Assay Detail
Functional
CHEMBL1103665
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IL-8 production in TNFalpha challenged human whole blood after 16 to 18 hrs
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
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 | 14 | 8.26 | 8.82 |
| Ki | 1 | 8.27 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1092012 | — | — | 1 | 8.82 |
| CHEMBL1089865 | — | — | 1 | 8.77 |
| CHEMBL1091929 | — | — | 1 | 8.77 |
| CHEMBL1089866 | — | — | 1 | 8.62 |
| CHEMBL1089534 | — | — | 1 | 8.43 |
| CHEMBL1091199 | — | — | 1 | 8.41 |
| CHEMBL1091928 | — | — | 1 | 8.36 |
| CHEMBL1089513 | — | — | 1 | 8.27 |
| CHEMBL1091930 | — | — | 1 | 8.19 |
| CHEMBL1089456 | — | — | 1 | 8.06 |
| CHEMBL1092011 | — | — | 1 | 7.96 |
| CHEMBL1089122 | — | — | 1 | 7.92 |
| CHEMBL1089457 | — | — | 1 | 7.62 |
| CHEMBL1091927 | — | — | 1 | 7.40 |
| CHEMBL1093461 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1092012 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1089865 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1091929 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1089866 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1089534 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1091199 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1091928 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1089513 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL1091930 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL1089456 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL1092011 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1089122 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL1089457 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1091927 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1093461 | — | IC50 | > | 2500.0 | nM | - |