Assay Detail
Binding
CHEMBL3991808
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.
225
Total Activities
225
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 | 225 | 7.11 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270995 | BRIVANIB ALANINATE | 3.0 | 1 | 8.52 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 8.15 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.62 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.60 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.14 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 6.34 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.15 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.37 |
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | - |
| CHEMBL571546 | TIRBANIBULIN | 4.0 | 1 | - |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | - |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | - |
| CHEMBL536151 | IMD-0354 | 1.0 | 1 | - |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | - |
| CHEMBL1614707 | MUBRITINIB | 2.0 | 1 | - |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | - |
| CHEMBL3545076 | LY-2584702 | 1.0 | 1 | - |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | - |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | - |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | - |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | - |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | - |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | - |
| CHEMBL3991931 | — | — | 1 | - |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | - |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | - |
| CHEMBL3334567 | SAVOLITINIB | 3.0 | 1 | - |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | - |
| CHEMBL3991927 | HMN-214 | 1.0 | 1 | - |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL482967 | CYC-116 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 454.0 | nM | 6.34 |
| CHEMBL3544932 | TAK-901 | Kd | = | 705.0 | nM | 6.15 |
| CHEMBL522892 | DOVITINIB | Kd | = | 4242.0 | nM | 5.37 |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1922094 | APITOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1952329 | SGI-1776 | Kd | > | 30000.0 | nM | - |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |
| CHEMBL3813873 | PEXIDARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908397 | KW-2449 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1946170 | REGORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991933 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL3039517 | RABUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1088751 | PH-797804 | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL2140408 | AMG-900 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL38380 | FASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |
| CHEMBL217092 | SARACATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL607707 | PELITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2017974 | BUPARLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2364611 | GALUNISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 30000.0 | nM | - |