Assay Detail
Binding
CHEMBL3991697
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.
240
Total Activities
240
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
Eukaryotic translation initiation factor 2-alpha kinase 1 (CHEMBL6029) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 240 | 5.86 | 7.24 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 7.24 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 6.77 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.47 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.18 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.02 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 5.97 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.78 |
| CHEMBL3182621 | AZD-8330 | 1.0 | 1 | 5.74 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.69 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.48 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 5.48 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 5.45 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 5.43 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 5.42 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 5.36 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 5.32 |
| CHEMBL1801204 | AZD-8055 | 1.0 | 1 | - |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | - |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | - |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | - |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | - |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | - |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | - |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | - |
| CHEMBL488436 | AZD-5438 | 1.0 | 1 | - |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | - |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | - |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | - |
| CHEMBL475251 | R-406 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL428690 | ALVOCIDIB | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 335.0 | nM | 6.47 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 666.0 | nM | 6.18 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 949.0 | nM | 6.02 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 1080.0 | nM | 5.97 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 1661.0 | nM | 5.78 |
| CHEMBL3182621 | AZD-8330 | Kd | = | 1821.0 | nM | 5.74 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 2047.0 | nM | 5.69 |
| CHEMBL3545085 | XL-228 | Kd | = | 3342.0 | nM | 5.48 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 3292.0 | nM | 5.48 |
| CHEMBL253969 | OSI-632 | Kd | = | 3572.0 | nM | 5.45 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 3724.0 | nM | 5.43 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 3803.0 | nM | 5.42 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 4326.0 | nM | 5.36 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 4836.0 | nM | 5.32 |
| CHEMBL3545154 | POZIOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL1079175 | MK-2206 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 30000.0 | nM | - |
| CHEMBL598797 | CUDC-101 | Kd | > | 30000.0 | nM | - |
| CHEMBL3301622 | GILTERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482967 | CYC-116 | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL2140408 | AMG-900 | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2035187 | PACRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1738797 | ALECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL217092 | SARACATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL1287853 | FEDRATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3699142 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL2336325 | VISTUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545215 | BMS-911543 | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL2180604 | TAK-593 | Kd | > | 30000.0 | nM | - |