Assay Detail
Binding
CHEMBL3380178
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-fused full-length human IRAK4 (1 to 460 amino acids) assessed as reduction in phosphorylated substrates by Caliper assay
10
Total Activities
10
Compounds Tested
2
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
Recent advances in the discovery of small molecule inhibitors of interleukin-1 receptor-associated kinase 4 (IRAK4) as a therapeutic target for inflammation and oncology disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.00 | 7.00 |
| Ki | 3 | 8.14 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3361255 | — | — | 1 | 9.00 |
| CHEMBL3361254 | — | — | 1 | 8.12 |
| CHEMBL3361252 | — | — | 1 | 7.30 |
| CHEMBL3353186 | — | — | 1 | 7.00 |
| CHEMBL3353185 | — | — | 1 | 7.00 |
| CHEMBL3353184 | — | — | 1 | 7.00 |
| CHEMBL3361258 | — | — | 1 | - |
| CHEMBL3361257 | — | — | 1 | - |
| CHEMBL3361256 | — | — | 1 | - |
| CHEMBL3361253 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3361255 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3361254 | — | Ki | = | 7.5 | nM | 8.12 |
| CHEMBL3361252 | — | Ki | = | 50.0 | nM | 7.30 |
| CHEMBL3353186 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3353185 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3353184 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3361258 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL3361257 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL3361256 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL3361253 | — | IC50 | <= | 5000.0 | nM | - |