Assay Detail
Binding
CHEMBL1908634
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for FLT3(ITD) 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 | 6.92 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475251 | R-406 | 2.0 | 1 | 9.27 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 9.15 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.00 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.82 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.74 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.62 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.59 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.44 |
| CHEMBL1908395 | — | — | 1 | 8.38 |
| CHEMBL509032 | TAE-684 | — | 1 | 8.07 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.06 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.06 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 8.04 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.96 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 7.96 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.80 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.70 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.35 |
| CHEMBL450786 | PHA-665752 | — | 1 | 7.24 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 7.14 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.10 |
| CHEMBL379218 | — | — | 1 | 7.08 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.85 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.60 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.55 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.14 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.09 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 6.00 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 5.82 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475251 | R-406 | Kd | = | 0.54 | nM | 9.27 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL535 | SUNITINIB | Kd | = | 0.99 | nM | 9.00 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL1721885 | SU-014813 | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL1230609 | FORETINIB | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL522892 | DOVITINIB | Kd | = | 3.6 | nM | 8.44 |
| CHEMBL1908395 | — | Kd | = | 4.2 | nM | 8.38 |
| CHEMBL509032 | TAE-684 | Kd | = | 8.6 | nM | 8.07 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 8.8 | nM | 8.06 |
| CHEMBL223360 | LINIFANIB | Kd | = | 8.8 | nM | 8.06 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 9.1 | nM | 8.04 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL574738 | AST-487 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL1908397 | KW-2449 | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL450786 | PHA-665752 | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 72.0 | nM | 7.14 |
| CHEMBL1336 | SORAFENIB | Kd | = | 79.0 | nM | 7.10 |
| CHEMBL379218 | — | Kd | = | 83.0 | nM | 7.08 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL1289926 | AXITINIB | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 730.0 | nM | 6.14 |
| CHEMBL553 | ERLOTINIB | Kd | = | 820.0 | nM | 6.09 |
| CHEMBL572881 | MOTESANIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 1500.0 | nM | 5.82 |
| CHEMBL24828 | VANDETANIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL1241674 | — | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL1908396 | — | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL521851 | PICTILISIB | Kd | = | 2200.0 | nM | 5.66 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL386051 | — | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL939 | GEFITINIB | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL31965 | CANERTINIB | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 6100.0 | nM | 5.21 |
| CHEMBL941 | IMATINIB | Kd | = | 6300.0 | nM | 5.20 |
| CHEMBL573339 | PI-103 | Kd | = | 7200.0 | nM | 5.14 |
| CHEMBL5416410 | DASATINIB | Kd | = | 9900.0 | nM | 5.00 |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |