Assay Detail
Binding
CHEMBL760760
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Competition of [3H]rolipram binding sites in the central nervous system (HPDE4) in rat brain cytosol
19
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Subcellular | Cytosol |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.73 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL430893 | (-)-ROLIPRAM | — | 1 | 8.30 |
| CHEMBL167638 | — | — | 1 | 8.30 |
| CHEMBL167166 | — | — | 1 | 7.40 |
| CHEMBL169746 | — | — | 1 | 7.35 |
| CHEMBL325795 | S-ROLIPRAM | — | 1 | 7.35 |
| CHEMBL167486 | — | — | 1 | 7.16 |
| CHEMBL352857 | — | — | 1 | 6.96 |
| CHEMBL167258 | — | — | 1 | 6.92 |
| CHEMBL352628 | — | — | 1 | 6.92 |
| CHEMBL511115 | CILOMILAST | 3.0 | 4 | 6.92 |
| CHEMBL169537 | — | — | 1 | 6.52 |
| CHEMBL354447 | — | — | 1 | 6.50 |
| CHEMBL169834 | — | — | 1 | 6.30 |
| CHEMBL166529 | — | — | 1 | 6.16 |
| CHEMBL354656 | — | — | 1 | 5.22 |
| CHEMBL168989 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL167638 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL430893 | (-)-ROLIPRAM | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL167166 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL325795 | S-ROLIPRAM | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL169746 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL167486 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL352857 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL352628 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL167258 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL169537 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL354447 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL169834 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL166529 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL354656 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL168989 | — | IC50 | = | 7000.0 | nM | 5.16 |