Assay Detail
Binding
CHEMBL4198222
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged full length recombinant human PDE6C expressed in Baculovirus infected Sf9 insect cells using FAM-cAMP as substrate after 1 hr by fluorescence polarization assay
8
Total Activities
8
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
Cone cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha' (CHEMBL3977) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design and synthesis of furyl/thineyl pyrroloquinolones based on natural alkaloid perlolyrine, lead to the discovery of potent and selective PDE5 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 8.40 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4217054 | — | — | 1 | 8.92 |
| CHEMBL4217579 | — | — | 1 | 8.82 |
| CHEMBL4212630 | — | — | 1 | 8.64 |
| CHEMBL4218398 | — | — | 1 | 8.43 |
| CHEMBL4208249 | — | — | 1 | 8.42 |
| CHEMBL4209716 | — | — | 1 | 8.32 |
| CHEMBL4204725 | — | — | 1 | 8.21 |
| CHEMBL4205338 | — | — | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4217054 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4217579 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4212630 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4218398 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4208249 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4209716 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4204725 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4205338 | — | IC50 | = | 34.1 | nM | 7.47 |