | 5.73 |
| CHEMBL2179097 | — | — | 1 | 5.47 |
| CHEMBL2179095 | — | — | 1 | 5.25 |
| CHEMBL2179094 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL572934 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2179093 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2179099 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL2179096 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL2179100 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL2177125 | — | IC50 | = | 693.0 | nM | 6.16 |
| CHEMBL2179098 | — | IC50 | = | 889.0 | nM | 6.05 |
| CHEMBL2179102 | — | IC50 | = | 979.0 | nM | 6.01 |
| CHEMBL2179105 | EDELINONTRINE | IC50 | = | 1394.0 | nM | 5.86 |
| CHEMBL2179103 | — | IC50 | = | 1603.0 | nM | 5.79 |
| CHEMBL2179104 | — | IC50 | = | 1872.0 | nM | 5.73 |
| CHEMBL2179101 | — | IC50 | = | 1858.0 | nM | 5.73 |
| CHEMBL2179097 | — | IC50 | = | 3421.0 | nM | 5.47 |
| CHEMBL2179095 | — | IC50 | = | 5601.0 | nM | 5.25 |
| CHEMBL2179094 | — | IC50 | > | 1000.0 | nM | - |