Assay Detail
Binding
CHEMBL909385
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Inhibition of rat recombinant PDE10A transfected in Sf9 cells by SPA
32
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Sf9 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 7.19 | 8.40 |
| IC50 | 2 | 8.04 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219445 | — | — | 2 | 8.40 |
| CHEMBL410834 | — | — | 2 | 7.92 |
| CHEMBL263641 | — | — | 1 | 7.92 |
| CHEMBL409613 | — | — | 1 | 7.92 |
| CHEMBL19224 | PAPAVERINE | 3.0 | 1 | 7.77 |
| CHEMBL218955 | — | — | 1 | 7.77 |
| CHEMBL261711 | — | — | 1 | 7.75 |
| CHEMBL409651 | — | — | 1 | 7.75 |
| CHEMBL220185 | — | — | 1 | 7.72 |
| CHEMBL219121 | — | — | 1 | 7.60 |
| CHEMBL385754 | — | — | 1 | 7.36 |
| CHEMBL375200 | — | — | 1 | 7.27 |
| CHEMBL441704 | — | — | 1 | 7.25 |
| CHEMBL408977 | — | — | 1 | 7.17 |
| CHEMBL409862 | — | — | 1 | 7.17 |
| CHEMBL219451 | — | — | 1 | 7.03 |
| CHEMBL387167 | — | — | 1 | 7.00 |
| CHEMBL259295 | — | — | 1 | 6.95 |
| CHEMBL260006 | — | — | 1 | 6.91 |
| CHEMBL409484 | — | — | 1 | 6.89 |
| CHEMBL374993 | — | — | 1 | 6.89 |
| CHEMBL218855 | — | — | 1 | 6.87 |
| CHEMBL219123 | — | — | 1 | 6.77 |
| CHEMBL387166 | — | — | 1 | 6.73 |
| CHEMBL408978 | — | — | 1 | 6.70 |
| CHEMBL263642 | — | — | 1 | 6.68 |
| CHEMBL427777 | — | — | 1 | 6.62 |
| CHEMBL262088 | — | — | 1 | 6.49 |
| CHEMBL2096844 | — | — | 1 | 6.19 |
| CHEMBL428445 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219445 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL219445 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL410834 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL263641 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL409613 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL410834 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL19224 | PAPAVERINE | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL218955 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL261711 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL409651 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL220185 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL219121 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL385754 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL375200 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL441704 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL409862 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL408977 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL219451 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL387167 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL259295 | — | Ki | = | 112.0 | nM | 6.95 |
| CHEMBL260006 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL409484 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL374993 | — | Ki | = | 128.0 | nM | 6.89 |
| CHEMBL218855 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL219123 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL387166 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL408978 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL263642 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL427777 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL262088 | — | Ki | = | 326.0 | nM | 6.49 |
| CHEMBL2096844 | — | Ki | = | 641.0 | nM | 6.19 |
| CHEMBL428445 | — | Ki | = | 811.0 | nM | 6.09 |