Assay Detail
Binding
CHEMBL3991740
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
242
Total Activities
242
Compounds Tested
1
Activity Types
1
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | K-562, COLO 205, SK-N-BE(2) and MV-4-11 |
| Subcellular | Cell lysate |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Interleukin-1 receptor-associated kinase 1 (CHEMBL3357) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 242 | 5.94 | 6.90 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.90 |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 6.61 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.59 |
| CHEMBL3688339 | — | — | 1 | 6.36 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.19 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.16 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 5.81 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 5.80 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 5.69 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.68 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.64 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.53 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.40 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 5.36 |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | 5.33 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | - |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | - |
| CHEMBL1088751 | PH-797804 | 2.0 | 1 | - |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | - |
| CHEMBL1615025 | TAK-733 | 2.0 | 1 | - |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | - |
| CHEMBL3545076 | LY-2584702 | 1.0 | 1 | - |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | - |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | - |
| CHEMBL3545215 | BMS-911543 | 2.0 | 1 | - |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | - |
| CHEMBL2376648 | — | — | 1 | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | 2.0 | 1 | - |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 126.0 | nM | 6.90 |
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 247.0 | nM | 6.61 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 258.0 | nM | 6.59 |
| CHEMBL3688339 | — | Kd | = | 441.0 | nM | 6.36 |
| CHEMBL475251 | R-406 | Kd | = | 647.0 | nM | 6.19 |
| CHEMBL1171837 | PONATINIB | Kd | = | 691.0 | nM | 6.16 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 1564.0 | nM | 5.81 |
| CHEMBL3600873 | MK-5108 | Kd | = | 1581.0 | nM | 5.80 |
| CHEMBL206834 | BAFETINIB | Kd | = | 2059.0 | nM | 5.69 |
| CHEMBL564829 | MILCICLIB | Kd | = | 2064.0 | nM | 5.68 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 2303.0 | nM | 5.64 |
| CHEMBL482967 | CYC-116 | Kd | = | 2988.0 | nM | 5.53 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 3942.0 | nM | 5.40 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 4366.0 | nM | 5.36 |
| CHEMBL3301607 | FILGOTINIB | Kd | = | 4714.0 | nM | 5.33 |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218575 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3426621 | RIPASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL3334567 | SAVOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545328 | XL-019 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL491473 | CEDIRANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2336325 | VISTUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1801204 | AZD-8055 | Kd | > | 30000.0 | nM | - |
| CHEMBL3137336 | UPROSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL2325741 | CAPIVASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |