Evidence map›Paper›PMID 40709733›Full record

ArticleJournal of medicinal chemistry2025

Discovery of BI-2493, a Pan-KRAS Inhibitor Showing

Joachim Bröker, Alex G Waterson, Timothy R Hodges, Jason R Abbott, Allison Arnold, Jark Böttcher, Nina Braun, Jianwen Cui, Julian E Fuchs, Thomas Gerstberger and 15 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
–field-weighted citation impact
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

12 citing papers in PubMed.

  1. Article
  2. Review
  3. Review
  4. Targeted therapeutic strategies forTranslational lung cancer research · 2026
    Review
  5. Article
  6. Review
  7. Article
  8. Systematic and precise interventions for KRAS-mutant cancers.Experimental hematology & oncology · 2026
    Review
  9. Article
  10. Review
  11. Review
  12. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

25 authors.

Joachim BrökerBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.ORCID 0000-0002-7371-8481
Alex G WatersonVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0002-0153-5723
Timothy R HodgesVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0003-1216-9551
Jason R AbbottVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0002-2291-2903
Allison ArnoldVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Jark BöttcherBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Nina BraunBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.ORCID 0000-0002-4697-4690
Jianwen CuiVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Julian E FuchsBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Thomas GerstbergerBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.ORCID 0000-0002-6837-1401
Sebastian GoggBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Sabine HannerBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Lorenz HerdeisBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Lucas W HowellVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0009-0009-1533-0647
Andreas MantoulidisBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Moriz MayerBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Jason PhanVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Francesca RocchettiBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Kyra SankarBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Dhruba SarkarVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0003-0597-3066
Otmar SchaafBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
John L SensintaffarVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Qi SunVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Tobias WunbergBoehringer Ingelheim RCV GmbH & Co., KG, Dr. Boehringer Gasse 5-11, A-1121 Vienna, Austria.
Stephen W FesikVanderbilt University School of Medicine, Department of Biochemistry, 2215 Garland Ave., 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0001-5957-6192

Funding

The Vanderbilt Molecular Target Discovery and Development CenterRC2CA148375 · NCI · VANDERBILT UNIVERSITY · PI MARNETT, LAWRENCE J. · 2009 to 2010
$4.7M
Expanding the druggable genomeDP1OD006933 · OD · VANDERBILT UNIVERSITY · PI FESIK, STEPHEN W. · 2010 to 2011
$1.5M
NCI NIH HHS RC2 CA148375NIH HHS DP1 OD006933
6 · The paper itself

Abstract

KRAS is one of the most highly validated cancer targets. Here we describe the design and synthesis of two reversible pan-KRAS inhibitors, BI-2865 and BI-2493. From our KRAS

Indexed as

Antineoplastic AgentsProto-Oncogene Proteins p21(ras)Spiro CompoundsAnimalsCell Line, TumorDrug DiscoveryHumansMiceStructure-Activity RelationshipXenograft Model Antitumor AssaysAntineoplastic AgentsKRAS protein, humanProto-Oncogene Proteins p21(ras)Spiro Compounds

Identifiers

PMID40709733
PMCPMC12362595

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.