Assay Detail
Binding
CHEMBL3991664
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.
152
Total Activities
152
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 | 152 | 6.90 | 7.80 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 7.80 |
| CHEMBL3699142 | — | — | 1 | 7.70 |
| CHEMBL3991935 | — | — | 1 | 7.62 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 5.71 |
| CHEMBL3188267 | CAPMATINIB | 4.0 | 1 | 5.69 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | - |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | - |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | - |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | - |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | - |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | - |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | - |
| CHEMBL3218575 | — | — | 1 | - |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | - |
| CHEMBL3991927 | HMN-214 | 1.0 | 1 | - |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | - |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | - |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | - |
| CHEMBL415049 | BARASERTIB | 3.0 | 1 | - |
| CHEMBL3991931 | — | — | 1 | - |
| CHEMBL1236682 | REFAMETINIB | 2.0 | 1 | - |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | - |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | - |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | - |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | - |
| CHEMBL3545215 | BMS-911543 | 2.0 | 1 | - |
| CHEMBL3184679 | AZD-4547 | — | 1 | - |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | - |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3137331 | DEFACTINIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL3699142 | — | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL3991935 | — | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 1930.0 | nM | 5.71 |
| CHEMBL3188267 | CAPMATINIB | Kd | = | 2042.0 | nM | 5.69 |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL495727 | AT-9283 | Kd | > | 30000.0 | nM | - |
| CHEMBL2403108 | CERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614707 | MUBRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1084546 | PF-00562271 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103839 | RIDAFOROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103842 | VARLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103830 | FOSTAMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL411907 | SONOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL3600873 | MK-5108 | Kd | > | 30000.0 | nM | - |
| CHEMBL2220486 | LUCITANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545137 | PF-00477736 | Kd | > | 30000.0 | nM | - |
| CHEMBL1090090 | VX-702 | Kd | > | 30000.0 | nM | - |
| CHEMBL5416410 | DASATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3301622 | GILTERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989868 | TUCATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482968 | ENMD-2076 | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL274654 | ORANTINIB | Kd | > | 30000.0 | nM | - |