Assay Detail
Binding
CHEMBL1103663
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Inhibition of human recombinant p38alpha-mediated AFT2 phosphorylation after 1 hr by HTRF assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| 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 |
|---|---|---|---|
| Ki | 15 | 8.64 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1089866 | — | — | 1 | 9.22 |
| CHEMBL1091929 | — | — | 1 | 9.10 |
| CHEMBL1089456 | — | — | 1 | 9.05 |
| CHEMBL1092012 | — | — | 1 | 9.00 |
| CHEMBL1091928 | — | — | 1 | 8.96 |
| CHEMBL1089865 | — | — | 1 | 8.85 |
| CHEMBL1091930 | — | — | 1 | 8.82 |
| CHEMBL1092011 | — | — | 1 | 8.77 |
| CHEMBL1089122 | — | — | 1 | 8.72 |
| CHEMBL1089534 | — | — | 1 | 8.72 |
| CHEMBL1089513 | — | — | 1 | 8.70 |
| CHEMBL1089457 | — | — | 1 | 8.64 |
| CHEMBL1091199 | — | — | 1 | 8.64 |
| CHEMBL1091927 | — | — | 1 | 8.10 |
| CHEMBL1093461 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1089866 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL1091929 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL1089456 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1092012 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1091928 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL1089865 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL1091930 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1092011 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL1089122 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL1089534 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL1089513 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1089457 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1091199 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1091927 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1093461 | — | Ki | = | 458.0 | nM | 6.34 |