Assay Detail
Binding
CHEMBL968866
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Inhibition of PDE5
49
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
In silico prediction of novel phosphodiesterase type-5 inhibitors derived from Sildenafil, Vardenafil and Tadalafil.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 7.44 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL168949 | — | — | 1 | 9.22 |
| CHEMBL1520 | VARDENAFIL | 4.0 | 1 | 9.15 |
| CHEMBL53538 | LODENAFIL | -1.0 | 1 | 8.72 |
| CHEMBL457207 | — | — | 1 | 8.68 |
| CHEMBL509728 | — | — | 1 | 8.52 |
| CHEMBL192 | SILDENAFIL | 4.0 | 2 | 8.44 |
| CHEMBL456142 | — | — | 1 | 8.40 |
| CHEMBL352722 | — | — | 1 | 8.30 |
| CHEMBL337587 | — | — | 1 | 8.30 |
| CHEMBL779 | TADALAFIL | 4.0 | 1 | 8.30 |
| CHEMBL910 | — | — | 1 | 8.24 |
| CHEMBL456577 | — | — | 1 | 8.22 |
| CHEMBL458714 | — | — | 1 | 8.15 |
| CHEMBL508321 | — | — | 1 | 8.15 |
| CHEMBL422104 | — | — | 1 | 8.10 |
| CHEMBL515979 | — | — | 1 | 8.00 |
| CHEMBL169843 | — | — | 1 | 8.00 |
| CHEMBL353248 | — | — | 1 | 8.00 |
| CHEMBL456552 | — | — | 1 | 8.00 |
| CHEMBL458713 | — | — | 1 | 7.74 |
| CHEMBL344630 | — | — | 1 | 7.70 |
| CHEMBL514402 | — | — | 1 | 7.70 |
| CHEMBL336457 | — | — | 1 | 7.70 |
| CHEMBL456548 | — | — | 1 | 7.70 |
| CHEMBL54079 | — | — | 2 | 7.57 |
| CHEMBL456370 | — | — | 1 | 7.52 |
| CHEMBL335148 | — | — | 1 | 7.52 |
| CHEMBL139048 | — | — | 1 | 7.30 |
| CHEMBL502020 | — | — | 1 | 7.30 |
| CHEMBL141633 | — | — | 1 | 7.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL168949 | — | IC50 | = | 0.6026 | nM | 9.22 |
| CHEMBL1520 | VARDENAFIL | IC50 | = | 0.7079 | nM | 9.15 |
| CHEMBL53538 | LODENAFIL | IC50 | = | 1.905 | nM | 8.72 |
| CHEMBL457207 | — | IC50 | = | 2.089 | nM | 8.68 |
| CHEMBL509728 | — | IC50 | = | 3.02 | nM | 8.52 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 3.631 | nM | 8.44 |
| CHEMBL456142 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL779 | TADALAFIL | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL337587 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL352722 | — | IC50 | = | 5.012 | nM | 8.30 |
| CHEMBL910 | — | IC50 | = | 5.754 | nM | 8.24 |
| CHEMBL456577 | — | IC50 | = | 6.026 | nM | 8.22 |
| CHEMBL192 | SILDENAFIL | IC50 | = | 6.607 | nM | 8.18 |
| CHEMBL508321 | — | IC50 | = | 7.079 | nM | 8.15 |
| CHEMBL458714 | — | IC50 | = | 7.079 | nM | 8.15 |
| CHEMBL422104 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL515979 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL456552 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL353248 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL169843 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL458713 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL456548 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL514402 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL336457 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL344630 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL54079 | — | IC50 | = | 26.92 | nM | 7.57 |
| CHEMBL335148 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL456370 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL54079 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL139048 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL141633 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL502020 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL423550 | — | IC50 | = | 60.26 | nM | 7.22 |
| CHEMBL431544 | — | IC50 | = | 81.28 | nM | 7.09 |
| CHEMBL140493 | — | IC50 | = | 91.2 | nM | 7.04 |
| CHEMBL462983 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL141980 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL336248 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL141506 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL51814 | — | IC50 | = | 331.13 | nM | 6.48 |
| CHEMBL52245 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL141975 | — | IC50 | = | 912.01 | nM | 6.04 |
| CHEMBL52141 | — | IC50 | = | 954.99 | nM | 6.02 |
| CHEMBL525436 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL504118 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL138359 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL28079 | ZAPRINAST | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL52072 | — | IC50 | = | 4365.16 | nM | 5.36 |
| CHEMBL511513 | — | IC50 | = | 4466.84 | nM | 5.35 |