Assay Detail
Binding
CHEMBL3991748
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 | 5.99 | 7.58 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 7.58 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 7.48 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.88 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 6.45 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.27 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.21 |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | 6.20 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.15 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.01 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 5.99 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.95 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.77 |
| CHEMBL3991933 | — | — | 1 | 5.73 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.72 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.68 |
| CHEMBL1950289 | TANZISERTIB | 2.0 | 1 | 5.66 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 5.64 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 5.62 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 5.49 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 5.40 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 5.29 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 4.68 |
| CHEMBL2087361 | ICOTINIB | 3.0 | 1 | - |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | 2.0 | 1 | - |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | - |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | - |
| CHEMBL536151 | IMD-0354 | 1.0 | 1 | - |
| CHEMBL2103875 | TRAMETINIB | 4.0 | 1 | - |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 133.0 | nM | 6.88 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 357.0 | nM | 6.45 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 535.0 | nM | 6.27 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 616.0 | nM | 6.21 |
| CHEMBL587723 | AEE-788 | Kd | = | 632.0 | nM | 6.20 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 701.0 | nM | 6.15 |
| CHEMBL482967 | CYC-116 | Kd | = | 984.0 | nM | 6.01 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 1021.0 | nM | 5.99 |
| CHEMBL5416410 | DASATINIB | Kd | = | 1133.0 | nM | 5.95 |
| CHEMBL495727 | AT-9283 | Kd | = | 1692.0 | nM | 5.77 |
| CHEMBL3991933 | — | Kd | = | 1850.0 | nM | 5.73 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 1890.0 | nM | 5.72 |
| CHEMBL3545085 | XL-228 | Kd | = | 2067.0 | nM | 5.68 |
| CHEMBL1950289 | TANZISERTIB | Kd | = | 2173.0 | nM | 5.66 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 2307.0 | nM | 5.64 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 2392.0 | nM | 5.62 |
| CHEMBL3545328 | XL-019 | Kd | = | 3242.0 | nM | 5.49 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 3978.0 | nM | 5.40 |
| CHEMBL3600873 | MK-5108 | Kd | = | 5085.0 | nM | 5.29 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 21089.0 | nM | 4.68 |
| CHEMBL3426621 | RIPASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL2180604 | TAK-593 | Kd | > | 30000.0 | nM | - |
| CHEMBL1090090 | VX-702 | Kd | > | 30000.0 | nM | - |
| CHEMBL411907 | SONOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230165 | SILMITASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2220486 | LUCITANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3137336 | UPROSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1090479 | GSK-1070916 | Kd | > | 30000.0 | nM | - |
| CHEMBL2336325 | VISTUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289601 | LENVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL281948 | K-252A | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL482968 | ENMD-2076 | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1879463 | DACTOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 30000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 30000.0 | nM | - |