Assay Detail
Binding
CHEMBL3991770
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.
238
Total Activities
238
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 | 238 | 6.55 | 9.00 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1950289 | TANZISERTIB | 2.0 | 1 | 9.00 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 7.96 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.55 |
| CHEMBL1236682 | REFAMETINIB | 2.0 | 1 | 7.44 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 7.14 |
| CHEMBL3688339 | — | — | 1 | 6.95 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.83 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 6.71 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.51 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.45 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.42 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.29 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 5.92 |
| CHEMBL3120215 | OSI-027 | 2.0 | 1 | 5.79 |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | 5.67 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.58 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 5.51 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 5.49 |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | 5.33 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | - |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | - |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | - |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | - |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | - |
| CHEMBL281948 | K-252A | — | 1 | - |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | - |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | - |
| CHEMBL483321 | CP-724714 | 2.0 | 1 | - |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | - |
| CHEMBL1234354 | PF-04691502 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1950289 | TANZISERTIB | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL1236682 | REFAMETINIB | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL3688339 | — | Kd | = | 112.0 | nM | 6.95 |
| CHEMBL482967 | CYC-116 | Kd | = | 147.0 | nM | 6.83 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 195.0 | nM | 6.71 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 308.0 | nM | 6.51 |
| CHEMBL495727 | AT-9283 | Kd | = | 358.0 | nM | 6.45 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 378.0 | nM | 6.42 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 512.0 | nM | 6.29 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 1191.0 | nM | 5.92 |
| CHEMBL3120215 | OSI-027 | Kd | = | 1617.0 | nM | 5.79 |
| CHEMBL3301607 | FILGOTINIB | Kd | = | 2140.0 | nM | 5.67 |
| CHEMBL564829 | MILCICLIB | Kd | = | 2642.0 | nM | 5.58 |
| CHEMBL3600873 | MK-5108 | Kd | = | 3076.0 | nM | 5.51 |
| CHEMBL1614713 | CC-401 | Kd | = | 3243.0 | nM | 5.49 |
| CHEMBL1822792 | MK-2461 | Kd | = | 4701.0 | nM | 5.33 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |
| CHEMBL217092 | SARACATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614707 | MUBRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545328 | XL-019 | Kd | > | 30000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL3334567 | SAVOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL2041933 | AZD-7762 | Kd | > | 30000.0 | nM | - |
| CHEMBL38380 | FASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL274654 | ORANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 30000.0 | nM | - |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289601 | LENVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL2323775 | MK-8033 | Kd | > | 30000.0 | nM | - |