Assay Detail
Binding
CHEMBL3991772
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 | 6.60 | 8.30 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1088751 | PH-797804 | 2.0 | 1 | 8.30 |
| CHEMBL1090090 | VX-702 | 2.0 | 1 | 8.15 |
| CHEMBL514201 | TALMAPIMOD | 2.0 | 1 | 8.10 |
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | 8.05 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 7.38 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.81 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 6.66 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.45 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 6.27 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.25 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.15 |
| CHEMBL1950289 | TANZISERTIB | 2.0 | 1 | 6.14 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 6.13 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.03 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.03 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 5.98 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 5.95 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.56 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 5.07 |
| CHEMBL1879463 | DACTOLISIB | 3.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | - |
| CHEMBL2103842 | VARLITINIB | 2.0 | 1 | - |
| CHEMBL3991931 | — | — | 1 | - |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | - |
| CHEMBL4084193 | — | — | 1 | - |
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | - |
| CHEMBL270995 | BRIVANIB ALANINATE | 3.0 | 1 | - |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | - |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1088751 | PH-797804 | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL1090090 | VX-702 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL514201 | TALMAPIMOD | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL1088752 | LOSMAPIMOD | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 42.0 | nM | 7.38 |
| CHEMBL1171837 | PONATINIB | Kd | = | 154.0 | nM | 6.81 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 217.0 | nM | 6.66 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 358.0 | nM | 6.45 |
| CHEMBL206834 | BAFETINIB | Kd | = | 536.0 | nM | 6.27 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 566.0 | nM | 6.25 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 705.0 | nM | 6.15 |
| CHEMBL1950289 | TANZISERTIB | Kd | = | 729.0 | nM | 6.14 |
| CHEMBL2140408 | AMG-900 | Kd | = | 735.0 | nM | 6.13 |
| CHEMBL255863 | NILOTINIB | Kd | = | 927.0 | nM | 6.03 |
| CHEMBL5416410 | DASATINIB | Kd | = | 945.0 | nM | 6.03 |
| CHEMBL1173655 | AFATINIB | Kd | = | 1047.0 | nM | 5.98 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 1111.0 | nM | 5.95 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 2763.0 | nM | 5.56 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 8500.0 | nM | 5.07 |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL2180604 | TAK-593 | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482968 | ENMD-2076 | Kd | > | 30000.0 | nM | - |
| CHEMBL3334567 | SAVOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL3128043 | PF-03758309 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545154 | POZIOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL460702 | BMS-777607 | Kd | > | 30000.0 | nM | - |
| CHEMBL1230165 | SILMITASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544960 | AT-13148 | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545307 | MERESTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908397 | KW-2449 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL274654 | ORANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |