Assay Detail
Binding
CHEMBL3991802
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 Nek9 (CHEMBL5257) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.08 | 7.39 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 7.39 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 7.28 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.88 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.75 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.32 |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | 6.18 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.83 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.82 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.79 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 5.75 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 5.69 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.69 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 5.66 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 5.53 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 4.71 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | - |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | - |
| CHEMBL283120 | AXL-1717 | 2.0 | 1 | - |
| CHEMBL1615025 | TAK-733 | 2.0 | 1 | - |
| CHEMBL400402 | — | — | 1 | - |
| CHEMBL405130 | WHI-P131 | 1.0 | 1 | - |
| CHEMBL592445 | GEDATOLISIB | 3.0 | 1 | - |
| CHEMBL2001019 | PF-04217903 | 1.0 | 1 | - |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | - |
| CHEMBL514201 | TALMAPIMOD | 2.0 | 1 | - |
| CHEMBL3991931 | — | — | 1 | - |
| CHEMBL3545307 | MERESTINIB | 2.0 | 1 | - |
| CHEMBL1983268 | ENTRECTINIB | 4.0 | 1 | - |
| CHEMBL2323775 | MK-8033 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL482967 | CYC-116 | Kd | = | 133.0 | nM | 6.88 |
| CHEMBL475251 | R-406 | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 474.0 | nM | 6.32 |
| CHEMBL575448 | BMS-754807 | Kd | = | 654.0 | nM | 6.18 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1492.0 | nM | 5.83 |
| CHEMBL495727 | AT-9283 | Kd | = | 1532.0 | nM | 5.82 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1634.0 | nM | 5.79 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 1780.0 | nM | 5.75 |
| CHEMBL522892 | DOVITINIB | Kd | = | 2051.0 | nM | 5.69 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 2034.0 | nM | 5.69 |
| CHEMBL3545328 | XL-019 | Kd | = | 2186.0 | nM | 5.66 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 2977.0 | nM | 5.53 |
| CHEMBL564829 | MILCICLIB | Kd | = | 19617.0 | nM | 4.71 |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989868 | TUCATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230607 | PHA-793887 | Kd | > | 30000.0 | nM | - |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3186534 | RIVOCERANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |
| CHEMBL3301607 | FILGOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL1738757 | REBASTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544932 | TAK-901 | Kd | > | 30000.0 | nM | - |
| CHEMBL2107832 | PIMASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3699142 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL3600873 | MK-5108 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545360 | ASP-3026 | Kd | > | 30000.0 | nM | - |
| CHEMBL536151 | IMD-0354 | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2041933 | AZD-7762 | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3688339 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL1094408 | NMS-1286937 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1084546 | PF-00562271 | Kd | > | 30000.0 | nM | - |