Assay Detail
Binding
CHEMBL760595
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity against PDE4 was determined using [3H]- rolipram in guinea pig brain membrane binding assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 7.23 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 9.40 |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 8.35 |
| CHEMBL55046 | — | — | 1 | 8.15 |
| CHEMBL53710 | — | — | 1 | 7.89 |
| CHEMBL54988 | — | — | 1 | 7.68 |
| CHEMBL301448 | — | — | 1 | 7.62 |
| CHEMBL54361 | — | — | 1 | 7.39 |
| CHEMBL292925 | — | — | 1 | 7.27 |
| CHEMBL54590 | — | — | 1 | 7.22 |
| CHEMBL55203 | — | — | 1 | 7.18 |
| CHEMBL53559 | — | — | 1 | 7.12 |
| CHEMBL300395 | — | — | 1 | 7.12 |
| CHEMBL417930 | — | — | 1 | 7.12 |
| CHEMBL299332 | — | — | 1 | 6.92 |
| CHEMBL301201 | — | — | 1 | 6.87 |
| CHEMBL294831 | — | — | 1 | 6.76 |
| CHEMBL54767 | — | — | 1 | 6.73 |
| CHEMBL56406 | — | — | 1 | 6.66 |
| CHEMBL429356 | — | — | 1 | 6.55 |
| CHEMBL445354 | — | — | 1 | 6.52 |
| CHEMBL55867 | — | — | 1 | 6.43 |
| CHEMBL52712 | — | — | 1 | 6.15 |
| CHEMBL300129 | — | — | 1 | - |
| CHEMBL53373 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL63 | ROLIPRAM | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL55046 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL53710 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL54988 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL301448 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL54361 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL292925 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL54590 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL55203 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL53559 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL300395 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL417930 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL299332 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL301201 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL294831 | — | Ki | = | 172.0 | nM | 6.76 |
| CHEMBL54767 | — | Ki | = | 187.0 | nM | 6.73 |
| CHEMBL56406 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL429356 | — | Ki | = | 280.0 | nM | 6.55 |
| CHEMBL445354 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL55867 | — | Ki | = | 374.0 | nM | 6.43 |
| CHEMBL52712 | — | Ki | = | 712.0 | nM | 6.15 |
| CHEMBL300129 | — | Ki | > | 3745.0 | nM | - |
| CHEMBL53373 | — | Ki | > | 3745.0 | nM | - |