Evidence map›Paper›PMID 27910877›Full record

ReviewNature reviews. Drug discovery2017

A comprehensive map of molecular drug targets.

Rita Santos, Oleg Ursu, Anna Gaulton, A Patrícia Bento, Ramesh S Donadi, Cristian G Bologa, Anneli Karlsson, Bissan Al-Lazikani, Anne Hersey, Tudor I Oprea and 1 more

Abstract readReview
In one paragraph

Review in Nature reviews. Drug discovery, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1,159 papers.

0numbers the graph read from it
0cells of the map it votes in
1,159citing papers in PubMed
94.2field-weighted citation impact, top 1% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

1,159 citing papers in PubMed, 2,383 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Review
  6. The evolving landscape of drug targets.Nature reviews. Drug discovery · 2026
    Review
  7. Technology profiles in FDA-approved new molecular entities, 2013-2024: a latent class analysis.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2026
    Article
  8. Modulating pseudokinase conformation from the ATP-binding site.Structure (London, England : 1993) · 2026
    Article
  9. Artificial intelligence-assisted lead optimization in drug discovery: bridging computational advances and translational challenges.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026
    Review
  10. Article
  11. Article
  12. Article
  13. Review
  14. Review
  15. Review
  16. Article
  17. Review
  18. Review
  19. Article
  20. Review

1,099 more citing papers are in PubMed but not listed here.

4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

11 authors at 4 institutions in 2 countries.

Rita SantosEuropean Molecular Biology Laboratory-European Bioinformatics Institute (EMBL-EBI), Wellcome Genome Campus, Hinxton, Cambridge CB10 1SD, UK.
Oleg UrsuTranslational Informatics Division, University of New Mexico School of Medicine, MSC09 5025, 700 Camino de Salud NE, Albuquerque, New Mexico 87131, USA.
Anna GaultonEuropean Molecular Biology Laboratory-European Bioinformatics Institute (EMBL-EBI), Wellcome Genome Campus, Hinxton, Cambridge CB10 1SD, UK.
A Patrícia BentoEuropean Molecular Biology Laboratory-European Bioinformatics Institute (EMBL-EBI), Wellcome Genome Campus, Hinxton, Cambridge CB10 1SD, UK.
Ramesh S DonadiEuropean Molecular Biology Laboratory-European Bioinformatics Institute (EMBL-EBI), Wellcome Genome Campus, Hinxton, Cambridge CB10 1SD, UK.
Cristian G BologaTranslational Informatics Division, University of New Mexico School of Medicine, MSC09 5025, 700 Camino de Salud NE, Albuquerque, New Mexico 87131, USA.
Anneli KarlssonEuropean Molecular Biology Laboratory-European Bioinformatics Institute (EMBL-EBI), Wellcome Genome Campus, Hinxton, Cambridge CB10 1SD, UK.
Bissan Al-LazikaniCancer Research UK Cancer Therapeutics Unit, The Institute of Cancer Research, London SM2 5NG, UK.
Anne HerseyEuropean Molecular Biology Laboratory-European Bioinformatics Institute (EMBL-EBI), Wellcome Genome Campus, Hinxton, Cambridge CB10 1SD, UK.
Tudor I OpreaTranslational Informatics Division, University of New Mexico School of Medicine, MSC09 5025, 700 Camino de Salud NE, Albuquerque, New Mexico 87131, USA.
John P OveringtonEuropean Molecular Biology Laboratory-European Bioinformatics Institute (EMBL-EBI), Wellcome Genome Campus, Hinxton, Cambridge CB10 1SD, UK.
European Bioinformatics Institute · GBUniversity of New Mexico · USBenevolentAI (United Kingdom) · GBCancer Research UK · GB

Funding

WOMEN'S CANCERS RESEARCH PROGRAMP30CA118100 · NCI · UNIVERSITY OF NEW MEXICO HEALTH SCIS CTR · PI Yolanda Sanchez · 2005 to 2026
$57.1M
UNM HSC Clinical and Translational Science CenterUL1TR001449 · NCATS · UNIVERSITY OF NEW MEXICO HEALTH SCIS CTR · PI CAMPEN, MATTHEW J, PANDHI, NANCY · 2015 to 2024
$36.9M
Illuminating the Druggable Genome Knowledge Management Center (IDG KMC)U54CA189205 · NCI · UNIVERSITY OF NEW MEXICO HEALTH SCIS CTR · PI OPREA, TUDOR I · 2014 to 2017
$5.7M
Cancer Research UK 11566Cancer Research UK 22897NCATS NIH HHS UL1 TR001449NCI NIH HHS P30 CA118100NCI NIH HHS U54 CA189205Wellcome Trust
6 · The paper itself

Abstract

The success of mechanism-based drug discovery depends on the definition of the drug target. This definition becomes even more important as we try to link drug response to genetic variation, understand stratified clinical efficacy and safety, rationalize the differences between drugs in the same therapeutic class and predict drug utility in patient subgroups. However, drug targets are often poorly defined in the literature, both for launched drugs and for potential therapeutic agents in discovery and development. Here, we present an updated comprehensive map of molecular targets of approved drugs. We curate a total of 893 human and pathogen-derived biomolecules through which 1,578 US FDA-approved drugs act. These biomolecules include 667 human-genome-derived proteins targeted by drugs for human disease. Analysis of these drug targets indicates the continued dominance of privileged target families across disease areas, but also the growth of novel first-in-class mechanisms, particularly in oncology. We explore the relationships between bioactivity class and clinical success, as well as the presence of orthologues between human and animal models and between pathogen and human genomes. Through the collaboration of three independent teams, we highlight some of the ongoing challenges in accurately defining the targets of molecular therapeutics and present conventions for deconvoluting the complexities of molecular pharmacology and drug efficacy.

Indexed as

Databases, PharmaceuticalDrug ApprovalDrug Delivery SystemsDrug DiscoveryDrug PrescriptionsGenetic VariationGenome, HumanHumansPharmacogeneticsUnited StatesUnited States Food and Drug Administration

Identifiers

PMID27910877
PMCPMC6314433
OpenAlexW2558217333

What OpenQuestion holds

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Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.