Assay Detail
Binding
CHEMBL3991781
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
Serine/threonine-protein kinase MARK2 (CHEMBL3831) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 5.96 | 7.89 |
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 | 7.89 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.94 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.90 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.80 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.71 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 6.52 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.52 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 6.46 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.44 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.36 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.31 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.24 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.21 |
| CHEMBL281948 | K-252A | — | 1 | 6.15 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.12 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.87 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.69 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 5.68 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 5.66 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 5.64 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 5.64 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.63 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.63 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 5.58 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.52 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 5.50 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.50 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.50 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 5.35 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 5.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL574737 | UCN-01 | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 114.0 | nM | 6.94 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 125.0 | nM | 6.90 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 157.0 | nM | 6.80 |
| CHEMBL3545085 | XL-228 | Kd | = | 196.0 | nM | 6.71 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 302.0 | nM | 6.52 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL494089 | GSK-690693 | Kd | = | 351.0 | nM | 6.46 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 365.0 | nM | 6.44 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 442.0 | nM | 6.36 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 491.0 | nM | 6.31 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 580.0 | nM | 6.24 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 614.0 | nM | 6.21 |
| CHEMBL281948 | K-252A | Kd | = | 704.0 | nM | 6.15 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 759.0 | nM | 6.12 |
| CHEMBL495727 | AT-9283 | Kd | = | 1364.0 | nM | 5.87 |
| CHEMBL1908397 | KW-2449 | Kd | = | 2023.0 | nM | 5.69 |
| CHEMBL3137336 | UPROSERTIB | Kd | = | 2075.0 | nM | 5.68 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 2174.0 | nM | 5.66 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 2310.0 | nM | 5.64 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 2290.0 | nM | 5.64 |
| CHEMBL564829 | MILCICLIB | Kd | = | 2365.0 | nM | 5.63 |
| CHEMBL3544932 | TAK-901 | Kd | = | 2332.0 | nM | 5.63 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 2601.0 | nM | 5.58 |
| CHEMBL535 | SUNITINIB | Kd | = | 3013.0 | nM | 5.52 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 3184.0 | nM | 5.50 |
| CHEMBL3545328 | XL-019 | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL482967 | CYC-116 | Kd | = | 3147.0 | nM | 5.50 |
| CHEMBL1721885 | SU-014813 | Kd | = | 4507.0 | nM | 5.35 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 4960.0 | nM | 5.30 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 6017.0 | nM | 5.22 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 6626.0 | nM | 5.18 |
| CHEMBL522892 | DOVITINIB | Kd | = | 7728.0 | nM | 5.11 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 11103.0 | nM | 4.96 |
| CHEMBL507361 | MIRDAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2035187 | PACRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545307 | MERESTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL38380 | FASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL2103840 | DINACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL571546 | TIRBANIBULIN | Kd | > | 30000.0 | nM | - |
| CHEMBL2001019 | PF-04217903 | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614707 | MUBRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991931 | — | Kd | > | 30000.0 | nM | - |