Assay Detail
Binding
CHEMBL3991795
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.
230
Total Activities
230
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 |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 230 | 6.57 | 7.82 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.82 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 7.70 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 7.51 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.02 |
| CHEMBL281948 | K-252A | — | 1 | 7.01 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 7.01 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 6.98 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.96 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.89 |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | 6.72 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.46 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.46 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 6.32 |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | 5.96 |
| CHEMBL1094408 | NMS-1286937 | — | 1 | 5.53 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 5.44 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 5.41 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 4.98 |
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | - |
| CHEMBL3186534 | RIVOCERANIB | 3.0 | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
| CHEMBL2165191 | AZD-6482 | 2.0 | 1 | - |
| CHEMBL3188551 | GSK-2636771 | 2.0 | 1 | - |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | - |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | - |
| CHEMBL3545215 | BMS-911543 | 2.0 | 1 | - |
| CHEMBL1201182 | TEMSIROLIMUS | 4.0 | 1 | - |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | - |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | - |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL572878 | TOZASERTIB | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL1721885 | SU-014813 | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 95.0 | nM | 7.02 |
| CHEMBL3545328 | XL-019 | Kd | = | 98.0 | nM | 7.01 |
| CHEMBL281948 | K-252A | Kd | = | 98.0 | nM | 7.01 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 104.0 | nM | 6.98 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 109.0 | nM | 6.96 |
| CHEMBL495727 | AT-9283 | Kd | = | 129.0 | nM | 6.89 |
| CHEMBL2386889 | SCH-900776 | Kd | = | 189.0 | nM | 6.72 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 349.0 | nM | 6.46 |
| CHEMBL564829 | MILCICLIB | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL1614713 | CC-401 | Kd | = | 483.0 | nM | 6.32 |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | = | 1105.0 | nM | 5.96 |
| CHEMBL1094408 | NMS-1286937 | Kd | = | 2939.0 | nM | 5.53 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 3647.0 | nM | 5.44 |
| CHEMBL1289926 | AXITINIB | Kd | = | 3904.0 | nM | 5.41 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 10424.0 | nM | 4.98 |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1241855 | RIGOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1801204 | AZD-8055 | Kd | > | 30000.0 | nM | - |
| CHEMBL571546 | TIRBANIBULIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1946170 | REGORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614707 | MUBRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3688339 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1873475 | IBRUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2336325 | VISTUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | Kd | > | 30000.0 | nM | - |
| CHEMBL3039513 | DECERNOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL3402762 | TEPOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289494 | TIVOZANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |
| CHEMBL1088752 | LOSMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL402548 | DANUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545307 | MERESTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908397 | KW-2449 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991935 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL411907 | SONOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544983 | TESEVATINIB | Kd | > | 30000.0 | nM | - |