Assay Detail
Binding
CHEMBL3991783
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.
215
Total Activities
215
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 |
Target
MAP/microtubule affinity-regulating kinase 4 (CHEMBL5754) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 215 | 7.10 | 8.10 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 8.10 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 8.05 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 7.60 |
| CHEMBL281948 | K-252A | — | 1 | 7.55 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 7.54 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 7.44 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.14 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.14 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 6.85 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.63 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.32 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.01 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.99 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
| CHEMBL2103839 | RIDAFOROLIMUS | 3.0 | 1 | - |
| CHEMBL3187723 | BINIMETINIB | 4.0 | 1 | - |
| CHEMBL2133806 | JNJ-38877605 | 1.0 | 1 | - |
| CHEMBL1801204 | AZD-8055 | 1.0 | 1 | - |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | - |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | - |
| CHEMBL2165191 | AZD-6482 | 2.0 | 1 | - |
| CHEMBL1088751 | PH-797804 | 2.0 | 1 | - |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | - |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | - |
| CHEMBL3991935 | — | — | 1 | - |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | - |
| CHEMBL1241855 | RIGOSERTIB | 3.0 | 1 | - |
| CHEMBL2180604 | TAK-593 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL574737 | UCN-01 | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL281948 | K-252A | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL1908397 | KW-2449 | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 232.0 | nM | 6.63 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 475.0 | nM | 6.32 |
| CHEMBL522892 | DOVITINIB | Kd | = | 976.0 | nM | 6.01 |
| CHEMBL3544932 | TAK-901 | Kd | = | 1035.0 | nM | 5.99 |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | Kd | > | 30000.0 | nM | - |
| CHEMBL551064 | AEW-541 | Kd | > | 30000.0 | nM | - |
| CHEMBL1090479 | GSK-1070916 | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103840 | DINACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1171837 | PONATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614707 | MUBRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |
| CHEMBL1879463 | DACTOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103882 | TIVANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL2029988 | CEP-32496 | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2107832 | PIMASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3301612 | ENCORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1233528 | VOLASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL507361 | MIRDAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544983 | TESEVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |