Assay Detail
Binding
CHEMBL2185813
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PDE9A expressed in Sf9 cells using [3H]cGMP 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
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A (CHEMBL3535) ↗| 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 | 8.32 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL572934 | — | — | 1 | 9.10 |
| CHEMBL2179099 | — | — | 1 | 9.05 |
| CHEMBL2179093 | — | — | 1 | 9.00 |
| CHEMBL2177125 | — | — | 1 | 8.92 |
| CHEMBL2179096 | — | — | 1 | 8.77 |
| CHEMBL2179100 | — | — | 1 | 8.47 |
| CHEMBL2179102 | — | — | 1 | 8.42 |
| CHEMBL2179104 | — | — | 1 | 8.34 |
| CHEMBL2179098 | — | — | 1 | 8.34 |
| CHEMBL2179094 | — | — | 1 | 8.31 |
| CHEMBL2179101 | — | — | 1 | 8.20 |
| CHEMBL2179105 | EDELINONTRINE | 2.0 | 1 | 8.08 |
| CHEMBL2179103 | — | — | 1 | 7.92 |
| CHEMBL2179097 | — | — | 1 | 7.05 |
| CHEMBL2179095 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL572934 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL2179099 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2179093 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2177125 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2179096 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL2179100 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL2179102 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL2179104 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL2179098 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL2179094 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL2179101 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL2179105 | EDELINONTRINE | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL2179103 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2179097 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2179095 | — | IC50 | = | 152.0 | nM | 6.82 |