Assay Detail
Binding
CHEMBL4719215
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDE-4 in human PBMC assessed as LPS-induced TNFalpha production incubated for 15 mins followed by LPS stimulation and measured after 18 hrs by ELISA relative to control
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
In vivo effective dibenzo[b,d]furan-1-yl-thiazoles as novel PDE-4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 6.98 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | 4.0 | 1 | 8.37 |
| CHEMBL4744412 | — | — | 1 | 7.74 |
| CHEMBL4756900 | — | — | 1 | 7.56 |
| CHEMBL4791975 | — | — | 1 | 7.51 |
| CHEMBL4799096 | — | — | 1 | 7.42 |
| CHEMBL4764245 | — | — | 1 | 7.40 |
| CHEMBL4747406 | — | — | 1 | 7.26 |
| CHEMBL514800 | APREMILAST | 4.0 | 1 | 7.11 |
| CHEMBL4753261 | — | — | 1 | 6.41 |
| CHEMBL4744894 | — | — | 1 | 5.76 |
| CHEMBL4787884 | — | — | 1 | 5.66 |
| CHEMBL4750720 | — | — | 1 | 5.56 |
| CHEMBL4756735 | — | — | 1 | - |
| CHEMBL4758625 | — | — | 1 | - |
| CHEMBL4752629 | — | — | 1 | - |
| CHEMBL4798712 | — | — | 1 | - |
| CHEMBL4753966 | — | — | 1 | - |
| CHEMBL4781742 | — | — | 1 | - |
| CHEMBL4754301 | — | — | 1 | - |
| CHEMBL4744425 | — | — | 1 | - |
| CHEMBL4796802 | — | — | 1 | - |
| CHEMBL4761698 | — | — | 1 | - |
| CHEMBL4799146 | — | — | 1 | - |
| CHEMBL4751333 | — | — | 1 | - |
| CHEMBL4762734 | — | — | 1 | - |
| CHEMBL4755546 | — | — | 1 | - |
| CHEMBL4790625 | — | — | 1 | - |
| CHEMBL4754022 | — | — | 1 | - |
| CHEMBL4748998 | — | — | 1 | - |
| CHEMBL4760887 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL193240 | ROFLUMILAST | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4744412 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL4756900 | — | IC50 | = | 27.7 | nM | 7.56 |
| CHEMBL4791975 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4799096 | — | IC50 | = | 37.7 | nM | 7.42 |
| CHEMBL4764245 | — | IC50 | = | 39.6 | nM | 7.40 |
| CHEMBL4747406 | — | IC50 | = | 54.4 | nM | 7.26 |
| CHEMBL514800 | APREMILAST | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4753261 | — | IC50 | = | 385.7 | nM | 6.41 |
| CHEMBL4744894 | — | IC50 | = | 1753.0 | nM | 5.76 |
| CHEMBL4787884 | — | IC50 | = | 2208.0 | nM | 5.66 |
| CHEMBL4750720 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL4781742 | — | IC50 | - | — | - | |
| CHEMBL4753966 | — | IC50 | - | — | - | |
| CHEMBL4798712 | — | IC50 | - | — | - | |
| CHEMBL4752629 | — | IC50 | - | — | - | |
| CHEMBL4758625 | — | IC50 | - | — | - | |
| CHEMBL4756735 | — | IC50 | - | — | - | |
| CHEMBL4750994 | — | IC50 | - | — | - | |
| CHEMBL4762087 | — | IC50 | - | — | - | |
| CHEMBL4782414 | — | IC50 | - | — | - | |
| CHEMBL4789336 | — | IC50 | - | — | - | |
| CHEMBL4760774 | — | IC50 | - | — | - | |
| CHEMBL4784700 | — | IC50 | - | — | - | |
| CHEMBL4754301 | — | IC50 | - | — | - | |
| CHEMBL4744425 | — | IC50 | - | — | - | |
| CHEMBL4796802 | — | IC50 | - | — | - | |
| CHEMBL4761698 | — | IC50 | - | — | - | |
| CHEMBL4799146 | — | IC50 | - | — | - | |
| CHEMBL4751333 | — | IC50 | - | — | - | |
| CHEMBL4762734 | — | IC50 | - | — | - | |
| CHEMBL4755546 | — | IC50 | - | — | - | |
| CHEMBL4790625 | — | IC50 | - | — | - | |
| CHEMBL4754022 | — | IC50 | - | — | - | |
| CHEMBL4748998 | — | IC50 | - | — | - | |
| CHEMBL4760887 | — | IC50 | - | — | - |