ArticleChemistry & biology2012
Firefly luciferase in chemical biology: a compendium of inhibitors, mechanistic evaluation of chemotypes, and suggested use as a reporter.
Article in Chemistry & biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 63 papers.
What it found
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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.
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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.
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Who cites it
63 citing papers in PubMed, 137 citations in OpenAlex.
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- Pharmacodynamics of Akt drugs revealed by a kinase-modulated bioluminescent indicator.Nature chemical biology · 2025Article
- A general assay platform to study protein pharmacology using ligand-dependent structural dynamics.Nature communications · 2025Article
- A highly sensitive screening system to evaluate the reversibility of neuroendocrine prostate cancer to prostate adenocarcinoma.Cancer medicine · 2025Article
- A Putative Frizzled 7-Targeting Compound Acts as a Firefly Luciferase Inhibitor.Journal of medicinal chemistry · 2024Article
- Combining crystallographic and binding affinity data towards a novel dataset of small molecule overlays.Journal of computer-aided molecular design · 2024Article
- ChemFH: an integrated tool for screening frequent false positives in chemical biology and drug discovery.Nucleic acids research · 2024Article
- High-Throughput Methods for the Discovery of Small Molecule Modulators of Pancreatic Beta-Cell Function and Regeneration.Assay and drug development technologies · 2024Review
- Kinase-Modulated Bioluminescent Indicators Enable Noninvasive Imaging of Drug Activity in the Brain.ACS central science · 2023Article
- qHTSWaterfall: 3-dimensional visualization software for quantitative high-throughput screening (qHTS) data.Journal of cheminformatics · 2023Article
- Multiplexed bioluminescence imaging with a substrate unmixing platform.Cell chemical biology · 2022Article
- A reactive oxygen species CaThe New phytologist · 2022Article
- Luciferase assay system to monitor fibroblast growth factor signal disruption in human iPSCs.STAR protocols · 2022Article
- Development of a High-Throughput Screening Assay for Small-Molecule Inhibitors of Androgen Receptor Splice Variants.Assay and drug development technologies · 2022Article
- Structure-Based Design of a Chemical Probe Set for the 5-HTJournal of medicinal chemistry · 2022Article
- Accounting for Artifacts in High-Throughput Toxicity Assays.Methods in molecular biology (Clifton, N.J.) · 2022Article
- A practical guide to large-scale docking.Nature protocols · 2021Review
- Genome-Edited Coincidence and PMP22-HiBiT Fusion Reporter Cell Lines Enable an Artifact-Suppressive Quantitative High-Throughput Screening Strategy forACS pharmacology & translational science · 2021Article
3 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 3 institutions in 1 country.
Funding
Abstract
Firefly luciferase (FLuc) is frequently used as a reporter in high-throughput screening assays, owing to the exceptional sensitivity, dynamic range, and rapid measurement that bioluminescence affords. However, interaction of small molecules with FLuc has, to some extent, confounded its use in chemical biology and drug discovery. To identify and characterize chemotypes interacting with FLuc, we determined potency values for 360,864 compounds found in the NIH Molecular Libraries Small Molecule Repository, available in PubChem. FLuc inhibitory activity was observed for 12% of this library with discernible SAR. Characterization of 151 inhibitors demonstrated a variety of inhibition modes, including FLuc-catalyzed formation of multisubstrate adduct enzyme inhibitor complexes. As in some cell-based FLuc reporter assays, compounds acting as FLuc inhibitors yield paradoxical luminescence increases, thus data on compounds acquired from FLuc-dependent assays require careful analysis as described here.
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Registered trials
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.