Assay Detail
Binding
CHEMBL3991879
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
Serine/threonine-protein kinase SIK2 (CHEMBL5699) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.60 | 8.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 8.70 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 8.15 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.96 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 7.96 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 7.80 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 7.60 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.52 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 7.33 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 7.32 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.26 |
| CHEMBL281948 | K-252A | — | 1 | 7.24 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.96 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.94 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 6.91 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.91 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.89 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.69 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 6.68 |
| CHEMBL3688339 | — | — | 1 | 6.62 |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | 6.57 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.52 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.19 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 6.16 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.10 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.05 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.04 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.00 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.94 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 5.90 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL574737 | UCN-01 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL5416410 | DASATINIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL495727 | AT-9283 | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 47.0 | nM | 7.33 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 48.0 | nM | 7.32 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL281948 | K-252A | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL564829 | MILCICLIB | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL3544932 | TAK-901 | Kd | = | 115.0 | nM | 6.94 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 123.0 | nM | 6.91 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 122.0 | nM | 6.91 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 128.0 | nM | 6.89 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 206.0 | nM | 6.69 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 207.0 | nM | 6.68 |
| CHEMBL3688339 | — | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL2386889 | SCH-900776 | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL3545328 | XL-019 | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 649.0 | nM | 6.19 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 685.0 | nM | 6.16 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 790.0 | nM | 6.10 |
| CHEMBL475251 | R-406 | Kd | = | 890.0 | nM | 6.05 |
| CHEMBL253969 | OSI-632 | Kd | = | 904.0 | nM | 6.04 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1008.0 | nM | 6.00 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 1149.0 | nM | 5.94 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 1255.0 | nM | 5.90 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 1267.0 | nM | 5.90 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1296.0 | nM | 5.89 |
| CHEMBL482967 | CYC-116 | Kd | = | 1405.0 | nM | 5.85 |
| CHEMBL217092 | SARACATINIB | Kd | = | 1407.0 | nM | 5.85 |
| CHEMBL3545085 | XL-228 | Kd | = | 1796.0 | nM | 5.75 |
| CHEMBL3545110 | RIBOCICLIB | Kd | = | 2492.0 | nM | 5.60 |
| CHEMBL3699142 | — | Kd | = | 3513.0 | nM | 5.45 |
| CHEMBL1952329 | SGI-1776 | Kd | = | 6124.0 | nM | 5.21 |
| CHEMBL587723 | AEE-788 | Kd | = | 41795.0 | nM | 4.38 |
| CHEMBL1230607 | PHA-793887 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2140408 | AMG-900 | Kd | > | 30000.0 | nM | - |
| CHEMBL2403108 | CERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL571546 | TIRBANIBULIN | Kd | > | 30000.0 | nM | - |
| CHEMBL2030402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL2323775 | MK-8033 | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |