Assay Detail
Binding
CHEMBL763945
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Binding affinity at Phosphodiesterase 4 by measuring displacement of (+/-)-[3H]- Rolipram to guinea pig brain membranes.
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.29 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | 2.0 | 1 | 9.00 |
| CHEMBL134441 | — | — | 1 | 8.00 |
| CHEMBL135621 | — | — | 3 | 7.70 |
| CHEMBL334488 | — | — | 1 | 7.70 |
| CHEMBL134261 | — | — | 1 | 7.70 |
| CHEMBL423897 | — | — | 1 | 7.70 |
| CHEMBL135304 | — | — | 1 | 7.70 |
| CHEMBL422972 | — | — | 1 | 7.52 |
| CHEMBL337194 | — | — | 1 | 7.35 |
| CHEMBL335970 | — | — | 1 | 7.22 |
| CHEMBL335169 | — | — | 1 | 7.22 |
| CHEMBL335255 | — | — | 1 | 6.58 |
| CHEMBL337472 | — | — | 1 | 5.80 |
| CHEMBL337504 | — | — | 1 | 5.77 |
| CHEMBL133652 | — | — | 1 | 5.64 |
| CHEMBL335897 | — | — | 1 | - |
| CHEMBL334448 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42126 | PICLAMILAST | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL134441 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL135621 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL334488 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL135621 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL134261 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL423897 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL135304 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL135621 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL422972 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL337194 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL335970 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL335169 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL335255 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL337472 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL337504 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL133652 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL335897 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL334448 | — | Ki | > | 10000.0 | nM | - |