Assay Detail
Binding
CHEMBL763956
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Inhibition of rolipram binding to PDE4
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.21 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 8.82 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 8.80 |
| CHEMBL79902 | — | — | 1 | 7.77 |
| CHEMBL79471 | — | — | 1 | 7.47 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 7.42 |
| CHEMBL79535 | — | — | 1 | 7.05 |
| CHEMBL70391 | — | — | 1 | 6.83 |
| CHEMBL312375 | — | — | 1 | 6.69 |
| CHEMBL310387 | — | — | 1 | 6.57 |
| CHEMBL81364 | — | — | 1 | 6.42 |
| CHEMBL312322 | — | — | 1 | 6.36 |
| CHEMBL421151 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL63 | ROLIPRAM | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL79902 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL79471 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL511115 | CILOMILAST | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL79535 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL70391 | — | Ki | = | 149.0 | nM | 6.83 |
| CHEMBL312375 | — | Ki | = | 204.0 | nM | 6.69 |
| CHEMBL310387 | — | Ki | = | 271.0 | nM | 6.57 |
| CHEMBL81364 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL312322 | — | Ki | = | 436.0 | nM | 6.36 |
| CHEMBL421151 | — | Ki | = | 452.0 | nM | 6.34 |