Assay Detail
Binding
CHEMBL3991771
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.
238
Total Activities
238
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 | 238 | 6.52 | 8.30 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090090 | VX-702 | 2.0 | 1 | 8.30 |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 8.00 |
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | 7.54 |
| CHEMBL1088751 | PH-797804 | 2.0 | 1 | 6.99 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 6.72 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.17 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.06 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.00 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 5.76 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 5.72 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 5.55 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 5.43 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | - |
| CHEMBL2103875 | TRAMETINIB | 4.0 | 1 | - |
| CHEMBL2048872 | — | — | 1 | - |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | - |
| CHEMBL3402762 | TEPOTINIB | 4.0 | 1 | - |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | - |
| CHEMBL3699142 | — | — | 1 | - |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | - |
| CHEMBL2103842 | VARLITINIB | 2.0 | 1 | - |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | - |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | - |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL3991927 | HMN-214 | 1.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090090 | VX-702 | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL1088752 | LOSMAPIMOD | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL1088751 | PH-797804 | Kd | = | 102.0 | nM | 6.99 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 192.0 | nM | 6.72 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 684.0 | nM | 6.17 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 872.0 | nM | 6.06 |
| CHEMBL1171837 | PONATINIB | Kd | = | 1012.0 | nM | 6.00 |
| CHEMBL206834 | BAFETINIB | Kd | = | 1723.0 | nM | 5.76 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 1911.0 | nM | 5.72 |
| CHEMBL1173655 | AFATINIB | Kd | = | 2811.0 | nM | 5.55 |
| CHEMBL255863 | NILOTINIB | Kd | = | 3743.0 | nM | 5.43 |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1241855 | RIGOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 30000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL1789941 | RUXOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991933 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3218575 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544983 | TESEVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 30000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL3128043 | PF-03758309 | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL3301612 | ENCORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2140408 | AMG-900 | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908397 | KW-2449 | Kd | > | 30000.0 | nM | - |
| CHEMBL1287853 | FEDRATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |