Assay Detail
Binding
CHEMBL3991604
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 | 6.59 | 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 | 8.40 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 8.10 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 8.00 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 8.00 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.70 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.70 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 7.52 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 7.40 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.27 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.19 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 7.11 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 7.04 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 7.00 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.87 |
| CHEMBL3688339 | — | — | 1 | 6.73 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.54 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.52 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 6.52 |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | 6.50 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.46 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 6.46 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 6.45 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.38 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.37 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 6.20 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 6.14 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.05 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 6.04 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 6.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL5416410 | DASATINIB | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL3545085 | XL-228 | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL206834 | BAFETINIB | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL1171837 | PONATINIB | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL1230609 | FORETINIB | Kd | = | 54.0 | nM | 7.27 |
| CHEMBL941 | IMATINIB | Kd | = | 64.0 | nM | 7.19 |
| CHEMBL3600873 | MK-5108 | Kd | = | 77.0 | nM | 7.11 |
| CHEMBL217092 | SARACATINIB | Kd | = | 91.0 | nM | 7.04 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 99.0 | nM | 7.00 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 135.0 | nM | 6.87 |
| CHEMBL3688339 | — | Kd | = | 187.0 | nM | 6.73 |
| CHEMBL255863 | NILOTINIB | Kd | = | 291.0 | nM | 6.54 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 305.0 | nM | 6.52 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 302.0 | nM | 6.52 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 315.0 | nM | 6.50 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 347.0 | nM | 6.46 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 351.0 | nM | 6.46 |
| CHEMBL1908391 | MASITINIB | Kd | = | 354.0 | nM | 6.45 |
| CHEMBL3544932 | TAK-901 | Kd | = | 422.0 | nM | 6.38 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 427.0 | nM | 6.37 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 628.0 | nM | 6.20 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 722.0 | nM | 6.14 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 899.0 | nM | 6.05 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 918.0 | nM | 6.04 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 919.0 | nM | 6.04 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 939.0 | nM | 6.03 |
| CHEMBL483158 | ALISERTIB | Kd | = | 1009.0 | nM | 6.00 |
| CHEMBL403989 | TG100-801 | Kd | = | 1034.0 | nM | 5.99 |
| CHEMBL1289926 | AXITINIB | Kd | = | 1039.0 | nM | 5.98 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1042.0 | nM | 5.98 |
| CHEMBL495727 | AT-9283 | Kd | = | 1082.0 | nM | 5.97 |
| CHEMBL259084 | MLN-8054 | Kd | = | 1293.0 | nM | 5.89 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 1372.0 | nM | 5.86 |
| CHEMBL3699142 | — | Kd | = | 1480.0 | nM | 5.83 |
| CHEMBL460702 | BMS-777607 | Kd | = | 1508.0 | nM | 5.82 |
| CHEMBL564829 | MILCICLIB | Kd | = | 3754.0 | nM | 5.43 |
| CHEMBL2180604 | TAK-593 | Kd | = | 4058.0 | nM | 5.39 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 7071.0 | nM | 5.15 |
| CHEMBL587723 | AEE-788 | Kd | = | 14924.0 | nM | 4.83 |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103840 | DINACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 30000.0 | nM | - |