Assay Detail
Binding
CHEMBL3991922
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 ULK3 (CHEMBL5047) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.39 | 8.22 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 8.22 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.72 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.35 |
| CHEMBL281948 | K-252A | — | 1 | 6.97 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.67 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.57 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.54 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.53 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.36 |
| CHEMBL3688339 | — | — | 1 | 6.32 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 6.32 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.31 |
| CHEMBL3699142 | — | — | 1 | 6.21 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.20 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.18 |
| CHEMBL1922094 | APITOLISIB | 2.0 | 1 | 6.14 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.10 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.01 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.98 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.95 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 5.93 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 5.84 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 5.83 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 5.76 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 5.75 |
| CHEMBL1614710 | OSI-930 | 1.0 | 1 | - |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | - |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | - |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | - |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301622 | GILTERITINIB | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL495727 | AT-9283 | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL281948 | K-252A | Kd | = | 107.0 | nM | 6.97 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 212.0 | nM | 6.67 |
| CHEMBL475251 | R-406 | Kd | = | 272.0 | nM | 6.57 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 291.0 | nM | 6.54 |
| CHEMBL3545328 | XL-019 | Kd | = | 297.0 | nM | 6.53 |
| CHEMBL1721885 | SU-014813 | Kd | = | 433.0 | nM | 6.36 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 476.0 | nM | 6.32 |
| CHEMBL3688339 | — | Kd | = | 474.0 | nM | 6.32 |
| CHEMBL3545085 | XL-228 | Kd | = | 492.0 | nM | 6.31 |
| CHEMBL3699142 | — | Kd | = | 612.0 | nM | 6.21 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 626.0 | nM | 6.20 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 655.0 | nM | 6.18 |
| CHEMBL1922094 | APITOLISIB | Kd | = | 721.0 | nM | 6.14 |
| CHEMBL482967 | CYC-116 | Kd | = | 801.0 | nM | 6.10 |
| CHEMBL522892 | DOVITINIB | Kd | = | 968.0 | nM | 6.01 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1046.0 | nM | 5.98 |
| CHEMBL535 | SUNITINIB | Kd | = | 1125.0 | nM | 5.95 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 1167.0 | nM | 5.93 |
| CHEMBL274654 | ORANTINIB | Kd | = | 1455.0 | nM | 5.84 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 1480.0 | nM | 5.83 |
| CHEMBL1171837 | PONATINIB | Kd | = | 1720.0 | nM | 5.76 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 1789.0 | nM | 5.75 |
| CHEMBL3545307 | MERESTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL507361 | MIRDAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | Kd | > | 30000.0 | nM | - |
| CHEMBL2107832 | PIMASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL1091644 | LINSITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL206834 | BAFETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL2103842 | VARLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1738797 | ALECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL502835 | NINTEDANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |