Assay Detail
Binding
CHEMBL4026983
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
38
Total Activities
36
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 and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.58 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4097418 | — | — | 1 | 7.64 |
| CHEMBL4085735 | — | — | 1 | 7.54 |
| CHEMBL4104802 | — | — | 1 | 7.47 |
| CHEMBL4081502 | — | — | 2 | 7.47 |
| CHEMBL4087063 | — | — | 1 | 7.46 |
| CHEMBL4078222 | — | — | 1 | 7.42 |
| CHEMBL4078625 | — | — | 1 | 7.38 |
| CHEMBL4102501 | — | — | 1 | 7.38 |
| CHEMBL4064608 | — | — | 1 | 7.28 |
| CHEMBL4080574 | — | — | 1 | 7.24 |
| CHEMBL4089379 | — | — | 1 | 7.23 |
| CHEMBL4077215 | — | — | 1 | 7.20 |
| CHEMBL4061227 | — | — | 1 | 7.18 |
| CHEMBL4091013 | — | — | 1 | 7.12 |
| CHEMBL4067181 | — | — | 1 | 7.09 |
| CHEMBL4088438 | — | — | 1 | 6.92 |
| CHEMBL4063689 | — | — | 1 | 6.85 |
| CHEMBL4067302 | — | — | 1 | 6.80 |
| CHEMBL4063127 | — | — | 1 | 6.60 |
| CHEMBL4086115 | — | — | 1 | 6.57 |
| CHEMBL4097089 | — | — | 1 | 6.55 |
| CHEMBL4079194 | — | — | 1 | 6.52 |
| CHEMBL4104915 | — | — | 1 | 6.47 |
| CHEMBL4069890 | — | — | 1 | 6.40 |
| CHEMBL3361252 | — | — | 1 | 6.31 |
| CHEMBL4064168 | — | — | 1 | 6.09 |
| CHEMBL4075333 | — | — | 2 | 5.92 |
| CHEMBL4093475 | — | — | 1 | 5.85 |
| CHEMBL4087705 | — | — | 1 | 5.77 |
| CHEMBL4069060 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4097418 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4085735 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4081502 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4104802 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4087063 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4078222 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4102501 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4078625 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4064608 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4080574 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4089379 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4077215 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4061227 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4091013 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4067181 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4088438 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4063689 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4067302 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4063127 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4086115 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4097089 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4079194 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4104915 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4069890 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL3361252 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4081502 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4064168 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL4075333 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4093475 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4087705 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4075333 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL4069060 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4094760 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4096351 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4079819 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4097847 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4105582 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4086053 | — | IC50 | > | 30000.0 | nM | - |