Assay Detail
Binding
CHEMBL1048177
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Inhibition of human recombinant PDE4B by scintillation proximity assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 8.52 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL569791 | — | — | 1 | 11.00 |
| CHEMBL571381 | — | — | 1 | 10.70 |
| CHEMBL584327 | — | — | 1 | 10.00 |
| CHEMBL569556 | — | — | 1 | 9.90 |
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 9.40 |
| CHEMBL571171 | — | — | 1 | 9.20 |
| CHEMBL576479 | — | — | 1 | 9.10 |
| CHEMBL515240 | — | — | 1 | 8.80 |
| CHEMBL570029 | — | — | 1 | 8.80 |
| CHEMBL571593 | — | — | 1 | 8.70 |
| CHEMBL585528 | — | — | 1 | 8.60 |
| CHEMBL585937 | — | — | 1 | 8.50 |
| CHEMBL571386 | — | — | 1 | 8.50 |
| CHEMBL462150 | — | — | 1 | 8.40 |
| CHEMBL569352 | — | — | 1 | 8.20 |
| CHEMBL571594 | — | — | 1 | 8.00 |
| CHEMBL569555 | — | — | 1 | 7.90 |
| CHEMBL569790 | — | — | 1 | 7.60 |
| CHEMBL570956 | — | — | 1 | 7.50 |
| CHEMBL430893 | (-)-ROLIPRAM | — | 1 | 7.40 |
| CHEMBL585537 | — | — | 1 | 7.40 |
| CHEMBL571170 | — | — | 1 | 7.40 |
| CHEMBL571383 | — | — | 1 | 6.80 |
| CHEMBL576311 | — | — | 1 | 6.70 |
| CHEMBL570015 | GSK-256066 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL569791 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL571381 | — | IC50 | = | 0.01995 | nM | 10.70 |
| CHEMBL584327 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL569556 | — | IC50 | = | 0.1259 | nM | 9.90 |
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL571171 | — | IC50 | = | 0.631 | nM | 9.20 |
| CHEMBL576479 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL515240 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL570029 | — | IC50 | = | 1.585 | nM | 8.80 |
| CHEMBL571593 | — | IC50 | = | 1.995 | nM | 8.70 |
| CHEMBL585528 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL585937 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL571386 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL462150 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL569352 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL571594 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL569555 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL569790 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL570956 | — | IC50 | = | 31.62 | nM | 7.50 |
| CHEMBL430893 | (-)-ROLIPRAM | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL585537 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL571170 | — | IC50 | = | 39.81 | nM | 7.40 |
| CHEMBL571383 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL576311 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL570015 | GSK-256066 | IC50 | = | 0.007943 | nM | - |