Assay Detail
Binding
CHEMBL3991860
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 | 6.58 | 9.15 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 9.15 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 8.70 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 8.52 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 8.15 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 8.15 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 8.00 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 7.96 |
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | 7.89 |
| CHEMBL281948 | K-252A | — | 1 | 7.68 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 7.66 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.62 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 7.28 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 7.11 |
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 7.11 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.10 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 7.06 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.98 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 6.97 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.92 |
| CHEMBL3688339 | — | — | 1 | 6.81 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 6.71 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.69 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.56 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.54 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.53 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.37 |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | 6.33 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.30 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 6.09 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL482967 | CYC-116 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL3545328 | XL-019 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL281948 | K-252A | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL495727 | AT-9283 | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 52.0 | nM | 7.28 |
| CHEMBL3544966 | GSK-1059615 | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 88.0 | nM | 7.06 |
| CHEMBL522892 | DOVITINIB | Kd | = | 104.0 | nM | 6.98 |
| CHEMBL571948 | Y-39983 | Kd | = | 106.0 | nM | 6.97 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL3688339 | — | Kd | = | 155.0 | nM | 6.81 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 196.0 | nM | 6.71 |
| CHEMBL3545085 | XL-228 | Kd | = | 204.0 | nM | 6.69 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 277.0 | nM | 6.56 |
| CHEMBL1908397 | KW-2449 | Kd | = | 285.0 | nM | 6.54 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 293.0 | nM | 6.53 |
| CHEMBL535 | SUNITINIB | Kd | = | 431.0 | nM | 6.37 |
| CHEMBL3544964 | RAVOXERTINIB | Kd | = | 466.0 | nM | 6.33 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 502.0 | nM | 6.30 |
| CHEMBL1614701 | SELUMETINIB | Kd | = | 807.0 | nM | 6.09 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 822.0 | nM | 6.08 |
| CHEMBL2180604 | TAK-593 | Kd | = | 869.0 | nM | 6.06 |
| CHEMBL1721885 | SU-014813 | Kd | = | 945.0 | nM | 6.03 |
| CHEMBL574737 | UCN-01 | Kd | = | 961.0 | nM | 6.02 |
| CHEMBL274654 | ORANTINIB | Kd | = | 1183.0 | nM | 5.93 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 1311.0 | nM | 5.88 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 1357.0 | nM | 5.87 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 1388.0 | nM | 5.86 |
| CHEMBL3813873 | PEXIDARTINIB | Kd | = | 1452.0 | nM | 5.84 |
| CHEMBL405130 | WHI-P131 | Kd | = | 1542.0 | nM | 5.81 |
| CHEMBL564829 | MILCICLIB | Kd | = | 1860.0 | nM | 5.73 |
| CHEMBL1289926 | AXITINIB | Kd | = | 2299.0 | nM | 5.64 |
| CHEMBL1614713 | CC-401 | Kd | = | 2529.0 | nM | 5.60 |
| CHEMBL1822792 | MK-2461 | Kd | = | 2590.0 | nM | 5.59 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 2644.0 | nM | 5.58 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 2716.0 | nM | 5.57 |
| CHEMBL230011 | TG100-115 | Kd | = | 3015.0 | nM | 5.52 |
| CHEMBL2376648 | — | Kd | = | 3361.0 | nM | 5.47 |
| CHEMBL2140408 | AMG-900 | Kd | = | 3556.0 | nM | 5.45 |
| CHEMBL3301607 | FILGOTINIB | Kd | = | 4384.0 | nM | 5.36 |
| CHEMBL3545110 | RIBOCICLIB | Kd | = | 9311.0 | nM | 5.03 |