Assay Detail
Binding
CHEMBL1769104
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Inhibition of p38alpha
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (pamapimod) and 6-(2,4-difluorophenoxy)-8-methyl-2-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 8.72 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230122 | R-1487 | 1.0 | 1 | 9.70 |
| CHEMBL1766490 | — | — | 1 | 9.52 |
| CHEMBL1090089 | PAMAPIMOD | 2.0 | 1 | 8.89 |
| CHEMBL1234002 | — | — | 1 | 8.00 |
| CHEMBL1235713 | — | — | 1 | 7.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230122 | R-1487 | Kd | = | 0.2 | nM | 9.70 |
| CHEMBL1766490 | — | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL1090089 | PAMAPIMOD | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL1234002 | — | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL1235713 | — | Kd | = | 32.0 | nM | 7.50 |