Assay Detail
Binding
CHEMBL1908633
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for FLT3(D835Y) 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 | 6.99 | 9.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475251 | R-406 | 2.0 | 1 | 9.43 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 9.38 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 9.24 |
| CHEMBL1908395 | — | — | 1 | 8.82 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.70 |
| CHEMBL509032 | TAE-684 | — | 1 | 8.70 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.64 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.60 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.28 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.21 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 8.19 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.15 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.96 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.96 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.89 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 7.82 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 7.40 |
| CHEMBL379218 | — | — | 1 | 7.37 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.26 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.09 |
| CHEMBL450786 | PHA-665752 | — | 1 | 7.02 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.89 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.89 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.68 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.57 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 6.37 |
| CHEMBL1241674 | — | — | 1 | 6.25 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.17 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 6.15 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 6.14 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475251 | R-406 | Kd | = | 0.37 | nM | 9.43 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 0.42 | nM | 9.38 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 0.57 | nM | 9.24 |
| CHEMBL1908395 | — | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL1230609 | FORETINIB | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL509032 | TAE-684 | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL535 | SUNITINIB | Kd | = | 2.3 | nM | 8.64 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL522892 | DOVITINIB | Kd | = | 5.2 | nM | 8.28 |
| CHEMBL1721885 | SU-014813 | Kd | = | 6.1 | nM | 8.21 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 6.4 | nM | 8.19 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 7.1 | nM | 8.15 |
| CHEMBL223360 | LINIFANIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL574738 | AST-487 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1908397 | KW-2449 | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 40.0 | nM | 7.40 |
| CHEMBL379218 | — | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 55.0 | nM | 7.26 |
| CHEMBL1336 | SORAFENIB | Kd | = | 82.0 | nM | 7.09 |
| CHEMBL450786 | PHA-665752 | Kd | = | 96.0 | nM | 7.02 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL553 | ERLOTINIB | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL1289926 | AXITINIB | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL1241674 | — | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 670.0 | nM | 6.17 |
| CHEMBL521851 | PICTILISIB | Kd | = | 710.0 | nM | 6.15 |
| CHEMBL31965 | CANERTINIB | Kd | = | 730.0 | nM | 6.14 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 810.0 | nM | 6.09 |
| CHEMBL24828 | VANDETANIB | Kd | = | 830.0 | nM | 6.08 |
| CHEMBL939 | GEFITINIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL1173655 | AFATINIB | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL464552 | — | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL296468 | BMS-387032 | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL513909 | BI-2536 | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL180022 | NERATINIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL386051 | — | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL5416410 | DASATINIB | Kd | = | 4800.0 | nM | 5.32 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 6500.0 | nM | 5.19 |
| CHEMBL572881 | MOTESANIB | Kd | = | 9500.0 | nM | 5.02 |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |