Assay Detail
Binding
CHEMBL4359943
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of IRAK4 in human THP1-Xblue-MD2-CD14 cells assessed as reduction in LPS-induced NFkappaB transcription by measuring alkaline phosphatase level preincubated for 1 hr followed by LPS stimulation and measured after 20 hrs by quanti-blue reagent based reporter assay
40
Total Activities
40
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
Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 40 | 6.90 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4474636 | — | — | 1 | 8.10 |
| CHEMBL4483551 | — | — | 1 | 7.60 |
| CHEMBL4453861 | — | — | 1 | 7.46 |
| CHEMBL4467170 | — | — | 1 | 7.42 |
| CHEMBL3950656 | — | — | 1 | 7.39 |
| CHEMBL4464832 | — | — | 1 | 7.28 |
| CHEMBL4461516 | — | — | 1 | 7.28 |
| CHEMBL4452936 | — | — | 1 | 7.25 |
| CHEMBL4569547 | — | — | 1 | 7.25 |
| CHEMBL4520118 | — | — | 1 | 7.25 |
| CHEMBL4438027 | — | — | 1 | 7.22 |
| CHEMBL4515682 | — | — | 1 | 7.22 |
| CHEMBL4518559 | — | — | 1 | 7.18 |
| CHEMBL4568867 | — | — | 1 | 7.12 |
| CHEMBL4456286 | — | — | 1 | 7.08 |
| CHEMBL4483477 | — | — | 1 | 7.01 |
| CHEMBL4551768 | — | — | 1 | 7.01 |
| CHEMBL4584820 | — | — | 1 | 7.01 |
| CHEMBL4531013 | — | — | 1 | 6.89 |
| CHEMBL4459509 | — | — | 1 | 6.85 |
| CHEMBL4473269 | — | — | 1 | 6.77 |
| CHEMBL4466517 | — | — | 1 | 6.77 |
| CHEMBL4576141 | — | — | 1 | 6.77 |
| CHEMBL4524886 | — | — | 1 | 6.64 |
| CHEMBL4460055 | — | — | 1 | 6.60 |
| CHEMBL4466092 | — | — | 1 | 6.48 |
| CHEMBL4554579 | — | — | 1 | 6.48 |
| CHEMBL4439253 | — | — | 1 | 6.46 |
| CHEMBL3952937 | — | — | 1 | 6.43 |
| CHEMBL4436128 | — | — | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4474636 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4483551 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4453861 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4467170 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL3950656 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4464832 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4461516 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4520118 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4452936 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4569547 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4515682 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4438027 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4518559 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4568867 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4456286 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4483477 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4584820 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4551768 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4531013 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4459509 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4473269 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4576141 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4466517 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4524886 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4460055 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4466092 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4554579 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4439253 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL3952937 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4436128 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4462969 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4460458 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4544284 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4550566 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4474664 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4463353 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL3976860 | — | IC50 | - | — | - | |
| CHEMBL4569648 | — | IC50 | - | — | - | |
| CHEMBL4567291 | — | IC50 | - | — | - | |
| CHEMBL3979848 | — | IC50 | - | — | - |