Assay Detail
Binding
CHEMBL1050682
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of p38alpha active form expressed in Escherichia coli BL21(DE3) cells by HTRF assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Displacement assay for the detection of stabilizers of inactive kinase conformations.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 6.26 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL585902 | AMG-548 | 1.0 | 1 | 7.46 |
| CHEMBL514201 | TALMAPIMOD | 2.0 | 1 | 7.44 |
| CHEMBL522387 | — | — | 1 | 7.05 |
| CHEMBL585549 | — | — | 1 | 7.00 |
| CHEMBL313417 | — | — | 1 | 6.96 |
| CHEMBL583263 | — | — | 1 | 6.92 |
| CHEMBL566100 | — | — | 1 | 6.85 |
| CHEMBL568874 | — | — | 1 | 6.82 |
| CHEMBL578172 | — | — | 1 | 6.82 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 6.60 |
| CHEMBL570427 | — | — | 1 | 6.54 |
| CHEMBL571544 | — | — | 1 | 6.54 |
| CHEMBL497615 | — | — | 1 | 6.50 |
| CHEMBL569943 | — | — | 1 | 6.34 |
| CHEMBL497033 | — | — | 1 | 6.10 |
| CHEMBL570904 | — | — | 1 | 6.05 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 5.96 |
| CHEMBL568776 | — | — | 1 | 5.96 |
| CHEMBL87580 | — | — | 1 | 5.96 |
| CHEMBL568875 | — | — | 1 | 5.92 |
| CHEMBL569531 | — | — | 1 | 5.82 |
| CHEMBL526930 | — | — | 1 | 5.75 |
| CHEMBL498947 | — | — | 1 | 5.70 |
| CHEMBL568756 | — | — | 1 | 5.62 |
| CHEMBL306380 | — | — | 1 | 5.55 |
| CHEMBL101035 | — | — | 1 | 5.26 |
| CHEMBL510516 | — | — | 1 | 5.22 |
| CHEMBL87277 | — | — | 1 | 4.68 |
| CHEMBL584726 | — | — | 1 | - |
| CHEMBL388978 | STAUROSPORINE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL585902 | AMG-548 | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL514201 | TALMAPIMOD | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL522387 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL585549 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL313417 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL583263 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL566100 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL568874 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL578172 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL103667 | DORAMAPIMOD | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL570427 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL571544 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL497615 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL569943 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL497033 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL570904 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL568776 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL87580 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL568875 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL569531 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL526930 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL498947 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL568756 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL306380 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL101035 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL510516 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL87277 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL584726 | — | IC50 | - | — | - | |
| CHEMBL388978 | STAUROSPORINE | IC50 | - | — | - |