Assay Detail
Binding
CHEMBL3991791
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 |
Target
Macrophage-stimulating protein receptor (CHEMBL2689) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.19 | 7.60 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 7.60 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.12 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.04 |
| CHEMBL3545307 | MERESTINIB | 2.0 | 1 | 6.63 |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | 6.56 |
| CHEMBL3688339 | — | — | 1 | 6.51 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.24 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.13 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.11 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.09 |
| CHEMBL2323775 | MK-8033 | 1.0 | 1 | 6.02 |
| CHEMBL415049 | BARASERTIB | 3.0 | 1 | 5.85 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.70 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.67 |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | 5.63 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.63 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 5.60 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 5.34 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | - |
| CHEMBL3120215 | OSI-027 | 2.0 | 1 | - |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | - |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | - |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | - |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | - |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | - |
| CHEMBL3991934 | — | — | 1 | - |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | - |
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3039525 | GOLVATINIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL1230609 | FORETINIB | Kd | = | 91.0 | nM | 7.04 |
| CHEMBL3545307 | MERESTINIB | Kd | = | 232.0 | nM | 6.63 |
| CHEMBL1822792 | MK-2461 | Kd | = | 278.0 | nM | 6.56 |
| CHEMBL3688339 | — | Kd | = | 311.0 | nM | 6.51 |
| CHEMBL482967 | CYC-116 | Kd | = | 575.0 | nM | 6.24 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 732.0 | nM | 6.13 |
| CHEMBL253969 | OSI-632 | Kd | = | 775.0 | nM | 6.11 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 804.0 | nM | 6.09 |
| CHEMBL2323775 | MK-8033 | Kd | = | 956.0 | nM | 6.02 |
| CHEMBL415049 | BARASERTIB | Kd | = | 1416.0 | nM | 5.85 |
| CHEMBL564829 | MILCICLIB | Kd | = | 1990.0 | nM | 5.70 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 2132.0 | nM | 5.67 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 2320.0 | nM | 5.63 |
| CHEMBL3545085 | XL-228 | Kd | = | 2366.0 | nM | 5.63 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 2508.0 | nM | 5.60 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 4560.0 | nM | 5.34 |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL2035187 | PACRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1091644 | LINSITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 30000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 30000.0 | nM | - |
| CHEMBL571948 | Y-39983 | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3402762 | TEPOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL24828 | VANDETANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL38380 | FASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL5416410 | DASATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1201182 | TEMSIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3187723 | BINIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL1879463 | DACTOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL411907 | SONOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2107832 | PIMASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1922094 | APITOLISIB | Kd | > | 30000.0 | nM | - |