Assay Detail
Binding
CHEMBL3991630
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 | 7.19 | 10.00 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 10.00 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 8.70 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 8.52 |
| CHEMBL483158 | ALISERTIB | 3.0 | 1 | 8.30 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 8.22 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 8.15 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.96 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.85 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.80 |
| CHEMBL281948 | K-252A | — | 1 | 7.70 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 7.62 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.60 |
| CHEMBL415049 | BARASERTIB | 3.0 | 1 | 7.31 |
| CHEMBL3699142 | — | — | 1 | 7.23 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 7.15 |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | 7.12 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 7.10 |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | 6.93 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.93 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.85 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.74 |
| CHEMBL3688339 | — | — | 1 | 6.71 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.54 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 6.52 |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | 6.51 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.43 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.33 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.32 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.29 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3600873 | MK-5108 | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL259084 | MLN-8054 | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL3545085 | XL-228 | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL483158 | ALISERTIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL2140408 | AMG-900 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL495727 | AT-9283 | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL281948 | K-252A | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL3544932 | TAK-901 | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL415049 | BARASERTIB | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL3699142 | — | Kd | = | 59.0 | nM | 7.23 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 71.0 | nM | 7.15 |
| CHEMBL575448 | BMS-754807 | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL482967 | CYC-116 | Kd | = | 118.0 | nM | 6.93 |
| CHEMBL482767 | SNS-314 | Kd | = | 118.0 | nM | 6.93 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 141.0 | nM | 6.85 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 184.0 | nM | 6.74 |
| CHEMBL3688339 | — | Kd | = | 194.0 | nM | 6.71 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 285.0 | nM | 6.54 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL1231124 | AZD-1480 | Kd | = | 306.0 | nM | 6.51 |
| CHEMBL1289926 | AXITINIB | Kd | = | 374.0 | nM | 6.43 |
| CHEMBL1908397 | KW-2449 | Kd | = | 470.0 | nM | 6.33 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 477.0 | nM | 6.32 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 514.0 | nM | 6.29 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 622.0 | nM | 6.21 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 627.0 | nM | 6.20 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 981.0 | nM | 6.01 |
| CHEMBL274654 | ORANTINIB | Kd | = | 3254.0 | nM | 5.49 |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 30000.0 | nM | - |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | > | 30000.0 | nM | - |
| CHEMBL3991935 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545215 | BMS-911543 | Kd | > | 30000.0 | nM | - |
| CHEMBL5416410 | DASATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1287853 | FEDRATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103839 | RIDAFOROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3301607 | FILGOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |