Assay Detail
Functional
CHEMBL1932274
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Antiinflammatory activity in human PBMC assessed as inhibition of LPS-induced TNFalpha production preincubated for 1 hr before LPS challenge measured after 3 hrs by ELISA in presence of fresh human frozen plasma
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Plasma |
| Cell Type | PBMC |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 5.54 | 6.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1929238 | — | — | 1 | 6.07 |
| CHEMBL1929239 | — | — | 1 | 5.92 |
| CHEMBL1929235 | — | — | 1 | 5.66 |
| CHEMBL1929233 | — | — | 1 | 5.55 |
| CHEMBL1929232 | — | — | 1 | 5.42 |
| CHEMBL1929237 | — | — | 1 | 5.17 |
| CHEMBL1929234 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1929238 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL1929239 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1929235 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1929233 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1929232 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL1929237 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1929234 | — | IC50 | = | 9700.0 | nM | 5.01 |