Assay Detail
Binding
CHEMBL3991850
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 | 6.13 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 8.52 |
| CHEMBL281948 | K-252A | — | 1 | 7.42 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.28 |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | 7.19 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 7.05 |
| CHEMBL3688339 | — | — | 1 | 7.03 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.92 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.87 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.57 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 6.53 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 6.31 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.27 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 6.25 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.19 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 6.12 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.08 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 6.07 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.06 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 5.97 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.93 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.78 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 5.74 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.73 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 5.72 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 5.71 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 5.67 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 5.66 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.60 |
| CHEMBL3991935 | — | — | 1 | 5.59 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL281948 | K-252A | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL1230607 | PHA-793887 | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL1614713 | CC-401 | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL3688339 | — | Kd | = | 93.0 | nM | 7.03 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL564829 | MILCICLIB | Kd | = | 135.0 | nM | 6.87 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 268.0 | nM | 6.57 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 297.0 | nM | 6.53 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 493.0 | nM | 6.31 |
| CHEMBL495727 | AT-9283 | Kd | = | 532.0 | nM | 6.27 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 557.0 | nM | 6.25 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 650.0 | nM | 6.19 |
| CHEMBL571948 | Y-39983 | Kd | = | 762.0 | nM | 6.12 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 822.0 | nM | 6.08 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 857.0 | nM | 6.07 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 867.0 | nM | 6.06 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 1059.0 | nM | 5.97 |
| CHEMBL482967 | CYC-116 | Kd | = | 1163.0 | nM | 5.93 |
| CHEMBL535 | SUNITINIB | Kd | = | 1645.0 | nM | 5.78 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 1841.0 | nM | 5.74 |
| CHEMBL3545085 | XL-228 | Kd | = | 1857.0 | nM | 5.73 |
| CHEMBL2140408 | AMG-900 | Kd | = | 1912.0 | nM | 5.72 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 1933.0 | nM | 5.71 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 2136.0 | nM | 5.67 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 2207.0 | nM | 5.66 |
| CHEMBL1908397 | KW-2449 | Kd | = | 2509.0 | nM | 5.60 |
| CHEMBL3991935 | — | Kd | = | 2539.0 | nM | 5.59 |
| CHEMBL3137336 | UPROSERTIB | Kd | = | 2639.0 | nM | 5.58 |
| CHEMBL3545328 | XL-019 | Kd | = | 2957.0 | nM | 5.53 |
| CHEMBL296468 | BMS-387032 | Kd | = | 3139.0 | nM | 5.50 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 14768.0 | nM | 4.83 |
| CHEMBL189963 | PALBOCICLIB | Kd | = | 16296.0 | nM | 4.79 |
| CHEMBL38380 | FASUDIL | Kd | = | 23341.0 | nM | 4.63 |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2029988 | CEP-32496 | Kd | > | 30000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614710 | OSI-930 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3348923 | TOVORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103839 | RIDAFOROLIMUS | Kd | > | 30000.0 | nM | - |