Assay Detail
Binding
CHEMBL4015944
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged human full length IRAK4 preincubated for 20 mins followed by biotinylated-AGAGRDKYKTLRQIR substrate addition in presence of ATP measured after 60 mins by DELFIA method
24
Total Activities
24
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 of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 8.04 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4066705 | — | — | 1 | 10.00 |
| CHEMBL4081711 | ZIMLOVISERTIB | 2.0 | 1 | 9.70 |
| CHEMBL4093120 | — | — | 1 | 9.52 |
| CHEMBL4091434 | — | — | 1 | 9.30 |
| CHEMBL4085199 | — | — | 1 | 9.22 |
| CHEMBL4103497 | — | — | 1 | 8.89 |
| CHEMBL4083655 | — | — | 1 | 8.89 |
| CHEMBL4071526 | — | — | 1 | 8.72 |
| CHEMBL4084228 | — | — | 1 | 8.62 |
| CHEMBL4070515 | — | — | 1 | 8.57 |
| CHEMBL4061801 | — | — | 1 | 8.43 |
| CHEMBL4092338 | — | — | 1 | 8.34 |
| CHEMBL4075552 | — | — | 1 | 8.32 |
| CHEMBL4061890 | — | — | 1 | 8.23 |
| CHEMBL4100091 | — | — | 1 | 8.12 |
| CHEMBL4079243 | — | — | 1 | 7.92 |
| CHEMBL4073250 | — | — | 1 | 7.62 |
| CHEMBL4076912 | — | — | 1 | 7.54 |
| CHEMBL4086222 | — | — | 1 | 7.14 |
| CHEMBL4089619 | — | — | 1 | 6.92 |
| CHEMBL4061493 | — | — | 1 | 6.84 |
| CHEMBL4064661 | — | — | 1 | 6.08 |
| CHEMBL4104133 | — | — | 1 | 5.68 |
| CHEMBL4093989 | — | — | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4066705 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4081711 | ZIMLOVISERTIB | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4093120 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4091434 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4085199 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4103497 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4083655 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4071526 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4084228 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4070515 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4061801 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4092338 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4075552 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4061890 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4100091 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL4079243 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL4073250 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL4076912 | — | IC50 | = | 29.2 | nM | 7.54 |
| CHEMBL4086222 | — | IC50 | = | 71.9 | nM | 7.14 |
| CHEMBL4089619 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4061493 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4064661 | — | IC50 | = | 840.0 | nM | 6.08 |
| CHEMBL4104133 | — | IC50 | = | 2087.0 | nM | 5.68 |
| CHEMBL4093989 | — | IC50 | = | 55000.0 | nM | 4.26 |