Evidence map›Paper›PMID 40864607›Full record

ArticleJournal of medicinal chemistry2025

Discovery of Macrocyclic Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors that Demonstrate Potent Cellular Efficacy and In Vivo Activity in a Mouse Solid Tumor Xenograft Model.

James C Tarr, Kyuok Jeon, Nagarathanam Veerasamy, Martin Aichinger, James M Salovich, Bin Zhao, John L Sensintaffar, Heribert Arnhof, Tobias Wunberg, Danielle Sgubin and 14 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 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. HFGuidedDesign:Chemical science · 2026
    Article
  2. Review
  3. 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

24 authors.

James C TarrDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Kyuok JeonDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Nagarathanam VeerasamyDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Martin AichingerDiscovery Research, Boehringer Ingelheim Regional Center Vienna GmbH & Co KG, Vienna 1120, Austria.
James M SalovichDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Bin ZhaoDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
John L SensintaffarDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Heribert ArnhofDiscovery Research, Boehringer Ingelheim Regional Center Vienna GmbH & Co KG, Vienna 1120, Austria.
Tobias WunbergDiscovery Research, Boehringer Ingelheim Regional Center Vienna GmbH & Co KG, Vienna 1120, Austria.
Danielle SgubinDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Allison ArnoldDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Rakesh H VekariyaDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0001-8292-9793
Plamen P ChristovMolecular Design and Synthesis Center, Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37323-0146, United States.
Kwangho KimMolecular Design and Synthesis Center, Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37323-0146, United States.
Julian Emanuel FuchsDiscovery Research, Boehringer Ingelheim Regional Center Vienna GmbH & Co KG, Vienna 1120, Austria.
Pol KarierChemical Development Germany, Boehringer Ingelheim Pharma GmbH & Co. KG, Birkendorfer Straße 65, Biberach an der Riß 88397, Germany.
Bodo BetzemeierChemical Development Germany, Boehringer Ingelheim Pharma GmbH & Co. KG, Birkendorfer Straße 65, Biberach an der Riß 88397, Germany.
Mayme Van MeverenDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Nagaraju MiriyalaDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0002-1265-738X
Edward T OlejniczakDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Harald EngelhardtDiscovery Research, Boehringer Ingelheim Regional Center Vienna GmbH & Co KG, Vienna 1120, Austria.ORCID 0000-0001-8170-1893
Taekyu LeeDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.
Darryl McConnellDiscovery Research, Boehringer Ingelheim Regional Center Vienna GmbH & Co KG, Vienna 1120, Austria.
Stephen W FesikDepartment of Biochemistry, Vanderbilt University School of Medicine, 2215 Garland Avenue, 607 Light Hall, Nashville, Tennessee 37232-0146, United States.ORCID 0000-0001-5957-6192

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The B cell lymphoma 2 (Bcl-2) family of proteins are key regulators of intrinsic apoptosis. The antiapoptotic protein myeloid cell leukemia 1 (Mcl-1), which is associated with high tumor grade, poor survival, and resistance to treatment, has emerged as a promising candidate for treating hematological and solid cancers. Herein, we report the structure-guided design of small molecule macrocyclic Mcl-1 inhibitors based on the (

Indexed as

Antineoplastic AgentsMacrocyclic CompoundsMyeloid Cell Leukemia Sequence 1 ProteinAnimalsCell Line, TumorCell ProliferationDrug DiscoveryHumansMiceMice, NudeStructure-Activity RelationshipXenograft Model Antitumor AssaysAntineoplastic AgentsMacrocyclic CompoundsMyeloid Cell Leukemia Sequence 1 Protein

Identifiers

PMID40864607
PMCPMC12434668

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.