Assay Detail
Binding
CHEMBL677056
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibitory activity was determined against human Phosphodiesterase 4 isoform using a construct representing the common region of spliced variants expressed as a GST-fusion protein in Sf 9 cells
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf 9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of a tertiary alcohol series of phosphodiesterase-4 (PDE4) inhibitors: structure-activity relationship related to PDE4 inhibition and human ether-a-go-go related gene potassium channel binding affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 8.29 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2112296 | — | — | 1 | 9.40 |
| CHEMBL310303 | — | — | 1 | 9.30 |
| CHEMBL199015 | — | — | 1 | 9.30 |
| CHEMBL81491 | — | — | 1 | 9.15 |
| CHEMBL2112295 | — | — | 1 | 9.10 |
| CHEMBL78806 | — | — | 1 | 9.00 |
| CHEMBL276559 | — | — | 2 | 8.92 |
| CHEMBL2112294 | — | — | 1 | 8.80 |
| CHEMBL78439 | — | — | 2 | 8.68 |
| CHEMBL61191 | — | — | 1 | 8.68 |
| CHEMBL32442 | CDP840 | — | 1 | 8.37 |
| CHEMBL417776 | — | — | 2 | 7.46 |
| CHEMBL82663 | SIBENADET | 2.0 | 1 | 7.42 |
| CHEMBL383762 | — | — | 1 | 7.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2112296 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL310303 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL199015 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL81491 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL2112295 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL78806 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL276559 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2112294 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL61191 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL78439 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL32442 | CDP840 | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL417776 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL82663 | SIBENADET | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL383762 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL276559 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL78439 | — | IC50 | = | 334.0 | nM | 6.48 |
| CHEMBL417776 | — | IC50 | = | 520.0 | nM | 6.28 |