Assay Detail
Binding
CHEMBL909388
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Inhibition of human recombinant PDE3B transfected in Sf9 cells by SPA
29
Total Activities
29
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 | Intermediate |
Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B (CHEMBL290) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 6.48 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL263642 | — | — | 1 | 7.25 |
| CHEMBL219451 | — | — | 1 | 7.06 |
| CHEMBL220185 | — | — | 1 | 6.71 |
| CHEMBL263641 | — | — | 1 | 6.70 |
| CHEMBL260006 | — | — | 1 | 6.68 |
| CHEMBL409651 | — | — | 1 | 6.65 |
| CHEMBL408977 | — | — | 1 | 6.62 |
| CHEMBL409613 | — | — | 1 | 6.62 |
| CHEMBL409862 | — | — | 1 | 6.58 |
| CHEMBL219445 | — | — | 1 | 6.56 |
| CHEMBL261711 | — | — | 1 | 6.55 |
| CHEMBL218855 | — | — | 1 | 6.55 |
| CHEMBL218955 | — | — | 1 | 6.52 |
| CHEMBL375200 | — | — | 1 | 6.48 |
| CHEMBL385754 | — | — | 1 | 6.48 |
| CHEMBL19224 | PAPAVERINE | 3.0 | 1 | 6.38 |
| CHEMBL410834 | — | — | 1 | 6.33 |
| CHEMBL441704 | — | — | 1 | 6.33 |
| CHEMBL219123 | — | — | 1 | 6.32 |
| CHEMBL259295 | — | — | 1 | 6.16 |
| CHEMBL374993 | — | — | 1 | 6.13 |
| CHEMBL387166 | — | — | 1 | 5.74 |
| CHEMBL387167 | — | — | 1 | 5.72 |
| CHEMBL428445 | — | — | 1 | - |
| CHEMBL262088 | — | — | 1 | - |
| CHEMBL427777 | — | — | 1 | - |
| CHEMBL2096844 | — | — | 1 | - |
| CHEMBL408978 | — | — | 1 | - |
| CHEMBL409484 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL263642 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL219451 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL220185 | — | Ki | = | 196.0 | nM | 6.71 |
| CHEMBL263641 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL260006 | — | Ki | = | 207.0 | nM | 6.68 |
| CHEMBL409651 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL408977 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL409613 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL409862 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL219445 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL261711 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL218855 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL218955 | — | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL375200 | — | Ki | = | 328.0 | nM | 6.48 |
| CHEMBL385754 | — | Ki | = | 332.0 | nM | 6.48 |
| CHEMBL19224 | PAPAVERINE | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL410834 | — | Ki | = | 463.0 | nM | 6.33 |
| CHEMBL441704 | — | Ki | = | 471.0 | nM | 6.33 |
| CHEMBL219123 | — | Ki | = | 474.0 | nM | 6.32 |
| CHEMBL259295 | — | Ki | = | 685.0 | nM | 6.16 |
| CHEMBL374993 | — | Ki | = | 748.0 | nM | 6.13 |
| CHEMBL387166 | — | Ki | = | 1820.0 | nM | 5.74 |
| CHEMBL387167 | — | Ki | = | 1890.0 | nM | 5.72 |
| CHEMBL428445 | — | Ki | > | 100.0 | nM | - |
| CHEMBL262088 | — | Ki | < | 100.0 | nM | - |
| CHEMBL427777 | — | Ki | > | 100.0 | nM | - |
| CHEMBL2096844 | — | Ki | > | 100.0 | nM | - |
| CHEMBL408978 | — | Ki | < | 100.0 | nM | - |
| CHEMBL409484 | — | Ki | < | 100.0 | nM | - |