Assay Detail
Binding
CHEMBL3991905
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 TBK1 (CHEMBL5408) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.01 | 7.11 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.11 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.99 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.73 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.52 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.46 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.42 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 6.41 |
| CHEMBL3688339 | — | — | 1 | 6.34 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.25 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.25 |
| CHEMBL3699142 | — | — | 1 | 6.12 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.01 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 5.99 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.95 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.95 |
| CHEMBL281948 | K-252A | — | 1 | 5.94 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.93 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 5.88 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.82 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | 5.79 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.71 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.71 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 5.70 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 5.70 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.68 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.65 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.56 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 5.28 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 4.30 |
| CHEMBL2087361 | ICOTINIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4289017 | PF-03814735 | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL495727 | AT-9283 | Kd | = | 102.0 | nM | 6.99 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 188.0 | nM | 6.73 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 299.0 | nM | 6.52 |
| CHEMBL475251 | R-406 | Kd | = | 345.0 | nM | 6.46 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 377.0 | nM | 6.42 |
| CHEMBL574737 | UCN-01 | Kd | = | 393.0 | nM | 6.41 |
| CHEMBL3688339 | — | Kd | = | 452.0 | nM | 6.34 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 562.0 | nM | 6.25 |
| CHEMBL3545328 | XL-019 | Kd | = | 561.0 | nM | 6.25 |
| CHEMBL3699142 | — | Kd | = | 759.0 | nM | 6.12 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 977.0 | nM | 6.01 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 1022.0 | nM | 5.99 |
| CHEMBL3545085 | XL-228 | Kd | = | 1118.0 | nM | 5.95 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1114.0 | nM | 5.95 |
| CHEMBL281948 | K-252A | Kd | = | 1157.0 | nM | 5.94 |
| CHEMBL482967 | CYC-116 | Kd | = | 1162.0 | nM | 5.93 |
| CHEMBL1721885 | SU-014813 | Kd | = | 1330.0 | nM | 5.88 |
| CHEMBL535 | SUNITINIB | Kd | = | 1502.0 | nM | 5.82 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 1629.0 | nM | 5.79 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 1949.0 | nM | 5.71 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1966.0 | nM | 5.71 |
| CHEMBL274654 | ORANTINIB | Kd | = | 1982.0 | nM | 5.70 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 2007.0 | nM | 5.70 |
| CHEMBL564829 | MILCICLIB | Kd | = | 2088.0 | nM | 5.68 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 2230.0 | nM | 5.65 |
| CHEMBL3544932 | TAK-901 | Kd | = | 2762.0 | nM | 5.56 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 5306.0 | nM | 5.28 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 49601.0 | nM | 4.30 |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2029988 | CEP-32496 | Kd | > | 30000.0 | nM | - |
| CHEMBL1230165 | SILMITASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL3186534 | RIVOCERANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2220486 | LUCITANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1088752 | LOSMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1233528 | VOLASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |