Assay Detail
Binding
CHEMBL3991717
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.
242
Total Activities
242
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 | 242 | 6.52 | 9.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 9.52 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 8.70 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | 8.52 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 8.05 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.60 |
| CHEMBL3991934 | — | — | 1 | 7.40 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.09 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.72 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.68 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.61 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.57 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.40 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 6.39 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.26 |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | 6.11 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 6.06 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.05 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.02 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 6.02 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 5.89 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.86 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.85 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 5.72 |
| CHEMBL3699142 | — | — | 1 | 5.60 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 5.57 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.48 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.44 |
| CHEMBL3991933 | — | — | 1 | 5.42 |
| CHEMBL270995 | BRIVANIB ALANINATE | 3.0 | 1 | 5.41 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274654 | ORANTINIB | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL3545085 | XL-228 | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL495727 | AT-9283 | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL3991934 | — | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 192.0 | nM | 6.72 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 208.0 | nM | 6.68 |
| CHEMBL522892 | DOVITINIB | Kd | = | 243.0 | nM | 6.61 |
| CHEMBL1289926 | AXITINIB | Kd | = | 268.0 | nM | 6.57 |
| CHEMBL253969 | OSI-632 | Kd | = | 396.0 | nM | 6.40 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 409.0 | nM | 6.39 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 547.0 | nM | 6.26 |
| CHEMBL1231124 | AZD-1480 | Kd | = | 777.0 | nM | 6.11 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 865.0 | nM | 6.06 |
| CHEMBL475251 | R-406 | Kd | = | 892.0 | nM | 6.05 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 957.0 | nM | 6.02 |
| CHEMBL482967 | CYC-116 | Kd | = | 949.0 | nM | 6.02 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 1282.0 | nM | 5.89 |
| CHEMBL3544932 | TAK-901 | Kd | = | 1388.0 | nM | 5.86 |
| CHEMBL564829 | MILCICLIB | Kd | = | 1421.0 | nM | 5.85 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 1903.0 | nM | 5.72 |
| CHEMBL3699142 | — | Kd | = | 2511.0 | nM | 5.60 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 2675.0 | nM | 5.57 |
| CHEMBL1908397 | KW-2449 | Kd | = | 3302.0 | nM | 5.48 |
| CHEMBL535 | SUNITINIB | Kd | = | 3595.0 | nM | 5.44 |
| CHEMBL3991933 | — | Kd | = | 3777.0 | nM | 5.42 |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | = | 3896.0 | nM | 5.41 |
| CHEMBL598797 | CUDC-101 | Kd | > | 30000.0 | nM | - |
| CHEMBL206834 | BAFETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL2376648 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3426621 | RIPASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103839 | RIDAFOROLIMUS | Kd | > | 30000.0 | nM | - |