Development of G Protein-Coupled Receptor 183 Benzimidazole Antagonists Utilizing a Core-Hopping Approach.

Angelina Ellis, Israel Olayide, Vanja Kalajdzic, Daniela Salvemini, Christopher Arnatt

Abstract read

In one paragraph

Article in Molecules (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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0citing papers in PubMed

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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

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3 · Its place in the literature

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0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

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5 · Who and what money

Authors and funding

5 authors.

Angelina EllisDepartment of Chemistry, Saint Louis University, St. Louis, MO 63103, USA.ORCID 0009-0005-4225-9306

Israel OlayideDepartment of Chemistry, Saint Louis University, St. Louis, MO 63103, USA.

Vanja KalajdzicDepartment of Chemistry, Saint Louis University, St. Louis, MO 63103, USA.

Daniela SalveminiDepartment of Chemistry, Saint Louis University, St. Louis, MO 63103, USA.

Christopher ArnattDepartment of Chemistry, Saint Louis University, St. Louis, MO 63103, USA.ORCID 0000-0002-9445-4796

Funding

Uncovering the roles of oxysterols in neuropathic painR01NS128004 · NINDS · SAINT LOUIS UNIVERSITY · PI Christopher K Arnatt, DANIELA SALVEMINI · 2022 to 2026

$2.2M

NINDS NIH HHS R01 NS128004NINDS NIH HHS R01NS128004

6 · The paper itself

Abstract

G protein-coupled receptor 183 (GPR183, EBI2) has emerged as a promising therapeutic target for neuropathic pain due to its role in neuroinflammatory signaling. Previously, our group identified SAE-14 as a potent GPR183 antagonist and lead scaffold for analgesic development. To further explore the structural requirements for receptor antagonism, a ligand-based core-hopping strategy was employed to identify novel chemotypes derived from SAE-14. Virtual screening identified a trisubstituted benzimidazole scaffold as a promising candidate for further investigation. A focused series of benzimidazole analogs was synthesized and evaluated for inhibition of 7α,25-dihydroxycholesterol (7α,25-OHC)-induced GPR183 activation using calcium mobilization assays. Several compounds exhibited potent antagonistic activity, with four analogs demonstrating comparable potency relative to SAE-14. The most active compounds displayed IC

Indexed as

BenzimidazolesReceptors, G-Protein-CoupledAnimalsHumansMolecular StructureStructure-Activity RelationshipbenzimidazoleBenzimidazolesReceptors, G-Protein-Coupledcore-hoppingdrug discoveryG protein-coupled receptorheterocyclic compoundsneuropathic painsmall molecule

Identifiers

PMID42883234

DOI10.3390/molecules31193469

PMCPMC13666532

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.