Assay Detail
Binding
CHEMBL3991925
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 | 6.45 | 9.00 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 9.00 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.40 |
| CHEMBL3991931 | — | — | 1 | 8.30 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 7.66 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.57 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.26 |
| CHEMBL3699142 | — | — | 1 | 7.03 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 7.02 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.77 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.76 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.66 |
| CHEMBL2103842 | VARLITINIB | 2.0 | 1 | 6.49 |
| CHEMBL551064 | AEW-541 | 1.0 | 1 | 6.47 |
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | 6.37 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.36 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 6.36 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.35 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.24 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.23 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.21 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.12 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 6.11 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.05 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 6.01 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 5.99 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 5.89 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.84 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.42 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 5.41 |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | 5.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL5416410 | DASATINIB | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL3991931 | — | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL3544932 | TAK-901 | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL3699142 | — | Kd | = | 94.0 | nM | 7.03 |
| CHEMBL217092 | SARACATINIB | Kd | = | 95.0 | nM | 7.02 |
| CHEMBL3545085 | XL-228 | Kd | = | 171.0 | nM | 6.77 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 172.0 | nM | 6.76 |
| CHEMBL1171837 | PONATINIB | Kd | = | 218.0 | nM | 6.66 |
| CHEMBL2103842 | VARLITINIB | Kd | = | 321.0 | nM | 6.49 |
| CHEMBL551064 | AEW-541 | Kd | = | 337.0 | nM | 6.47 |
| CHEMBL2180604 | TAK-593 | Kd | = | 423.0 | nM | 6.37 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 435.0 | nM | 6.36 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 441.0 | nM | 6.36 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 445.0 | nM | 6.35 |
| CHEMBL495727 | AT-9283 | Kd | = | 574.0 | nM | 6.24 |
| CHEMBL522892 | DOVITINIB | Kd | = | 591.0 | nM | 6.23 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 623.0 | nM | 6.21 |
| CHEMBL535 | SUNITINIB | Kd | = | 758.0 | nM | 6.12 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 781.0 | nM | 6.11 |
| CHEMBL253969 | OSI-632 | Kd | = | 881.0 | nM | 6.05 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 969.0 | nM | 6.01 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 1026.0 | nM | 5.99 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 1276.0 | nM | 5.89 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 1441.0 | nM | 5.84 |
| CHEMBL564829 | MILCICLIB | Kd | = | 3789.0 | nM | 5.42 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 3936.0 | nM | 5.41 |
| CHEMBL403989 | TG100-801 | Kd | = | 4435.0 | nM | 5.35 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 5557.0 | nM | 5.25 |
| CHEMBL2138625 | AV-412 FREE BASE | Kd | = | 6267.0 | nM | 5.20 |
| CHEMBL587723 | AEE-788 | Kd | = | 17152.0 | nM | 4.77 |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL598797 | CUDC-101 | Kd | > | 30000.0 | nM | - |
| CHEMBL1233528 | VOLASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL571546 | TIRBANIBULIN | Kd | > | 30000.0 | nM | - |
| CHEMBL206834 | BAFETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL460702 | BMS-777607 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |