Compound class:
Synthetic organic
Comment: RG7112 is a clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket. In cancer cells expressing wild-type p53, this compound stabilizes it and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumour xenografts [2].
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. Lowe JM, Menendez D, Bushel PR, Shatz M, Kirk EL, Troester MA, Garantziotis S, Fessler MB, Resnick MA. (2014)
p53 and NF-κB coregulate proinflammatory gene responses in human macrophages. Cancer Res, 74 (8): 2182-92. [PMID:24737129] |
2. Vu B, Wovkulich P, Pizzolato G, Lovey A, Ding Q, Jiang N, Liu JJ, Zhao C, Glenn K, Wen Y et al.. (2013)
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Med Chem Lett, 4 (5): 466-9. [PMID:24900694] |