Assay Detail
Binding
CHEMBL3991769
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 | 6.39 | 7.66 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | 7.66 |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | 6.74 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 5.91 |
| CHEMBL1950289 | TANZISERTIB | 2.0 | 1 | 5.91 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 5.71 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | - |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | - |
| CHEMBL2103839 | RIDAFOROLIMUS | 3.0 | 1 | - |
| CHEMBL3991927 | HMN-214 | 1.0 | 1 | - |
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | - |
| CHEMBL3545157 | TIDEGLUSIB | 2.0 | 1 | - |
| CHEMBL2376648 | — | — | 1 | - |
| CHEMBL3218576 | COPANLISIB | 4.0 | 1 | - |
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | - |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | - |
| CHEMBL270995 | BRIVANIB ALANINATE | 3.0 | 1 | - |
| CHEMBL3186534 | RIVOCERANIB | 3.0 | 1 | - |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | - |
| CHEMBL3991931 | — | — | 1 | - |
| CHEMBL598797 | CUDC-101 | 1.0 | 1 | - |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL2030402 | — | — | 1 | - |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | - |
| CHEMBL2396661 | ALPELISIB | 4.0 | 1 | - |
| CHEMBL2103842 | VARLITINIB | 2.0 | 1 | - |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3544964 | RAVOXERTINIB | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL3590106 | ULIXERTINIB | Kd | = | 183.0 | nM | 6.74 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 1237.0 | nM | 5.91 |
| CHEMBL1950289 | TANZISERTIB | Kd | = | 1233.0 | nM | 5.91 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 1965.0 | nM | 5.71 |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL3426621 | RIPASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3688339 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL2386889 | SCH-900776 | Kd | > | 30000.0 | nM | - |
| CHEMBL2220486 | LUCITANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL587723 | AEE-788 | Kd | > | 30000.0 | nM | - |
| CHEMBL281948 | K-252A | Kd | > | 30000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 30000.0 | nM | - |
| CHEMBL2017974 | BUPARLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545215 | BMS-911543 | Kd | > | 30000.0 | nM | - |
| CHEMBL2001019 | PF-04217903 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL1090479 | GSK-1070916 | Kd | > | 30000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1091644 | LINSITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908397 | KW-2449 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105728 | CRENOLANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1801204 | AZD-8055 | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL1088752 | LOSMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL1241855 | RIGOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL575448 | BMS-754807 | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103830 | FOSTAMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |