Assay Detail
Binding
CHEMBL3991893
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.
167
Total Activities
167
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 | 167 | 6.96 | 7.96 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | 7.96 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.72 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.60 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 7.24 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 6.68 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.64 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.43 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.39 |
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
| CHEMBL270995 | BRIVANIB ALANINATE | 3.0 | 1 | - |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | - |
| CHEMBL3218575 | — | — | 1 | - |
| CHEMBL1645462 | AC-480 | 1.0 | 1 | - |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | - |
| CHEMBL281948 | K-252A | — | 1 | - |
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | - |
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | - |
| CHEMBL1201182 | TEMSIROLIMUS | 4.0 | 1 | - |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | - |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | - |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | - |
| CHEMBL2048872 | — | — | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | - |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | - |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | - |
| CHEMBL3186534 | RIVOCERANIB | 3.0 | 1 | - |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | - |
| CHEMBL2079588 | TELATINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1088752 | LOSMAPIMOD | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 57.0 | nM | 7.24 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 207.0 | nM | 6.68 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 369.0 | nM | 6.43 |
| CHEMBL535 | SUNITINIB | Kd | = | 4084.0 | nM | 5.39 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |
| CHEMBL2165191 | AZD-6482 | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289601 | LENVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2107832 | PIMASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2376648 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL1241855 | RIGOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL24828 | VANDETANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545360 | ASP-3026 | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2017974 | BUPARLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL1233528 | VOLASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544983 | TESEVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103842 | VARLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3187723 | BINIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908397 | KW-2449 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL1873475 | IBRUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545328 | XL-019 | Kd | > | 30000.0 | nM | - |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |