Assay Detail
Binding
CHEMBL3991719
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
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.81 | 9.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 9.52 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 9.10 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.70 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.70 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 8.40 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.40 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 8.30 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 8.15 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 8.15 |
| CHEMBL482968 | ENMD-2076 | 2.0 | 1 | 8.10 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 7.82 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.75 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 7.75 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.43 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 7.43 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | 7.36 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 7.30 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 7.28 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 7.28 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 7.27 |
| CHEMBL3813873 | PEXIDARTINIB | 4.0 | 1 | 7.26 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.22 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.19 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 7.17 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 6.99 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.91 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.90 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 6.85 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 6.85 |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | 6.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL522892 | DOVITINIB | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL274654 | ORANTINIB | Kd | = | 0.8 | nM | 9.10 |
| CHEMBL1721885 | SU-014813 | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL535 | SUNITINIB | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL3545085 | XL-228 | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL1171837 | PONATINIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL475251 | R-406 | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL1908397 | KW-2449 | Kd | = | 37.0 | nM | 7.43 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 37.0 | nM | 7.43 |
| CHEMBL230011 | TG100-115 | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 50.0 | nM | 7.30 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL564829 | MILCICLIB | Kd | = | 54.0 | nM | 7.27 |
| CHEMBL3813873 | PEXIDARTINIB | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL1230609 | FORETINIB | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL495727 | AT-9283 | Kd | = | 64.0 | nM | 7.19 |
| CHEMBL574737 | UCN-01 | Kd | = | 67.0 | nM | 7.17 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 102.0 | nM | 6.99 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 122.0 | nM | 6.91 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 127.0 | nM | 6.90 |
| CHEMBL217092 | SARACATINIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL223360 | LINIFANIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL1952329 | SGI-1776 | Kd | = | 143.0 | nM | 6.84 |
| CHEMBL3699142 | — | Kd | = | 148.0 | nM | 6.83 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 179.0 | nM | 6.75 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 228.0 | nM | 6.64 |
| CHEMBL281948 | K-252A | Kd | = | 227.0 | nM | 6.64 |
| CHEMBL460702 | BMS-777607 | Kd | = | 228.0 | nM | 6.64 |
| CHEMBL415049 | BARASERTIB | Kd | = | 257.0 | nM | 6.59 |
| CHEMBL482967 | CYC-116 | Kd | = | 276.0 | nM | 6.56 |
| CHEMBL3545307 | MERESTINIB | Kd | = | 309.0 | nM | 6.51 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 308.0 | nM | 6.51 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 323.0 | nM | 6.49 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 341.0 | nM | 6.47 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 418.0 | nM | 6.38 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 461.0 | nM | 6.34 |
| CHEMBL3991934 | — | Kd | = | 465.0 | nM | 6.33 |
| CHEMBL3544932 | TAK-901 | Kd | = | 554.0 | nM | 6.26 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 550.0 | nM | 6.26 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 562.0 | nM | 6.25 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 627.0 | nM | 6.20 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 670.0 | nM | 6.17 |