Assay Detail
Binding
CHEMBL1769102
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant p38alpha assessed as incorporation of 33P from gamma-[33P]ATP into myelin basic protein after 30 mins by scintillation counting
35
Total Activities
35
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
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 |
|---|---|---|---|
| IC50 | 35 | 7.84 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1766572 | — | — | 1 | 9.00 |
| CHEMBL1766498 | — | — | 1 | 9.00 |
| CHEMBL1766579 | — | — | 1 | 9.00 |
| CHEMBL1766503 | — | — | 1 | 9.00 |
| CHEMBL1232784 | — | — | 1 | 8.70 |
| CHEMBL1766500 | — | — | 1 | 8.70 |
| CHEMBL1766506 | — | — | 1 | 8.70 |
| CHEMBL1232772 | — | — | 1 | 8.40 |
| CHEMBL1766580 | — | — | 1 | 8.40 |
| CHEMBL1232769 | — | — | 1 | 8.30 |
| CHEMBL1766502 | — | — | 1 | 8.22 |
| CHEMBL1766505 | — | — | 1 | 8.15 |
| CHEMBL1766499 | — | — | 1 | 8.05 |
| CHEMBL1230122 | R-1487 | 1.0 | 1 | 8.00 |
| CHEMBL1230351 | — | — | 1 | 7.96 |
| CHEMBL1766504 | — | — | 1 | 7.92 |
| CHEMBL1766491 | — | — | 1 | 7.85 |
| CHEMBL1090089 | PAMAPIMOD | 2.0 | 1 | 7.85 |
| CHEMBL1766493 | — | — | 1 | 7.82 |
| CHEMBL1766581 | — | — | 1 | 7.82 |
| CHEMBL1766497 | — | — | 1 | 7.75 |
| CHEMBL1766501 | — | — | 1 | 7.70 |
| CHEMBL1766490 | — | — | 1 | 7.68 |
| CHEMBL1766576 | — | — | 1 | 7.60 |
| CHEMBL1766574 | — | — | 1 | 7.51 |
| CHEMBL1766496 | — | — | 1 | 7.40 |
| CHEMBL1766495 | — | — | 1 | 7.38 |
| CHEMBL1230610 | — | — | 1 | 7.30 |
| CHEMBL1766575 | — | — | 1 | 7.17 |
| CHEMBL1232773 | — | — | 1 | 6.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1766572 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1766503 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1766579 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1766498 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1232784 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1766500 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1766506 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1232772 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1766580 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1232769 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1766502 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1766505 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1766499 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1230122 | R-1487 | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1230351 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1766504 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1090089 | PAMAPIMOD | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1766491 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1766493 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1766581 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1766497 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1766501 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1766490 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1766576 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1766574 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL1766496 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1766495 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1230610 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1766575 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL1232773 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL1766494 | — | IC50 | = | 111.0 | nM | 6.96 |
| CHEMBL1766577 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL1766578 | — | IC50 | = | 223.0 | nM | 6.65 |
| CHEMBL1766573 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL1766492 | — | IC50 | = | 594.0 | nM | 6.23 |