Assay Detail
Binding
CHEMBL860120
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Inhibitory activity against PDE4B
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 9.15 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL381681 | — | — | 1 | 10.15 |
| CHEMBL197392 | — | — | 1 | 9.70 |
| CHEMBL197494 | — | — | 1 | 9.52 |
| CHEMBL196969 | — | — | 1 | 9.52 |
| CHEMBL198674 | — | — | 1 | 9.52 |
| CHEMBL371037 | — | — | 1 | 9.52 |
| CHEMBL371089 | — | — | 1 | 9.52 |
| CHEMBL197386 | — | — | 1 | 9.52 |
| CHEMBL199015 | — | — | 1 | 9.40 |
| CHEMBL198853 | — | — | 1 | 9.40 |
| CHEMBL372575 | — | — | 1 | 9.30 |
| CHEMBL198527 | — | — | 1 | 9.30 |
| CHEMBL198732 | — | — | 1 | 8.96 |
| CHEMBL198722 | — | — | 1 | 8.96 |
| CHEMBL32442 | CDP840 | — | 1 | 8.85 |
| CHEMBL198564 | — | — | 1 | 8.74 |
| CHEMBL198432 | — | — | 1 | 8.64 |
| CHEMBL370220 | — | — | 1 | 8.52 |
| CHEMBL382545 | — | — | 1 | 8.19 |
| CHEMBL198464 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL381681 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL197392 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL197494 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL196969 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL198674 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL371037 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL371089 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL197386 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL199015 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL198853 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL372575 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL198527 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL198732 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL198722 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL32442 | CDP840 | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL198564 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL198432 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL370220 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL382545 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL198464 | — | IC50 | = | 19.0 | nM | 7.72 |