Evidence map›Paper›PMID 30143422›Full record

ArticleBioorganic & medicinal chemistry letters2018

Identification of potent RORβ modulators: Scaffold variation.

Christelle Doebelin, Rémi Patouret, Ruben D Garcia-Ordonez, Mi Ra Chang, Venkatasubramanian Dharmarajan, Scott Novick, Anthony Ciesla, Sean Campbell, Laura A Solt, Patrick R Griffin and 1 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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

11 authors.

Christelle DoebelinThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
Rémi PatouretThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
Ruben D Garcia-OrdonezThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
Mi Ra ChangThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
Venkatasubramanian DharmarajanThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
Scott NovickThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
Anthony CieslaThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
Sean CampbellThe Scripps Research Institute, Scripps Florida, Department of Immunology and Microbiology, 130 Scripps Way #C2A, Jupiter, FL 33458, USA.
Laura A SoltThe Scripps Research Institute, Scripps Florida, Department of Immunology and Microbiology, 130 Scripps Way #C2A, Jupiter, FL 33458, USA.
Patrick R GriffinThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA.
Theodore M KameneckaThe Scripps Research Institute, Scripps Florida, Department of Molecular Medicine, 130 Scripps Way #A2A, Jupiter, FL 33458, USA. Electronic address: kameneck@scripps.edu.

Funding

Development of RORbeta-selective modulators as in vivo probesR01MH108173 · NIMH · SCRIPPS FLORIDA · PI GRIFFIN, PATRICK ROBERT, KAMENECKA, THEODORE M · 2015 to 2017
$1.4M
NIMH NIH HHS R01 MH108173
6 · The paper itself

Abstract

We sought to develop RORβ-selective probe molecules in order to investigate the function of the receptor in vitro and in vivo and its role in the pathophysiology of disease. To accomplish this, we modified a potent dual RORβ/RORγ inverse agonist from the primary literature with the goal of improving selectivity for RORβ vs RORγ. Truncation of the Western portion of the molecule ablated activity at RORγ and led to a potent series of RORβ modulators. Continued exploration of this series investigated alternate replacement cores for the aminothiazole ring. Numerous suitable replacements were found during the course of our SAR investigations and are reported herein.

Indexed as

HumansMass SpectrometryNuclear Receptor Subfamily 1, Group F, Member 2ThiophenesNuclear Receptor Subfamily 1, Group F, Member 2RORB protein, humanThiophenesAminothiopheneNuclear receptorRORβSelective ligand

Identifiers

PMID30143422
PMCPMC6238650

What OpenQuestion holds

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Registered trials

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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.