Assay Detail
Binding
CHEMBL3991720
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.
243
Total Activities
243
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 | 243 | 6.43 | 9.00 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 9.00 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.30 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.57 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.55 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.03 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.95 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 6.84 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.76 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.65 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 6.48 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 6.41 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 6.37 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 6.25 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.25 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 6.23 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.20 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 6.19 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 6.14 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.14 |
| CHEMBL3699142 | — | — | 1 | 6.13 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 6.10 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.07 |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | 5.96 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 5.92 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 5.81 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.79 |
| CHEMBL3991934 | — | — | 1 | 5.73 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 5.63 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.52 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL5416410 | DASATINIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL1230609 | FORETINIB | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL1171837 | PONATINIB | Kd | = | 94.0 | nM | 7.03 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 112.0 | nM | 6.95 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 145.0 | nM | 6.84 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 172.0 | nM | 6.76 |
| CHEMBL3544932 | TAK-901 | Kd | = | 222.0 | nM | 6.65 |
| CHEMBL460702 | BMS-777607 | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL206834 | BAFETINIB | Kd | = | 428.0 | nM | 6.37 |
| CHEMBL255863 | NILOTINIB | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 589.0 | nM | 6.23 |
| CHEMBL253969 | OSI-632 | Kd | = | 627.0 | nM | 6.20 |
| CHEMBL1908391 | MASITINIB | Kd | = | 643.0 | nM | 6.19 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 727.0 | nM | 6.14 |
| CHEMBL3600873 | MK-5108 | Kd | = | 724.0 | nM | 6.14 |
| CHEMBL3699142 | — | Kd | = | 736.0 | nM | 6.13 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 795.0 | nM | 6.10 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 850.0 | nM | 6.07 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 1104.0 | nM | 5.96 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 1207.0 | nM | 5.92 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 1548.0 | nM | 5.81 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 1630.0 | nM | 5.79 |
| CHEMBL3991934 | — | Kd | = | 1864.0 | nM | 5.73 |
| CHEMBL217092 | SARACATINIB | Kd | = | 2330.0 | nM | 5.63 |
| CHEMBL564829 | MILCICLIB | Kd | = | 3023.0 | nM | 5.52 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 10837.0 | nM | 4.96 |
| CHEMBL2048872 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3334567 | SAVOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 30000.0 | nM | - |
| CHEMBL3402762 | TEPOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2165191 | AZD-6482 | Kd | > | 30000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2030402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL598797 | CUDC-101 | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL587723 | AEE-788 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103830 | FOSTAMATINIB | Kd | > | 30000.0 | nM | - |