Assay Detail
Binding
CHEMBL820636
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Inhibition of [3H]rolipram binding to Wistar rat brain membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Subcellular | Membrane |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 6.65 | 8.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | 8.28 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 7.31 |
| CHEMBL423931 | — | — | 1 | 6.51 |
| CHEMBL343243 | — | — | 1 | 6.47 |
| CHEMBL112366 | — | — | 1 | 6.18 |
| CHEMBL144570 | — | — | 1 | 6.00 |
| CHEMBL342285 | — | — | 1 | 5.77 |
| CHEMBL111925 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL63 | ROLIPRAM | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL423931 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL343243 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL112366 | — | IC50 | = | 654.0 | nM | 6.18 |
| CHEMBL144570 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL342285 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL111925 | — | IC50 | > | 3000.0 | nM | - |