Assay Detail
Binding
CHEMBL1908636
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for FLT3(N841I) 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 | 6.89 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.85 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 8.82 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.82 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.68 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 8.64 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.62 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.59 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.59 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.39 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 8.37 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.32 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.27 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 8.22 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.96 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.96 |
| CHEMBL1908395 | — | — | 1 | 7.89 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.89 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.70 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 7.54 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 7.37 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.70 |
| CHEMBL379218 | — | — | 1 | 6.70 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 6.60 |
| CHEMBL450786 | PHA-665752 | — | 1 | 6.33 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 6.30 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 6.16 |
| CHEMBL386051 | — | — | 1 | 6.11 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.07 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.01 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL603469 | LESTAURTINIB | Kd | = | 1.4 | nM | 8.85 |
| CHEMBL475251 | R-406 | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL1230609 | FORETINIB | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 2.1 | nM | 8.68 |
| CHEMBL574738 | AST-487 | Kd | = | 2.3 | nM | 8.64 |
| CHEMBL535 | SUNITINIB | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL223360 | LINIFANIB | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 4.1 | nM | 8.39 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 4.3 | nM | 8.37 |
| CHEMBL522892 | DOVITINIB | Kd | = | 4.8 | nM | 8.32 |
| CHEMBL1721885 | SU-014813 | Kd | = | 5.4 | nM | 8.27 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL509032 | TAE-684 | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1336 | SORAFENIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1908395 | — | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL1908397 | KW-2449 | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL1289926 | AXITINIB | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL379218 | — | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL450786 | PHA-665752 | Kd | = | 470.0 | nM | 6.33 |
| CHEMBL553 | ERLOTINIB | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 690.0 | nM | 6.16 |
| CHEMBL386051 | — | Kd | = | 780.0 | nM | 6.11 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 860.0 | nM | 6.07 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 980.0 | nM | 6.01 |
| CHEMBL572881 | MOTESANIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL1241674 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL24828 | VANDETANIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL31965 | CANERTINIB | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL939 | GEFITINIB | Kd | = | 3000.0 | nM | 5.52 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 3400.0 | nM | 5.47 |
| CHEMBL521851 | PICTILISIB | Kd | = | 3900.0 | nM | 5.41 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 3900.0 | nM | 5.41 |
| CHEMBL1908396 | — | Kd | = | 4200.0 | nM | 5.38 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL1173655 | AFATINIB | Kd | = | 6200.0 | nM | 5.21 |
| CHEMBL180022 | NERATINIB | Kd | = | 6400.0 | nM | 5.19 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 6500.0 | nM | 5.19 |
| CHEMBL5416410 | DASATINIB | Kd | = | 7000.0 | nM | 5.16 |
| CHEMBL296468 | BMS-387032 | Kd | = | 9300.0 | nM | 5.03 |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |