Assay Detail
Functional
CHEMBL1053416
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Inhibition of LPS-induced TNFalpha release in human THP1 cells after 3 hrs
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| 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 | 8.40 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL558448 | — | — | 1 | 9.36 |
| CHEMBL564054 | — | — | 1 | 9.21 |
| CHEMBL550519 | — | — | 1 | 9.17 |
| CHEMBL558912 | — | — | 1 | 9.06 |
| CHEMBL562527 | — | — | 1 | 9.00 |
| CHEMBL560730 | — | — | 1 | 9.00 |
| CHEMBL563941 | — | — | 1 | 9.00 |
| CHEMBL559401 | — | — | 1 | 9.00 |
| CHEMBL561932 | — | — | 1 | 8.96 |
| CHEMBL559597 | — | — | 1 | 8.96 |
| CHEMBL563097 | — | — | 1 | 8.96 |
| CHEMBL560390 | — | — | 1 | 8.96 |
| CHEMBL559403 | — | — | 1 | 8.89 |
| CHEMBL562528 | — | — | 1 | 8.74 |
| CHEMBL552271 | — | — | 1 | 8.72 |
| CHEMBL559242 | — | — | 1 | 8.49 |
| CHEMBL563284 | — | — | 1 | 8.46 |
| CHEMBL561468 | — | — | 1 | 8.30 |
| CHEMBL559935 | — | — | 1 | 8.17 |
| CHEMBL550798 | — | — | 1 | 8.12 |
| CHEMBL564121 | — | — | 1 | 7.92 |
| CHEMBL558711 | — | — | 1 | 7.85 |
| CHEMBL557515 | — | — | 1 | 7.19 |
| CHEMBL563091 | — | — | 1 | 6.68 |
| CHEMBL550596 | — | — | 1 | 6.26 |
| CHEMBL562736 | — | — | 1 | 6.03 |
| CHEMBL556212 | — | — | 1 | - |
| CHEMBL563326 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL558448 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL564054 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL550519 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL558912 | — | IC50 | = | 0.87 | nM | 9.06 |
| CHEMBL562527 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL560730 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL563941 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL559401 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL561932 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL559597 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL563097 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL560390 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL559403 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL562528 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL552271 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL559242 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL563284 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL561468 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL559935 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL550798 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL564121 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL558711 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL557515 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL563091 | — | IC50 | = | 208.0 | nM | 6.68 |
| CHEMBL550596 | — | IC50 | = | 546.0 | nM | 6.26 |
| CHEMBL562736 | — | IC50 | = | 937.0 | nM | 6.03 |
| CHEMBL556212 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL563326 | — | IC50 | > | 2500.0 | nM | - |