Assay Detail
Functional
CHEMBL866235
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to block TNFalpha release through inhibition of PDE4 in LPS-stimulated human whole blood
22
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.52 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL206968 | — | — | 1 | 7.52 |
| CHEMBL380321 | — | — | 1 | 7.40 |
| CHEMBL208100 | — | — | 1 | 7.30 |
| CHEMBL383225 | — | — | 1 | 7.10 |
| CHEMBL209295 | — | — | 1 | 7.10 |
| CHEMBL207996 | — | — | 1 | 7.05 |
| CHEMBL377709 | — | — | 1 | 7.00 |
| CHEMBL208149 | — | — | 1 | 6.85 |
| CHEMBL382168 | — | — | 1 | 6.85 |
| CHEMBL383837 | — | — | 1 | 6.70 |
| CHEMBL206592 | — | — | 1 | 6.68 |
| CHEMBL208382 | — | — | 3 | 6.60 |
| CHEMBL380933 | — | — | 1 | 6.57 |
| CHEMBL207559 | — | — | 1 | 6.40 |
| CHEMBL379768 | — | — | 1 | 6.10 |
| CHEMBL208236 | — | — | 1 | 6.00 |
| CHEMBL378681 | — | — | 1 | 5.75 |
| CHEMBL204522 | — | — | 1 | 5.70 |
| CHEMBL207424 | — | — | 1 | 5.40 |
| CHEMBL207775 | — | — | 1 | 5.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL206968 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL380321 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL208100 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL383225 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL209295 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL207996 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL377709 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL208149 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL382168 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL383837 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL206592 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL208382 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL380933 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL207559 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL208382 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL379768 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL208236 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL208382 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL378681 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL204522 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL207424 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL207775 | — | IC50 | = | 7000.0 | nM | 5.16 |