Assay Detail
Binding
CHEMBL3991701
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 | 6.58 | 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 | 8.22 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.62 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.57 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 7.52 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 7.50 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.20 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 7.05 |
| CHEMBL3688339 | — | — | 1 | 6.96 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.93 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.84 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 6.83 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.75 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 6.70 |
| CHEMBL483158 | ALISERTIB | 3.0 | 1 | 6.51 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 6.30 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 6.20 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.18 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 6.14 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 6.13 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.11 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.09 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.08 |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | 5.92 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.90 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 5.90 |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | 5.87 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.84 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 5.59 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL5416410 | DASATINIB | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 24.0 | nM | 7.62 |
| CHEMBL1171837 | PONATINIB | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL3545085 | XL-228 | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL1230609 | FORETINIB | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL206834 | BAFETINIB | Kd | = | 90.0 | nM | 7.05 |
| CHEMBL3688339 | — | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 118.0 | nM | 6.93 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 144.0 | nM | 6.84 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 147.0 | nM | 6.83 |
| CHEMBL3544932 | TAK-901 | Kd | = | 178.0 | nM | 6.75 |
| CHEMBL3600873 | MK-5108 | Kd | = | 202.0 | nM | 6.70 |
| CHEMBL483158 | ALISERTIB | Kd | = | 309.0 | nM | 6.51 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 501.0 | nM | 6.30 |
| CHEMBL259084 | MLN-8054 | Kd | = | 626.0 | nM | 6.20 |
| CHEMBL564829 | MILCICLIB | Kd | = | 661.0 | nM | 6.18 |
| CHEMBL217092 | SARACATINIB | Kd | = | 729.0 | nM | 6.14 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 746.0 | nM | 6.13 |
| CHEMBL255863 | NILOTINIB | Kd | = | 772.0 | nM | 6.11 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 807.0 | nM | 6.09 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 832.0 | nM | 6.08 |
| CHEMBL403989 | TG100-801 | Kd | = | 1188.0 | nM | 5.92 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 1252.0 | nM | 5.90 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 1266.0 | nM | 5.90 |
| CHEMBL575448 | BMS-754807 | Kd | = | 1350.0 | nM | 5.87 |
| CHEMBL495727 | AT-9283 | Kd | = | 1429.0 | nM | 5.84 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 2565.0 | nM | 5.59 |
| CHEMBL482967 | CYC-116 | Kd | = | 3931.0 | nM | 5.41 |
| CHEMBL2408045 | SAPITINIB | Kd | = | 8198.0 | nM | 5.09 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL2323775 | MK-8033 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL1088752 | LOSMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL2041933 | AZD-7762 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544960 | AT-13148 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3402762 | TEPOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1201182 | TEMSIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL2048872 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 30000.0 | nM | - |
| CHEMBL1789941 | RUXOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | > | 30000.0 | nM | - |
| CHEMBL2325741 | CAPIVASERTIB | Kd | > | 30000.0 | nM | - |