Assay Detail
Binding
CHEMBL3863952
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDE4 in human whole blood assessed as reduction in LPS-induced TNFalpha production incubated for 24 hrs by ELISA
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 6.88 | 7.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 7.44 |
| CHEMBL3968147 | — | — | 1 | 7.24 |
| CHEMBL3986586 | — | — | 1 | 7.23 |
| CHEMBL3903604 | — | — | 1 | 7.19 |
| CHEMBL3958944 | — | — | 1 | 7.17 |
| CHEMBL3952586 | — | — | 1 | 7.16 |
| CHEMBL3918173 | — | — | 1 | 7.16 |
| CHEMBL3958869 | — | — | 1 | 7.12 |
| CHEMBL3941513 | — | — | 1 | 7.09 |
| CHEMBL3920544 | — | — | 1 | 7.03 |
| CHEMBL3969954 | — | — | 1 | 7.02 |
| CHEMBL3957296 | — | — | 1 | 7.00 |
| CHEMBL3889823 | — | — | 1 | 6.93 |
| CHEMBL3925776 | — | — | 1 | 6.92 |
| CHEMBL3916846 | — | — | 1 | 6.90 |
| CHEMBL3974515 | — | — | 1 | 6.81 |
| CHEMBL3950249 | — | — | 1 | 6.72 |
| CHEMBL3979212 | — | — | 1 | 6.70 |
| CHEMBL3950166 | — | — | 1 | 6.68 |
| CHEMBL3892121 | — | — | 1 | 6.59 |
| CHEMBL3957127 | — | — | 1 | 6.49 |
| CHEMBL3905929 | — | — | 1 | 6.43 |
| CHEMBL3984674 | — | — | 1 | 6.43 |
| CHEMBL3980193 | — | — | 1 | 6.37 |
| CHEMBL3896989 | — | — | 1 | 6.28 |
| CHEMBL3898745 | — | — | 1 | - |
| CHEMBL3978291 | — | — | 1 | - |
| CHEMBL3912622 | — | — | 1 | - |
| CHEMBL3966020 | — | — | 1 | - |
| CHEMBL3935796 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3968147 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3986586 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3903604 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL3958944 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3952586 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL3918173 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3958869 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3941513 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL3920544 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL3969954 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL3957296 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3889823 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL3925776 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3916846 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL3974515 | — | IC50 | = | 154.0 | nM | 6.81 |
| CHEMBL3950249 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3979212 | — | IC50 | = | 202.0 | nM | 6.70 |
| CHEMBL3950166 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL3892121 | — | IC50 | = | 257.0 | nM | 6.59 |
| CHEMBL3957127 | — | IC50 | = | 323.0 | nM | 6.49 |
| CHEMBL3905929 | — | IC50 | = | 374.0 | nM | 6.43 |
| CHEMBL3984674 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL3980193 | — | IC50 | = | 425.0 | nM | 6.37 |
| CHEMBL3896989 | — | IC50 | = | 525.0 | nM | 6.28 |
| CHEMBL3898745 | — | IC50 | - | — | - | |
| CHEMBL3978291 | — | IC50 | - | — | - | |
| CHEMBL3912622 | — | IC50 | - | — | - | |
| CHEMBL3966020 | — | IC50 | - | — | - | |
| CHEMBL3935796 | — | IC50 | - | — | - | |
| CHEMBL3909436 | — | IC50 | - | — | - | |
| CHEMBL3931354 | — | IC50 | - | — | - | |
| CHEMBL3963331 | — | IC50 | - | — | - |