Assay Detail
Binding
CHEMBL3991800
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 Nek3 (CHEMBL5679) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 5.68 | 6.54 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.54 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.45 |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | 6.08 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.08 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 5.96 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.69 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.62 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 5.55 |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | 5.53 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 4.53 |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | 4.42 |
| CHEMBL283120 | AXL-1717 | 2.0 | 1 | - |
| CHEMBL3991934 | — | — | 1 | - |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | - |
| CHEMBL2079588 | TELATINIB | 2.0 | 1 | - |
| CHEMBL403989 | TG100-801 | 2.0 | 1 | - |
| CHEMBL3188551 | GSK-2636771 | 2.0 | 1 | - |
| CHEMBL514201 | TALMAPIMOD | 2.0 | 1 | - |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | - |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | - |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | - |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | - |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | - |
| CHEMBL3186534 | RIVOCERANIB | 3.0 | 1 | - |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | - |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | - |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | - |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 286.0 | nM | 6.54 |
| CHEMBL3545328 | XL-019 | Kd | = | 353.0 | nM | 6.45 |
| CHEMBL482967 | CYC-116 | Kd | = | 830.0 | nM | 6.08 |
| CHEMBL1976040 | ADAVOSERTIB | Kd | = | 837.0 | nM | 6.08 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 1105.0 | nM | 5.96 |
| CHEMBL495727 | AT-9283 | Kd | = | 2055.0 | nM | 5.69 |
| CHEMBL564829 | MILCICLIB | Kd | = | 2390.0 | nM | 5.62 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 2840.0 | nM | 5.55 |
| CHEMBL1233528 | VOLASERTIB | Kd | = | 2965.0 | nM | 5.53 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 29867.0 | nM | 4.53 |
| CHEMBL587723 | AEE-788 | Kd | = | 38088.0 | nM | 4.42 |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL1952329 | SGI-1776 | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614710 | OSI-930 | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3301610 | ABEMACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |
| CHEMBL2336325 | VISTUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3348923 | TOVORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL2029988 | CEP-32496 | Kd | > | 30000.0 | nM | - |
| CHEMBL1950289 | TANZISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL551064 | AEW-541 | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL502835 | NINTEDANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL411907 | SONOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103839 | RIDAFOROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 30000.0 | nM | - |
| CHEMBL2180604 | TAK-593 | Kd | > | 30000.0 | nM | - |