Assay Detail
Binding
CHEMBL4337359
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Inhibition of P38alpha MAPK (unknown origin)
32
Total Activities
26
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
Discovery of potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.09 | 9.10 |
| Ki | 8 | 7.99 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL492265 | — | — | 2 | 9.40 |
| CHEMBL1232751 | — | — | 1 | 9.05 |
| CHEMBL494072 | — | — | 1 | 9.05 |
| CHEMBL4575052 | — | — | 1 | 9.00 |
| CHEMBL1082158 | — | — | 2 | 9.00 |
| CHEMBL3086685 | — | — | 1 | 9.00 |
| CHEMBL1800911 | — | — | 1 | 8.89 |
| CHEMBL252535 | — | — | 1 | 8.66 |
| CHEMBL1091199 | — | — | 1 | 8.64 |
| CHEMBL1234931 | — | — | 1 | 8.52 |
| CHEMBL252128 | — | — | 1 | 8.51 |
| CHEMBL559401 | — | — | 1 | 8.49 |
| CHEMBL258202 | — | — | 1 | 8.46 |
| CHEMBL1230070 | — | — | 1 | 8.41 |
| CHEMBL1807446 | — | — | 1 | 8.40 |
| CHEMBL4593539 | — | — | 1 | 8.15 |
| CHEMBL2401978 | — | — | 1 | 8.15 |
| CHEMBL1232887 | — | — | 2 | 8.05 |
| CHEMBL522579 | — | — | 1 | 8.00 |
| CHEMBL4535046 | — | — | 1 | 8.00 |
| CHEMBL478649 | — | — | 2 | 7.92 |
| CHEMBL1230065 | BMS-582949 | 2.0 | 1 | 7.89 |
| CHEMBL2177219 | — | — | 1 | 7.46 |
| CHEMBL1938764 | — | — | 1 | 7.24 |
| CHEMBL270164 | GW607117X | — | 2 | 6.62 |
| CHEMBL273158 | — | — | 2 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL492265 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL492265 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL494072 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1232751 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4575052 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1082158 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3086685 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1800911 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL1082158 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL252535 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL1091199 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL1234931 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL252128 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL559401 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL258202 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL1230070 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL1807446 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL2401978 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4593539 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1232887 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL522579 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4535046 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL478649 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1230065 | BMS-582949 | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2177219 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1938764 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL478649 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL270164 | GW607117X | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL1232887 | — | IC50 | = | 316.2 | nM | 6.50 |
| CHEMBL273158 | — | Ki | = | 480.0 | nM | 6.32 |
| CHEMBL270164 | GW607117X | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL273158 | — | IC50 | = | 3000.0 | nM | 5.52 |