Assay Detail
Binding
CHEMBL3991632
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 | 6.57 | 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 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.52 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 8.52 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 8.30 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.30 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 8.15 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 7.96 |
| CHEMBL3688339 | — | — | 1 | 7.85 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 7.82 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 7.80 |
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | 7.46 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 7.39 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.30 |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | 7.19 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 7.11 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 7.07 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.97 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 6.95 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.88 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.81 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 6.80 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.73 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.53 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.52 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 6.47 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.42 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.30 |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | 6.30 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.19 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 6.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL3545085 | XL-228 | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL5416410 | DASATINIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL941 | IMATINIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL3600873 | MK-5108 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL3688339 | — | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL206834 | BAFETINIB | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL217092 | SARACATINIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL2180604 | TAK-593 | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL1171837 | PONATINIB | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL403989 | TG100-801 | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL1908391 | MASITINIB | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 85.0 | nM | 7.07 |
| CHEMBL1230609 | FORETINIB | Kd | = | 106.0 | nM | 6.97 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 113.0 | nM | 6.95 |
| CHEMBL3544932 | TAK-901 | Kd | = | 133.0 | nM | 6.88 |
| CHEMBL495727 | AT-9283 | Kd | = | 156.0 | nM | 6.81 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL1289926 | AXITINIB | Kd | = | 188.0 | nM | 6.73 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 296.0 | nM | 6.53 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 301.0 | nM | 6.52 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 342.0 | nM | 6.47 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 381.0 | nM | 6.42 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 505.0 | nM | 6.30 |
| CHEMBL587723 | AEE-788 | Kd | = | 495.0 | nM | 6.30 |
| CHEMBL255863 | NILOTINIB | Kd | = | 651.0 | nM | 6.19 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 681.0 | nM | 6.17 |
| CHEMBL31965 | CANERTINIB | Kd | = | 687.0 | nM | 6.16 |
| CHEMBL564829 | MILCICLIB | Kd | = | 685.0 | nM | 6.16 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 703.0 | nM | 6.15 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 739.0 | nM | 6.13 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 858.0 | nM | 6.07 |
| CHEMBL24828 | VANDETANIB | Kd | = | 879.0 | nM | 6.06 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 1108.0 | nM | 5.96 |
| CHEMBL607707 | PELITINIB | Kd | = | 1193.0 | nM | 5.92 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 1235.0 | nM | 5.91 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 1282.0 | nM | 5.89 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1274.0 | nM | 5.89 |
| CHEMBL259084 | MLN-8054 | Kd | = | 1421.0 | nM | 5.85 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 1459.0 | nM | 5.84 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1727.0 | nM | 5.76 |
| CHEMBL553 | ERLOTINIB | Kd | = | 1832.0 | nM | 5.74 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 1907.0 | nM | 5.72 |
| CHEMBL2140408 | AMG-900 | Kd | = | 1968.0 | nM | 5.71 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 2313.0 | nM | 5.64 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 2485.0 | nM | 5.61 |
| CHEMBL253969 | OSI-632 | Kd | = | 2596.0 | nM | 5.59 |