Assay Detail
Binding
CHEMBL3860990
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 cGMP as substrate after 30 mins by HTRF assay
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 48 | 7.79 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3954968 | — | — | 1 | 9.30 |
| CHEMBL3986487 | — | — | 1 | 9.22 |
| CHEMBL3925737 | — | — | 1 | 9.00 |
| CHEMBL3926754 | — | — | 1 | 8.70 |
| CHEMBL3899814 | — | — | 1 | 8.70 |
| CHEMBL3970984 | — | — | 1 | 8.52 |
| CHEMBL3898716 | — | — | 1 | 8.52 |
| CHEMBL192 | SILDENAFIL | 4.0 | 1 | 8.40 |
| CHEMBL3956031 | — | — | 1 | 8.40 |
| CHEMBL3984639 | — | — | 1 | 8.40 |
| CHEMBL3907730 | — | — | 1 | 8.30 |
| CHEMBL3895860 | — | — | 1 | 8.30 |
| CHEMBL3966438 | — | — | 1 | 8.30 |
| CHEMBL3895838 | — | — | 1 | 8.15 |
| CHEMBL3923840 | — | — | 1 | 8.15 |
| CHEMBL3979179 | — | — | 1 | 8.00 |
| CHEMBL3936651 | — | — | 1 | 8.00 |
| CHEMBL3945565 | — | — | 1 | 7.96 |
| CHEMBL3894057 | — | — | 1 | 7.92 |
| CHEMBL3970271 | — | — | 1 | 7.89 |
| CHEMBL3932796 | — | — | 1 | 7.89 |
| CHEMBL3978271 | — | — | 1 | 7.77 |
| CHEMBL3901988 | — | — | 1 | 7.77 |
| CHEMBL3927691 | — | — | 1 | 7.72 |
| CHEMBL3969922 | — | — | 1 | 7.70 |
| CHEMBL3908767 | — | — | 1 | 7.70 |
| CHEMBL3898715 | — | — | 1 | 7.66 |
| CHEMBL3940720 | — | — | 1 | 7.66 |
| CHEMBL3974954 | — | — | 1 | 7.64 |
| CHEMBL3962991 | — | — | 1 | 7.62 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3954968 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3986487 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3925737 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3926754 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3899814 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3970984 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3898716 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3956031 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3984639 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3907730 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3895860 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3966438 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3895838 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3923840 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3979179 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3936651 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3945565 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3894057 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3970271 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3932796 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3978271 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3901988 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3927691 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3969922 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3908767 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3898715 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3940720 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3974954 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3962991 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3955253 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3976546 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3962031 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3954259 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3897643 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3982024 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3955306 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3890386 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3914813 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3900593 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3950140 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3936720 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3982925 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL3955289 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL3904785 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL3944571 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL3893017 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL3973027 | — | IC50 | = | 303.0 | nM | 6.52 |