Evidence map›Paper›PMID 36793423›Full record

ArticleACS medicinal chemistry letters2023

Macrocyclic Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonists.

Mark E Schnute, John I Trujillo, Katherine L Lee, Ray Unwalla, Felix F Vajdos, Björn Kauppi, Philippe Nuhant, Andrew C Flick, Kimberly K Crouse, Yajuan Zhao and 7 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
0.7field-weighted citation impact, top 29% 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, 4 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

17 authors at 2 institutions in 2 countries.

Mark E SchnuteMedicine Design, Pfizer Inc., Cambridge, Massachusetts 02139, United States.ORCID https://orcid.org/0000-0003-3075-4578
John I TrujilloMedicine Design, Pfizer Inc., Groton, Connecticut 06340, United States.ORCID https://orcid.org/0000-0003-2303-0256
Katherine L LeeMedicine Design, Pfizer Inc., Cambridge, Massachusetts 02139, United States.ORCID https://orcid.org/0000-0003-0155-290X
Ray UnwallaMedicine Design, Pfizer Inc., Cambridge, Massachusetts 02139, United States.
Felix F VajdosMedicine Design, Pfizer Inc., Groton, Connecticut 06340, United States.
Björn KauppiKaro Pharma AB, 111 48 Stockholm, Sweden.ORCID https://orcid.org/0000-0002-2813-5180
Philippe NuhantMedicine Design, Pfizer Inc., Groton, Connecticut 06340, United States.
Andrew C FlickMedicine Design, Pfizer Inc., Groton, Connecticut 06340, United States.
Kimberly K CrouseInflammation and Immunology Research, Pfizer Inc., Cambridge, Massachusetts 02139, United States.
Yajuan ZhaoInflammation and Immunology Research, Pfizer Inc., Cambridge, Massachusetts 02139, United States.
Amanda SamuelDrug Product Design, Pfizer Inc., San Diego, California 92121, United States.
Vincent LombardoMedicine Design, Pfizer Inc., Groton, Connecticut 06340, United States.
Alexandria P TaylorMedicine Design, Pfizer Inc., Groton, Connecticut 06340, United States.
Amy L BraultMedicine Design, Pfizer Inc., Groton, Connecticut 06340, United States.
John D KnafelsMedicine Design, Pfizer Inc., Groton, Connecticut 06340, United States.
Michael L VazquezMedicine Design, Pfizer Inc., Cambridge, Massachusetts 02139, United States.
Gabriel BersteinInflammation and Immunology Research, Pfizer Inc., Cambridge, Massachusetts 02139, United States.
Pfizer (United States) · USKaro Pharma (Sweden) · SE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Macrocyclic retinoic acid receptor-related orphan receptor C2 (RORC2) inverse agonists have been designed with favorable properties for topical administration. Inspired by the unanticipated bound conformation of an acyclic sulfonamide-based RORC2 ligand from cocrystal structure analysis, macrocyclic linker connections between the halves of the molecule were explored. Further optimization of analogues was accomplished to maximize potency and refine physiochemical properties (MW, lipophilicity) best suited for topical application. Compound

Identifiers

PMID36793423
PMCPMC9923832
OpenAlexW4317352832

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.