Assay Detail
Binding
CHEMBL3991633
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 | 6.29 | 9.10 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 9.10 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 8.22 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 8.15 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 8.10 |
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | 7.89 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 7.85 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.82 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 7.70 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.47 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 7.41 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.35 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 7.34 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.19 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 7.11 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.06 |
| CHEMBL281948 | K-252A | — | 1 | 7.05 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 6.77 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 6.75 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.74 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.67 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.67 |
| CHEMBL3688339 | — | — | 1 | 6.61 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 6.52 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.41 |
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 6.40 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.38 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.29 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.28 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.16 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 0.8 | nM | 9.10 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL482967 | CYC-116 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL3545085 | XL-228 | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL3545328 | XL-019 | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL495727 | AT-9283 | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 39.0 | nM | 7.41 |
| CHEMBL1908397 | KW-2449 | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 46.0 | nM | 7.34 |
| CHEMBL522892 | DOVITINIB | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL1721885 | SU-014813 | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL535 | SUNITINIB | Kd | = | 87.0 | nM | 7.06 |
| CHEMBL281948 | K-252A | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 169.0 | nM | 6.77 |
| CHEMBL571948 | Y-39983 | Kd | = | 179.0 | nM | 6.75 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 181.0 | nM | 6.74 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 216.0 | nM | 6.67 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 214.0 | nM | 6.67 |
| CHEMBL3688339 | — | Kd | = | 245.0 | nM | 6.61 |
| CHEMBL274654 | ORANTINIB | Kd | = | 303.0 | nM | 6.52 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 387.0 | nM | 6.41 |
| CHEMBL3544966 | GSK-1059615 | Kd | = | 402.0 | nM | 6.40 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 422.0 | nM | 6.38 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 519.0 | nM | 6.29 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 528.0 | nM | 6.28 |
| CHEMBL3544932 | TAK-901 | Kd | = | 695.0 | nM | 6.16 |
| CHEMBL488436 | AZD-5438 | Kd | = | 826.0 | nM | 6.08 |
| CHEMBL574737 | UCN-01 | Kd | = | 832.0 | nM | 6.08 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 870.0 | nM | 6.06 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 1488.0 | nM | 5.83 |
| CHEMBL1614713 | CC-401 | Kd | = | 1467.0 | nM | 5.83 |
| CHEMBL1614701 | SELUMETINIB | Kd | = | 1624.0 | nM | 5.79 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 1712.0 | nM | 5.77 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 2199.0 | nM | 5.66 |
| CHEMBL1289926 | AXITINIB | Kd | = | 2223.0 | nM | 5.65 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 2539.0 | nM | 5.59 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 2611.0 | nM | 5.58 |
| CHEMBL2386889 | SCH-900776 | Kd | = | 2676.0 | nM | 5.57 |
| CHEMBL607707 | PELITINIB | Kd | = | 2811.0 | nM | 5.55 |
| CHEMBL3544964 | RAVOXERTINIB | Kd | = | 2985.0 | nM | 5.53 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 2958.0 | nM | 5.53 |
| CHEMBL1094408 | NMS-1286937 | Kd | = | 3203.0 | nM | 5.49 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 3886.0 | nM | 5.41 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 5754.0 | nM | 5.24 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 5878.0 | nM | 5.23 |
| CHEMBL553 | ERLOTINIB | Kd | = | 6228.0 | nM | 5.21 |