Assay Detail
ADMET
CHEMBL4359941
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Inhibition of human recombinant full length N-terminal His6-tagged IRAK1 (Argl94 to Ser712 residues) expressed in insect cells using H-KKARFSRFAGSSPSQSSMVAR as substrate incubated for 60 mins by fluorescence polarisation assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Interleukin-1 receptor-associated kinase 1 (CHEMBL3357) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 6.30 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4474636 | — | — | 1 | 7.62 |
| CHEMBL4464832 | — | — | 1 | 7.02 |
| CHEMBL4568867 | — | — | 1 | 6.72 |
| CHEMBL4515682 | — | — | 1 | 6.47 |
| CHEMBL4453861 | — | — | 1 | 6.40 |
| CHEMBL4551768 | — | — | 1 | 6.30 |
| CHEMBL3950656 | — | — | 1 | 6.29 |
| CHEMBL3952937 | — | — | 1 | 5.55 |
| CHEMBL4460458 | — | — | 1 | 5.33 |
| CHEMBL4544284 | — | — | 1 | 5.27 |
| CHEMBL4569648 | — | — | 1 | - |
| CHEMBL3976860 | — | — | 1 | - |
| CHEMBL4554579 | — | — | 1 | - |
| CHEMBL4460055 | — | — | 1 | - |
| CHEMBL4483477 | — | — | 1 | - |
| CHEMBL4436128 | — | — | 1 | - |
| CHEMBL4567291 | — | — | 1 | - |
| CHEMBL3979848 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4474636 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4464832 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL4568867 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL4515682 | — | Ki | = | 340.0 | nM | 6.47 |
| CHEMBL4453861 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL4551768 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL3950656 | — | Ki | = | 510.0 | nM | 6.29 |
| CHEMBL3952937 | — | Ki | = | 2800.0 | nM | 5.55 |
| CHEMBL4460458 | — | Ki | = | 4700.0 | nM | 5.33 |
| CHEMBL4544284 | — | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL4569648 | — | Ki | - | — | - | |
| CHEMBL3976860 | — | Ki | - | — | - | |
| CHEMBL4554579 | — | Ki | > | 5700.0 | nM | - |
| CHEMBL4460055 | — | Ki | > | 5500.0 | nM | - |
| CHEMBL4483477 | — | Ki | > | 6100.0 | nM | - |
| CHEMBL4436128 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4567291 | — | Ki | - | — | - | |
| CHEMBL3979848 | — | Ki | - | — | - |