The Illuminating the Druggable Genome Knowledge Management Center (IDGKMC) evaluates, organizes and distils more than 80 protein-centric and over 20 gene-centric resources, currently focused on G-Protein Coupled Receptors, Nuclear Receptors, Ion Channels and Kinases. Data wrangling, coupled with algorithmic processing, text mining of drug labels, patents, medical literature, as well as human curation and drug-target ontology development, yield emergent properties and knowledge for target-disease associations. Tissue expression data from GTEx and other sources, disease-centric text mining and other resources are integrated using a number of specialized ontologies, e.g., the Disease Ontology. Using metrics derived from text mining and gene reference into function, as well as the number of antibodies, IDGKMC catalogs proteins into four categories: “Tdark”, i.e., proteins that lack functional information and disease relevance, "Tclin", proteins with confirmed drug mechanism of action, "Tchem", for which potent) small molecules are known, and literature, functional and disease annotations data are available (“Tbio”) - see Figure 1. Data can be mined via the user interface portal, Pharos. This integrative effort led to the following observations: i) there appears to be a knowledge deficit, i.e., we lack understanding of protein function for 38% of human proteome; ii) less than 3% of the human proteome is therapeutically addressed by drugs; iii) given current understanding of disease (~8,800 disease concepts), as well as all diseases addressed via on-label (~2,000) and off-label (~400) indications, we currently address at most a quarter of all diseases via therapeutic agents.

Illuminating the druggable genome: Linking diseases, targets and drugs

252nd National Meeting (2016)

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