Assay Detail
Binding
CHEMBL2073616
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Inhibition of PDE8B expressed in Sf9 insect cells
111
Total Activities
111
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
High affinity cAMP-specific and IBMX-insensitive 3',5'-cyclic phosphodiesterase 8B (CHEMBL4408) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 111 | 7.07 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2070733 | — | — | 1 | 9.05 |
| CHEMBL2070735 | — | — | 1 | 8.89 |
| CHEMBL2070732 | — | — | 1 | 8.80 |
| CHEMBL2070914 | — | — | 1 | 8.44 |
| CHEMBL2070736 | — | — | 1 | 8.38 |
| CHEMBL2070604 | — | — | 1 | 8.17 |
| CHEMBL2070935 | — | — | 1 | 8.17 |
| CHEMBL2070595 | — | — | 1 | 8.00 |
| CHEMBL2070901 | — | — | 1 | 7.92 |
| CHEMBL2070907 | — | — | 1 | 7.88 |
| CHEMBL2070592 | — | — | 1 | 7.85 |
| CHEMBL2070591 | — | — | 1 | 7.85 |
| CHEMBL2070769 | — | — | 1 | 7.77 |
| CHEMBL2070912 | — | — | 1 | 7.77 |
| CHEMBL2070919 | — | — | 1 | 7.77 |
| CHEMBL2070932 | — | — | 1 | 7.75 |
| CHEMBL2070737 | — | — | 1 | 7.72 |
| CHEMBL2070773 | — | — | 1 | 7.67 |
| CHEMBL2070933 | — | — | 1 | 7.67 |
| CHEMBL2070729 | — | — | 1 | 7.64 |
| CHEMBL2070734 | — | — | 1 | 7.64 |
| CHEMBL2070600 | — | — | 1 | 7.60 |
| CHEMBL2070916 | — | — | 1 | 7.59 |
| CHEMBL2070920 | — | — | 1 | 7.50 |
| CHEMBL2070925 | — | — | 1 | 7.50 |
| CHEMBL2070768 | — | — | 1 | 7.41 |
| CHEMBL2070927 | — | — | 1 | 7.41 |
| CHEMBL2070731 | — | — | 1 | 7.39 |
| CHEMBL2070922 | — | — | 1 | 7.36 |
| CHEMBL2070594 | — | — | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2070733 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2070735 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2070732 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2070914 | — | IC50 | = | 3.63 | nM | 8.44 |
| CHEMBL2070736 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL2070935 | — | IC50 | = | 6.79 | nM | 8.17 |
| CHEMBL2070604 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2070595 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2070901 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL2070907 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL2070592 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2070591 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2070919 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL2070912 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL2070769 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL2070932 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL2070737 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2070773 | — | IC50 | = | 21.6 | nM | 7.67 |
| CHEMBL2070933 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL2070729 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2070734 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2070600 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2070916 | — | IC50 | = | 25.5 | nM | 7.59 |
| CHEMBL2070920 | — | IC50 | = | 31.7 | nM | 7.50 |
| CHEMBL2070925 | — | IC50 | = | 31.5 | nM | 7.50 |
| CHEMBL2070768 | — | IC50 | = | 39.2 | nM | 7.41 |
| CHEMBL2070927 | — | IC50 | = | 38.8 | nM | 7.41 |
| CHEMBL2070731 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2070922 | — | IC50 | = | 43.9 | nM | 7.36 |
| CHEMBL2070594 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL2070926 | — | IC50 | = | 48.4 | nM | 7.32 |
| CHEMBL2070921 | — | IC50 | = | 52.4 | nM | 7.28 |
| CHEMBL2070934 | — | IC50 | = | 53.8 | nM | 7.27 |
| CHEMBL2070917 | — | IC50 | = | 55.1 | nM | 7.26 |
| CHEMBL2070899 | — | IC50 | = | 61.2 | nM | 7.21 |
| CHEMBL2070770 | — | IC50 | = | 70.7 | nM | 7.15 |
| CHEMBL2070898 | — | IC50 | = | 72.7 | nM | 7.14 |
| CHEMBL2070923 | — | IC50 | = | 74.6 | nM | 7.13 |
| CHEMBL2070906 | — | IC50 | = | 77.4 | nM | 7.11 |
| CHEMBL2070929 | — | IC50 | = | 78.4 | nM | 7.11 |
| CHEMBL2070918 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL2070597 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2070603 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL2070771 | — | IC50 | = | 84.4 | nM | 7.07 |
| CHEMBL2070775 | — | IC50 | = | 87.2 | nM | 7.06 |
| CHEMBL2070589 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL2070609 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL2070596 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL2070766 | — | IC50 | = | 90.7 | nM | 7.04 |
| CHEMBL2070606 | — | IC50 | = | 93.0 | nM | 7.03 |