Assay Detail
Binding
CHEMBL765477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration against human PDE4A isoform using a construct representing the common region of spliced variants expressed as GST-fusion protein in Sf9 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.90 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL36348 | — | — | 1 | 9.30 |
| CHEMBL35954 | — | — | 1 | 8.66 |
| CHEMBL287348 | — | — | 1 | 8.55 |
| CHEMBL287114 | — | — | 1 | 8.51 |
| CHEMBL286224 | — | — | 1 | 8.38 |
| CHEMBL32442 | CDP840 | — | 1 | 8.37 |
| CHEMBL285247 | — | — | 1 | 8.34 |
| CHEMBL36242 | — | — | 1 | 8.14 |
| CHEMBL266000 | — | — | 1 | 8.12 |
| CHEMBL35350 | — | — | 1 | 8.07 |
| CHEMBL289023 | — | — | 1 | 8.02 |
| CHEMBL285895 | — | — | 1 | 7.96 |
| CHEMBL35672 | — | — | 1 | 7.89 |
| CHEMBL35234 | — | — | 1 | 7.89 |
| CHEMBL35440 | — | — | 1 | 7.80 |
| CHEMBL32153 | — | — | 1 | 7.62 |
| CHEMBL284852 | — | — | 1 | 7.50 |
| CHEMBL511115 | CILOMILAST | 3.0 | 1 | 7.42 |
| CHEMBL285500 | — | — | 1 | 7.36 |
| CHEMBL286392 | — | — | 1 | 7.35 |
| CHEMBL418231 | — | — | 1 | 7.28 |
| CHEMBL284479 | — | — | 1 | 6.96 |
| CHEMBL284091 | — | — | 1 | 6.11 |
| CHEMBL33090 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL36348 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL35954 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL287348 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL287114 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL286224 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL32442 | CDP840 | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL285247 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL36242 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL266000 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL35350 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL289023 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL285895 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL35672 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL35234 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL35440 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL32153 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL284852 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL511115 | CILOMILAST | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL285500 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL286392 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL418231 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL284479 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL284091 | — | IC50 | = | 772.0 | nM | 6.11 |
| CHEMBL33090 | — | IC50 | > | 1000.0 | nM | - |