Assay Detail
Functional
CHEMBL1932273
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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
29
Total Activities
29
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 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 | 29 | 5.95 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1929235 | — | — | 1 | 6.80 |
| CHEMBL1929239 | — | — | 1 | 6.77 |
| CHEMBL1929230 | — | — | 1 | 6.64 |
| CHEMBL1929227 | — | — | 1 | 6.64 |
| CHEMBL1926710 | — | — | 1 | 6.60 |
| CHEMBL1929222 | — | — | 1 | 6.57 |
| CHEMBL1929238 | — | — | 1 | 6.41 |
| CHEMBL1929234 | — | — | 1 | 6.41 |
| CHEMBL1929237 | — | — | 1 | 6.28 |
| CHEMBL1929217 | — | — | 1 | 6.23 |
| CHEMBL1929233 | — | — | 1 | 6.08 |
| CHEMBL1929218 | — | — | 1 | 5.89 |
| CHEMBL1929224 | — | — | 1 | 5.89 |
| CHEMBL1929225 | — | — | 1 | 5.80 |
| CHEMBL1929220 | — | — | 1 | 5.80 |
| CHEMBL1929197 | — | — | 1 | 5.68 |
| CHEMBL1929219 | — | — | 1 | 5.60 |
| CHEMBL1929195 | — | — | 1 | 5.60 |
| CHEMBL1929215 | — | — | 1 | 5.60 |
| CHEMBL1929196 | — | — | 1 | 5.57 |
| CHEMBL1929216 | — | — | 1 | 5.55 |
| CHEMBL1929223 | — | — | 1 | 5.55 |
| CHEMBL1929231 | — | — | 1 | 5.52 |
| CHEMBL1929232 | — | — | 1 | 5.38 |
| CHEMBL1929226 | — | — | 1 | 5.32 |
| CHEMBL1929229 | — | — | 1 | 5.24 |
| CHEMBL1929228 | — | — | 1 | 5.16 |
| CHEMBL1929236 | — | — | 1 | - |
| CHEMBL1929221 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1929235 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1929239 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1929230 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1929227 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL1926710 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1929222 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL1929238 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1929234 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1929237 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL1929217 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1929233 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL1929218 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1929224 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1929225 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1929220 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL1929197 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1929219 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1929195 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1929215 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1929196 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1929216 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1929223 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL1929231 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL1929232 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL1929226 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL1929229 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1929228 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL1929236 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1929221 | — | IC50 | > | 3000.0 | nM | - |