Evidence map›Paper›PMID 38116446›Full record

ArticleACS medicinal chemistry letters2023

Discovery of 5-Azaquinoxaline Derivatives as Potent and Orally Bioavailable Allosteric SHP2 Inhibitors.

Mohamed S A Elsayed, James F Blake, Mark L Boys, Eric Brown, Bruno D Chapsal, Mark J Chicarelli, Adam W Cook, Jay B Fell, John P Fischer, Lauren Hanson and 12 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2023. 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
0.8field-weighted citation impact, top 26% 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

2 citing papers in PubMed, 5 citations in OpenAlex.

  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

22 authors at 1 institution in 1 country.

Mohamed S A ElsayedMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.ORCID https://orcid.org/0000-0002-1353-7259
James F BlakeComputational Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Mark L BoysMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Eric BrownPharmacology, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Bruno D ChapsalMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Mark J ChicarelliMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Adam W CookMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Jay B FellMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.ORCID https://orcid.org/0000-0002-5770-1225
John P FischerMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Lauren HansonEnzymology, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Christine LemieuxCellular Biology, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Matthew C MartinsonEnzymology, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Joseph McCownADME Sciences, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Oren T McNultyMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Macedonio J MejiaMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Nickolas A NeitzelDMPK, Pfizer-Boulder, Boulder, Colorado 80301, United States.ORCID https://orcid.org/0009-0000-6786-1890
Jennifer N OttenADME Sciences, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Martha E RodriguezMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Daniel WilcoxMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Christina E WongMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Yeyun ZhouStructural Biology, Pfizer-Boulder, Boulder, Colorado 80301, United States.
Ronald J HinklinMedicinal Chemistry, Pfizer-Boulder, Boulder, Colorado 80301, United States.ORCID https://orcid.org/0000-0003-2494-5888
Pfizer (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

SHP2 has emerged as an important target for oncology small-molecule drug discovery. As a nonreceptor tyrosine phosphatase within the MAPK pathway, it has been shown to control cell growth, differentiation, and oncogenic transformation. We used structure-based design to find a novel class of potent and orally bioavailable SHP2 inhibitors. Our efforts led to the discovery of the 5-azaquinoxaline as a new core for developing this class of compounds. Optimization of the potency and properties of this scaffold generated compound

Identifiers

PMID38116446
PMCPMC10726463
OpenAlexW4388696054

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.