Assay Detail
Binding
CHEMBL3991736
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.
242
Total Activities
242
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
Inhibitor of nuclear factor kappa-B kinase subunit epsilon (CHEMBL3529) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 242 | 6.08 | 6.76 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.76 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.75 |
| CHEMBL3688339 | — | — | 1 | 6.74 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.70 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.67 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.47 |
| CHEMBL3699142 | — | — | 1 | 6.39 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.35 |
| CHEMBL281948 | K-252A | — | 1 | 6.31 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 6.28 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.19 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.18 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.16 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.15 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.10 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.08 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 6.00 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 5.89 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.88 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.86 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 5.84 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 5.83 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.82 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.76 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 5.72 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 5.69 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | 5.69 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.64 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.58 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.56 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL502835 | NINTEDANIB | Kd | = | 173.0 | nM | 6.76 |
| CHEMBL475251 | R-406 | Kd | = | 176.0 | nM | 6.75 |
| CHEMBL3688339 | — | Kd | = | 182.0 | nM | 6.74 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL495727 | AT-9283 | Kd | = | 215.0 | nM | 6.67 |
| CHEMBL3545328 | XL-019 | Kd | = | 342.0 | nM | 6.47 |
| CHEMBL3699142 | — | Kd | = | 408.0 | nM | 6.39 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 443.0 | nM | 6.35 |
| CHEMBL281948 | K-252A | Kd | = | 494.0 | nM | 6.31 |
| CHEMBL574737 | UCN-01 | Kd | = | 528.0 | nM | 6.28 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 642.0 | nM | 6.19 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 658.0 | nM | 6.18 |
| CHEMBL482967 | CYC-116 | Kd | = | 689.0 | nM | 6.16 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 715.0 | nM | 6.15 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 796.0 | nM | 6.10 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 838.0 | nM | 6.08 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 992.0 | nM | 6.00 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 1291.0 | nM | 5.89 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 1320.0 | nM | 5.88 |
| CHEMBL3545085 | XL-228 | Kd | = | 1387.0 | nM | 5.86 |
| CHEMBL274654 | ORANTINIB | Kd | = | 1430.0 | nM | 5.84 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 1468.0 | nM | 5.83 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1510.0 | nM | 5.82 |
| CHEMBL535 | SUNITINIB | Kd | = | 1731.0 | nM | 5.76 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 1902.0 | nM | 5.72 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 2057.0 | nM | 5.69 |
| CHEMBL1721885 | SU-014813 | Kd | = | 2034.0 | nM | 5.69 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 2264.0 | nM | 5.64 |
| CHEMBL1908397 | KW-2449 | Kd | = | 2620.0 | nM | 5.58 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 2728.0 | nM | 5.56 |
| CHEMBL564829 | MILCICLIB | Kd | = | 2966.0 | nM | 5.53 |
| CHEMBL571948 | Y-39983 | Kd | > | 30000.0 | nM | - |
| CHEMBL1091644 | LINSITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3186534 | RIVOCERANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1922094 | APITOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | > | 30000.0 | nM | - |
| CHEMBL1952329 | SGI-1776 | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105728 | CRENOLANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |