Evidence map›Paper›PMID 35912476›Full record

ArticleJournal of medicinal chemistry2022

Optimization of Covalent MKK7 Inhibitors

Paul Gehrtz, Shir Marom, Mike Bührmann, Julia Hardick, Silke Kleinbölting, Amit Shraga, Christian Dubiella, Ronen Gabizon, Jan N Wiese, Matthias P Müller and 8 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
1.2field-weighted citation impact, top 24% 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

10 citing papers in PubMed, 13 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Review
  5. Article
  6. Computational Design of Lysine Targeting Covalent Binders Using Rosetta.Journal of chemical information and modeling · 2025
    Article
  7. Review
  8. Article
  9. Article
  10. 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

18 authors at 2 institutions in 2 countries.

Paul GehrtzDepartment of Chemical and Structural Biology, Weizmann Institute of Science, 7610001 Rehovot, Israel.
Shir MaromDepartment of Chemical and Structural Biology, Weizmann Institute of Science, 7610001 Rehovot, Israel.ORCID 0000-0001-8339-7311
Mike BührmannDepartment of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany.
Julia HardickDepartment of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany.
Silke KleinböltingDepartment of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany.
Amit ShragaDepartment of Chemical and Structural Biology, Weizmann Institute of Science, 7610001 Rehovot, Israel.
Christian DubiellaDepartment of Chemical and Structural Biology, Weizmann Institute of Science, 7610001 Rehovot, Israel.
Ronen GabizonDepartment of Chemical and Structural Biology, Weizmann Institute of Science, 7610001 Rehovot, Israel.ORCID 0000-0002-3626-5073
Jan N WieseDepartment of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany.
Matthias P MüllerDepartment of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany.ORCID 0000-0002-1529-8933
Galit CohenThe Nancy and Stephen Grand Israel National Center for Personalized Medicine, Weizmann Institute of Science, 7610001 Rehovot, Israel.
Ilana BabaevThe Nancy and Stephen Grand Israel National Center for Personalized Medicine, Weizmann Institute of Science, 7610001 Rehovot, Israel.
Khriesto ShurrushThe Nancy and Stephen Grand Israel National Center for Personalized Medicine, Weizmann Institute of Science, 7610001 Rehovot, Israel.
Liat AvramDepartment of Chemical Research Support, Weizmann Institute of Science, 7610001 Rehovot, Israel.ORCID 0000-0001-6535-3470
Efrat ResnickDepartment of Chemical and Structural Biology, Weizmann Institute of Science, 7610001 Rehovot, Israel.
Haim BarrThe Nancy and Stephen Grand Israel National Center for Personalized Medicine, Weizmann Institute of Science, 7610001 Rehovot, Israel.
Daniel RauhDepartment of Chemistry and Chemical Biology, TU Dortmund University, Otto-Hahn-Strasse 4a, 44227 Dortmund, Germany.ORCID 0000-0002-1970-7642
Nir LondonDepartment of Chemical and Structural Biology, Weizmann Institute of Science, 7610001 Rehovot, Israel.ORCID 0000-0003-2687-0699
Weizmann Institute of Science · ILTU Dortmund University · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

High-throughput nanomole-scale synthesis allows for late-stage functionalization (LSF) of compounds in an efficient and economical manner. Here, we demonstrated that copper-catalyzed azide-alkyne cycloaddition could be used for the LSF of covalent kinase inhibitors at the nanoscale, enabling the synthesis of hundreds of compounds that did not require purification for biological assay screening, thus reducing experimental time drastically. We generated crude libraries of inhibitors for the kinase MKK7, derived from two different parental precursors, and analyzed them

Indexed as

AlkynesAzidesCycloaddition ReactionHigh-Throughput Screening AssaysMass SpectrometryAlkynesAzides

Identifiers

PMID35912476
PMCPMC9376956
OpenAlexW4288802438

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.