Evidence map›Paper›PMID 36646172›Full record

ArticleSLAS discovery : advancing life sciences R & D2023

High throughput screening for drugs that inhibit 3C-like protease in SARS-CoV-2.

Emery Smith, Meredith E Davis-Gardner, Ruben D Garcia-Ordonez, Tu-Trinh Nguyen, Mitchell Hull, Emily Chen, Xuerong Yu, Thomas D Bannister, Pierre Baillargeon, Louis Scampavia and 3 more

Open access · diamondAbstract read
In one paragraph

Article in SLAS discovery : advancing life sciences R & D, 2023. 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
2.8field-weighted citation impact, top 8% 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, 14 citations in OpenAlex.

  1. A Novel Fluorescence Polarization Binding Assay for the Main Protease (MACS pharmacology & translational science · 2025
    Article
  2. High throughput screening for SARS-CoV-2 inhibitors targeting 5 helix bundle.SLAS discovery : advancing life sciences R & D · 2025
    Article
  3. Article
  4. Rapid luminescence-based screening method for SARS- CoV-2 inhibitors discovery.SLAS discovery : advancing life sciences R & D · 2025
    Article
  5. SARS-CoV-2 MSLAS discovery : advancing life sciences R & D · 2024
    Article
  6. Review
  7. Article
  8. Review
  9. Article
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

13 authors at 3 institutions in 1 country.

Emery SmithDepartment of Molecular Medicine, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Meredith E Davis-GardnerImmunology and Microbiology, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Ruben D Garcia-OrdonezDepartment of Molecular Medicine, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Tu-Trinh NguyenCalibr at Scripps Research, La Jolla, CA 92037, United States.
Mitchell HullCalibr at Scripps Research, La Jolla, CA 92037, United States.
Emily ChenCalibr at Scripps Research, La Jolla, CA 92037, United States.
Xuerong YuDepartment of Chemistry, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Thomas D BannisterDepartment of Chemistry, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Pierre BaillargeonDepartment of Molecular Medicine, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Louis ScampaviaDepartment of Molecular Medicine, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Patrick GriffinDepartment of Molecular Medicine, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Michael FarzanImmunology and Microbiology, UF Scripps Biomedical Research, Jupiter, FL 33458, United States.
Timothy P SpicerDepartment of Molecular Medicine, UF Scripps Biomedical Research, Jupiter, FL 33458, United States. Electronic address: spicert@ufl.edu.
Scripps (United States) · USScripps Institution of Oceanography · USScripps Research Institute · US

Funding

Project 5: Pandemic Virus Helicase InhibitorsU19AI171954 · NIAID · UNIVERSITY OF MINNESOTA · PI Donghoon Chung · 2022 to 2026
$100.9M
Integrated Acoustic Transfer System for HTS Library ManagementS10OD025279 · OD · SCRIPPS FLORIDA · PI SCAMPAVIA, LOUIS DANIEL · 2018 to 2018
$624k
Tandem Multi-modal Plate Readers for a High Throughput Screening platformS10OD030330 · OD · UNIVERSITY OF FLORIDA · PI SCAMPAVIA, LOUIS DANIEL · 2021 to 2021
$600k
HTS Drug  Discovery DispensersS10OD026857 · OD · SCRIPPS FLORIDA · PI SCAMPAVIA, LOUIS DANIEL · 2019 to 2019
$452k
MaxCyte Scalable Transfection SystemS10OD032248 · OD · UNIVERSITY OF FLORIDA · PI SPICER, TIMOTHY PATRICK · 2022 to 2022
$105k
NIAID NIH HHS U19 AI171954NIH HHS S10 OD025279NIH HHS S10 OD026857NIH HHS S10 OD030330NIH HHS S10 OD032248
6 · The paper itself

Abstract

The SARS coronavirus 2 (SARS-CoV-2) pandemic remains a major problem in many parts of the world and infection rates remain at extremely high levels. This high prevalence drives the continued emergence of new variants, and possibly ones that are more vaccine-resistant and that can drive infections even in highly vaccinated populations. The high rate of variant evolution makes clear the need for new therapeutics that can be clinically applied to minimize or eliminate the effects of COVID-19. With a hurdle of 10 years, on average, for first in class small molecule therapeutics to achieve FDA approval, the fastest way to identify therapeutics is by drug repurposing. To this end, we developed a high throughput cell-based screen that incorporates the essential viral 3C-like protease and its peptide cleavage site into a luciferase complementation assay to evaluate the efficacy of known drugs encompassing approximately 15,000 clinical-stage or FDA-approved small molecules. Confirmed inhibitors were also tested to determine their cytotoxic properties. Medicinal chemistry efforts to optimize the hits identified Tranilast as a potential lead. Here, we report the rapid screening and identification of potentially relevant drugs that exhibit selective inhibition of the SARS-CoV-2 viral 3C-like protease.

Indexed as

COVID-19SARS-CoV-2Cysteine EndopeptidasesHigh-Throughput Screening AssaysHumansPeptide HydrolasesProtease InhibitorsCysteine EndopeptidasesPeptide HydrolasesProtease Inhibitors3CL-PROCell-basedCOVID-19HTSM-PROPL-PRO

Identifiers

PMID36646172
PMCPMC9839384
OpenAlexW4316019896

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.