Assay Detail
Binding
CHEMBL3991863
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.
229
Total Activities
229
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 | 229 | 7.48 | 7.48 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415049 | BARASERTIB | 3.0 | 1 | 7.48 |
| CHEMBL536151 | IMD-0354 | 1.0 | 1 | - |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | - |
| CHEMBL3545215 | BMS-911543 | 2.0 | 1 | - |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | - |
| CHEMBL3402762 | TEPOTINIB | 4.0 | 1 | - |
| CHEMBL1094408 | NMS-1286937 | — | 1 | - |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | - |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | - |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | - |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | - |
| CHEMBL3218575 | — | — | 1 | - |
| CHEMBL1615025 | TAK-733 | 2.0 | 1 | - |
| CHEMBL3688339 | — | — | 1 | - |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | - |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | - |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | - |
| CHEMBL571546 | TIRBANIBULIN | 4.0 | 1 | - |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
| CHEMBL3186534 | RIVOCERANIB | 3.0 | 1 | - |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | - |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | - |
| CHEMBL1236682 | REFAMETINIB | 2.0 | 1 | - |
| CHEMBL2107832 | PIMASERTIB | 2.0 | 1 | - |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | - |
| CHEMBL1614725 | TAK-285 | 1.0 | 1 | - |
| CHEMBL3408248 | AZD-8186 | 1.0 | 1 | - |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415049 | BARASERTIB | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103882 | TIVANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2035187 | PACRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2041933 | AZD-7762 | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545154 | POZIOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3334567 | SAVOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL281948 | K-252A | Kd | > | 30000.0 | nM | - |
| CHEMBL3301612 | ENCORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2029988 | CEP-32496 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2180604 | TAK-593 | Kd | > | 30000.0 | nM | - |
| CHEMBL1952329 | SGI-1776 | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991935 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1287853 | FEDRATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL2165191 | AZD-6482 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3187723 | BINIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544932 | TAK-901 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545307 | MERESTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | > | 30000.0 | nM | - |