Assay Detail
Binding
CHEMBL3991884
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 |
Target
STE20-like serine/threonine-protein kinase (CHEMBL4202) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 5.67 | 7.24 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 7.24 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 7.17 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 7.05 |
| CHEMBL3688339 | — | — | 1 | 6.95 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.86 |
| CHEMBL384304 | RG-547 | 2.0 | 1 | 6.80 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 6.66 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.57 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.40 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.16 |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | 6.16 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.12 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.06 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.06 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 5.98 |
| CHEMBL2087361 | ICOTINIB | 3.0 | 1 | 5.98 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 5.96 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.93 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.87 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 5.83 |
| CHEMBL3699142 | — | — | 1 | 5.83 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 5.71 |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | 5.68 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.66 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 5.64 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 5.62 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 5.60 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 5.56 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.55 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 68.0 | nM | 7.17 |
| CHEMBL574737 | UCN-01 | Kd | = | 89.0 | nM | 7.05 |
| CHEMBL3688339 | — | Kd | = | 113.0 | nM | 6.95 |
| CHEMBL3545085 | XL-228 | Kd | = | 138.0 | nM | 6.86 |
| CHEMBL384304 | RG-547 | Kd | = | 157.0 | nM | 6.80 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL253969 | OSI-632 | Kd | = | 268.0 | nM | 6.57 |
| CHEMBL495727 | AT-9283 | Kd | = | 402.0 | nM | 6.40 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 687.0 | nM | 6.16 |
| CHEMBL1231124 | AZD-1480 | Kd | = | 686.0 | nM | 6.16 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 750.0 | nM | 6.12 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 873.0 | nM | 6.06 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 865.0 | nM | 6.06 |
| CHEMBL2087361 | ICOTINIB | Kd | = | 1051.0 | nM | 5.98 |
| CHEMBL180022 | NERATINIB | Kd | = | 1043.0 | nM | 5.98 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 1093.0 | nM | 5.96 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 1179.0 | nM | 5.93 |
| CHEMBL3544932 | TAK-901 | Kd | = | 1348.0 | nM | 5.87 |
| CHEMBL3699142 | — | Kd | = | 1494.0 | nM | 5.83 |
| CHEMBL553 | ERLOTINIB | Kd | = | 1491.0 | nM | 5.83 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 1970.0 | nM | 5.71 |
| CHEMBL2386889 | SCH-900776 | Kd | = | 2085.0 | nM | 5.68 |
| CHEMBL5416410 | DASATINIB | Kd | = | 2189.0 | nM | 5.66 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 2264.0 | nM | 5.64 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 2420.0 | nM | 5.62 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 2522.0 | nM | 5.60 |
| CHEMBL377300 | BRIVANIB | Kd | = | 2741.0 | nM | 5.56 |
| CHEMBL1908397 | KW-2449 | Kd | = | 2804.0 | nM | 5.55 |
| CHEMBL535 | SUNITINIB | Kd | = | 3184.0 | nM | 5.50 |
| CHEMBL281948 | K-252A | Kd | = | 3305.0 | nM | 5.48 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 3421.0 | nM | 5.47 |
| CHEMBL1952329 | SGI-1776 | Kd | = | 3588.0 | nM | 5.45 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 3815.0 | nM | 5.42 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 3851.0 | nM | 5.41 |
| CHEMBL3544966 | GSK-1059615 | Kd | = | 4315.0 | nM | 5.37 |
| CHEMBL405130 | WHI-P131 | Kd | = | 4373.0 | nM | 5.36 |
| CHEMBL1289926 | AXITINIB | Kd | = | 5960.0 | nM | 5.22 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 6370.0 | nM | 5.20 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 7790.0 | nM | 5.11 |
| CHEMBL3301607 | FILGOTINIB | Kd | = | 9273.0 | nM | 5.03 |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | = | 9488.0 | nM | 5.02 |
| CHEMBL1922094 | APITOLISIB | Kd | = | 10170.0 | nM | 4.99 |
| CHEMBL2138625 | AV-412 FREE BASE | Kd | = | 13417.0 | nM | 4.87 |
| CHEMBL1721885 | SU-014813 | Kd | = | 18981.0 | nM | 4.72 |
| CHEMBL217092 | SARACATINIB | Kd | = | 31713.0 | nM | 4.50 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 36309.0 | nM | 4.44 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 41005.0 | nM | 4.39 |
| CHEMBL482967 | CYC-116 | Kd | = | 90800.0 | nM | 4.04 |
| CHEMBL587723 | AEE-788 | Kd | = | 99232.0 | nM | 4.00 |