Assay Detail
Functional
CHEMBL1099509
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antiinflammatory activity against TNF-alpha-induced IL8 production in human whole blood cells treated 1 hr before TNFalpha challenge measured after 16 to 18 hrs by antibody sandwich assay
22
Total Activities
22
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 2: 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 | 22 | 7.70 | 8.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1081208 | — | — | 1 | 8.74 |
| CHEMBL1081991 | — | — | 1 | 8.59 |
| CHEMBL1080673 | — | — | 1 | 8.59 |
| CHEMBL1082206 | — | — | 1 | 8.42 |
| CHEMBL1088032 | — | — | 1 | 8.35 |
| CHEMBL1082158 | — | — | 1 | 8.17 |
| CHEMBL1088443 | — | — | 1 | 8.11 |
| CHEMBL1082205 | — | — | 1 | 7.96 |
| CHEMBL1076560 | — | — | 1 | 7.89 |
| CHEMBL1082182 | — | — | 1 | 7.68 |
| CHEMBL1082159 | — | — | 1 | 7.68 |
| CHEMBL1081037 | — | — | 1 | 7.64 |
| CHEMBL1076741 | — | — | 1 | 7.58 |
| CHEMBL1088442 | — | — | 1 | 7.52 |
| CHEMBL1081990 | — | — | 1 | 7.52 |
| CHEMBL1082183 | — | — | 1 | 7.34 |
| CHEMBL1088166 | — | — | 1 | 7.25 |
| CHEMBL1087386 | — | — | 1 | 7.12 |
| CHEMBL1088441 | — | — | 1 | 7.02 |
| CHEMBL1088440 | — | — | 1 | 6.99 |
| CHEMBL1088031 | — | — | 1 | 6.75 |
| CHEMBL1088167 | — | — | 1 | 6.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1081208 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL1081991 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1080673 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL1082206 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1088032 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1082158 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL1088443 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL1082205 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1076560 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1082182 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1082159 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1081037 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1076741 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1088442 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1081990 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1082183 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL1088166 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL1087386 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1088441 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL1088440 | — | IC50 | = | 103.0 | nM | 6.99 |
| CHEMBL1088031 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL1088167 | — | IC50 | = | 371.0 | nM | 6.43 |