Assay Detail
Binding
CHEMBL4028015
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human N-terminal FLAG-tagged PDE2A3 expressed in sf21 cells using [3H]cGMP as substrate after 30 mins by SPA
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
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.35 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3655786 | — | — | 1 | 9.52 |
| CHEMBL4080109 | — | — | 1 | 8.89 |
| CHEMBL2381192 | — | — | 1 | 8.80 |
| CHEMBL3092562 | PF-05180999 | 1.0 | 1 | 8.80 |
| CHEMBL3655780 | — | — | 1 | 8.09 |
| CHEMBL3092561 | — | — | 1 | 8.05 |
| CHEMBL4081035 | — | — | 1 | 7.96 |
| CHEMBL4086493 | — | — | 1 | 7.92 |
| CHEMBL4099071 | — | — | 1 | 7.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3655786 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4080109 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2381192 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3092562 | PF-05180999 | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3655780 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL3092561 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4081035 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4086493 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4099071 | — | IC50 | = | 72.0 | nM | 7.14 |