Assay Detail
Binding
CHEMBL5730008
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Radioactive Assay: For all experiments the Phosphodiesterase [3H]cAMP SPA Enzyme Assay (TRKQ7090, GE Healthcare Europe GmbH) were used. The enzymatic activity of the PDE2 and the inhibitory potency of compounds was measured by the conversion of [3H]cAMP to [3H]AMP. [3H]AMP associate to the scintillator soaked yttrium-silicate beads resulting in an increase in scintillation events. Compounds that inhibit the respective enzymes decrease the generation of [3H]AMP and accordingly the number of counts detected.SF9 lysate containing PDE2A is incubated at room temperature for 1 h with [3H]cAMP and the reaction is terminated by addition of SPA beads in 18 mM zinc sulphate. The [3H]AMP bound to SPA beads is determined after at least 3 hours of sedimentation of the beads, the signal is recorded using the TopCount with a recording time of 3 min/well.PDE 2A protein is expressed upon baculovirus infection in SF9 cells. The cells have been incubated upon infection for 3 days and protein production was confirmed.
96
Total Activities
30
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL2652) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted pyrido[3,2-E][1,2,4]-triazolo[4,3-A]pyrazines for the treatment of central nervous system disorders
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.35 | 8.52 |
| kon | 32 | - | - |
| k_off | 32 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3693289 | — | — | 3 | 8.52 |
| CHEMBL3693261 | — | — | 3 | 8.40 |
| CHEMBL3693284 | — | — | 3 | 8.40 |
| CHEMBL3693291 | — | — | 3 | 8.40 |
| CHEMBL3693288 | — | — | 3 | 8.15 |
| CHEMBL3693292 | — | — | 3 | 8.05 |
| CHEMBL3693293 | — | — | 3 | 8.05 |
| CHEMBL3693285 | — | — | 3 | 8.05 |
| CHEMBL3693260 | — | — | 3 | 7.80 |
| CHEMBL3693286 | — | — | 3 | 7.77 |
| CHEMBL3693287 | — | — | 3 | 7.57 |
| CHEMBL3693279 | — | — | 3 | 7.55 |
| CHEMBL3693274 | — | — | 3 | 7.40 |
| CHEMBL3693272 | — | — | 3 | 7.28 |
| CHEMBL3693282 | — | — | 3 | 7.26 |
| CHEMBL3693275 | — | — | 3 | 7.24 |
| CHEMBL3693280 | — | — | 3 | 7.16 |
| CHEMBL3693277 | — | — | 3 | 7.15 |
| CHEMBL3693281 | — | — | 9 | 7.15 |
| CHEMBL3693299 | — | — | 3 | 7.10 |
| CHEMBL3693276 | — | — | 3 | 7.01 |
| CHEMBL3693283 | — | — | 3 | 6.94 |
| CHEMBL3693263 | — | — | 3 | 6.86 |
| CHEMBL3693278 | — | — | 3 | 6.84 |
| CHEMBL3693262 | — | — | 3 | 6.81 |
| CHEMBL3693296 | — | — | 3 | 6.77 |
| CHEMBL3693273 | — | — | 3 | 6.70 |
| CHEMBL3693295 | — | — | 3 | 6.66 |
| CHEMBL3693297 | — | — | 3 | 6.38 |
| CHEMBL3693298 | — | — | 3 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3693289 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3693284 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3693291 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3693261 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3693288 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3693285 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3693292 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3693293 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3693260 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3693286 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3693287 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3693279 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3693274 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3693272 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3693282 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3693275 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3693280 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3693281 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3693277 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3693299 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3693276 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL3693281 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL3693283 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL3693263 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL3693281 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL3693278 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL3693262 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL3693296 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL3693273 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3693295 | — | IC50 | = | 219.0 | nM | 6.66 |
| CHEMBL3693297 | — | IC50 | = | 417.0 | nM | 6.38 |
| CHEMBL3693298 | — | IC50 | = | 914.0 | nM | 6.04 |
| CHEMBL3693293 | — | kon | = | - | — | - |
| CHEMBL3693293 | — | k_off | = | - | s-1 | - |
| CHEMBL3693295 | — | kon | = | - | — | - |
| CHEMBL3693295 | — | k_off | = | - | s-1 | - |
| CHEMBL3693296 | — | kon | = | - | — | - |
| CHEMBL3693296 | — | k_off | = | - | s-1 | - |
| CHEMBL3693297 | — | kon | = | - | — | - |
| CHEMBL3693297 | — | k_off | = | - | s-1 | - |
| CHEMBL3693292 | — | k_off | = | - | s-1 | - |
| CHEMBL3693299 | — | k_off | = | - | s-1 | - |
| CHEMBL3693285 | — | kon | = | - | — | - |
| CHEMBL3693288 | — | kon | = | - | — | - |
| CHEMBL3693285 | — | k_off | = | - | s-1 | - |
| CHEMBL3693299 | — | kon | = | - | — | - |
| CHEMBL3693287 | — | k_off | = | - | s-1 | - |
| CHEMBL3693287 | — | kon | = | - | — | - |
| CHEMBL3693286 | — | kon | = | - | — | - |
| CHEMBL3693286 | — | k_off | = | - | s-1 | - |