Assay Detail
Binding
CHEMBL3991913
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
Non-receptor tyrosine-protein kinase TNK1 (CHEMBL5334) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.48 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 8.52 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 8.22 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 7.57 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 7.48 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 7.41 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 7.34 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.31 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 7.26 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 7.18 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.08 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.97 |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | 6.82 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 6.80 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.76 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 6.54 |
| CHEMBL281948 | K-252A | — | 1 | 6.54 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.43 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 6.27 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.25 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.21 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.17 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.06 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.05 |
| CHEMBL3991934 | — | — | 1 | 5.90 |
| CHEMBL483158 | ALISERTIB | 3.0 | 1 | 5.90 |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | 5.90 |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | 5.83 |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | 5.83 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 5.78 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545085 | XL-228 | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL3600873 | MK-5108 | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL2403108 | CERITINIB | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 39.0 | nM | 7.41 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 46.0 | nM | 7.34 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 66.0 | nM | 7.18 |
| CHEMBL1171837 | PONATINIB | Kd | = | 84.0 | nM | 7.08 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 108.0 | nM | 6.97 |
| CHEMBL575448 | BMS-754807 | Kd | = | 152.0 | nM | 6.82 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL475251 | R-406 | Kd | = | 173.0 | nM | 6.76 |
| CHEMBL281948 | K-252A | Kd | = | 287.0 | nM | 6.54 |
| CHEMBL3545308 | ROCILETINIB | Kd | = | 289.0 | nM | 6.54 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 369.0 | nM | 6.43 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 536.0 | nM | 6.27 |
| CHEMBL3544932 | TAK-901 | Kd | = | 558.0 | nM | 6.25 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 622.0 | nM | 6.21 |
| CHEMBL5416410 | DASATINIB | Kd | = | 678.0 | nM | 6.17 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 863.0 | nM | 6.06 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 888.0 | nM | 6.05 |
| CHEMBL1231124 | AZD-1480 | Kd | = | 1264.0 | nM | 5.90 |
| CHEMBL483158 | ALISERTIB | Kd | = | 1270.0 | nM | 5.90 |
| CHEMBL3991934 | — | Kd | = | 1265.0 | nM | 5.90 |
| CHEMBL1983268 | ENTRECTINIB | Kd | = | 1486.0 | nM | 5.83 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 1495.0 | nM | 5.83 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 1661.0 | nM | 5.78 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 1683.0 | nM | 5.77 |
| CHEMBL3545154 | POZIOTINIB | Kd | = | 1682.0 | nM | 5.77 |
| CHEMBL3688339 | — | Kd | = | 1778.0 | nM | 5.75 |
| CHEMBL1289926 | AXITINIB | Kd | = | 1870.0 | nM | 5.73 |
| CHEMBL1230609 | FORETINIB | Kd | = | 2653.0 | nM | 5.58 |
| CHEMBL564829 | MILCICLIB | Kd | = | 5684.0 | nM | 5.25 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 11269.0 | nM | 4.95 |
| CHEMBL3991933 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3301607 | FILGOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL1091644 | LINSITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |