Assay Detail
Binding
CHEMBL3991741
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.
243
Total Activities
243
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 3 (CHEMBL5081) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.46 | 8.15 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 8.15 |
| CHEMBL3688339 | — | — | 1 | 7.92 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 7.62 |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | 7.58 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 7.57 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 7.46 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.37 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 7.24 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 7.10 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.83 |
| CHEMBL281948 | K-252A | — | 1 | 6.59 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.54 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 6.54 |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | 6.30 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.21 |
| CHEMBL488436 | AZD-5438 | 1.0 | 1 | 6.11 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.89 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.85 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 5.82 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.80 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 5.53 |
| CHEMBL1236962 | OMIPALISIB | 2.0 | 1 | 5.52 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.42 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 5.34 |
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 5.06 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 4.59 |
| CHEMBL2376648 | — | — | 1 | - |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | - |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | - |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301622 | GILTERITINIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL3688339 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL3600873 | MK-5108 | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL1952329 | SGI-1776 | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL3544932 | TAK-901 | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL475251 | R-406 | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL482967 | CYC-116 | Kd | = | 57.0 | nM | 7.24 |
| CHEMBL3545085 | XL-228 | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 147.0 | nM | 6.83 |
| CHEMBL281948 | K-252A | Kd | = | 254.0 | nM | 6.59 |
| CHEMBL564829 | MILCICLIB | Kd | = | 291.0 | nM | 6.54 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 286.0 | nM | 6.54 |
| CHEMBL1822792 | MK-2461 | Kd | = | 502.0 | nM | 6.30 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 623.0 | nM | 6.21 |
| CHEMBL488436 | AZD-5438 | Kd | = | 771.0 | nM | 6.11 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 1290.0 | nM | 5.89 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1415.0 | nM | 5.85 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 1506.0 | nM | 5.82 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1567.0 | nM | 5.80 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 2959.0 | nM | 5.53 |
| CHEMBL1236962 | OMIPALISIB | Kd | = | 3033.0 | nM | 5.52 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 3759.0 | nM | 5.42 |
| CHEMBL259084 | MLN-8054 | Kd | = | 4609.0 | nM | 5.34 |
| CHEMBL3544966 | GSK-1059615 | Kd | = | 8673.0 | nM | 5.06 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 25581.0 | nM | 4.59 |
| CHEMBL3544960 | AT-13148 | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3402762 | TEPOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL1738757 | REBASTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL535 | SUNITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2325741 | CAPIVASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL1922094 | APITOLISIB | Kd | > | 30000.0 | nM | - |