Compound class:
Synthetic organic
Comment: Compound 5e is a potent FMS-like tyrosine kinase 3 (FLT3, a type III receptor tyrosine kinase) inhibitor that is in preclinical evaluation for the treatment of acute myelogenous leukemia (AML) [3].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Gilliland DG, Griffin JD. (2002)
The roles of FLT3 in hematopoiesis and leukemia. Blood, 100 (5): 1532-42. [PMID:12176867] |
2. Hayakawa F, Towatari M, Kiyoi H, Tanimoto M, Kitamura T, Saito H, Naoe T. (2000)
Tandem-duplicated Flt3 constitutively activates STAT5 and MAP kinase and introduces autonomous cell growth in IL-3-dependent cell lines. Oncogene, 19 (5): 624-31. [PMID:10698507] |
3. Jarusiewicz JA, Jeon JY, Connelly MC, Chen Y, Yang L, Baker SD, Guy RK. (2017)
Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia. ACS Omega, 2 (5): 1985-2009. [PMID:28580438] |
4. Lagunas-Rangel FA, Chávez-Valencia V. (2017)
FLT3-ITD and its current role in acute myeloid leukaemia. Med Oncol, 34 (6): 114. [PMID:28470536] |
5. Mizuki M, Fenski R, Halfter H, Matsumura I, Schmidt R, Müller C, Grüning W, Kratz-Albers K, Serve S, Steur C et al.. (2000)
Flt3 mutations from patients with acute myeloid leukemia induce transformation of 32D cells mediated by the Ras and STAT5 pathways. Blood, 96 (12): 3907-14. [PMID:11090077] |
6. Naoe T, Kiyoi H. (2004)
Normal and oncogenic FLT3. Cell Mol Life Sci, 61 (23): 2932-8. [PMID:15583855] |
7. Yokota S, Kiyoi H, Nakao M, Iwai T, Misawa S, Okuda T, Sonoda Y, Abe T, Kahsima K, Matsuo Y et al.. (1997)
Internal tandem duplication of the FLT3 gene is preferentially seen in acute myeloid leukemia and myelodysplastic syndrome among various hematological malignancies. A study on a large series of patients and cell lines. Leukemia, 11 (10): 1605-9. [PMID:9324277] |