Assay Detail
Binding
CHEMBL4268474
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant human N-terminal GST-tagged PDE5A1 expressed in baculovirus infected sf9 cells using FAM-cyclic-3',5-GMP as substrate after 1 hr by fluorescence polarization assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of furyl/thienyl β-carboline derivatives as potent and selective PDE5 inhibitors with excellent vasorelaxant effect.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.52 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4281766 | — | — | 1 | 8.54 |
| CHEMBL4286052 | — | — | 1 | 8.41 |
| CHEMBL779 | TADALAFIL | 4.0 | 1 | 8.33 |
| CHEMBL4277243 | — | — | 1 | 8.28 |
| CHEMBL4281081 | — | — | 1 | 8.15 |
| CHEMBL4289471 | — | — | 1 | 8.14 |
| CHEMBL4289291 | — | — | 1 | 8.07 |
| CHEMBL4278136 | — | — | 1 | 8.06 |
| CHEMBL4292389 | — | — | 1 | 7.98 |
| CHEMBL4281590 | — | — | 1 | 7.90 |
| CHEMBL4283473 | — | — | 1 | 7.70 |
| CHEMBL4285199 | — | — | 1 | 7.67 |
| CHEMBL4284224 | — | — | 1 | 7.56 |
| CHEMBL4280648 | — | — | 1 | 7.52 |
| CHEMBL4291228 | — | — | 1 | 7.44 |
| CHEMBL4279202 | — | — | 1 | 7.43 |
| CHEMBL4287438 | — | — | 1 | 7.40 |
| CHEMBL4287523 | — | — | 1 | 7.30 |
| CHEMBL4292970 | — | — | 1 | 7.28 |
| CHEMBL4291310 | — | — | 1 | 7.25 |
| CHEMBL4278311 | — | — | 1 | 7.21 |
| CHEMBL4279614 | — | — | 1 | 7.10 |
| CHEMBL4288548 | — | — | 1 | 7.09 |
| CHEMBL4278056 | — | — | 1 | 7.01 |
| CHEMBL4279700 | — | — | 1 | 6.81 |
| CHEMBL4288727 | — | — | 1 | 6.75 |
| CHEMBL4289780 | — | — | 1 | 6.64 |
| CHEMBL4280196 | — | — | 1 | 6.63 |
| CHEMBL4293856 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4281766 | — | IC50 | = | 2.92 | nM | 8.54 |
| CHEMBL4286052 | — | IC50 | = | 3.87 | nM | 8.41 |
| CHEMBL779 | TADALAFIL | IC50 | = | 4.67 | nM | 8.33 |
| CHEMBL4277243 | — | IC50 | = | 5.24 | nM | 8.28 |
| CHEMBL4281081 | — | IC50 | = | 7.02 | nM | 8.15 |
| CHEMBL4289471 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4289291 | — | IC50 | = | 8.44 | nM | 8.07 |
| CHEMBL4278136 | — | IC50 | = | 8.68 | nM | 8.06 |
| CHEMBL4292389 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL4281590 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4283473 | — | IC50 | = | 19.9 | nM | 7.70 |
| CHEMBL4285199 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL4284224 | — | IC50 | = | 27.6 | nM | 7.56 |
| CHEMBL4280648 | — | IC50 | = | 30.3 | nM | 7.52 |
| CHEMBL4291228 | — | IC50 | = | 36.4 | nM | 7.44 |
| CHEMBL4279202 | — | IC50 | = | 36.9 | nM | 7.43 |
| CHEMBL4287438 | — | IC50 | = | 39.7 | nM | 7.40 |
| CHEMBL4287523 | — | IC50 | = | 50.2 | nM | 7.30 |
| CHEMBL4292970 | — | IC50 | = | 52.5 | nM | 7.28 |
| CHEMBL4291310 | — | IC50 | = | 56.4 | nM | 7.25 |
| CHEMBL4278311 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4279614 | — | IC50 | = | 80.2 | nM | 7.10 |
| CHEMBL4288548 | — | IC50 | = | 81.2 | nM | 7.09 |
| CHEMBL4278056 | — | IC50 | = | 97.5 | nM | 7.01 |
| CHEMBL4279700 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4288727 | — | IC50 | = | 177.0 | nM | 6.75 |
| CHEMBL4289780 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4280196 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL4293856 | — | IC50 | = | 383.0 | nM | 6.42 |