Assay Detail
Binding
CHEMBL3991708
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.
237
Total Activities
237
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 | 237 | 6.66 | 9.22 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 9.22 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | 8.15 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.92 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 7.58 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 7.47 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 7.14 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.78 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.65 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.62 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 6.59 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 6.59 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | 6.47 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.38 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.35 |
| CHEMBL3688339 | — | — | 1 | 6.28 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.26 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.24 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 5.82 |
| CHEMBL1614725 | TAK-285 | 1.0 | 1 | 5.73 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 5.48 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 5.44 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 5.42 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | - |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | - |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | - |
| CHEMBL1090090 | VX-702 | 2.0 | 1 | - |
| CHEMBL2103842 | VARLITINIB | 2.0 | 1 | - |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | - |
| CHEMBL2216870 | IDELALISIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 0.6 | nM | 9.22 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL495727 | AT-9283 | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL3545085 | XL-228 | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL5416410 | DASATINIB | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL482967 | CYC-116 | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 167.0 | nM | 6.78 |
| CHEMBL253969 | OSI-632 | Kd | = | 226.0 | nM | 6.65 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 241.0 | nM | 6.62 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 259.0 | nM | 6.59 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 255.0 | nM | 6.59 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 337.0 | nM | 6.47 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 412.0 | nM | 6.38 |
| CHEMBL3544932 | TAK-901 | Kd | = | 451.0 | nM | 6.35 |
| CHEMBL3688339 | — | Kd | = | 521.0 | nM | 6.28 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 545.0 | nM | 6.26 |
| CHEMBL1230609 | FORETINIB | Kd | = | 570.0 | nM | 6.24 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 1525.0 | nM | 5.82 |
| CHEMBL1614725 | TAK-285 | Kd | = | 1849.0 | nM | 5.73 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 3344.0 | nM | 5.48 |
| CHEMBL217092 | SARACATINIB | Kd | = | 3602.0 | nM | 5.44 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 3772.0 | nM | 5.42 |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL1241855 | RIGOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230607 | PHA-793887 | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3402762 | TEPOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2048872 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 30000.0 | nM | - |
| CHEMBL1230165 | SILMITASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105728 | CRENOLANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614710 | OSI-930 | Kd | > | 30000.0 | nM | - |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991932 | PEXMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL3137336 | UPROSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2030402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1801204 | AZD-8055 | Kd | > | 30000.0 | nM | - |
| CHEMBL3989868 | TUCATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL587723 | AEE-788 | Kd | > | 30000.0 | nM | - |