Nuclear Receptor Screening & Profiling Services

IntroductionService OverviewCovered NRs SpectrumApplicationAdvantageContact Us

Introduction

Nuclear receptors (NRs) are ligand-dependent transcription factors that sense lipophilic signals and regulate gene networks controlling metabolism, immunity, proliferation, and differentiation. With the full characterization of the 48 human NRs, understanding of ligand binding, conformational dynamics, co-regulator recruitment, and tissue-specific activity has advanced substantially, establishing NRs as a major drug target class. Approved therapeutics such as glucocorticoids, estrogen modulators, PPAR, and vitamin D receptor ligands demonstrate how precise modulation of NR subtypes or conformational states can dramatically influence efficacy and safety. In early drug discovery, comprehensive evaluation of compound binding affinity, transcriptional activation or repression, co-regulator interactions, and potential off-target effects is therefore essential.

Nuclear Receptor Screening & Profiling Services Figure 1. Nuclear receptors are ligand-activated transcription factors that regulate target gene transcription. (Chen T. 2008)

Service Overview

Creative Biogene's assessment framework centers on the "structure–function relationship." Using a combination of cellular activity assays, transcriptional reporter systems, ligand-competition binding, biochemical co-regulator binding analyses, nuclear translocation monitoring, and cross-subfamily selectivity evaluation, compounds of various types—including full agonists, partial agonists, antagonists, inverse agonists, and tissue-selective modulators—can be systematically and reproducibly profiled. For projects requiring detailed mechanistic insight, complementary differential transcriptomics services are available to further elucidate NR-dependent transcription programs and potential off-target risks.

Mechanism Evaluation

Ligand-binding assays and transcriptional activity measurements are performed in parallel to distinguish antagonists, partial agonists, and selective modulators, enabling rapid clarification of the mechanism of action.

Cell-Based Assays

Stable reporter cell lines quantify transcriptional activation, inhibition, and co-regulator recruitment. For receptors regulated by nuclear translocation, dynamic imaging captures ligand-driven localization changes.

Biochemical Assays

TR-FRET, AlphaScreen, radioligand competition, and co-regulator peptide binding assays provide versatile biochemical platforms for profiling diverse compound types.

HTS and Selectivity

The platform supports high-throughput screening, precise IC₅₀/EC₅₀ analysis, and multi-subtype or multi-species selectivity studies to identify off-target interactions.

For rare or unavailable receptors, custom cell lines or recombinant proteins can be developed to meet specific research needs.

Covered Nuclear Receptor Spectrum

Our platform supports all major NR families, including GR, PR, AR, MR, ER, RAR/RXR, PPAR, VDR, LXR, FXR, PXR/CAR, and additional NR subtypes with undefined endogenous ligands. Each subtype is supported by a complete system for primary screening, dose–response testing, co-regulator interaction profiling, and selectivity assessment.

Applications and Research Utility

Researchers can generate datasets including:

Confirmation-dependent activity profiles for selective agonists or partial agonists
Differential behavior of tissue-selective modulators (e.g., SERM, SEGRM, SARM) across receptors and co-regulator systems
PXR, CAR, and other drug-metabolism-related NR-mediated regulation of CYP, UGT, and ABC transporters for predicting metabolic and tolerance risk
Identification and preliminary functional evaluation of potential ligands for orphan NRs
Comprehensive NR off-target risk assessment for novel compounds

Technical Advantages and Platform Features

Creative Biogene has over a decade of experience in NR drug discovery and screening. Our systems cover critical aspects, including NR conformational dynamics, ligand-binding kinetics, transcriptional activation patterns, and co-regulator selectivity, ensuring consistent data quality, reproducibility, and system compatibility. The team can design customized experimental strategies, including the generation of stable cell lines, the expression of receptor variants, and the development of specific co-regulator-binding systems, allowing complex mechanistic questions to be dissected in controlled models. Automated workflows support large-scale screening while maintaining batch-to-batch consistency.

Our integrated NR product suite—including stable cell lines, recombinant proteins, viral vectors, expression clones, and RNAi/CRISPR tools—supports end-to-end workflows from screening to validation to mechanistic dissection, minimizing variability from system transitions.

Collaboration and Customization

Whether exploring a candidate compound for a specific NR or systematically profiling a series of molecules for receptor selectivity and mechanistic characterization, Creative Biogene's NR screening and functional profiling platform provides a complete experimental infrastructure. Flexible evaluation strategies and mechanism-oriented data support can be tailored to meet research goals. Contact us to discuss project objectives and experimental requirements so that we can design the most suitable experimental pathway.

* For research use only. Not intended for any clinical use.

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NR0B1	NR0B2	NR1A1	NR1A2	NR1B1	NR1B2	NR1B3	NR1C1
NR1C2	NR1C3	NR1D1	NR1D2	NR1F1	NR1F2	NR1F3	NR1H2
NR1H3	NR1H4	NR1H5	NR1I1	NR1I2	NR1I3	NR2A1	NR2A2
NR2B1	NR2B2	NR2B3	NR2C1	NR2C2	NR2E1	NR2E3	NR2F1
NR2F2	NR2F6	NR3A1	NR3A2	NR3B1	NR3B2	NR3B3	NR3C1
NR3C2	NR3C3	NR3C4	NR4A1	NR4A2	NR4A3	NR5A1	NR5A2
NR6A1