Assay Detail
Binding
CHEMBL3991880
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
Serine/threonine-protein kinase SIK3 (CHEMBL6149) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 242 | 6.36 | 8.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 8.70 |
| CHEMBL400402 | — | — | 1 | 8.52 |
| CHEMBL411907 | SONOLISIB | 2.0 | 1 | 7.96 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 7.37 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 7.25 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 7.15 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.83 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.80 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.69 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.58 |
| CHEMBL3688339 | — | — | 1 | 6.45 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.41 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.07 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.07 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 5.89 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 5.81 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 5.70 |
| CHEMBL1950289 | TANZISERTIB | 2.0 | 1 | 5.53 |
| CHEMBL281948 | K-252A | — | 1 | 5.39 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.39 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 5.31 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 5.02 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 4.99 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 4.87 |
| CHEMBL551064 | AEW-541 | 1.0 | 1 | - |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | - |
| CHEMBL3186534 | RIVOCERANIB | 3.0 | 1 | - |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL3991933 | — | — | 1 | - |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105728 | CRENOLANIB | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL400402 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL411907 | SONOLISIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL574737 | UCN-01 | Kd | = | 56.0 | nM | 7.25 |
| CHEMBL571948 | Y-39983 | Kd | = | 71.0 | nM | 7.15 |
| CHEMBL5416410 | DASATINIB | Kd | = | 147.0 | nM | 6.83 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL3545328 | XL-019 | Kd | = | 206.0 | nM | 6.69 |
| CHEMBL564829 | MILCICLIB | Kd | = | 266.0 | nM | 6.58 |
| CHEMBL3688339 | — | Kd | = | 356.0 | nM | 6.45 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 386.0 | nM | 6.41 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 859.0 | nM | 6.07 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 848.0 | nM | 6.07 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL253969 | OSI-632 | Kd | = | 1564.0 | nM | 5.81 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 2005.0 | nM | 5.70 |
| CHEMBL1950289 | TANZISERTIB | Kd | = | 2981.0 | nM | 5.53 |
| CHEMBL281948 | K-252A | Kd | = | 4027.0 | nM | 5.39 |
| CHEMBL495727 | AT-9283 | Kd | = | 4108.0 | nM | 5.39 |
| CHEMBL217092 | SARACATINIB | Kd | = | 4851.0 | nM | 5.31 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 9648.0 | nM | 5.02 |
| CHEMBL482967 | CYC-116 | Kd | = | 10318.0 | nM | 4.99 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 13559.0 | nM | 4.87 |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545154 | POZIOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3301622 | GILTERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2364611 | GALUNISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3039517 | RABUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL551064 | AEW-541 | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL1287853 | FEDRATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL3301612 | ENCORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103842 | VARLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3334567 | SAVOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1084546 | PF-00562271 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |