Assay Detail
Binding
CHEMBL4345131
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IRAK4 in human whole blood assessed as inhibition of R848-induced IL-6 production preincubated for 90 mins followed by R848 stimulation and measured after 3.5 hrs by MSD assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 9.31 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4556091 | — | — | 1 | 10.59 |
| CHEMBL4566431 | — | — | 1 | 10.11 |
| CHEMBL4545898 | — | — | 1 | 10.09 |
| CHEMBL4445098 | — | — | 1 | 10.00 |
| CHEMBL4568894 | — | — | 1 | 9.96 |
| CHEMBL4472406 | — | — | 1 | 9.80 |
| CHEMBL4475494 | — | — | 1 | 9.72 |
| CHEMBL4466981 | — | — | 1 | 9.49 |
| CHEMBL4468790 | — | — | 1 | 9.42 |
| CHEMBL4452765 | — | — | 1 | 9.33 |
| CHEMBL4536154 | — | — | 1 | 8.92 |
| CHEMBL4473269 | — | — | 1 | 8.44 |
| CHEMBL4537890 | — | — | 1 | 8.14 |
| CHEMBL4466517 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4556091 | — | IC50 | = | 0.026 | nM | 10.59 |
| CHEMBL4566431 | — | IC50 | = | 0.078 | nM | 10.11 |
| CHEMBL4545898 | — | IC50 | = | 0.081 | nM | 10.09 |
| CHEMBL4445098 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4568894 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL4472406 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4475494 | — | IC50 | = | 0.19 | nM | 9.72 |
| CHEMBL4466981 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL4468790 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL4452765 | — | IC50 | = | 0.47 | nM | 9.33 |
| CHEMBL4536154 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4473269 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4537890 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL4466517 | — | IC50 | = | 460.0 | nM | 6.34 |