Assay Detail
Binding
CHEMBL3991914
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 | 6.36 | 8.30 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 8.30 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 7.57 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.23 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.19 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 7.12 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.86 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 6.83 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 6.79 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 6.68 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.55 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.52 |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | 6.38 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 6.33 |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | 6.29 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.05 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 6.03 |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | 6.00 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 5.97 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 5.96 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 5.87 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.85 |
| CHEMBL3699142 | — | — | 1 | 5.81 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 5.80 |
| CHEMBL281948 | K-252A | — | 1 | 5.76 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 5.50 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 5.33 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 5.03 |
| CHEMBL283120 | AXL-1717 | 2.0 | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
| CHEMBL384304 | RG-547 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3545360 | ASP-3026 | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL5416410 | DASATINIB | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 59.0 | nM | 7.23 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 64.0 | nM | 7.19 |
| CHEMBL3545085 | XL-228 | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 138.0 | nM | 6.86 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 148.0 | nM | 6.83 |
| CHEMBL574737 | UCN-01 | Kd | = | 162.0 | nM | 6.79 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 208.0 | nM | 6.68 |
| CHEMBL3544932 | TAK-901 | Kd | = | 281.0 | nM | 6.55 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 303.0 | nM | 6.52 |
| CHEMBL1983268 | ENTRECTINIB | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL3600873 | MK-5108 | Kd | = | 473.0 | nM | 6.33 |
| CHEMBL1231124 | AZD-1480 | Kd | = | 515.0 | nM | 6.29 |
| CHEMBL564829 | MILCICLIB | Kd | = | 900.0 | nM | 6.05 |
| CHEMBL2403108 | CERITINIB | Kd | = | 929.0 | nM | 6.03 |
| CHEMBL587723 | AEE-788 | Kd | = | 1006.0 | nM | 6.00 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 1062.0 | nM | 5.97 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 1091.0 | nM | 5.96 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 1358.0 | nM | 5.87 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1419.0 | nM | 5.85 |
| CHEMBL3699142 | — | Kd | = | 1549.0 | nM | 5.81 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 1597.0 | nM | 5.80 |
| CHEMBL281948 | K-252A | Kd | = | 1717.0 | nM | 5.76 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 3149.0 | nM | 5.50 |
| CHEMBL217092 | SARACATINIB | Kd | = | 4650.0 | nM | 5.33 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 9334.0 | nM | 5.03 |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL598797 | CUDC-101 | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL1230607 | PHA-793887 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2336325 | VISTUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL491473 | CEDIRANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL2364611 | GALUNISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |