Evidence map›Paper›PMID 34613724›Full record

ArticleJournal of medicinal chemistry2021

Discovery of EEDi-5273 as an Exceptionally Potent and Orally Efficacious EED Inhibitor Capable of Achieving Complete and Persistent Tumor Regression.

Rohan Kalyan Rej, Changwei Wang, Jianfeng Lu, Mi Wang, Elyse Petrunak, Kaitlin P Zawacki, Donna McEachern, Chao-Yie Yang, Lu Wang, Ruiting Li and 8 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
1.6field-weighted citation impact, top 16% 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

9 citing papers in PubMed, 26 citations in OpenAlex.

  1. Review
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  6. Article
  7. The roles of EZH2 in cancer and its inhibitors.Medical oncology (Northwood, London, England) · 2023
    Review
  8. Review
  9. Know when to fold 'em: Polycomb complexes in oncogenic 3D genome regulation.Frontiers in cell and developmental biology · 2022
    Review
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 1 country.

Rohan Kalyan Rej
Changwei Wang
Jianfeng Lu
Mi Wang
Elyse Petrunak
Kaitlin P Zawacki
Donna McEachern
Chao-Yie YangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID 0000-0002-5445-0109
Lu Wang
Ruiting Li
Krishnapriya Chinnaswamy
Bo Wen
Jeanne A Stuckey
Yunlong ZhouAscentage Pharma Group, Suzhou, Jiangsu 215216, China.
Jianyong ChenAscentage Pharma Group, Suzhou, Jiangsu 215216, China.
Guozhi TangAscentage Pharma Group, Suzhou, Jiangsu 215216, China.
University of Michigan · USUniversity of Tennessee Health Science Center · US

Funding

XenograftP30CA046592 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI THEODORE S LAWRENCE · 1988 to 2026
$178.2M
NCI NIH HHS P30 CA046592
6 · The paper itself

Abstract

Embryonic ectoderm development (EED) is a promising therapeutic target for human cancers and other diseases. We report herein the discovery of exceptionally potent and efficacious EED inhibitors. By conformational restriction of a previously reported EED inhibitor, we obtained a potent lead compound. Further optimization of the lead yielded exceptionally potent EED inhibitors. The best compound EEDi-5273 binds to EED with an IC

Indexed as

Administration, OralAntineoplastic AgentsHumansNeoplasmsStructure-Activity RelationshipAntineoplastic Agents

Identifiers

PMID34613724
PMCPMC8862192
OpenAlexW3204721296

What OpenQuestion holds

Textmetadata
LicenceTDM
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.