Assay Detail
Binding
CHEMBL987299
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Inhibition of human recombinant p38alpha-mediated ATF2 phosphorylation by TR-FRET assay
6
Total Activities
6
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
Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 8.14 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL477583 | GW743024X | — | 1 | 8.22 |
| CHEMBL476351 | GW775608X | — | 1 | 8.22 |
| CHEMBL478649 | — | — | 1 | 8.05 |
| CHEMBL476141 | — | — | 1 | 8.05 |
| CHEMBL95692 | SB-242235 | — | 1 | - |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL477583 | GW743024X | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL476351 | GW775608X | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL478649 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL476141 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL95692 | SB-242235 | Ki | - | — | - | |
| CHEMBL103667 | DORAMAPIMOD | Ki | < | 46.0 | nM | - |