Assay Detail
Binding
CHEMBL1787754
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of p38alpha-dependent TNFalpha production in human PBMC preincubated for 1 hr before LPS challenge by ELISA
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 8 | 7.00 | 7.60 |
| pIC50 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1784176 | — | — | 1 | 7.60 |
| CHEMBL1784174 | — | — | 1 | 7.20 |
| CHEMBL1784164 | — | — | 1 | 7.00 |
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | 7.00 |
| CHEMBL1784172 | — | — | 1 | 6.90 |
| CHEMBL1784165 | — | — | 1 | 6.80 |
| CHEMBL1784173 | — | — | 1 | 6.80 |
| CHEMBL478649 | — | — | 1 | 6.70 |
| CHEMBL1784166 | — | — | 1 | - |
| CHEMBL1784167 | — | — | 1 | - |
| CHEMBL1784175 | — | — | 1 | - |
| CHEMBL1784177 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1784176 | — | IC50 | = | 25.12 | nM | 7.60 |
| CHEMBL1784174 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL1784164 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1088752 | LOSMAPIMOD | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1784172 | — | IC50 | = | 125.89 | nM | 6.90 |
| CHEMBL1784165 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL1784173 | — | IC50 | = | 158.49 | nM | 6.80 |
| CHEMBL478649 | — | IC50 | = | 199.53 | nM | 6.70 |
| CHEMBL1784166 | — | pIC50 | - | — | - | |
| CHEMBL1784167 | — | pIC50 | - | — | - | |
| CHEMBL1784175 | — | pIC50 | - | — | - | |
| CHEMBL1784177 | — | pIC50 | - | — | - |