Assay Detail
Binding
CHEMBL4041342
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length His-tagged PDE2A3 expressed in fall armyworm Sf9 cells using [3H]cGMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by scintillation counting
36
Total Activities
33
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 Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.86 | 9.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4060569 | TAK-915 | 1.0 | 1 | 9.21 |
| CHEMBL4102321 | — | — | 1 | 8.80 |
| CHEMBL4064402 | — | — | 1 | 8.55 |
| CHEMBL4072982 | — | — | 1 | 8.46 |
| CHEMBL4067117 | — | — | 2 | 8.14 |
| CHEMBL4085207 | — | — | 1 | 8.06 |
| CHEMBL4098223 | — | — | 1 | 7.72 |
| CHEMBL4079459 | — | — | 1 | 7.68 |
| CHEMBL4068452 | — | — | 1 | 7.62 |
| CHEMBL4097310 | — | — | 1 | 7.54 |
| CHEMBL4093680 | — | — | 1 | 7.48 |
| CHEMBL4082199 | — | — | 1 | 7.40 |
| CHEMBL4078948 | — | — | 1 | 7.38 |
| CHEMBL4088107 | — | — | 1 | 7.28 |
| CHEMBL4081720 | — | — | 1 | 7.21 |
| CHEMBL4089589 | — | — | 1 | 7.19 |
| CHEMBL4064344 | — | — | 3 | 7.18 |
| CHEMBL4073981 | — | — | 1 | 7.14 |
| CHEMBL4085934 | — | — | 1 | 7.11 |
| CHEMBL4094525 | — | — | 1 | 7.10 |
| CHEMBL4063592 | — | — | 1 | 7.07 |
| CHEMBL4071171 | — | — | 1 | 6.68 |
| CHEMBL4059794 | — | — | 1 | 6.60 |
| CHEMBL4087340 | — | — | 1 | 6.32 |
| CHEMBL4084307 | — | — | 1 | 6.30 |
| CHEMBL4072924 | — | — | 1 | 6.21 |
| CHEMBL4082451 | — | — | 1 | 6.04 |
| CHEMBL4102271 | — | — | 1 | 5.39 |
| CHEMBL4089762 | — | — | 1 | 5.19 |
| CHEMBL4103219 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4060569 | TAK-915 | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL4102321 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4064402 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4072982 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL4067117 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4085207 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4098223 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4079459 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4068452 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4097310 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4093680 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4082199 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4078948 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4088107 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4081720 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4089589 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4064344 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4073981 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4064344 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4085934 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4094525 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4063592 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4071171 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL4059794 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4087340 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL4084307 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4072924 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL4082451 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4102271 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4089762 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL4103219 | — | IC50 | = | 8100.0 | nM | 5.09 |
| CHEMBL4068646 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4067117 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL4078053 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL4092061 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL4064344 | — | IC50 | > | 100000.0 | nM | - |