Assay Detail
Binding
CHEMBL1908632
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Binding constant for FLT3(D835H) 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 | 6.95 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL475251 | R-406 | 2.0 | 1 | 9.19 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 9.18 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 9.15 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.85 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.68 |
| CHEMBL1908395 | — | — | 1 | 8.62 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.57 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.43 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.37 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 8.31 |
| CHEMBL509032 | TAE-684 | — | 1 | 8.31 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 8.31 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.21 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.20 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 8.17 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.89 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.85 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.52 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 7.31 |
| CHEMBL379218 | — | — | 1 | 7.11 |
| CHEMBL450786 | PHA-665752 | — | 1 | 6.85 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.68 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.68 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 6.51 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.48 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.46 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 6.39 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.30 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.25 |
| CHEMBL1241674 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL475251 | R-406 | Kd | = | 0.65 | nM | 9.19 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 0.66 | nM | 9.18 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 0.71 | nM | 9.15 |
| CHEMBL1230609 | FORETINIB | Kd | = | 1.4 | nM | 8.85 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 2.1 | nM | 8.68 |
| CHEMBL1908395 | — | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL223360 | LINIFANIB | Kd | = | 2.7 | nM | 8.57 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 3.7 | nM | 8.43 |
| CHEMBL535 | SUNITINIB | Kd | = | 4.3 | nM | 8.37 |
| CHEMBL574738 | AST-487 | Kd | = | 4.9 | nM | 8.31 |
| CHEMBL509032 | TAE-684 | Kd | = | 4.9 | nM | 8.31 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 4.9 | nM | 8.31 |
| CHEMBL522892 | DOVITINIB | Kd | = | 6.1 | nM | 8.21 |
| CHEMBL1721885 | SU-014813 | Kd | = | 6.3 | nM | 8.20 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 6.8 | nM | 8.17 |
| CHEMBL1908397 | KW-2449 | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL1336 | SORAFENIB | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL379218 | — | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL450786 | PHA-665752 | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 310.0 | nM | 6.51 |
| CHEMBL1289926 | AXITINIB | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL553 | ERLOTINIB | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL24828 | VANDETANIB | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL1241674 | — | Kd | = | 630.0 | nM | 6.20 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL939 | GEFITINIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL31965 | CANERTINIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL386051 | — | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL521851 | PICTILISIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL1173655 | AFATINIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL464552 | — | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL572881 | MOTESANIB | Kd | = | 4500.0 | nM | 5.35 |
| CHEMBL180022 | NERATINIB | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL573339 | PI-103 | Kd | = | 5900.0 | nM | 5.23 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 6100.0 | nM | 5.21 |
| CHEMBL296468 | BMS-387032 | Kd | = | 7400.0 | nM | 5.13 |
| CHEMBL5416410 | DASATINIB | Kd | = | 8100.0 | nM | 5.09 |
| CHEMBL1908396 | — | Kd | = | 9500.0 | nM | 5.02 |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |