Assay Detail
Binding
CHEMBL4398699
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of bovine aortic smooth muscle PDE5 using cGMP as substrate incubated for 30 mins in presence of EGTA and [3H]cGMP by liquid scintillation counting method
74
Total Activities
74
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL3478) ↗| Type | SINGLE PROTEIN |
| Organism | Bos taurus |
Publication
Design and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 74 | 5.50 | 7.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4441100 | — | — | 1 | 7.19 |
| CHEMBL4566048 | — | — | 1 | 6.80 |
| CHEMBL28079 | ZAPRINAST | 2.0 | 1 | 6.52 |
| CHEMBL4462235 | — | — | 1 | 6.46 |
| CHEMBL4516439 | — | — | 1 | 6.39 |
| CHEMBL4441701 | — | — | 1 | 6.07 |
| CHEMBL4474310 | — | — | 1 | 6.03 |
| CHEMBL4444580 | — | — | 1 | 6.02 |
| CHEMBL4451127 | — | — | 1 | 5.84 |
| CHEMBL4471948 | — | — | 1 | 5.78 |
| CHEMBL4586506 | — | — | 1 | 5.75 |
| CHEMBL4469331 | — | — | 1 | 5.56 |
| CHEMBL4451333 | — | — | 1 | 5.52 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 5.48 |
| CHEMBL4473323 | — | — | 1 | 5.29 |
| CHEMBL4565771 | — | — | 1 | 5.28 |
| CHEMBL4472638 | — | — | 1 | 5.26 |
| CHEMBL4463175 | — | — | 1 | 5.20 |
| CHEMBL332898 | — | — | 1 | 5.17 |
| CHEMBL4459078 | — | — | 1 | 5.14 |
| CHEMBL4436379 | — | — | 1 | 5.14 |
| CHEMBL4572825 | — | — | 1 | 4.97 |
| CHEMBL4580388 | — | — | 1 | 4.95 |
| CHEMBL4591523 | — | — | 1 | 4.94 |
| CHEMBL4473392 | — | — | 1 | 4.90 |
| CHEMBL4437196 | — | — | 1 | 4.82 |
| CHEMBL4460956 | — | — | 1 | 4.72 |
| CHEMBL4453422 | — | — | 1 | 4.72 |
| CHEMBL4453732 | — | — | 1 | 4.62 |
| CHEMBL4527792 | — | — | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4441100 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL4566048 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL28079 | ZAPRINAST | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4462235 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4516439 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4441701 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4474310 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4444580 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL4451127 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL4471948 | — | IC50 | = | 1670.0 | nM | 5.78 |
| CHEMBL4586506 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4469331 | — | IC50 | = | 2740.0 | nM | 5.56 |
| CHEMBL4451333 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4473323 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL4565771 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4472638 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4463175 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL332898 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4459078 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4436379 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4572825 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4580388 | — | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL4591523 | — | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4473392 | — | IC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL4437196 | — | IC50 | = | 15100.0 | nM | 4.82 |
| CHEMBL4453422 | — | IC50 | = | 19200.0 | nM | 4.72 |
| CHEMBL4460956 | — | IC50 | = | 19000.0 | nM | 4.72 |
| CHEMBL4453732 | — | IC50 | = | 23700.0 | nM | 4.62 |
| CHEMBL4527792 | — | IC50 | = | 38100.0 | nM | 4.42 |
| CHEMBL4448259 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4462589 | — | IC50 | - | — | - | |
| CHEMBL4561469 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4464772 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4450870 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2088641 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4589945 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4469095 | — | IC50 | - | — | - | |
| CHEMBL4475413 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4563939 | — | IC50 | - | — | - | |
| CHEMBL4586085 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4460160 | — | IC50 | >= | 10000.0 | nM | - |
| CHEMBL4534190 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4459901 | — | IC50 | - | — | - | |
| CHEMBL4524253 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4470619 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4457498 | — | IC50 | - | — | - | |
| CHEMBL1497599 | — | IC50 | - | — | - | |
| CHEMBL1511685 | — | IC50 | - | — | - | |
| CHEMBL4570903 | — | IC50 | - | — | - |