Assay Detail
Binding
CHEMBL3991892
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 | 6.05 | 7.02 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.02 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 6.86 |
| CHEMBL3688339 | — | — | 1 | 6.73 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.68 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.53 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.30 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 6.29 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.25 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 6.15 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.07 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.07 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 6.05 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.96 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 5.91 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 5.89 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.89 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 5.73 |
| CHEMBL3991933 | — | — | 1 | 5.70 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.61 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 5.26 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 5.08 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.00 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | - |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | - |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | - |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | - |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475251 | R-406 | Kd | = | 95.0 | nM | 7.02 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 138.0 | nM | 6.86 |
| CHEMBL3688339 | — | Kd | = | 186.0 | nM | 6.73 |
| CHEMBL482967 | CYC-116 | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 295.0 | nM | 6.53 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 495.0 | nM | 6.30 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 515.0 | nM | 6.29 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 566.0 | nM | 6.25 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 702.0 | nM | 6.15 |
| CHEMBL1908397 | KW-2449 | Kd | = | 855.0 | nM | 6.07 |
| CHEMBL3544932 | TAK-901 | Kd | = | 849.0 | nM | 6.07 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 893.0 | nM | 6.05 |
| CHEMBL564829 | MILCICLIB | Kd | = | 1095.0 | nM | 5.96 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 1243.0 | nM | 5.91 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 1281.0 | nM | 5.89 |
| CHEMBL495727 | AT-9283 | Kd | = | 1281.0 | nM | 5.89 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 1867.0 | nM | 5.73 |
| CHEMBL3991933 | — | Kd | = | 2013.0 | nM | 5.70 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 2484.0 | nM | 5.61 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 5446.0 | nM | 5.26 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 8337.0 | nM | 5.08 |
| CHEMBL189963 | PALBOCICLIB | Kd | = | 9969.0 | nM | 5.00 |
| CHEMBL2376648 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL551064 | AEW-541 | Kd | > | 30000.0 | nM | - |
| CHEMBL1241855 | RIGOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545137 | PF-00477736 | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1952329 | SGI-1776 | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3039513 | DECERNOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289601 | LENVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL598797 | CUDC-101 | Kd | > | 30000.0 | nM | - |
| CHEMBL3187723 | BINIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545307 | MERESTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545360 | ASP-3026 | Kd | > | 30000.0 | nM | - |