Assay Detail
Binding
CHEMBL4040926
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human His-tagged PDE2A3 expressed in fall armyworm Sf9 cells using [3H]cGMP as substrate preincubated for 30 mins followed by substrate addition after 60 mins by scintillation proximity assay
23
Total Activities
23
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 an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.45 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4059831 | — | — | 1 | 7.62 |
| CHEMBL4088107 | — | — | 1 | 7.28 |
| CHEMBL4104510 | — | — | 1 | 6.31 |
| CHEMBL4064136 | — | — | 1 | 6.00 |
| CHEMBL4085701 | — | — | 1 | 5.85 |
| CHEMBL4094364 | — | — | 1 | 5.66 |
| CHEMBL4102110 | — | — | 1 | 5.44 |
| CHEMBL4076518 | — | — | 1 | 5.42 |
| CHEMBL4068494 | — | — | 1 | 5.21 |
| CHEMBL4086618 | — | — | 1 | 5.16 |
| CHEMBL4066865 | — | — | 1 | 4.80 |
| CHEMBL4065234 | — | — | 1 | 4.68 |
| CHEMBL4077849 | — | — | 1 | 4.64 |
| CHEMBL4101192 | — | — | 1 | 4.55 |
| CHEMBL4083192 | — | — | 1 | 4.31 |
| CHEMBL4103591 | — | — | 1 | 4.28 |
| CHEMBL4074901 | — | — | 1 | - |
| CHEMBL4095339 | — | — | 1 | - |
| CHEMBL4087643 | — | — | 1 | - |
| CHEMBL4080230 | — | — | 1 | - |
| CHEMBL4095833 | — | — | 1 | - |
| CHEMBL4079320 | — | — | 1 | - |
| CHEMBL4066287 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4059831 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4088107 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4104510 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4064136 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4085701 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4094364 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL4102110 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4076518 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4068494 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4086618 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL4066865 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL4065234 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4077849 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4101192 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL4083192 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL4103591 | — | IC50 | = | 52000.0 | nM | 4.28 |
| CHEMBL4074901 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4095339 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4087643 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4080230 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4095833 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4079320 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4066287 | — | IC50 | > | 100000.0 | nM | - |