核激素受体配体
Nuclear hormone receptors (NHRs) are representatives of a large class of proteins within cells. They act as receptors for a wide range of molecules, such as vitamin A-derivative retinoids, steroid and thyroid hormones, and others. Activated by binding of the signal molecule, the ligand–NHR complex changes its conformation and modifies the expression of certain genes by binding to control elements in the DNA. Thus, NHRs play a major role in embryonic development and adult homeostasis. Over 10% of FDA-approved drugs target NHRs as perspective objects in the control of various diseases.
Nuclear Hormone Receptor Ligands Library is composed of 456 small ligands. The collection includes ligands that display all major types of action on NHR targets: agonistic, antagonistic, and inverse agonistic.
Related terms: pregnane X receptor, peroxisome proliferator-activated receptor, estrogen, androgen, farnesoid X receptor, vitamin D
Mechanism of action for class I NHRs(Created by BioRender.com)
Highlights
Dienogest, progesterone receptor agonist
Darolutamide, androgen receptor antagonist
GSK805, ROR-gamma receptor inverse antagonist
Product Features
A set of 456 NHR-binding molecules with sub-10 micromolar activity coefficient values for HTS/HCS programs.
The library is composed of ligands that target all major pharmaceutically relevant NHR targets.
Nuclear Hormone Receptor Ligands Library covers novel promising preclinical lead compounds, clinical candidates and approved drugs.
Calculated structural diversity of the collection: 0.87.
Comprehensive documentation with structures, trivial names, synonyms, activity coefficients values, types of action on target and references to original literature.
NMR and LCMS validated purity.
All the compounds are available in stock for hit follow-up.
The library is continuously updated.
Product Details
Format: 10 - 100 µL of 10 mM DMSO stock solutions; dry powders (1 mg);
Container: 384-well microplates;
Storage: - 18 °C;
Shipping: Dry ice.
Utility
High throughput screening (HTS);
High content screening (HCS);
Cherry picking.
