Assay Detail
Binding
CHEMBL940740
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Inhibition of PDE10
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (CHEMBL4409) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.28 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL251107 | — | — | 1 | 7.70 |
| CHEMBL400976 | — | — | 1 | 6.92 |
| CHEMBL399298 | — | — | 1 | 6.89 |
| CHEMBL401186 | — | — | 1 | 6.37 |
| CHEMBL437020 | — | — | 1 | 6.22 |
| CHEMBL401345 | — | — | 1 | 6.12 |
| CHEMBL249691 | — | — | 1 | 5.96 |
| CHEMBL250137 | — | — | 1 | 5.82 |
| CHEMBL249933 | — | — | 1 | 5.77 |
| CHEMBL399385 | — | — | 1 | 5.72 |
| CHEMBL399690 | — | — | 1 | 5.55 |
| CHEMBL249285 | — | — | 1 | - |
| CHEMBL401120 | — | — | 1 | - |
| CHEMBL249486 | — | — | 1 | - |
| CHEMBL401121 | — | — | 1 | - |
| CHEMBL399297 | — | — | 1 | - |
| CHEMBL250546 | SCH-351591 | — | 1 | - |
| CHEMBL40200 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL251107 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL400976 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL399298 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL401186 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL437020 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL401345 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL249691 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL250137 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL249933 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL399385 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL399690 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL249285 | — | IC50 | - | — | - | |
| CHEMBL401120 | — | IC50 | - | — | - | |
| CHEMBL249486 | — | IC50 | - | — | - | |
| CHEMBL401121 | — | IC50 | - | — | - | |
| CHEMBL399297 | — | IC50 | - | — | - | |
| CHEMBL250546 | SCH-351591 | IC50 | > | 10000.0 | nM | - |
| CHEMBL40200 | — | IC50 | > | 10000.0 | nM | - |