Evidence map›Paper›PMID 42441922›Full record

ArticleJournal of medicinal chemistry2026

Riding toward Selectivity: Optimization of Covalent 7-Azaindole-Based BMX Kinase Inhibitors.

Xiaojun Julia Liang, Claudia Albertini, Thales Kronenberger, Ekaterina Shevchenko, Alexander Rasch, Benedict-Tilman Berger, Martin Schwalm, Lena Marie Berger, Andreas Krämer, Ricardo A M Serafim and 8 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

18 authors.

Xiaojun Julia LiangDepartment for Medicinal Chemistry, Institute for Biomedical Engineering, Faculty of Medicine, University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.
Claudia AlbertiniDepartment of Pharmaceutical/Medicinal Chemistry, Institute of Pharmaceutical Sciences, Faculty of Sciences, University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.
Thales KronenbergerDepartment of Pharmaceutical/Medicinal Chemistry, Institute of Pharmaceutical Sciences, Faculty of Sciences, University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.ORCID 0000-0001-6933-7590
Ekaterina ShevchenkoDepartment of Pharmaceutical/Medicinal Chemistry, Institute of Pharmaceutical Sciences, Faculty of Sciences, University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.
Alexander RaschDepartment of Pharmaceutical/Medicinal Chemistry, Institute of Pharmaceutical Sciences, Faculty of Sciences, University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.
Benedict-Tilman BergerStructural Genomics Consortium, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany.ORCID 0000-0002-3314-2617
Martin SchwalmStructural Genomics Consortium, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany.ORCID 0000-0002-1252-1829
Lena Marie BergerStructural Genomics Consortium, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany.
Andreas KrämerStructural Genomics Consortium, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany.
Ricardo A M SerafimDepartment for Medicinal Chemistry, Institute for Biomedical Engineering, Faculty of Medicine, University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.ORCID 0000-0003-0614-1798
Michael ForsterCluster of Excellence iFIT (EXC 2180) 'Image-Guided & Functionally Instructed Tumor Therapies', University of Tübingen, 72076 Tübingen, Germany.ORCID 0009-0008-7446-3733
Apirat ChaikuadStructural Genomics Consortium, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany.ORCID 0000-0003-1120-2209
Maria Laura BolognesiDepartment of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy.ORCID 0000-0002-1289-5361
Susanne MüllerStructural Genomics Consortium, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany.ORCID 0000-0003-2402-4157
Antti PosoCluster of Excellence iFIT (EXC 2180) 'Image-Guided & Functionally Instructed Tumor Therapies', University of Tübingen, 72076 Tübingen, Germany.ORCID 0000-0003-4196-4204
Stefan LauferCluster of Excellence iFIT (EXC 2180) 'Image-Guided & Functionally Instructed Tumor Therapies', University of Tübingen, 72076 Tübingen, Germany.ORCID 0000-0001-6952-1486
Stefan KnappStructural Genomics Consortium, Goethe University Frankfurt, Buchmann Institute for Molecular Life Sciences, Max-von-Laue-Straße 15, 60438 Frankfurt am Main, Germany.ORCID 0000-0001-5995-6494
Matthias GehringerDepartment for Medicinal Chemistry, Institute for Biomedical Engineering, Faculty of Medicine, University of Tübingen, Auf der Morgenstelle 8, 72076 Tübingen, Germany.ORCID 0000-0003-0163-3419

Funding

Wellcome Trust
6 · The paper itself

Abstract

The tyrosine kinase expressed in hepatocellular carcinoma (TEC) family comprises five nonreceptor tyrosine kinases─BTK, ITK, BMX, TXK, and TEC─with key roles in immune signaling. Although BTK and ITK have been extensively studied, selective inhibitors for TEC, TXK, and BMX remain scarce. Recently, we identified 7-azaindole-based covalent BMX inhibitors with potent inhibitory activity and robust cellular target engagement but limited selectivity across TEC family members, especially BTK. Here, we describe a new generation of BMX inhibitors designed to exploit subtle structural differences between BMX and BTK by incorporating diverse

Indexed as

IndolesProtein Kinase InhibitorsAnimalsHumansProtein-Tyrosine KinasesStructure-Activity RelationshipTyrosine Kinase Inhibitors7-azaindole dimerIndolesProtein Kinase InhibitorsProtein-Tyrosine KinasesTyrosine Kinase Inhibitors

Identifiers

PMID42441922
PMCPMC13403314

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.