Assay Detail
Functional
CHEMBL3375591
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of LPS-induced TNFalpha release in human PBMC preincubated for 30 mins before LPS stimulation measured after 18 hrs by TR-FRET assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery and early clinical development of 2-{6-[2-(3,5-dichloro-4-pyridyl)acetyl]-2,3-dimethoxyphenoxy}-N-propylacetamide (LEO 29102), a soft-drug inhibitor of phosphodiesterase 4 for topical treatment of atopic dermatitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.25 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3315084 | — | — | 1 | 8.40 |
| CHEMBL3315072 | — | — | 1 | 7.96 |
| CHEMBL3315089 | — | — | 1 | 7.96 |
| CHEMBL3315083 | — | — | 1 | 7.92 |
| CHEMBL3315080 | — | — | 1 | 7.92 |
| CHEMBL3315088 | — | — | 1 | 7.80 |
| CHEMBL3315087 | — | — | 1 | 7.77 |
| CHEMBL48017 | — | — | 1 | 7.72 |
| CHEMBL3315086 | — | — | 1 | 7.66 |
| CHEMBL3315077 | — | — | 1 | 7.58 |
| CHEMBL3315079 | — | — | 1 | 7.52 |
| CHEMBL3315090 | — | — | 1 | 7.26 |
| CHEMBL3315085 | — | — | 1 | 6.95 |
| CHEMBL3315081 | — | — | 1 | 6.87 |
| CHEMBL3315076 | — | — | 1 | 6.80 |
| CHEMBL3315078 | — | — | 1 | 6.64 |
| CHEMBL3313943 | — | — | 1 | 6.59 |
| CHEMBL3315073 | — | — | 1 | 6.36 |
| CHEMBL3315074 | — | — | 1 | 6.25 |
| CHEMBL3315075 | — | — | 1 | 5.02 |
| CHEMBL3315082 | — | — | 1 | - |
| CHEMBL3315071 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3315084 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3315072 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3315089 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3315083 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3315080 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3315088 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3315087 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL48017 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3315086 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3315077 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3315079 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3315090 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL3315085 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL3315081 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL3315076 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL3315078 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3313943 | — | IC50 | = | 259.0 | nM | 6.59 |
| CHEMBL3315073 | — | IC50 | = | 436.0 | nM | 6.36 |
| CHEMBL3315074 | — | IC50 | = | 564.0 | nM | 6.25 |
| CHEMBL3315075 | — | IC50 | = | 9470.0 | nM | 5.02 |
| CHEMBL3315082 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3315071 | — | IC50 | > | 5000.0 | nM | - |