Assay Detail
Binding
CHEMBL4182273
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human PDE2A catalytic domain (580 to 919 residues) expressed in Escherichia coli BL21 (Codonplus) using [3H]cGMP as substrate after 15 mins by liquid scintillation counting method
17
Total Activities
17
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
Discovery of novel purine nucleoside derivatives as phosphodiesterase 2 (PDE2) inhibitors: Structure-based virtual screening, optimization and biological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.12 | 6.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4215803 | — | — | 1 | 6.50 |
| CHEMBL4217875 | — | — | 1 | 6.43 |
| CHEMBL4206935 | — | — | 1 | 6.39 |
| CHEMBL4206994 | — | — | 1 | 6.33 |
| CHEMBL4212765 | — | — | 1 | 6.21 |
| CHEMBL4218153 | — | — | 1 | 6.17 |
| CHEMBL4213652 | — | — | 1 | 6.13 |
| CHEMBL4215310 | — | — | 1 | 5.94 |
| CHEMBL296435 | (+)-EHNA | — | 1 | 5.61 |
| CHEMBL1750 | CLOFARABINE | 4.0 | 1 | 5.51 |
| CHEMBL4207219 | — | — | 1 | - |
| CHEMBL1619 | CLADRIBINE | 4.0 | 1 | - |
| CHEMBL285819 | — | — | 1 | - |
| CHEMBL3797375 | — | — | 1 | - |
| CHEMBL4210738 | — | — | 1 | - |
| CHEMBL4208598 | — | — | 1 | - |
| CHEMBL2032002 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4215803 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4217875 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4206935 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4206994 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL4212765 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL4218153 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4213652 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4215310 | — | IC50 | = | 1150.0 | nM | 5.94 |
| CHEMBL296435 | (+)-EHNA | IC50 | = | 2460.0 | nM | 5.61 |
| CHEMBL1750 | CLOFARABINE | IC50 | = | 3120.0 | nM | 5.51 |
| CHEMBL4207219 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1619 | CLADRIBINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL285819 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3797375 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4210738 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4208598 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2032002 | — | IC50 | > | 10000.0 | nM | - |