Assay Detail
Binding
CHEMBL3991912
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.
233
Total Activities
233
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
TRAF2 and NCK-interacting protein kinase (CHEMBL4527) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 233 | 6.40 | 8.00 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281948 | K-252A | — | 1 | 8.00 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 7.92 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.64 |
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 7.42 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 7.05 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 7.03 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 6.97 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.74 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.60 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.54 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.42 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.41 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 6.25 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.13 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.10 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 5.95 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | 5.92 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.90 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.90 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 5.89 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 5.86 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 5.86 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 5.75 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.73 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.67 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 5.63 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 5.42 |
| CHEMBL3991934 | — | — | 1 | - |
| CHEMBL1738797 | ALECTINIB | 4.0 | 1 | - |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281948 | K-252A | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL274654 | ORANTINIB | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL565612 | SOTRASTAURIN | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 89.0 | nM | 7.05 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 94.0 | nM | 7.03 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 107.0 | nM | 6.97 |
| CHEMBL3545085 | XL-228 | Kd | = | 184.0 | nM | 6.74 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 251.0 | nM | 6.60 |
| CHEMBL1908397 | KW-2449 | Kd | = | 291.0 | nM | 6.54 |
| CHEMBL1171837 | PONATINIB | Kd | = | 385.0 | nM | 6.42 |
| CHEMBL535 | SUNITINIB | Kd | = | 387.0 | nM | 6.41 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 565.0 | nM | 6.25 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 746.0 | nM | 6.13 |
| CHEMBL495727 | AT-9283 | Kd | = | 801.0 | nM | 6.10 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 1130.0 | nM | 5.95 |
| CHEMBL2364611 | GALUNISERTIB | Kd | = | 1208.0 | nM | 5.92 |
| CHEMBL564829 | MILCICLIB | Kd | = | 1247.0 | nM | 5.90 |
| CHEMBL5416410 | DASATINIB | Kd | = | 1262.0 | nM | 5.90 |
| CHEMBL607707 | PELITINIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 1387.0 | nM | 5.86 |
| CHEMBL217092 | SARACATINIB | Kd | = | 1375.0 | nM | 5.86 |
| CHEMBL1289926 | AXITINIB | Kd | = | 1770.0 | nM | 5.75 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 1881.0 | nM | 5.73 |
| CHEMBL482967 | CYC-116 | Kd | = | 2135.0 | nM | 5.67 |
| CHEMBL1614713 | CC-401 | Kd | = | 2343.0 | nM | 5.63 |
| CHEMBL1230609 | FORETINIB | Kd | = | 3787.0 | nM | 5.42 |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL402548 | DANUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL3128043 | PF-03758309 | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3137336 | UPROSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1079175 | MK-2206 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991933 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL536151 | IMD-0354 | Kd | > | 30000.0 | nM | - |
| CHEMBL3813873 | PEXIDARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL2376648 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1090479 | GSK-1070916 | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL507361 | MIRDAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1088751 | PH-797804 | Kd | > | 30000.0 | nM | - |