Evidence map›Paper›PMID 40236540›Full record

ArticleACS medicinal chemistry letters2025

Discovery of a Series of Covalent Ligands That Bind to Cys77 of the Von Hippel-Lindau Tumor Suppressor Protein (VHL).

Simon C C Lucas, Yong Xu, Sarah Hewitt, Gavin W Collie, Lucia Fusani, Ganesh Kadamur, Thomas E Hadfield, Nancy Su, Caroline Truman, Sylvain Demanze and 2 more

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Article
  2. 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

12 authors.

Simon C C LucasHit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.ORCID https://orcid.org/0000-0002-9172-8739
Yong XuAssays, Profiling and Cell Sciences, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.
Sarah HewittAssays, Profiling and Cell Sciences, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.
Gavin W CollieProtein, Structure and Biophysics, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.ORCID https://orcid.org/0000-0002-0406-922X
Lucia FusaniHit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.
Ganesh KadamurAssays, Profiling and Cell Sciences, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.ORCID https://orcid.org/0000-0002-7019-1485
Thomas E HadfieldHit Discovery, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.
Nancy SuAssays, Profiling and Cell Sciences, Discovery Sciences, R&D, AstraZeneca, Waltham, Massachusetts 02451, United States.
Caroline TrumanAssays, Profiling and Cell Sciences, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.
Sylvain DemanzeMedicinal Chemistry, Oncology R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.ORCID https://orcid.org/0000-0003-4533-6280
Haie HaoPharmaron Beijing Co. Ltd., Beijing, 100176, P. R. China.
Christopher PhillipsProtein, Structure and Biophysics, Discovery Sciences, R&D, AstraZeneca, Cambridge, CB2 0AA, U.K.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Most ligands for the Von Hippel-Lindau tumor suppressor (VHL) bind at the HIF-1α binding site. Ligands that bind to allosteric sites on VHL could be highly valuable for the field of protein degradation, therefore, a covalent hit identification campaign was run targeting Cys77 on VHL. Hit

Identifiers

PMID40236540
PMCPMC11995237

What OpenQuestion holds

Textmetadata
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.