Assay Detail
Binding
CHEMBL2176531
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDE4A-mediated [3H]CAMP hydrolysis after 30 to 60 mins by scintillation proximity assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.64 | 7.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2172376 | — | — | 1 | 7.57 |
| CHEMBL2172373 | — | — | 1 | 6.97 |
| CHEMBL2172374 | — | — | 1 | 6.91 |
| CHEMBL2172375 | — | — | 1 | 6.80 |
| CHEMBL2172372 | — | — | 1 | 6.62 |
| CHEMBL2172370 | — | — | 1 | 6.57 |
| CHEMBL2172369 | — | — | 1 | 6.44 |
| CHEMBL2172367 | — | — | 1 | 6.43 |
| CHEMBL2172366 | — | — | 1 | 6.27 |
| CHEMBL2172368 | — | — | 1 | 6.23 |
| CHEMBL2172371 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2172376 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL2172373 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL2172374 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL2172375 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2172372 | — | IC50 | = | 242.0 | nM | 6.62 |
| CHEMBL2172370 | — | IC50 | = | 271.0 | nM | 6.57 |
| CHEMBL2172369 | — | IC50 | = | 364.0 | nM | 6.44 |
| CHEMBL2172367 | — | IC50 | = | 371.0 | nM | 6.43 |
| CHEMBL2172366 | — | IC50 | = | 537.0 | nM | 6.27 |
| CHEMBL2172368 | — | IC50 | = | 587.0 | nM | 6.23 |
| CHEMBL2172371 | — | IC50 | = | 587.0 | nM | 6.23 |