Assay Detail
Functional
CHEMBL1099508
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Antiinflammatory activity against LPS-induced TNFalpha production in human THP1 cells after 3 hrs
22
Total Activities
22
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 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 | 8.14 | 8.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1082158 | — | — | 1 | 8.77 |
| CHEMBL1080673 | — | — | 1 | 8.77 |
| CHEMBL1082206 | — | — | 1 | 8.68 |
| CHEMBL1081991 | — | — | 1 | 8.68 |
| CHEMBL1088443 | — | — | 1 | 8.55 |
| CHEMBL1081208 | — | — | 1 | 8.49 |
| CHEMBL1088032 | — | — | 1 | 8.43 |
| CHEMBL1076560 | — | — | 1 | 8.31 |
| CHEMBL1076741 | — | — | 1 | 8.31 |
| CHEMBL1082182 | — | — | 1 | 8.30 |
| CHEMBL1082159 | — | — | 1 | 8.10 |
| CHEMBL1082183 | — | — | 1 | 8.09 |
| CHEMBL1081037 | — | — | 1 | 8.08 |
| CHEMBL1088166 | — | — | 1 | 8.06 |
| CHEMBL1081990 | — | — | 1 | 8.06 |
| CHEMBL1082205 | — | — | 1 | 8.03 |
| CHEMBL1088442 | — | — | 1 | 7.85 |
| CHEMBL1087386 | — | — | 1 | 7.75 |
| CHEMBL1088440 | — | — | 1 | 7.72 |
| CHEMBL1088441 | — | — | 1 | 7.60 |
| CHEMBL1088167 | — | — | 1 | 7.28 |
| CHEMBL1088031 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1082158 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1080673 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1082206 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1081991 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1088443 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL1081208 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1088032 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1076560 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1076741 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1082182 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1082159 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL1082183 | — | IC50 | = | 8.2 | nM | 8.09 |
| CHEMBL1081037 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL1088166 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL1081990 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL1082205 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL1088442 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1087386 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1088440 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL1088441 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1088167 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1088031 | — | IC50 | = | 64.0 | nM | 7.19 |