Assay Detail
Binding
CHEMBL1104503
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of LPS-induced MK2 phosphorylation in human whole blood treated 30 mins before LPS challenge measured after 45 mins by FACS analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
MAP kinase-activated protein kinase 2 (CHEMBL2208) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 8.25 | 8.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1089865 | — | — | 1 | 8.37 |
| CHEMBL1091199 | — | — | 1 | 8.24 |
| CHEMBL1091928 | — | — | 1 | 8.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1089865 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1091199 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL1091928 | — | IC50 | = | 7.0 | nM | 8.15 |