• What is the Historeceptomics Profiler?

    The Historeceptomics Profiler (HR Profiler) is a drug discovery informatics tool pioneered by Dr. Timothy Cardozo at NYU School of Medicine (Shmelkov et al., 2015). Historeceptomics is a visualization of how the anatomic tissue map (“histo”) of a drug's ensemble of target receptors (“recept”) provides new insights into a drug’s mechanism of action, both for beneficial and adverse phenotypes elicited by the drug. We created the Historeceptomics profiler in order to try and fill some major gaps in the current drug development process. Specifically, many investigators overlook the fact that, in order for a drug to be effective against a disease, it must target proteins expressed in tissues related to the disease (Kumar et al., 2016). Our HR Profiler returns this information and can take any drug-like compound and determine its historeceptomic profile, or the list of target-tissue pairs most affected by the drug. For an illustrative use case of this method, check out our analysis  of antipsychotic drugs, (Cardozo et al., 2017). 

  • Who is GeneCentrix?

    GeneCentrix was founded in 2015 by Dr. Timothy Cardozo and his team and spun out of New York University to develop commercial products using the historeceptomics method.

  • Who are GeneCentrix's partners and sponsors?

    The R&D of GeneCentrix is funded by the National Institute of General Medical Sciences, the National Library of Medicine of the National Institutes of Health, and the National Institute on Drug Abuse to develop informatics products to predict drug activity in humans. New York University is an equity partner in GeneCentrix. 

  • What bioactivity data do you use? What docking data do you use?

    We currently use experimentally derived Ki, Kd, and IC50 data for human proteins from major cheminformatics databases such as ChEMBL and DrugBank for our bioactivity data. We also provide access, through the Historeceptomics profiler, to our proprietary database of in silico docking results that grows daily and currently includes over 1700 drugs docked against 6500 proteins, with over 352,000 hits. Additionally, we are working on a product that will allow users to upload their own bioactivity data in order to make it possible for users to generate a historeceptomics profile for a drug at any stage of development. Stay tuned for updates. 

  • What is an HR score?

    The historeceptomics (HR) score allows ranking of all human target-tissue pairs for a given drug. It is computed using a model that incorporates the affinity of the drug for a protein target, and the expression level of that target across tissues. By comparing across all tissues, we can calculate an HR score for each individual target-tissue pair simultaneously.  A high HR score (>~40) indicates high potential activity for a drug in a given tissue.

  • What future features will there be?

    We are constantly updating the Historeceptomics profiler with new datasets, features and search types. We’re currently working on incorporating expression data from cell lines, disease-specific expression data, and brain-specific tissue expression data. Further down the line, we will be adding other ways to look at the problem of tissue-specific drug activity: proteomics and protein expression, metabolic data, pharmacokinetics and tissue distribution of the drug.

  • Can I get a free trial?

    Yes! Click here to register.

  • Anything else?

    If you have a question that wasn’t answered here, feel free to contact us and we will get back to you shortly. More detailed information about Historeceptomics is available on the platform.