Assay Detail
Binding
CHEMBL761480
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Inhibitory concentration required to inhibit human phosphodiesterase 3A expressed in Escherichia coli
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A (CHEMBL241) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 8.01 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL338860 | — | — | 1 | 9.96 |
| CHEMBL339210 | — | — | 1 | 9.96 |
| CHEMBL131355 | — | — | 1 | 9.48 |
| CHEMBL131111 | — | — | 1 | 9.41 |
| CHEMBL338381 | — | — | 1 | 9.08 |
| CHEMBL128621 | — | — | 1 | 9.03 |
| CHEMBL128391 | — | — | 1 | 8.92 |
| CHEMBL128456 | — | — | 1 | 8.89 |
| CHEMBL130026 | — | — | 1 | 8.80 |
| CHEMBL338179 | — | — | 1 | 8.80 |
| CHEMBL129668 | — | — | 1 | 8.66 |
| CHEMBL129255 | — | — | 1 | 8.64 |
| CHEMBL341231 | — | — | 1 | 8.55 |
| CHEMBL129692 | — | — | 1 | 8.54 |
| CHEMBL341354 | — | — | 1 | 8.51 |
| CHEMBL131939 | — | — | 1 | 8.43 |
| CHEMBL130081 | — | — | 1 | 8.14 |
| CHEMBL129283 | — | — | 1 | 8.12 |
| CHEMBL128017 | — | — | 1 | 7.82 |
| CHEMBL131672 | — | — | 1 | 7.80 |
| CHEMBL34431 | CILOSTAMIDE | 2.0 | 1 | 7.80 |
| CHEMBL128485 | — | — | 1 | 7.70 |
| CHEMBL421249 | — | — | 1 | 7.66 |
| CHEMBL128338 | — | — | 1 | 7.62 |
| CHEMBL129691 | — | — | 1 | 7.62 |
| CHEMBL129689 | — | — | 1 | 7.42 |
| CHEMBL129407 | — | — | 1 | 7.37 |
| CHEMBL341327 | — | — | 1 | 7.36 |
| CHEMBL128783 | — | — | 1 | 7.34 |
| CHEMBL128619 | — | — | 1 | 7.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL338860 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL339210 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL131355 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL131111 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL338381 | — | IC50 | = | 0.83 | nM | 9.08 |
| CHEMBL128621 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL128391 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL128456 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL130026 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL338179 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL129668 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL129255 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL341231 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL129692 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL341354 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL131939 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL130081 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL129283 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL128017 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL131672 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL34431 | CILOSTAMIDE | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL128485 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL421249 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL128338 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL129691 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL129689 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL129407 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL341327 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL128783 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL128619 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL128263 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL128877 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL340118 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL340785 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL131118 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL341160 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL129600 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL189 | MILRINONE | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL273816 | — | IC50 | = | 550.0 | nM | 6.26 |