Assay Detail
Binding
CHEMBL3991806
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
Ribosyldihydronicotinamide dehydrogenase [quinone] (CHEMBL3959) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 5.77 | 8.40 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 8.40 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 7.40 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.39 |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | 6.91 |
| CHEMBL3334567 | SAVOLITINIB | 3.0 | 1 | 6.69 |
| CHEMBL2133806 | JNJ-38877605 | 1.0 | 1 | 6.49 |
| CHEMBL4084193 | — | — | 1 | 6.43 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 6.33 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.19 |
| CHEMBL3402762 | TEPOTINIB | 4.0 | 1 | 6.06 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 5.99 |
| CHEMBL3120215 | OSI-027 | 2.0 | 1 | 5.86 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 5.85 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 5.83 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 5.82 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 5.77 |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | 5.63 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 5.61 |
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | 5.61 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.52 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 5.49 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 5.47 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.44 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.44 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 5.43 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.40 |
| CHEMBL281948 | K-252A | — | 1 | 5.39 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.37 |
| CHEMBL3545215 | BMS-911543 | 2.0 | 1 | 5.23 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2035187 | PACRITINIB | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL941 | IMATINIB | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL1236107 | SGX-523 | Kd | = | 124.0 | nM | 6.91 |
| CHEMBL3334567 | SAVOLITINIB | Kd | = | 206.0 | nM | 6.69 |
| CHEMBL2133806 | JNJ-38877605 | Kd | = | 323.0 | nM | 6.49 |
| CHEMBL4084193 | — | Kd | = | 370.0 | nM | 6.43 |
| CHEMBL1908391 | MASITINIB | Kd | = | 469.0 | nM | 6.33 |
| CHEMBL482967 | CYC-116 | Kd | = | 648.0 | nM | 6.19 |
| CHEMBL3402762 | TEPOTINIB | Kd | = | 875.0 | nM | 6.06 |
| CHEMBL521851 | PICTILISIB | Kd | = | 1028.0 | nM | 5.99 |
| CHEMBL3120215 | OSI-027 | Kd | = | 1390.0 | nM | 5.86 |
| CHEMBL1614713 | CC-401 | Kd | = | 1413.0 | nM | 5.85 |
| CHEMBL255863 | NILOTINIB | Kd | = | 1484.0 | nM | 5.83 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 1523.0 | nM | 5.82 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 1701.0 | nM | 5.77 |
| CHEMBL2386889 | SCH-900776 | Kd | = | 2359.0 | nM | 5.63 |
| CHEMBL3989868 | TUCATINIB | Kd | = | 2463.0 | nM | 5.61 |
| CHEMBL38380 | FASUDIL | Kd | = | 2451.0 | nM | 5.61 |
| CHEMBL522892 | DOVITINIB | Kd | = | 3011.0 | nM | 5.52 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 3257.0 | nM | 5.49 |
| CHEMBL2140408 | AMG-900 | Kd | = | 3353.0 | nM | 5.47 |
| CHEMBL3353410 | OSIMERTINIB | Kd | = | 3658.0 | nM | 5.44 |
| CHEMBL1908397 | KW-2449 | Kd | = | 3597.0 | nM | 5.44 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 3699.0 | nM | 5.43 |
| CHEMBL535 | SUNITINIB | Kd | = | 4022.0 | nM | 5.40 |
| CHEMBL281948 | K-252A | Kd | = | 4031.0 | nM | 5.39 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 4314.0 | nM | 5.37 |
| CHEMBL3545215 | BMS-911543 | Kd | = | 5864.0 | nM | 5.23 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 6363.0 | nM | 5.20 |
| CHEMBL206834 | BAFETINIB | Kd | = | 6869.0 | nM | 5.16 |
| CHEMBL514201 | TALMAPIMOD | Kd | = | 9918.0 | nM | 5.00 |
| CHEMBL3187723 | BINIMETINIB | Kd | = | 14700.0 | nM | 4.83 |
| CHEMBL1241855 | RIGOSERTIB | Kd | = | 15224.0 | nM | 4.82 |
| CHEMBL1822792 | MK-2461 | Kd | = | 52632.0 | nM | 4.28 |
| CHEMBL3544932 | TAK-901 | Kd | = | 88903.0 | nM | 4.05 |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | > | 30000.0 | nM | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2138625 | AV-412 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL551064 | AEW-541 | Kd | > | 30000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL411907 | SONOLISIB | Kd | > | 30000.0 | nM | - |