Assay Detail
Binding
CHEMBL3991754
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.
100
Total Activities
100
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 |
Target
Dual specificity mitogen-activated protein kinase kinase 4 (CHEMBL2897) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 100 | 6.28 | 6.84 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.84 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.10 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.90 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
| CHEMBL2103842 | VARLITINIB | 2.0 | 1 | - |
| CHEMBL475251 | R-406 | 2.0 | 1 | - |
| CHEMBL3182621 | AZD-8330 | 1.0 | 1 | - |
| CHEMBL571546 | TIRBANIBULIN | 4.0 | 1 | - |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | - |
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | - |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | - |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | - |
| CHEMBL3264002 | AVUTOMETINIB | 3.0 | 1 | - |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | - |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | - |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | - |
| CHEMBL2087361 | ICOTINIB | 3.0 | 1 | - |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | - |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | - |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | - |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | - |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | - |
| CHEMBL483158 | ALISERTIB | 3.0 | 1 | - |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | - |
| CHEMBL1094408 | NMS-1286937 | — | 1 | - |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | - |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | - |
| CHEMBL3991931 | — | — | 1 | - |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 146.0 | nM | 6.84 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 790.0 | nM | 6.10 |
| CHEMBL189963 | PALBOCICLIB | Kd | = | 1251.0 | nM | 5.90 |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103842 | VARLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL217092 | SARACATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2165191 | AZD-6482 | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL402548 | DANUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105728 | CRENOLANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544932 | TAK-901 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL2001019 | PF-04217903 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103840 | DINACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991931 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL491473 | CEDIRANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482968 | ENMD-2076 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908397 | KW-2449 | Kd | > | 30000.0 | nM | - |
| CHEMBL507361 | MIRDAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289494 | TIVOZANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL206834 | BAFETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL274654 | ORANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3128043 | PF-03758309 | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3600873 | MK-5108 | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL571546 | TIRBANIBULIN | Kd | > | 30000.0 | nM | - |