Assay Detail
Binding
CHEMBL3991894
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.
239
Total Activities
239
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 | 239 | 6.45 | 7.92 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 7.92 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 7.89 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 7.89 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 7.77 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 7.54 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 7.01 |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | 6.76 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 6.03 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 5.98 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 5.95 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 5.95 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 5.94 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.77 |
| CHEMBL3991933 | — | — | 1 | 5.66 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.65 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 5.57 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 5.52 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 5.30 |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | - |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | - |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | - |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | - |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | - |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | - |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | - |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | - |
| CHEMBL598797 | CUDC-101 | 1.0 | 1 | - |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1084546 | PF-00562271 | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL482967 | CYC-116 | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL2103840 | DINACICLIB | Kd | = | 98.0 | nM | 7.01 |
| CHEMBL1230607 | PHA-793887 | Kd | = | 175.0 | nM | 6.76 |
| CHEMBL180022 | NERATINIB | Kd | = | 926.0 | nM | 6.03 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 1052.0 | nM | 5.98 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 1135.0 | nM | 5.95 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 1120.0 | nM | 5.95 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 1143.0 | nM | 5.94 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 1713.0 | nM | 5.77 |
| CHEMBL3991933 | — | Kd | = | 2190.0 | nM | 5.66 |
| CHEMBL535 | SUNITINIB | Kd | = | 2234.0 | nM | 5.65 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 2721.0 | nM | 5.57 |
| CHEMBL2140408 | AMG-900 | Kd | = | 3023.0 | nM | 5.52 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 4996.0 | nM | 5.30 |
| CHEMBL206834 | BAFETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991932 | PEXMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614707 | MUBRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1738797 | ALECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL592445 | GEDATOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545154 | POZIOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL2376648 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | > | 30000.0 | nM | - |
| CHEMBL3813873 | PEXIDARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |
| CHEMBL3301607 | FILGOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991931 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |