Assay Detail
Binding
CHEMBL2027255
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Inhibition of p38alpha kinase using KRELVEPLTPSGEAPNQALLR as substrate for 20 mins by lactate dehydrogenase-coupled spectrophotometric assay
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.17 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL119385 | NEFLAMAPIMOD | 2.0 | 1 | 8.05 |
| CHEMBL420134 | — | — | 1 | 7.44 |
| CHEMBL326629 | — | — | 1 | 6.91 |
| CHEMBL115491 | — | — | 1 | 6.75 |
| CHEMBL326089 | — | — | 1 | 6.70 |
| CHEMBL324091 | — | — | 1 | 6.66 |
| CHEMBL113806 | — | — | 1 | 6.60 |
| CHEMBL331361 | — | — | 1 | 6.58 |
| CHEMBL114430 | — | — | 1 | 6.55 |
| CHEMBL117211 | — | — | 1 | 6.44 |
| CHEMBL114962 | — | — | 1 | 6.35 |
| CHEMBL431865 | — | — | 1 | 6.30 |
| CHEMBL2024530 | — | — | 1 | 6.12 |
| CHEMBL114057 | — | — | 1 | 6.10 |
| CHEMBL114121 | — | — | 1 | 5.85 |
| CHEMBL324089 | — | — | 1 | 5.85 |
| CHEMBL2024528 | — | — | 1 | 5.77 |
| CHEMBL326944 | — | — | 1 | 5.72 |
| CHEMBL2024529 | — | — | 1 | 5.46 |
| CHEMBL2024352 | — | — | 1 | 5.39 |
| CHEMBL2024349 | — | — | 1 | 5.36 |
| CHEMBL2024347 | — | — | 1 | 5.30 |
| CHEMBL2024351 | — | — | 1 | 4.96 |
| CHEMBL2024350 | — | — | 1 | 4.92 |
| CHEMBL2024348 | — | — | 1 | - |
| CHEMBL2024353 | — | — | 1 | - |
| CHEMBL2024526 | — | — | 1 | - |
| CHEMBL2024527 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL119385 | NEFLAMAPIMOD | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL420134 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL326629 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL115491 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL326089 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL324091 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL113806 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL331361 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL114430 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL117211 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL114962 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL431865 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL2024530 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL114057 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL114121 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL324089 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL2024528 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL326944 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2024529 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2024352 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL2024349 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2024347 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL2024351 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2024350 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2024348 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2024353 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2024526 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL2024527 | — | IC50 | > | 20000.0 | nM | - |