Assay Detail
Binding
CHEMBL4397905
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Inhibition of PDE4 in human PBMC assessed as reduction in LPS-stimulated TNFalpha production preincubated for 1 hr followed by LPS stimulation and measured after 18 to 20 hrs by ELISA
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.64 | 6.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4527894 | — | — | 1 | 6.19 |
| CHEMBL4443701 | — | — | 1 | 5.67 |
| CHEMBL4536368 | — | — | 1 | 5.59 |
| CHEMBL4543264 | — | — | 1 | 5.57 |
| CHEMBL4520636 | — | — | 1 | 5.56 |
| CHEMBL4592339 | — | — | 1 | 5.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4527894 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL4443701 | — | IC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL4536368 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL4543264 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL4520636 | — | IC50 | = | 2730.0 | nM | 5.56 |
| CHEMBL4592339 | — | IC50 | = | 5830.0 | nM | 5.23 |