Assay Detail
Binding
CHEMBL4266473
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IRAK4 in human KARPAS299 cells assessed as reduction in IL-1 stimulated IRAK4 phosphorylation at Thr345/Ser346 residues preincubated for 1 hr followed by IL-1 stimulation for 10 mins by flow cytometry analysis
27
Total Activities
14
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
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.13 | 6.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4280559 | — | — | 2 | 6.86 |
| CHEMBL4293607 | — | — | 2 | 6.85 |
| CHEMBL4278882 | — | — | 2 | 6.71 |
| CHEMBL4294023 | — | — | 2 | 6.57 |
| CHEMBL4285338 | — | — | 2 | 6.48 |
| CHEMBL4288305 | — | — | 2 | 6.45 |
| CHEMBL4286802 | — | — | 2 | 6.44 |
| CHEMBL4290222 | — | — | 2 | 6.38 |
| CHEMBL4279192 | — | — | 1 | 6.12 |
| CHEMBL4282348 | — | — | 2 | 5.78 |
| CHEMBL4290202 | — | — | 2 | 5.70 |
| CHEMBL4283453 | — | — | 2 | 5.63 |
| CHEMBL4280028 | — | — | 2 | 5.05 |
| CHEMBL4292700 | — | — | 2 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4280559 | — | IC50 | = | 138.04 | nM | 6.86 |
| CHEMBL4293607 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL4293607 | — | IC50 | = | 141.25 | nM | 6.85 |
| CHEMBL4280559 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4278882 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4278882 | — | IC50 | = | 194.98 | nM | 6.71 |
| CHEMBL4294023 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL4294023 | — | IC50 | = | 269.15 | nM | 6.57 |
| CHEMBL4285338 | — | IC50 | = | 331.0 | nM | 6.48 |
| CHEMBL4285338 | — | IC50 | = | 331.13 | nM | 6.48 |
| CHEMBL4288305 | — | IC50 | = | 359.0 | nM | 6.45 |
| CHEMBL4286802 | — | IC50 | = | 363.08 | nM | 6.44 |
| CHEMBL4286802 | — | IC50 | = | 361.0 | nM | 6.44 |
| CHEMBL4288305 | — | IC50 | = | 363.08 | nM | 6.44 |
| CHEMBL4290222 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4290222 | — | IC50 | = | 416.87 | nM | 6.38 |
| CHEMBL4279192 | — | IC50 | = | 758.0 | nM | 6.12 |
| CHEMBL4282348 | — | IC50 | = | 1659.59 | nM | 5.78 |
| CHEMBL4282348 | — | IC50 | = | 1650.0 | nM | 5.78 |
| CHEMBL4290202 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL4290202 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4283453 | — | IC50 | = | 2344.23 | nM | 5.63 |
| CHEMBL4283453 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4280028 | — | IC50 | = | 8910.0 | nM | 5.05 |
| CHEMBL4280028 | — | IC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL4292700 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL4292700 | — | IC50 | = | 13600.0 | nM | 4.87 |