Assay Detail
Binding
CHEMBL3705111
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition Assay: The activity of the compounds in accordance with the present invention as PDE2 inhibitors may be readily determined using a fluorescence polarization (FP) methodology (Huang, W., et al., J. Biomol Screen, 2002, 7: 215). In particular, the compounds of the following examples had activity in reference assays by exhibiting the ability to inhibit the hydrolysis of the phosphosphate ester bond of a cyclic nucleotide.
9
Total Activities
9
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
cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL2652) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Quinolinone PDE2 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.33 | 8.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3092564 | — | — | 1 | 8.89 |
| CHEMBL3665541 | — | — | 1 | 8.74 |
| CHEMBL3665542 | — | — | 1 | 7.47 |
| CHEMBL3665538 | — | — | 1 | 7.21 |
| CHEMBL3665536 | — | — | 1 | 7.14 |
| CHEMBL3665543 | — | — | 1 | 6.96 |
| CHEMBL3665539 | — | — | 1 | 6.80 |
| CHEMBL3665537 | — | — | 1 | 6.70 |
| CHEMBL3665540 | — | — | 1 | 6.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3092564 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3665541 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3665542 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL3665538 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL3665536 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL3665543 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL3665539 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL3665537 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL3665540 | — | Ki | = | 900.0 | nM | 6.05 |