Assay Detail
Binding
CHEMBL3991696
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 |
|---|---|---|---|---|
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | 9.00 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 8.70 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 8.70 |
| CHEMBL1645462 | AC-480 | 1.0 | 1 | 8.52 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | 8.30 |
| CHEMBL2103842 | VARLITINIB | 2.0 | 1 | 8.30 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 8.10 |
| CHEMBL2138625 | AV-412 FREE BASE | 1.0 | 1 | 8.00 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 7.92 |
| CHEMBL3991931 | — | — | 1 | 7.72 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.47 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 7.42 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.37 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | 7.29 |
| CHEMBL483321 | CP-724714 | 2.0 | 1 | 7.15 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 6.81 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 6.65 |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | 6.39 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.38 |
| CHEMBL3545308 | ROCILETINIB | 3.0 | 1 | 6.30 |
| CHEMBL3109738 | JNJ-26483327 | 1.0 | 1 | 6.22 |
| CHEMBL1614725 | TAK-285 | 1.0 | 1 | 6.17 |
| CHEMBL598797 | CUDC-101 | 1.0 | 1 | 6.13 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.09 |
| CHEMBL405130 | WHI-P131 | 1.0 | 1 | 5.93 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.83 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 5.76 |
| CHEMBL415049 | BARASERTIB | 3.0 | 1 | 5.76 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.73 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2408045 | SAPITINIB | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL1173655 | AFATINIB | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL3545154 | POZIOTINIB | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL1645462 | AC-480 | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL2103842 | VARLITINIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL31965 | CANERTINIB | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL2138625 | AV-412 FREE BASE | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL607707 | PELITINIB | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL3991931 | — | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL180022 | NERATINIB | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL554 | LAPATINIB | Kd | = | 51.0 | nM | 7.29 |
| CHEMBL483321 | CP-724714 | Kd | = | 71.0 | nM | 7.15 |
| CHEMBL3353410 | OSIMERTINIB | Kd | = | 155.0 | nM | 6.81 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 225.0 | nM | 6.65 |
| CHEMBL587723 | AEE-788 | Kd | = | 403.0 | nM | 6.39 |
| CHEMBL939 | GEFITINIB | Kd | = | 413.0 | nM | 6.38 |
| CHEMBL3545308 | ROCILETINIB | Kd | = | 498.0 | nM | 6.30 |
| CHEMBL3109738 | JNJ-26483327 | Kd | = | 602.0 | nM | 6.22 |
| CHEMBL1614725 | TAK-285 | Kd | = | 677.0 | nM | 6.17 |
| CHEMBL598797 | CUDC-101 | Kd | = | 739.0 | nM | 6.13 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 808.0 | nM | 6.09 |
| CHEMBL405130 | WHI-P131 | Kd | = | 1163.0 | nM | 5.93 |
| CHEMBL3544932 | TAK-901 | Kd | = | 1468.0 | nM | 5.83 |
| CHEMBL415049 | BARASERTIB | Kd | = | 1734.0 | nM | 5.76 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 1722.0 | nM | 5.76 |
| CHEMBL5416410 | DASATINIB | Kd | = | 1881.0 | nM | 5.73 |
| CHEMBL553 | ERLOTINIB | Kd | = | 2164.0 | nM | 5.67 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 2255.0 | nM | 5.65 |
| CHEMBL3989868 | TUCATINIB | Kd | = | 2534.0 | nM | 5.60 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 2733.0 | nM | 5.56 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 3502.0 | nM | 5.46 |
| CHEMBL24828 | VANDETANIB | Kd | = | 3741.0 | nM | 5.43 |
| CHEMBL1922094 | APITOLISIB | Kd | = | 4874.0 | nM | 5.31 |
| CHEMBL535 | SUNITINIB | Kd | = | 6788.0 | nM | 5.17 |
| CHEMBL2087361 | ICOTINIB | Kd | = | 10128.0 | nM | 4.99 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 20827.0 | nM | 4.68 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 79933.0 | nM | 4.10 |
| CHEMBL571948 | Y-39983 | Kd | > | 30000.0 | nM | - |
| CHEMBL2030402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3137336 | UPROSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL1952329 | SGI-1776 | Kd | > | 30000.0 | nM | - |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL274654 | ORANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1084546 | PF-00562271 | Kd | > | 30000.0 | nM | - |