Assay Detail
Binding
CHEMBL3991870
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 | 6.16 | 8.10 |
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 | 8.10 |
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | 7.77 |
| CHEMBL3544960 | AT-13148 | 1.0 | 1 | 7.57 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 7.48 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.32 |
| CHEMBL1233300 | HYDROXYFASUDIL | — | 1 | 6.27 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 6.15 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 6.09 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 6.04 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 6.02 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 5.94 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 5.87 |
| CHEMBL2219422 | AFURESERTIB | 3.0 | 1 | 5.67 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 5.57 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 5.56 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 5.55 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 4.87 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 4.00 |
| CHEMBL2103839 | RIDAFOROLIMUS | 3.0 | 1 | - |
| CHEMBL598797 | CUDC-101 | 1.0 | 1 | - |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | - |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | - |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | - |
| CHEMBL2048872 | — | — | 1 | - |
| CHEMBL3218576 | COPANLISIB | 4.0 | 1 | - |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | - |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | - |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | - |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL571948 | Y-39983 | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL3544960 | AT-13148 | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 482.0 | nM | 6.32 |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | = | 532.0 | nM | 6.27 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 706.0 | nM | 6.15 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 819.0 | nM | 6.09 |
| CHEMBL38380 | FASUDIL | Kd | = | 906.0 | nM | 6.04 |
| CHEMBL574737 | UCN-01 | Kd | = | 955.0 | nM | 6.02 |
| CHEMBL3137336 | UPROSERTIB | Kd | = | 1152.0 | nM | 5.94 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 1362.0 | nM | 5.87 |
| CHEMBL2219422 | AFURESERTIB | Kd | = | 2144.0 | nM | 5.67 |
| CHEMBL494089 | GSK-690693 | Kd | = | 2676.0 | nM | 5.57 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 2730.0 | nM | 5.56 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 2816.0 | nM | 5.55 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 13462.0 | nM | 4.87 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 99233.0 | nM | 4.00 |
| CHEMBL3544932 | TAK-901 | Kd | > | 30000.0 | nM | - |
| CHEMBL507361 | MIRDAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | Kd | > | 30000.0 | nM | - |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | > | 30000.0 | nM | - |
| CHEMBL5416410 | DASATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL411907 | SONOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2165191 | AZD-6482 | Kd | > | 30000.0 | nM | - |
| CHEMBL2041933 | AZD-7762 | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103882 | TIVANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989868 | TUCATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2103840 | DINACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3301622 | GILTERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2220486 | LUCITANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2035187 | PACRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3039525 | GOLVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991935 | — | Kd | > | 30000.0 | nM | - |