Assay Detail
Binding
CHEMBL1102672
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Inhibition of human recombinant p38alpha assessed as phosphorylated ATF2 after 1 hr by HTRF assay
23
Total Activities
23
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
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 | 23 | 8.37 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL558448 | — | — | 1 | 9.00 |
| CHEMBL1082158 | — | — | 1 | 8.85 |
| CHEMBL1076741 | — | — | 1 | 8.80 |
| CHEMBL1082206 | — | — | 1 | 8.80 |
| CHEMBL1081208 | — | — | 1 | 8.77 |
| CHEMBL1081991 | — | — | 1 | 8.77 |
| CHEMBL1081990 | — | — | 1 | 8.68 |
| CHEMBL1076560 | — | — | 1 | 8.64 |
| CHEMBL1080673 | — | — | 1 | 8.57 |
| CHEMBL1088443 | — | — | 1 | 8.52 |
| CHEMBL1082159 | — | — | 1 | 8.52 |
| CHEMBL1088032 | — | — | 1 | 8.48 |
| CHEMBL1082182 | — | — | 1 | 8.39 |
| CHEMBL1087386 | — | — | 1 | 8.34 |
| CHEMBL1088440 | — | — | 1 | 8.30 |
| CHEMBL1081037 | — | — | 1 | 8.20 |
| CHEMBL1082183 | — | — | 1 | 8.11 |
| CHEMBL1088441 | — | — | 1 | 8.07 |
| CHEMBL1088166 | — | — | 1 | 8.00 |
| CHEMBL1082205 | — | — | 1 | 8.00 |
| CHEMBL1088442 | — | — | 1 | 7.92 |
| CHEMBL1088167 | — | — | 1 | 7.44 |
| CHEMBL1088031 | — | — | 1 | 7.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL558448 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1082158 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1076741 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1082206 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL1081208 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1081991 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1081990 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1076560 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1080673 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL1088443 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1082159 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1088032 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1082182 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1087386 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL1088440 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1081037 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL1082183 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL1088441 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL1088166 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1082205 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1088442 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1088167 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL1088031 | — | IC50 | = | 43.0 | nM | 7.37 |