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Synonyms: Klisyri® | KX 2-391 | KX-01 | KX-2-391 | KX2-391
tirbanibulin is an approved drug (FDA (2020), EMA (2021))
Compound class: Synthetic organic
Comment: Tirbanibulin (KX2-391) is an orally bioavailable small molecule with a dual mode of action. It is a Src kinase inhibitor with potential antiproliferative activity [7-8] and an inhibitor of tubulin polymerization .
Synthesis of KX2-391 is described in US patent US20060160800 , where it is compound 134.
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.✖
|The binding affinity of KX2-391 for isolated Src protien is low . However, KX2-391 inhibits both auto- and trans-phosphorylation activites mediated by Src, and these correlate with the potency of growth inhibition observed in whole cells. Although an IC50 value of 20nM for inhibition of Src activity by KX2-391 is referred to in articles such as  and , we have been unable to find the primary source of this data.
Several articles demonstrate the effectiveness of KX2-391 as an inhibitor of tumour cell proliferation both in vitro and in vivo [1,3-4], and indeed this compound showed preliminary signs of clinical efficacy against solid tumours in a Phase I study . Patent data (US20060160800 ) provides GI50 values of 13nM and 26nM for growth inhibition of c-Src 3T3 cells and HT-29 cells respectively. α and β tubulin binding was shown using a photoaffinity analogue of KX2-391 .
|Selectivity at enzymes|
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