Assay Detail
Functional
CHEMBL1769288
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of TNFalpha-induced IL1-beta production in human whole blood after 2 to 5 hrs by ELISA
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Tissue | Blood |
| Confidence | 1 — Organism |
| 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 | 32 | 6.99 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1232784 | — | — | 1 | 8.05 |
| CHEMBL1766503 | — | — | 1 | 7.96 |
| CHEMBL1766499 | — | — | 1 | 7.89 |
| CHEMBL1766500 | — | — | 1 | 7.85 |
| CHEMBL1766498 | — | — | 1 | 7.82 |
| CHEMBL1766505 | — | — | 1 | 7.82 |
| CHEMBL1766502 | — | — | 1 | 7.75 |
| CHEMBL1766506 | — | — | 1 | 7.55 |
| CHEMBL1766579 | — | — | 1 | 7.52 |
| CHEMBL1232772 | — | — | 1 | 7.35 |
| CHEMBL1232769 | — | — | 1 | 7.30 |
| CHEMBL1766572 | — | — | 1 | 7.28 |
| CHEMBL1766493 | — | — | 1 | 7.19 |
| CHEMBL1766580 | — | — | 1 | 7.17 |
| CHEMBL1766497 | — | — | 1 | 7.08 |
| CHEMBL1766504 | — | — | 1 | 7.08 |
| CHEMBL1766490 | — | — | 1 | 7.07 |
| CHEMBL1090089 | PAMAPIMOD | 2.0 | 1 | 7.00 |
| CHEMBL1230122 | R-1487 | 1.0 | 1 | 6.77 |
| CHEMBL1766577 | — | — | 1 | 6.72 |
| CHEMBL1766501 | — | — | 1 | 6.51 |
| CHEMBL1230351 | — | — | 1 | 6.50 |
| CHEMBL1766574 | — | — | 1 | 6.43 |
| CHEMBL1766495 | — | — | 1 | 6.39 |
| CHEMBL1232773 | — | — | 1 | 6.35 |
| CHEMBL1766491 | — | — | 1 | 6.26 |
| CHEMBL1766496 | — | — | 1 | 6.15 |
| CHEMBL1766494 | — | — | 1 | 6.14 |
| CHEMBL1766581 | — | — | 1 | 6.11 |
| CHEMBL1766492 | — | — | 1 | 5.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1232784 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1766503 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1766499 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1766500 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1766498 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1766505 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1766502 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1766506 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1766579 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL1232772 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL1232769 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL1766572 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL1766493 | — | IC50 | = | 64.8 | nM | 7.19 |
| CHEMBL1766580 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL1766504 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1766497 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1766490 | — | IC50 | = | 85.7 | nM | 7.07 |
| CHEMBL1090089 | PAMAPIMOD | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL1230122 | R-1487 | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL1766577 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL1766501 | — | IC50 | = | 308.0 | nM | 6.51 |
| CHEMBL1230351 | — | IC50 | = | 318.0 | nM | 6.50 |
| CHEMBL1766574 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL1766495 | — | IC50 | = | 407.0 | nM | 6.39 |
| CHEMBL1232773 | — | IC50 | = | 451.0 | nM | 6.35 |
| CHEMBL1766491 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL1766496 | — | IC50 | = | 713.0 | nM | 6.15 |
| CHEMBL1766494 | — | IC50 | = | 731.0 | nM | 6.14 |
| CHEMBL1766581 | — | IC50 | = | 769.0 | nM | 6.11 |
| CHEMBL1766492 | — | IC50 | = | 1219.0 | nM | 5.91 |
| CHEMBL1766578 | — | IC50 | = | 1487.0 | nM | 5.83 |
| CHEMBL1230610 | — | IC50 | > | 3000.0 | nM | - |