Assay Detail
Binding
CHEMBL4015947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IRAK4 in human PBMC assessed as reduction in R848-stimulated TNF alpha production after 3 hrs
20
Total Activities
20
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 |
Target
Interleukin-1 receptor-associated kinase 4 (CHEMBL3778) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 7.09 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4081711 | ZIMLOVISERTIB | 2.0 | 1 | 8.70 |
| CHEMBL4066705 | — | — | 1 | 8.19 |
| CHEMBL4091434 | — | — | 1 | 8.05 |
| CHEMBL4093120 | — | — | 1 | 7.90 |
| CHEMBL4085199 | — | — | 1 | 7.78 |
| CHEMBL4103497 | — | — | 1 | 7.55 |
| CHEMBL4071526 | — | — | 1 | 7.53 |
| CHEMBL4083655 | — | — | 1 | 7.43 |
| CHEMBL4070515 | — | — | 1 | 7.28 |
| CHEMBL4084228 | — | — | 1 | 7.28 |
| CHEMBL4061801 | — | — | 1 | 7.06 |
| CHEMBL4075552 | — | — | 1 | 6.94 |
| CHEMBL4092338 | — | — | 1 | 6.88 |
| CHEMBL4100091 | — | — | 1 | 6.46 |
| CHEMBL4079243 | — | — | 1 | 6.43 |
| CHEMBL4073250 | — | — | 1 | 6.17 |
| CHEMBL4089619 | — | — | 1 | 5.81 |
| CHEMBL4061890 | — | — | 1 | 5.67 |
| CHEMBL4076912 | — | — | 1 | 5.55 |
| CHEMBL4064661 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4081711 | ZIMLOVISERTIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4066705 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4091434 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4093120 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4085199 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL4103497 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL4071526 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL4083655 | — | IC50 | = | 37.1 | nM | 7.43 |
| CHEMBL4070515 | — | IC50 | = | 52.3 | nM | 7.28 |
| CHEMBL4084228 | — | IC50 | = | 52.1 | nM | 7.28 |
| CHEMBL4061801 | — | IC50 | = | 87.1 | nM | 7.06 |
| CHEMBL4075552 | — | IC50 | = | 115.0 | nM | 6.94 |
| CHEMBL4092338 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4100091 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL4079243 | — | IC50 | = | 373.0 | nM | 6.43 |
| CHEMBL4073250 | — | IC50 | = | 672.0 | nM | 6.17 |
| CHEMBL4089619 | — | IC50 | = | 1552.0 | nM | 5.81 |
| CHEMBL4061890 | — | IC50 | = | 2118.0 | nM | 5.67 |
| CHEMBL4076912 | — | IC50 | = | 2836.0 | nM | 5.55 |
| CHEMBL4064661 | — | IC50 | - | — | - |