Assay Detail
Binding
CHEMBL1787755
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Inhibition of p38alpha-dependent TNFalpha production in human whole blood preincubated for 1 hr before LPS challenge by ELISA
17
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.01 | 8.20 |
| pIC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1784177 | — | — | 1 | 8.20 |
| CHEMBL1784174 | — | — | 1 | 7.70 |
| CHEMBL1784176 | — | — | 1 | 7.60 |
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | 7.60 |
| CHEMBL1784175 | — | — | 1 | 7.60 |
| CHEMBL1784173 | — | — | 1 | 7.30 |
| CHEMBL1784172 | — | — | 1 | 7.10 |
| CHEMBL1784171 | — | — | 1 | 7.10 |
| CHEMBL1784169 | — | — | 1 | 7.10 |
| CHEMBL1784164 | — | — | 1 | 6.60 |
| CHEMBL1784170 | — | — | 1 | 6.50 |
| CHEMBL1784168 | — | — | 1 | 6.50 |
| CHEMBL1232887 | — | — | 1 | 6.50 |
| CHEMBL1784165 | — | — | 1 | 5.90 |
| CHEMBL478649 | — | — | 1 | 5.80 |
| CHEMBL1784167 | — | — | 1 | - |
| CHEMBL1784166 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1784177 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL1784174 | — | IC50 | = | 19.95 | nM | 7.70 |
| CHEMBL1784176 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1088752 | LOSMAPIMOD | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1784175 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1784173 | — | IC50 | = | 50.12 | nM | 7.30 |
| CHEMBL1784172 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1784171 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1784169 | — | IC50 | = | 79.43 | nM | 7.10 |
| CHEMBL1784164 | — | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL1784170 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL1784168 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL1232887 | — | IC50 | = | 316.23 | nM | 6.50 |
| CHEMBL1784165 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL478649 | — | IC50 | = | 1584.89 | nM | 5.80 |
| CHEMBL1784167 | — | pIC50 | - | — | - | |
| CHEMBL1784166 | — | pIC50 | - | — | - |