Assay Detail
Binding
CHEMBL3991668
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.
222
Total Activities
222
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 CLK1 (CHEMBL4224) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 222 | 6.46 | 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 | 8.15 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 8.10 |
| CHEMBL281948 | K-252A | — | 1 | 8.00 |
| CHEMBL3688339 | — | — | 1 | 7.96 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 7.85 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 7.75 |
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 7.60 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 7.05 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.86 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 6.82 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.75 |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | 6.61 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 6.56 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 6.44 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.36 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 6.32 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.23 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.22 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 6.19 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 6.15 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.11 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.04 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.03 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 5.97 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 5.74 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.69 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 5.68 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.67 |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545083 | RGB-286638 | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL564829 | MILCICLIB | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL281948 | K-252A | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL3688339 | — | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL571948 | Y-39983 | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL3544966 | GSK-1059615 | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 138.0 | nM | 6.86 |
| CHEMBL38380 | FASUDIL | Kd | = | 152.0 | nM | 6.82 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 179.0 | nM | 6.75 |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | = | 246.0 | nM | 6.61 |
| CHEMBL189963 | PALBOCICLIB | Kd | = | 276.0 | nM | 6.56 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 363.0 | nM | 6.44 |
| CHEMBL535 | SUNITINIB | Kd | = | 440.0 | nM | 6.36 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 475.0 | nM | 6.32 |
| CHEMBL482967 | CYC-116 | Kd | = | 586.0 | nM | 6.23 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 598.0 | nM | 6.22 |
| CHEMBL3545308 | ROCILETINIB | Kd | = | 651.0 | nM | 6.19 |
| CHEMBL2103840 | DINACICLIB | Kd | = | 714.0 | nM | 6.15 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 778.0 | nM | 6.11 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 918.0 | nM | 6.04 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 942.0 | nM | 6.03 |
| CHEMBL2403108 | CERITINIB | Kd | = | 1059.0 | nM | 5.97 |
| CHEMBL296468 | BMS-387032 | Kd | = | 1841.0 | nM | 5.74 |
| CHEMBL495727 | AT-9283 | Kd | = | 2045.0 | nM | 5.69 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 2107.0 | nM | 5.68 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 2139.0 | nM | 5.67 |
| CHEMBL1230607 | PHA-793887 | Kd | = | 2184.0 | nM | 5.66 |
| CHEMBL1908397 | KW-2449 | Kd | = | 2351.0 | nM | 5.63 |
| CHEMBL2140408 | AMG-900 | Kd | = | 2458.0 | nM | 5.61 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 3233.0 | nM | 5.49 |
| CHEMBL445813 | AT-7519 | Kd | = | 4466.0 | nM | 5.35 |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | = | 24056.0 | nM | 4.62 |
| CHEMBL1738797 | ALECTINIB | Kd | = | 29881.0 | nM | 4.53 |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545137 | PF-00477736 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3301622 | GILTERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3600873 | MK-5108 | Kd | > | 30000.0 | nM | - |
| CHEMBL1090090 | VX-702 | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |