Assay Detail
Binding
CHEMBL3991603
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 | 6.29 | 8.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 8.70 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.30 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.72 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.62 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 7.58 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.44 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 7.30 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 7.28 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 7.21 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 7.12 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.98 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.97 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 6.89 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 6.71 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 6.68 |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | 6.62 |
| CHEMBL3688339 | — | — | 1 | 6.55 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.52 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.51 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.50 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.50 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.32 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.30 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 6.28 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.23 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.23 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 6.23 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.21 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 6.20 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL5416410 | DASATINIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL206834 | BAFETINIB | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL1171837 | PONATINIB | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL217092 | SARACATINIB | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL3600873 | MK-5108 | Kd | = | 62.0 | nM | 7.21 |
| CHEMBL3545085 | XL-228 | Kd | = | 75.0 | nM | 7.12 |
| CHEMBL1230609 | FORETINIB | Kd | = | 104.0 | nM | 6.98 |
| CHEMBL941 | IMATINIB | Kd | = | 106.0 | nM | 6.97 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 128.0 | nM | 6.89 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 195.0 | nM | 6.71 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 211.0 | nM | 6.68 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 241.0 | nM | 6.62 |
| CHEMBL3688339 | — | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL255863 | NILOTINIB | Kd | = | 301.0 | nM | 6.52 |
| CHEMBL3544932 | TAK-901 | Kd | = | 310.0 | nM | 6.51 |
| CHEMBL495727 | AT-9283 | Kd | = | 315.0 | nM | 6.50 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 317.0 | nM | 6.50 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 479.0 | nM | 6.32 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 498.0 | nM | 6.30 |
| CHEMBL460702 | BMS-777607 | Kd | = | 523.0 | nM | 6.28 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 591.0 | nM | 6.23 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 584.0 | nM | 6.23 |
| CHEMBL1908391 | MASITINIB | Kd | = | 593.0 | nM | 6.23 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 610.0 | nM | 6.21 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 631.0 | nM | 6.20 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 753.0 | nM | 6.12 |
| CHEMBL1922094 | APITOLISIB | Kd | = | 814.0 | nM | 6.09 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 803.0 | nM | 6.09 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 842.0 | nM | 6.08 |
| CHEMBL2180604 | TAK-593 | Kd | = | 918.0 | nM | 6.04 |
| CHEMBL1289926 | AXITINIB | Kd | = | 906.0 | nM | 6.04 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 921.0 | nM | 6.04 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 1098.0 | nM | 5.96 |
| CHEMBL587723 | AEE-788 | Kd | = | 1091.0 | nM | 5.96 |
| CHEMBL24828 | VANDETANIB | Kd | = | 1183.0 | nM | 5.93 |
| CHEMBL564829 | MILCICLIB | Kd | = | 1167.0 | nM | 5.93 |
| CHEMBL259084 | MLN-8054 | Kd | = | 1485.0 | nM | 5.83 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 1545.0 | nM | 5.81 |
| CHEMBL3699142 | — | Kd | = | 1592.0 | nM | 5.80 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 1694.0 | nM | 5.77 |
| CHEMBL2140408 | AMG-900 | Kd | = | 1899.0 | nM | 5.72 |
| CHEMBL1908397 | KW-2449 | Kd | = | 2059.0 | nM | 5.69 |
| CHEMBL253969 | OSI-632 | Kd | = | 2164.0 | nM | 5.67 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 2532.0 | nM | 5.60 |
| CHEMBL522892 | DOVITINIB | Kd | = | 2560.0 | nM | 5.59 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 3474.0 | nM | 5.46 |