Assay Detail
Functional
CHEMBL1063390
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TNF-alpha-stimulated IL8 production in human whole blood incubated for 1 hr before TNFalpha challenge measured after 16 to 18 hrs
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.24 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL562527 | — | — | 1 | 9.03 |
| CHEMBL558448 | — | — | 1 | 8.96 |
| CHEMBL558912 | — | — | 1 | 8.89 |
| CHEMBL550519 | — | — | 1 | 8.89 |
| CHEMBL563097 | — | — | 1 | 8.85 |
| CHEMBL564054 | — | — | 1 | 8.82 |
| CHEMBL559403 | — | — | 1 | 8.77 |
| CHEMBL560390 | — | — | 1 | 8.72 |
| CHEMBL559597 | — | — | 1 | 8.72 |
| CHEMBL559401 | — | — | 1 | 8.62 |
| CHEMBL563941 | — | — | 1 | 8.60 |
| CHEMBL561932 | — | — | 1 | 8.60 |
| CHEMBL560730 | — | — | 1 | 8.59 |
| CHEMBL552271 | — | — | 1 | 8.47 |
| CHEMBL550798 | — | — | 1 | 8.15 |
| CHEMBL559242 | — | — | 1 | 8.09 |
| CHEMBL562528 | — | — | 1 | 7.89 |
| CHEMBL563284 | — | — | 1 | 7.80 |
| CHEMBL561468 | — | — | 1 | 7.80 |
| CHEMBL559935 | — | — | 1 | 7.72 |
| CHEMBL564121 | — | — | 1 | 7.54 |
| CHEMBL558711 | — | — | 1 | 7.10 |
| CHEMBL557515 | — | — | 1 | 6.69 |
| CHEMBL563091 | — | — | 1 | 6.39 |
| CHEMBL563326 | — | — | 1 | - |
| CHEMBL562736 | — | — | 1 | - |
| CHEMBL550596 | — | — | 1 | - |
| CHEMBL556212 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL562527 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL558448 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL558912 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL550519 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL563097 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL564054 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL559403 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL560390 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL559597 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL559401 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL563941 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL561932 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL560730 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL552271 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL550798 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL559242 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL562528 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL563284 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL561468 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL559935 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL564121 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL558711 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL557515 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL563091 | — | IC50 | = | 403.0 | nM | 6.39 |
| CHEMBL563326 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL562736 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL550596 | — | IC50 | > | 833.0 | nM | - |
| CHEMBL556212 | — | IC50 | > | 2500.0 | nM | - |