Assay Detail
Binding
CHEMBL3991671
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.
163
Total Activities
163
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
Dual specificity protein kinase CLK4 (CHEMBL4203) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 163 | 7.33 | 8.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 8.70 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 7.89 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 7.89 |
| CHEMBL281948 | K-252A | — | 1 | 7.82 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 7.75 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.69 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 6.29 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.60 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | - |
| CHEMBL1090090 | VX-702 | 2.0 | 1 | - |
| CHEMBL3188551 | GSK-2636771 | 2.0 | 1 | - |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | - |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | - |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | - |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | - |
| CHEMBL598797 | CUDC-101 | 1.0 | 1 | - |
| CHEMBL3991931 | — | — | 1 | - |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | - |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | - |
| CHEMBL483158 | ALISERTIB | 3.0 | 1 | - |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | - |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | - |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | - |
| CHEMBL3334567 | SAVOLITINIB | 3.0 | 1 | - |
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | - |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | - |
| CHEMBL3545307 | MERESTINIB | 2.0 | 1 | - |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | - |
| CHEMBL405130 | WHI-P131 | 1.0 | 1 | - |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545083 | RGB-286638 | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL281948 | K-252A | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL564829 | MILCICLIB | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL475251 | R-406 | Kd | = | 203.0 | nM | 6.69 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 513.0 | nM | 6.29 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 2528.0 | nM | 5.60 |
| CHEMBL1090479 | GSK-1070916 | Kd | > | 30000.0 | nM | - |
| CHEMBL2386889 | SCH-900776 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1801204 | AZD-8055 | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL1233528 | VOLASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545360 | ASP-3026 | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL592445 | GEDATOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2140408 | AMG-900 | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL38380 | FASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL1738797 | ALECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3039525 | GOLVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2107832 | PIMASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL1091644 | LINSITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL502835 | NINTEDANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482968 | ENMD-2076 | Kd | > | 30000.0 | nM | - |
| CHEMBL3186534 | RIVOCERANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL2336325 | VISTUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL3348923 | TOVORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1287853 | FEDRATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |