Chemical probes & TEPs

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Overview
To support further assessments about the suitability of targets for a discovery pipeline, the Open Targets Platform integrates information from various sources on chemical probes and Target Enabling Packages (TEPs).
Chemical probes
A chemical probe is a small molecule that can act as chemical modulator of a system, such as a cell or an organism, by reversibly binding to a biological target. Chemical probes are expected to have a minimum standard of high affinity, binding selectivity and efficacy. As opposed to drugs, chemical probes do not need to meet the same requirements in terms of pharmacokinetics, pharmacodynamics, and bioavailability.
Target Enabling Packages
Target Enabling Packages (TEPs) are a critical mass of reagents and knowledge allowing for the rapid biochemical and chemical exploration of a given target.
As noted by the Structural Genomics Consortium, each TEP contains:
Protein production methods
Biochemical/biophysical assays for activity, affinity
Structures of the protein, potentially including wild type and disease mutant proteins; full-length or domains; protein-ligand complexes; structures of close homologues
Initial chemical matter from a fragment or small molecule screen
Additional components of TEPs may be developed on a case-by-case basis, based upon reasonable scientific need, in collaboration with TEP target nominators:
An antibody or nanobody
Cell-based assay
CRISPR knockout
Data sources
Probes & Drugs Portal
The Probes & Drugs Portal - https://www.probes-drugs.org/home/ - is a public resource joining together focused libraries of bioactive compounds (probes, drugs, specific inhibitor sets etc.) with commercially available screening libraries. The purpose of the Portal is to reflect the current state of bioactive compound space and to enable its exploration from different points of view. It is intended to serve as a central hub in chemical biology research by providing a unique integration of the most relevant probes sources such as the Chemical Probes Portal, Open Science Probes, and ProbeMiner.
Structural Genomics Consortium
The Structural Genomics Consortium (SGC) - https://www.thesgc.org/ - is a public-private partnership focused on accelerating drug discovery using open science. The SGC’s core research operations are funded by pharmaceutical companies, governments, and charities, all of which act as research partners and participate in the governance of the SGC.
Computational pipelines and datasets
Chemical probes datasets are downloaded from each data source listed above, mapped to the correct Ensembl gene ID, and ingested during our initial pipeline steps. The files are available for download from our data download page.
Safety
Baseline expression
Last modified 27d ago
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Contents
Overview
Chemical probes
Target Enabling Packages
Data sources
Probes & Drugs Portal
Structural Genomics Consortium
Computational pipelines and datasets