Assay Detail
Binding
CHEMBL3991871
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 | 5.94 | 8.05 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 8.05 |
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | 7.80 |
| CHEMBL3544960 | AT-13148 | 1.0 | 1 | 7.58 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 7.08 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.66 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 6.49 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.12 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 6.03 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 6.02 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 5.96 |
| CHEMBL1233300 | HYDROXYFASUDIL | — | 1 | 5.87 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 5.64 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 5.62 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 5.53 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 5.40 |
| CHEMBL2219422 | AFURESERTIB | 3.0 | 1 | 5.33 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 5.23 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.05 |
| CHEMBL551064 | AEW-541 | 1.0 | 1 | 4.74 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 4.25 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 4.23 |
| CHEMBL571546 | TIRBANIBULIN | 4.0 | 1 | - |
| CHEMBL1801204 | AZD-8055 | 1.0 | 1 | - |
| CHEMBL1614710 | OSI-930 | 1.0 | 1 | - |
| CHEMBL3218576 | COPANLISIB | 4.0 | 1 | - |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | - |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | - |
| CHEMBL2103875 | TRAMETINIB | 4.0 | 1 | - |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | - |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL571948 | Y-39983 | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL3544960 | AT-13148 | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 83.0 | nM | 7.08 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 219.0 | nM | 6.66 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 324.0 | nM | 6.49 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 756.0 | nM | 6.12 |
| CHEMBL38380 | FASUDIL | Kd | = | 943.0 | nM | 6.03 |
| CHEMBL494089 | GSK-690693 | Kd | = | 956.0 | nM | 6.02 |
| CHEMBL574737 | UCN-01 | Kd | = | 1096.0 | nM | 5.96 |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | = | 1349.0 | nM | 5.87 |
| CHEMBL3137336 | UPROSERTIB | Kd | = | 2277.0 | nM | 5.64 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 2402.0 | nM | 5.62 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 2977.0 | nM | 5.53 |
| CHEMBL3545328 | XL-019 | Kd | = | 3974.0 | nM | 5.40 |
| CHEMBL2219422 | AFURESERTIB | Kd | = | 4733.0 | nM | 5.33 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 5947.0 | nM | 5.23 |
| CHEMBL482967 | CYC-116 | Kd | = | 8885.0 | nM | 5.05 |
| CHEMBL551064 | AEW-541 | Kd | = | 18265.0 | nM | 4.74 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 56066.0 | nM | 4.25 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 58977.0 | nM | 4.23 |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL24828 | VANDETANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2035187 | PACRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | Kd | > | 30000.0 | nM | - |
| CHEMBL607707 | PELITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2001019 | PF-04217903 | Kd | > | 30000.0 | nM | - |
| CHEMBL3989868 | TUCATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL495727 | AT-9283 | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103830 | FOSTAMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL1230607 | PHA-793887 | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545085 | XL-228 | Kd | > | 30000.0 | nM | - |