Assay Detail
Binding
CHEMBL5338634
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IRAK4 in human PBMC cells assessed as reduction in R848-stimulated TNF-alpha production
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | PBMC |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Interleukin-1 receptor-associated kinase 4 (CHEMBL3778) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
In Retrospect: Root-Cause Analysis of Structure-Activity Relationships in IRAK4 Inhibitor Zimlovisertib (PF-06650833).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.28 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4081711 | ZIMLOVISERTIB | 2.0 | 1 | 8.62 |
| CHEMBL4066705 | — | — | 1 | 8.05 |
| CHEMBL4091434 | — | — | 1 | 8.05 |
| CHEMBL4093120 | — | — | 1 | 7.90 |
| CHEMBL4085199 | — | — | 1 | 7.78 |
| CHEMBL4071526 | — | — | 1 | 7.53 |
| CHEMBL4084228 | — | — | 1 | 7.28 |
| CHEMBL4070515 | — | — | 1 | 7.28 |
| CHEMBL4061801 | — | — | 1 | 7.06 |
| CHEMBL4092338 | — | — | 1 | 6.88 |
| CHEMBL4100091 | — | — | 1 | 6.46 |
| CHEMBL4073250 | — | — | 1 | 6.17 |
| CHEMBL4076912 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4081711 | ZIMLOVISERTIB | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4066705 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4091434 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4093120 | — | IC50 | = | 12.7 | nM | 7.90 |
| CHEMBL4085199 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL4071526 | — | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL4084228 | — | IC50 | = | 52.1 | nM | 7.28 |
| CHEMBL4070515 | — | IC50 | = | 52.3 | nM | 7.28 |
| CHEMBL4061801 | — | IC50 | = | 87.1 | nM | 7.06 |
| CHEMBL4092338 | — | IC50 | = | 133.0 | nM | 6.88 |
| CHEMBL4100091 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL4073250 | — | IC50 | = | 672.0 | nM | 6.17 |
| CHEMBL4076912 | — | IC50 | = | 2836.0 | nM | 5.55 |