Assay Detail
Binding
CHEMBL3991702
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 | 6.13 | 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 | 8.15 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 7.66 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.23 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.80 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.78 |
| CHEMBL3688339 | — | — | 1 | 6.74 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 6.36 |
| CHEMBL483158 | ALISERTIB | 3.0 | 1 | 6.34 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 6.04 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.03 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 5.99 |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | 5.71 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 5.70 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 5.49 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.46 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 5.25 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 5.15 |
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | 5.13 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.09 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 4.77 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 4.36 |
| CHEMBL2138625 | AV-412 FREE BASE | 1.0 | 1 | - |
| CHEMBL2219422 | AFURESERTIB | 3.0 | 1 | - |
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | - |
| CHEMBL405130 | WHI-P131 | 1.0 | 1 | - |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | - |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | - |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | - |
| CHEMBL3545110 | RIBOCICLIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL5416410 | DASATINIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL3544932 | TAK-901 | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 59.0 | nM | 7.23 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 159.0 | nM | 6.80 |
| CHEMBL3545085 | XL-228 | Kd | = | 167.0 | nM | 6.78 |
| CHEMBL3688339 | — | Kd | = | 181.0 | nM | 6.74 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 440.0 | nM | 6.36 |
| CHEMBL483158 | ALISERTIB | Kd | = | 455.0 | nM | 6.34 |
| CHEMBL217092 | SARACATINIB | Kd | = | 917.0 | nM | 6.04 |
| CHEMBL1230609 | FORETINIB | Kd | = | 930.0 | nM | 6.03 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 1033.0 | nM | 5.99 |
| CHEMBL403989 | TG100-801 | Kd | = | 1930.0 | nM | 5.71 |
| CHEMBL206834 | BAFETINIB | Kd | = | 1980.0 | nM | 5.70 |
| CHEMBL259084 | MLN-8054 | Kd | = | 3275.0 | nM | 5.49 |
| CHEMBL482967 | CYC-116 | Kd | = | 3461.0 | nM | 5.46 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 5563.0 | nM | 5.25 |
| CHEMBL3545154 | POZIOTINIB | Kd | = | 7057.0 | nM | 5.15 |
| CHEMBL2408045 | SAPITINIB | Kd | = | 7399.0 | nM | 5.13 |
| CHEMBL564829 | MILCICLIB | Kd | = | 8131.0 | nM | 5.09 |
| CHEMBL1171837 | PONATINIB | Kd | = | 17152.0 | nM | 4.77 |
| CHEMBL495727 | AT-9283 | Kd | = | 43942.0 | nM | 4.36 |
| CHEMBL603469 | LESTAURTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL3301607 | FILGOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2325741 | CAPIVASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2386889 | SCH-900776 | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1090090 | VX-702 | Kd | > | 30000.0 | nM | - |
| CHEMBL2165191 | AZD-6482 | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614707 | MUBRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL2029988 | CEP-32496 | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL2376648 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3813873 | PEXIDARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230607 | PHA-793887 | Kd | > | 30000.0 | nM | - |
| CHEMBL3128043 | PF-03758309 | Kd | > | 30000.0 | nM | - |
| CHEMBL1088752 | LOSMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1233528 | VOLASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991933 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |