- Guide to PHARMACOLOGY
Synonyms: SB-1518 | SB1518 | Vonjo®
pacritinib is an approved drug (FDA (2022))
Compound class: Synthetic organic
Comment: Pacritinib is an orally bioavailable and somewhat selective inhibitor of Janus kinase 2 (JAK2) and the JAK2 gain-of-function mutant JAK2V617F . At clinically relevant concentrations, pacritinib does not inhibit JAK1. It also has some inhibitory activity against FMS-like tyrosine kinase 3 (FLT3).
Ligand Activity Visualisation Charts
These 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.✖
1. Hart S, Goh KC, Novotny-Diermayr V, Hu CY, Hentze H, Tan YC, Madan B, Amalini C, Loh YK, Ong LC et al.. (2011)
SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies.
Leukemia, 25 (11): 1751-9. [PMID:21691275]
2. William AD, Lee AC, Blanchard S, Poulsen A, Teo EL, Nagaraj H, Tan E, Chen D, Williams M, Sun ET et al.. (2011)
Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[18.104.22.168(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JAK2/FLT3) inhibitor for the treatment of myelofibrosis and lymphoma.
J Med Chem, 54 (13): 4638-58. [PMID:21604762]