Assay Detail
Binding
CHEMBL3991782
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
MAP/microtubule affinity-regulating kinase 3 (CHEMBL5600) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 5.93 | 7.80 |
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 | 7.80 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.99 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.98 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.98 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.88 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 6.69 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 6.66 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.51 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.49 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.44 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.44 |
| CHEMBL281948 | K-252A | — | 1 | 6.42 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.41 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.38 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 6.25 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.96 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.86 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.82 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.80 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 5.79 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 5.77 |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | 5.71 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 5.68 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 5.64 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.62 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.59 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.46 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 5.35 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 5.04 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL574737 | UCN-01 | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 103.0 | nM | 6.99 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 105.0 | nM | 6.98 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 104.0 | nM | 6.98 |
| CHEMBL3545085 | XL-228 | Kd | = | 133.0 | nM | 6.88 |
| CHEMBL494089 | GSK-690693 | Kd | = | 204.0 | nM | 6.69 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 306.0 | nM | 6.51 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 321.0 | nM | 6.49 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 364.0 | nM | 6.44 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 361.0 | nM | 6.44 |
| CHEMBL281948 | K-252A | Kd | = | 384.0 | nM | 6.42 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 387.0 | nM | 6.41 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 417.0 | nM | 6.38 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 562.0 | nM | 6.25 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 1090.0 | nM | 5.96 |
| CHEMBL495727 | AT-9283 | Kd | = | 1370.0 | nM | 5.86 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1520.0 | nM | 5.82 |
| CHEMBL482967 | CYC-116 | Kd | = | 1581.0 | nM | 5.80 |
| CHEMBL3545328 | XL-019 | Kd | = | 1609.0 | nM | 5.79 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 1701.0 | nM | 5.77 |
| CHEMBL2386889 | SCH-900776 | Kd | = | 1932.0 | nM | 5.71 |
| CHEMBL3137336 | UPROSERTIB | Kd | = | 2087.0 | nM | 5.68 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 2314.0 | nM | 5.64 |
| CHEMBL3544932 | TAK-901 | Kd | = | 2416.0 | nM | 5.62 |
| CHEMBL535 | SUNITINIB | Kd | = | 2567.0 | nM | 5.59 |
| CHEMBL564829 | MILCICLIB | Kd | = | 3443.0 | nM | 5.46 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 4490.0 | nM | 5.35 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 9024.0 | nM | 5.04 |
| CHEMBL522892 | DOVITINIB | Kd | = | 10397.0 | nM | 4.98 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 10782.0 | nM | 4.97 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 14828.0 | nM | 4.83 |
| CHEMBL1721885 | SU-014813 | Kd | = | 26617.0 | nM | 4.58 |
| CHEMBL571948 | Y-39983 | Kd | = | 38457.0 | nM | 4.42 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 58240.0 | nM | 4.24 |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289494 | TIVOZANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545307 | MERESTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL1738797 | ALECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |