Assay Detail
Binding
CHEMBL1908637
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Binding constant for FLT3(R834Q) 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 | 6.87 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 9.66 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 9.13 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 8.36 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.29 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.15 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.12 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.96 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.96 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 7.92 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.80 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.77 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.77 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.54 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.47 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 7.36 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.22 |
| CHEMBL1908395 | — | — | 1 | 7.11 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.89 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.89 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 6.39 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 6.31 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 5.89 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 5.89 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 5.75 |
| CHEMBL379218 | — | — | 1 | 5.75 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 5.62 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.52 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 5.52 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 5.46 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | Kd | = | 0.22 | nM | 9.66 |
| CHEMBL574738 | AST-487 | Kd | = | 0.74 | nM | 9.13 |
| CHEMBL475251 | R-406 | Kd | = | 4.4 | nM | 8.36 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 5.1 | nM | 8.29 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL522892 | DOVITINIB | Kd | = | 7.5 | nM | 8.12 |
| CHEMBL1230609 | FORETINIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL535 | SUNITINIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL223360 | LINIFANIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL1336 | SORAFENIB | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL509032 | TAE-684 | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL1721885 | SU-014813 | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL1908397 | KW-2449 | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL1908395 | — | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL31965 | CANERTINIB | Kd | = | 490.0 | nM | 6.31 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL24828 | VANDETANIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL379218 | — | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL1289926 | AXITINIB | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL939 | GEFITINIB | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL572881 | MOTESANIB | Kd | = | 3800.0 | nM | 5.42 |
| CHEMBL450786 | PHA-665752 | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 4800.0 | nM | 5.32 |
| CHEMBL1241674 | — | Kd | = | 9600.0 | nM | 5.02 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 9600.0 | nM | 5.02 |
| CHEMBL249697 | BMS-345541 | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |
| CHEMBL386051 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL464552 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |