Assay Detail
Binding
CHEMBL3991714
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.
243
Total Activities
243
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 | 243 | 5.30 | 6.61 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 6.61 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.11 |
| CHEMBL1079175 | MK-2206 | 2.0 | 1 | 5.97 |
| CHEMBL3688339 | — | — | 1 | 5.96 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 5.85 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 5.62 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 5.58 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 5.57 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 5.55 |
| CHEMBL598797 | CUDC-101 | 1.0 | 1 | 5.54 |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | 5.51 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 5.51 |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | 5.47 |
| CHEMBL3699142 | — | — | 1 | 5.46 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 5.42 |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | 5.42 |
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | 5.41 |
| CHEMBL3109738 | JNJ-26483327 | 1.0 | 1 | 5.40 |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 5.38 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 5.38 |
| CHEMBL1241855 | RIGOSERTIB | 3.0 | 1 | 5.25 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 5.22 |
| CHEMBL551064 | AEW-541 | 1.0 | 1 | 5.19 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.17 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 5.17 |
| CHEMBL1801204 | AZD-8055 | 1.0 | 1 | 5.16 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.16 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 5.13 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 4.98 |
| CHEMBL3545110 | RIBOCICLIB | 4.0 | 1 | 4.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 243.0 | nM | 6.61 |
| CHEMBL482967 | CYC-116 | Kd | = | 783.0 | nM | 6.11 |
| CHEMBL1079175 | MK-2206 | Kd | = | 1069.0 | nM | 5.97 |
| CHEMBL3688339 | — | Kd | = | 1089.0 | nM | 5.96 |
| CHEMBL1229517 | VEMURAFENIB | Kd | = | 1419.0 | nM | 5.85 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 2415.0 | nM | 5.62 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 2628.0 | nM | 5.58 |
| CHEMBL494089 | GSK-690693 | Kd | = | 2701.0 | nM | 5.57 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 2806.0 | nM | 5.55 |
| CHEMBL598797 | CUDC-101 | Kd | = | 2867.0 | nM | 5.54 |
| CHEMBL475251 | R-406 | Kd | = | 3080.0 | nM | 5.51 |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | = | 3108.0 | nM | 5.51 |
| CHEMBL1822792 | MK-2461 | Kd | = | 3418.0 | nM | 5.47 |
| CHEMBL3699142 | — | Kd | = | 3481.0 | nM | 5.46 |
| CHEMBL513909 | BI-2536 | Kd | = | 3801.0 | nM | 5.42 |
| CHEMBL3039517 | RABUSERTIB | Kd | = | 3824.0 | nM | 5.42 |
| CHEMBL3989868 | TUCATINIB | Kd | = | 3912.0 | nM | 5.41 |
| CHEMBL3109738 | JNJ-26483327 | Kd | = | 3974.0 | nM | 5.40 |
| CHEMBL255863 | NILOTINIB | Kd | = | 4138.0 | nM | 5.38 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 4213.0 | nM | 5.38 |
| CHEMBL1241855 | RIGOSERTIB | Kd | = | 5577.0 | nM | 5.25 |
| CHEMBL180022 | NERATINIB | Kd | = | 6029.0 | nM | 5.22 |
| CHEMBL551064 | AEW-541 | Kd | = | 6501.0 | nM | 5.19 |
| CHEMBL1289926 | AXITINIB | Kd | = | 6840.0 | nM | 5.17 |
| CHEMBL939 | GEFITINIB | Kd | = | 6682.0 | nM | 5.17 |
| CHEMBL1801204 | AZD-8055 | Kd | = | 6896.0 | nM | 5.16 |
| CHEMBL553 | ERLOTINIB | Kd | = | 6905.0 | nM | 5.16 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 7354.0 | nM | 5.13 |
| CHEMBL607707 | PELITINIB | Kd | = | 10545.0 | nM | 4.98 |
| CHEMBL3545110 | RIBOCICLIB | Kd | = | 12308.0 | nM | 4.91 |
| CHEMBL3120215 | OSI-027 | Kd | = | 12611.0 | nM | 4.90 |
| CHEMBL483321 | CP-724714 | Kd | = | 28570.0 | nM | 4.54 |
| CHEMBL2323775 | MK-8033 | Kd | = | 32640.0 | nM | 4.49 |
| CHEMBL1614713 | CC-401 | Kd | = | 32384.0 | nM | 4.49 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 67914.0 | nM | 4.17 |
| CHEMBL2103842 | VARLITINIB | Kd | = | 76413.0 | nM | 4.12 |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL536151 | IMD-0354 | Kd | > | 30000.0 | nM | - |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2386889 | SCH-900776 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991931 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL402548 | DANUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL3128043 | PF-03758309 | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |