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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Immunopharmacology Comments |
Human macrophages integrate signals through p53 and NF-κB to drive proinflammatory cytokine induction and NF-κB is prominent in macrophage-initiated inflammatory responses. Therefore compounds activating p53, including indirectly via MMD2 as p53-activating chemotherapeutics acting upon p53-sufficient macrophages and precursor monocytes, may indirectly impact tumors lacking functional p53 [1] |