Assay Detail
Binding
CHEMBL3991834
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 PLK4 (CHEMBL3788) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 242 | 6.56 | 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 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 8.30 |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | 8.00 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 7.75 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.68 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 7.50 |
| CHEMBL3688339 | — | — | 1 | 7.48 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 7.39 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 7.37 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 7.16 |
| CHEMBL281948 | K-252A | — | 1 | 7.14 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.05 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.97 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 6.89 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.76 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 6.74 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.67 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.56 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 6.52 |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | 6.51 |
| CHEMBL3699142 | — | — | 1 | 6.48 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.29 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.28 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 6.24 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 6.24 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.21 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.17 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.14 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.14 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545085 | XL-228 | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL575448 | BMS-754807 | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL495727 | AT-9283 | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL3688339 | — | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL3544932 | TAK-901 | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL482967 | CYC-116 | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL281948 | K-252A | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL1230609 | FORETINIB | Kd | = | 106.0 | nM | 6.97 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 129.0 | nM | 6.89 |
| CHEMBL475251 | R-406 | Kd | = | 173.0 | nM | 6.76 |
| CHEMBL3600873 | MK-5108 | Kd | = | 183.0 | nM | 6.74 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 213.0 | nM | 6.67 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 277.0 | nM | 6.56 |
| CHEMBL460702 | BMS-777607 | Kd | = | 301.0 | nM | 6.52 |
| CHEMBL1231124 | AZD-1480 | Kd | = | 308.0 | nM | 6.51 |
| CHEMBL3699142 | — | Kd | = | 333.0 | nM | 6.48 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 512.0 | nM | 6.29 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 520.0 | nM | 6.28 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 575.0 | nM | 6.24 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 570.0 | nM | 6.24 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 619.0 | nM | 6.21 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 668.0 | nM | 6.17 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 722.0 | nM | 6.14 |
| CHEMBL1289926 | AXITINIB | Kd | = | 721.0 | nM | 6.14 |
| CHEMBL259084 | MLN-8054 | Kd | = | 816.0 | nM | 6.09 |
| CHEMBL3545328 | XL-019 | Kd | = | 908.0 | nM | 6.04 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL483158 | ALISERTIB | Kd | = | 1178.0 | nM | 5.93 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 1425.0 | nM | 5.85 |
| CHEMBL3545307 | MERESTINIB | Kd | = | 1610.0 | nM | 5.79 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 1961.0 | nM | 5.71 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1954.0 | nM | 5.71 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 4088.0 | nM | 5.39 |
| CHEMBL2403108 | CERITINIB | Kd | = | 7100.0 | nM | 5.15 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 8141.0 | nM | 5.09 |
| CHEMBL253969 | OSI-632 | Kd | = | 8397.0 | nM | 5.08 |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545215 | BMS-911543 | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2386889 | SCH-900776 | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL592445 | GEDATOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |