Synonyms: BGB-324 | BGB324 | R-428 | R428
Compound class:
Synthetic organic
Comment: Bemcentinib (BGB324, R428) is a potent, selective and orally active AXL receptor tyrosine kinase inhibitor that was discovered by Rigel as R428 [3] and which is being developed by BergenBio for anti-cancer potential [4].
![]() 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. Bohan D, Van Ert H, Ruggio N, Rogers KJ, Badreddine M, Aguilar Briseño JA, Elliff JM, Rojas Chavez RA, Gao B, Stokowy T et al.. (2021)
Phosphatidylserine receptors enhance SARS-CoV-2 infection. PLoS Pathog, 17 (11): e1009743. [PMID:34797899] |
2. Dittmar M, Lee JS, Whig K, Segrist E, Li M, Kamalia B, Castellana L, Ayyanathan K, Cardenas-Diaz FL, Morrisey EE et al.. (2021)
Drug repurposing screens reveal cell-type-specific entry pathways and FDA-approved drugs active against SARS-Cov-2. Cell Rep, 35 (1): 108959. [PMID:33811811] |
3. Holland SJ, Pan A, Franci C, Hu Y, Chang B, Li W, Duan M, Torneros A, Yu J, Heckrodt TJ et al.. (2010)
R428, a selective small molecule inhibitor of Axl kinase, blocks tumor spread and prolongs survival in models of metastatic breast cancer. Cancer Res, 70 (4): 1544-54. [PMID:20145120] |
4. Myers SH, Brunton VG, Unciti-Broceta A. (2016)
AXL Inhibitors in Cancer: A Medicinal Chemistry Perspective. J Med Chem, 59 (3): 3593-608. [PMID:26555154] |
5. Sonja L, Gjertsen BT, Heuser M, Chromik J, Batalla IS, Akyuz N, Micklem D, Brown A, Lorens J, Kebenko M et al.. (2016)
BGB324, an Orally Available Selective Axl Inhibitor Exerts Anti-Leukemic Activity in the First-in-Patient Trial BGBC003 and Induces Unique Changes in Biomarker Profiles. Blood, 128: 592. |
6. UK Department of Health and Social Care.
COVID-19 treatments could be fast-tracked through new national clinical trial initiative. Accessed on 01/06/2020. Modified on 01/06/2020. gov.uk, https://www.gov.uk/government/news/covid-19-treatments-could-be-fast-tracked-through-new-national-clinical-trial-initiative |