Assay Detail
Binding
CHEMBL1908635
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for FLT3(K663Q) kinase domain
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 7.22 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.66 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 9.29 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 9.17 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 9.15 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 9.09 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.96 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.89 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 8.82 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 8.70 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.66 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.48 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 8.41 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 8.35 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.35 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 8.32 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.27 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 8.18 |
| CHEMBL509032 | TAE-684 | — | 1 | 8.09 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.89 |
| CHEMBL1908395 | — | — | 1 | 7.70 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 7.51 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 7.27 |
| CHEMBL386051 | — | — | 1 | 6.89 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.72 |
| CHEMBL1908396 | — | — | 1 | 6.70 |
| CHEMBL450786 | PHA-665752 | — | 1 | 6.57 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.48 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 6.38 |
| CHEMBL379218 | — | — | 1 | 6.30 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | Kd | = | 0.22 | nM | 9.66 |
| CHEMBL574738 | AST-487 | Kd | = | 0.51 | nM | 9.29 |
| CHEMBL475251 | R-406 | Kd | = | 0.68 | nM | 9.17 |
| CHEMBL1721885 | SU-014813 | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL1230609 | FORETINIB | Kd | = | 0.82 | nM | 9.09 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL223360 | LINIFANIB | Kd | = | 1.3 | nM | 8.89 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 2.2 | nM | 8.66 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 3.3 | nM | 8.48 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 3.9 | nM | 8.41 |
| CHEMBL1336 | SORAFENIB | Kd | = | 4.5 | nM | 8.35 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 4.5 | nM | 8.35 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 4.8 | nM | 8.32 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 5.4 | nM | 8.27 |
| CHEMBL1908397 | KW-2449 | Kd | = | 6.6 | nM | 8.18 |
| CHEMBL509032 | TAE-684 | Kd | = | 8.2 | nM | 8.09 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL1908395 | — | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL1289926 | AXITINIB | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL572881 | MOTESANIB | Kd | = | 54.0 | nM | 7.27 |
| CHEMBL386051 | — | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL24828 | VANDETANIB | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL1908396 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL450786 | PHA-665752 | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 420.0 | nM | 6.38 |
| CHEMBL379218 | — | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 650.0 | nM | 6.19 |
| CHEMBL558752 | RAF-265 | Kd | = | 730.0 | nM | 6.14 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 740.0 | nM | 6.13 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 890.0 | nM | 6.05 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 900.0 | nM | 6.05 |
| CHEMBL553 | ERLOTINIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL1241674 | — | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL31965 | CANERTINIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL521851 | PICTILISIB | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL5416410 | DASATINIB | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL180022 | NERATINIB | Kd | = | 4900.0 | nM | 5.31 |
| CHEMBL939 | GEFITINIB | Kd | = | 5100.0 | nM | 5.29 |
| CHEMBL259084 | MLN-8054 | Kd | = | 9500.0 | nM | 5.02 |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |