Assay Detail
Binding
CHEMBL1787752
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Inhibition of GST-tagged p38alpha by fluorescence polarization method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 |
|---|---|---|---|
| Ki | 18 | 7.78 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1784164 | — | — | 1 | 8.40 |
| CHEMBL1784177 | — | — | 1 | 8.20 |
| CHEMBL1784172 | — | — | 1 | 8.10 |
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | 8.10 |
| CHEMBL1784175 | — | — | 1 | 8.10 |
| CHEMBL1784174 | — | — | 1 | 8.10 |
| CHEMBL1784173 | — | — | 1 | 8.10 |
| CHEMBL1784171 | — | — | 1 | 8.00 |
| CHEMBL1784169 | — | — | 1 | 8.00 |
| CHEMBL1784170 | — | — | 1 | 7.90 |
| CHEMBL1784165 | — | — | 1 | 7.90 |
| CHEMBL1784176 | — | — | 1 | 7.90 |
| CHEMBL478649 | — | — | 1 | 7.90 |
| CHEMBL1784168 | — | — | 1 | 7.80 |
| CHEMBL1232887 | — | — | 1 | 7.60 |
| CHEMBL1784166 | — | — | 1 | 7.00 |
| CHEMBL1784167 | — | — | 1 | 6.90 |
| CHEMBL1782167 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1784164 | — | Ki | = | 3.981 | nM | 8.40 |
| CHEMBL1784177 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL1784172 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1088752 | LOSMAPIMOD | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1784175 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1784174 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1784173 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL1784171 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1784169 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1784170 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1784165 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1784176 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL478649 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL1784168 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL1232887 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL1784166 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1784167 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL1782167 | — | Ki | = | 794.33 | nM | 6.10 |