Evidence map›Paper›PMID 37849537›Full record

ArticleACS medicinal chemistry letters2023

Design of Next-Generation DGAT2 Inhibitor PF-07202954 with Longer Predicted Half-Life.

Kevin J Filipski, David J Edmonds, Michelle R Garnsey, Daniel J Smaltz, Karen Coffman, Kentaro Futatsugi, Jack Lee, Steven V O'Neil, Ann Wright, Deane Nason and 10 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 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.6field-weighted citation impact, top 32% 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

1 citing paper in PubMed, 3 citations in OpenAlex.

  1. 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

20 authors at 1 institution in 1 country.

Kevin J FilipskiPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.ORCID https://orcid.org/0000-0003-0845-5723
David J EdmondsPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.ORCID https://orcid.org/0000-0001-9234-8618
Michelle R GarnseyPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.ORCID https://orcid.org/0000-0003-1226-1868
Daniel J SmaltzPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Karen CoffmanPfizer Research & Development, 558 Eastern Point Road, Groton, Connecticut 06340, United States.
Kentaro FutatsugiPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Jack LeePfizer Research & Development, 558 Eastern Point Road, Groton, Connecticut 06340, United States.ORCID https://orcid.org/0000-0003-0477-8568
Steven V O'NeilPfizer Research & Development, 558 Eastern Point Road, Groton, Connecticut 06340, United States.
Ann WrightPfizer Research & Development, 558 Eastern Point Road, Groton, Connecticut 06340, United States.
Deane NasonPfizer Research & Development, 558 Eastern Point Road, Groton, Connecticut 06340, United States.
James R GossetPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Christine C OrozcoPfizer Research & Development, 558 Eastern Point Road, Groton, Connecticut 06340, United States.ORCID https://orcid.org/0009-0001-4971-5491
Dan BlacklerPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Guila FakhouryPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Jemy A GutierrezPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Sylvie PerezPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Trenton RossPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Ingrid StockPfizer Research & Development, 558 Eastern Point Road, Groton, Connecticut 06340, United States.
Gregory TeszPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Robert DulleaPfizer Research & Development, 1 Portland Street, Cambridge, Massachusetts 02139, United States.
Pfizer (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Diacylglycerol O-acyltransferase 2 (DGAT2) inhibitors have been shown to lower liver triglyceride content and are being explored clinically as a treatment for non-alcoholic steatohepatitis (NASH). This work details efforts to find an extended-half-life DGAT2 inhibitor. A basic moiety was added to a known inhibitor template, and the basicity and lipophilicity were fine-tuned by the addition of electrophilic fluorines. A weakly basic profile was required to find an appropriate balance of potency, clearance, and permeability. This work culminated in the discovery of PF-07202954 (

Identifiers

PMID37849537
PMCPMC10577701
OpenAlexW4387245423

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.