Assay Detail
Binding
CHEMBL758788
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Inhibition of phosphodiesterase 3 (PDE3) isolated from the dog aorta
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Confidence | 4 — Cell-line / Tissue |
| 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 | 36 | 4.50 | 5.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL144258 | — | — | 1 | 5.50 |
| CHEMBL145499 | — | — | 1 | 5.35 |
| CHEMBL125671 | — | — | 1 | 4.99 |
| CHEMBL145390 | — | — | 1 | 4.97 |
| CHEMBL341662 | — | — | 1 | 4.75 |
| CHEMBL434838 | — | — | 1 | 4.71 |
| CHEMBL341671 | — | — | 1 | 4.71 |
| CHEMBL422653 | — | — | 1 | 4.65 |
| CHEMBL339749 | — | — | 1 | 4.54 |
| CHEMBL111925 | — | — | 1 | 4.45 |
| CHEMBL418848 | — | — | 1 | 4.39 |
| CHEMBL436207 | — | — | 1 | 4.34 |
| CHEMBL145258 | — | — | 1 | 4.31 |
| CHEMBL144245 | — | — | 1 | 4.31 |
| CHEMBL146218 | — | — | 1 | 4.29 |
| CHEMBL144404 | — | — | 1 | 4.27 |
| CHEMBL357616 | — | — | 1 | 4.26 |
| CHEMBL423931 | — | — | 1 | 4.24 |
| CHEMBL357197 | — | — | 1 | 4.16 |
| CHEMBL144287 | — | — | 1 | 4.10 |
| CHEMBL126581 | — | — | 1 | 4.08 |
| CHEMBL144570 | — | — | 1 | 4.06 |
| CHEMBL356548 | — | — | 1 | 4.05 |
| CHEMBL144605 | — | — | 1 | - |
| CHEMBL125123 | — | — | 1 | - |
| CHEMBL344726 | — | — | 1 | - |
| CHEMBL434516 | — | — | 1 | - |
| CHEMBL63 | ROLIPRAM | 2.0 | 1 | - |
| CHEMBL342285 | — | — | 1 | - |
| CHEMBL144370 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL144258 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL145499 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL125671 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL145390 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL341662 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL434838 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL341671 | — | IC50 | = | 19500.0 | nM | 4.71 |
| CHEMBL422653 | — | IC50 | = | 22200.0 | nM | 4.65 |
| CHEMBL339749 | — | IC50 | = | 28800.0 | nM | 4.54 |
| CHEMBL111925 | — | IC50 | = | 35800.0 | nM | 4.45 |
| CHEMBL418848 | — | IC50 | = | 40800.0 | nM | 4.39 |
| CHEMBL436207 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL145258 | — | IC50 | = | 48500.0 | nM | 4.31 |
| CHEMBL144245 | — | IC50 | = | 48600.0 | nM | 4.31 |
| CHEMBL146218 | — | IC50 | = | 51600.0 | nM | 4.29 |
| CHEMBL144404 | — | IC50 | = | 53900.0 | nM | 4.27 |
| CHEMBL357616 | — | IC50 | = | 54700.0 | nM | 4.26 |
| CHEMBL423931 | — | IC50 | = | 58200.0 | nM | 4.24 |
| CHEMBL357197 | — | IC50 | = | 70000.0 | nM | 4.16 |
| CHEMBL144287 | — | IC50 | = | 80000.0 | nM | 4.10 |
| CHEMBL126581 | — | IC50 | = | 82300.0 | nM | 4.08 |
| CHEMBL144570 | — | IC50 | = | 86800.0 | nM | 4.06 |
| CHEMBL356548 | — | IC50 | = | 90000.0 | nM | 4.05 |
| CHEMBL144452 | — | IC50 | = | - | nM | - |
| CHEMBL343243 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL125828 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL112366 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL422828 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL339408 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL144370 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL342285 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL63 | ROLIPRAM | IC50 | > | 100000.0 | nM | - |
| CHEMBL434516 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL344726 | — | IC50 | = | - | nM | - |
| CHEMBL125123 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL144605 | — | IC50 | > | 100000.0 | nM | - |