Proteins > Nuclear receptor subfamily 1 group I member 2
Page last updated: 2024-08-07 15:27:36
Nuclear receptor subfamily 1 group I member 2
A nuclear receptor subfamily 1 group I member 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O75469]
Synonyms
Orphan nuclear receptor PAR1;
Orphan nuclear receptor PXR;
Pregnane X receptor;
Steroid and xenobiotic receptor;
SXR
Research
Bioassay Publications (36)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 7 (19.44) | 29.6817 |
2010's | 25 (69.44) | 24.3611 |
2020's | 4 (11.11) | 2.80 |
Compounds (86)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
pleconaril | Homo sapiens (human) | EC50 | 0.2512 | 1 | 1 |
aa 861 | Homo sapiens (human) | EC50 | 15.9667 | 3 | 3 |
bithionol | Homo sapiens (human) | EC50 | 6.8000 | 2 | 2 |
chloroxine | Homo sapiens (human) | EC50 | 39.8000 | 1 | 1 |
ciglitazone | Homo sapiens (human) | EC50 | 9.5333 | 3 | 3 |
dimercaprol | Homo sapiens (human) | EC50 | 27.5500 | 2 | 2 |
famprofazone | Homo sapiens (human) | EC50 | 2.7250 | 4 | 4 |
felodipine | Homo sapiens (human) | EC50 | 4.3000 | 3 | 3 |
fenbendazole | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
fentanyl | Homo sapiens (human) | EC50 | 31.6000 | 3 | 3 |
flutrimazole | Homo sapiens (human) | EC50 | 6.1000 | 1 | 1 |
haloprogin | Homo sapiens (human) | EC50 | 10.0000 | 1 | 1 |
loratadine | Homo sapiens (human) | EC50 | 8.9000 | 4 | 4 |
nilvadipine | Homo sapiens (human) | EC50 | 1.5475 | 4 | 4 |
nimodipine | Homo sapiens (human) | EC50 | 0.3900 | 1 | 1 |
nisoldipine | Homo sapiens (human) | EC50 | 10.1667 | 3 | 3 |
oxatomide | Homo sapiens (human) | EC50 | 4.7250 | 4 | 4 |
raloxifene | Homo sapiens (human) | EC50 | 11.7100 | 1 | 1 |
spiroxatrine | Homo sapiens (human) | EC50 | 26.8667 | 3 | 3 |
vorinostat | Homo sapiens (human) | EC50 | 30.3000 | 2 | 2 |
suramin | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
troglitazone | Homo sapiens (human) | EC50 | 15.8000 | 3 | 3 |
ici 204,219 | Homo sapiens (human) | EC50 | 13.7275 | 4 | 4 |
cephaloridine | Homo sapiens (human) | EC50 | 3.2000 | 1 | 1 |
thyroxine | Homo sapiens (human) | EC50 | 55.6000 | 2 | 2 |
berlition | Homo sapiens (human) | EC50 | 2.8000 | 1 | 1 |
methylprednisolone | Homo sapiens (human) | EC50 | 12.6000 | 1 | 1 |
fluorometholone | Homo sapiens (human) | EC50 | 5.7000 | 3 | 3 |
2-tert-butylhydroquinone | Homo sapiens (human) | EC50 | 7.3000 | 2 | 2 |
dronabinol | Homo sapiens (human) | EC50 | 18.9333 | 3 | 3 |
dinaline | Homo sapiens (human) | EC50 | 28.2000 | 1 | 1 |
colforsin | Homo sapiens (human) | EC50 | 6.3500 | 4 | 4 |
amlodipine besylate | Homo sapiens (human) | EC50 | 30.4667 | 3 | 3 |
proadifen hydrochloride | Homo sapiens (human) | EC50 | 17.2667 | 3 | 3 |
bumecain | Homo sapiens (human) | EC50 | 6.0250 | 4 | 4 |
spiramide | Homo sapiens (human) | EC50 | 31.6000 | 1 | 1 |
ryodipine | Homo sapiens (human) | EC50 | 6.5667 | 3 | 3 |
droxidopa | Homo sapiens (human) | EC50 | 1.6020 | 2 | 2 |
fulvestrant | Homo sapiens (human) | EC50 | 1.9500 | 1 | 1 |
bosentan anhydrous | Homo sapiens (human) | EC50 | 11.8667 | 3 | 3 |
nbi 27914 | Homo sapiens (human) | EC50 | 4.9500 | 1 | 1 |
demecolcine | Homo sapiens (human) | EC50 | 13.3500 | 2 | 2 |
testosterone isocaproate | Homo sapiens (human) | EC50 | 23.6667 | 3 | 3 |
ritonavir | Homo sapiens (human) | EC50 | 4.0000 | 1 | 1 |
terconazole | Homo sapiens (human) | EC50 | 11.5000 | 2 | 2 |
tacrolimus | Homo sapiens (human) | EC50 | 5.0000 | 1 | 1 |
sr 12813 | Homo sapiens (human) | EC50 | 0.1933 | 3 | 3 |
5,11-diethyl-5,6,11,12-tetrahydrochrysene-2,8-diol | Homo sapiens (human) | EC50 | 8.6000 | 1 | 1 |
t0901317 | Homo sapiens (human) | EC50 | 0.0684 | 8 | 8 |
epothilone b | Homo sapiens (human) | EC50 | 22.1000 | 2 | 2 |
diclazuril | Homo sapiens (human) | EC50 | 25.0000 | 3 | 3 |
triiodothyronine, reverse | Homo sapiens (human) | EC50 | 12.6000 | 1 | 1 |
zeranol | Homo sapiens (human) | EC50 | 17.6000 | 3 | 3 |
orlistat | Homo sapiens (human) | EC50 | 14.9000 | 2 | 2 |
jhw 015 | Homo sapiens (human) | EC50 | 2.6400 | 1 | 1 |
alpha-linolenic acid | Homo sapiens (human) | EC50 | 1.2510 | 2 | 2 |
sirolimus | Homo sapiens (human) | EC50 | 5.4450 | 2 | 2 |
desoximetasone | Homo sapiens (human) | EC50 | 31.6000 | 1 | 1 |
rimexolone | Homo sapiens (human) | EC50 | 2.1250 | 4 | 4 |
indinavir sulfate | Homo sapiens (human) | EC50 | 14.9500 | 2 | 2 |
lasalocid sodium | Homo sapiens (human) | EC50 | 11.7000 | 2 | 2 |
rifaximin | Homo sapiens (human) | EC50 | 9.1200 | 5 | 5 |
pregna-4,17-diene-3,16-dione | Homo sapiens (human) | EC50 | 2.5000 | 1 | 1 |
lu 208075 | Homo sapiens (human) | EC50 | 31.6000 | 2 | 2 |
6-(4-chlorophenyl)imidazo(2,1-b)(1,3)thiazole-5-carbaldehyde o-(3,4-dichlorobenzyl)oxime | Homo sapiens (human) | EC50 | 0.9900 | 1 | 1 |
trans-delta-tocotrienoloic acid | Homo sapiens (human) | EC50 | 1.3000 | 1 | 1 |
trans-delta-tocotrienoloic acid | Homo sapiens (human) | Kd | 0.3300 | 1 | 1 |
anacetrapib | Homo sapiens (human) | EC50 | 3.9000 | 1 | 1 |
tianeptine | Homo sapiens (human) | EC50 | 25.4333 | 3 | 3 |
dabrafenib | Homo sapiens (human) | EC50 | 0.0871 | 2 | 2 |
mk-7246 | Homo sapiens (human) | EC50 | 30.0000 | 1 | 1 |
bms-911543 | Homo sapiens (human) | EC50 | 50.0000 | 1 | 1 |
methacycline monohydrochloride | Homo sapiens (human) | EC50 | 7.9000 | 2 | 2 |
rifampin | Homo sapiens (human) | EC50 | 2.1656 | 9 | 9 |
febantel | Homo sapiens (human) | EC50 | 12.9000 | 2 | 2 |
thiamet g | Homo sapiens (human) | EC50 | 30.0000 | 1 | 1 |
Drugs with Other Measurements
Discovery of 3α,7α,11β-Trihydroxy-6α-ethyl-5β-cholan-24-oic Acid (TC-100), a Novel Bile Acid as Potent and Highly Selective FXR Agonist for Enterohepatic Disorders.Journal of medicinal chemistry, , Oct-13, Volume: 59, Issue:19, 2016
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 24, Issue:22, 2014
Identification of clinically used drugs that activate pregnane X receptors.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 39, Issue:1, 2011
[no title available]Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Garcinoic Acid Is a Natural and Selective Agonist of Pregnane X Receptor.Journal of medicinal chemistry, , 04-09, Volume: 63, Issue:7, 2020
Exploiting Chemical Toolboxes for the Expedited Generation of Tetracyclic Quinolines as a Novel Class of PXR Agonists.ACS medicinal chemistry letters, , Apr-11, Volume: 10, Issue:4, 2019
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 28, Issue:2, 2018
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).Journal of medicinal chemistry, , Jul-24, Volume: 57, Issue:14, 2014
Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 23, Issue:24, 2013
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.Bioorganic & medicinal chemistry, , Mar-01, Volume: 15, Issue:5, 2007
Diethylstilbestrol-scaffold-based pregnane X receptor modulators.European journal of medicinal chemistry, , Oct-20, Volume: 103, 2015
Insights on pregnane-X-receptor modulation. Natural and semisynthetic steroids from Theonella marine sponges.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
Total synthesis and pharmacological characterization of solomonsterol A, a potent marine pregnane-X-receptor agonist endowed with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-14, Volume: 54, Issue:13, 2011
Identification of clinically used drugs that activate pregnane X receptors.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 39, Issue:1, 2011
Dissecting the allosteric FXR modulation: a chemical biology approach using guggulsterone as a chemical tool.MedChemComm, , Aug-01, Volume: 10, Issue:8, 2019
Is antagonism of E/Z-guggulsterone at the farnesoid X receptor mediated by a noncanonical binding site? A molecular modeling study.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
[no title available]Journal of medicinal chemistry, , 02-11, Volume: 64, Issue:3, 2021
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.Journal of medicinal chemistry, , 05-26, Volume: 59, Issue:10, 2016
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 26, Issue:7, 2016
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.Journal of medicinal chemistry, , Apr-26, Volume: 55, Issue:8, 2012
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 21, Issue:20, 2011
Identification of clinically used drugs that activate pregnane X receptors.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 39, Issue:1, 2011
Enables
This protein enables 9 target(s):
Target | Category | Definition |
RNA polymerase II transcription regulatory region sequence-specific DNA binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls the transcription of a gene or cistron by RNA polymerase II. [GOC:txnOH] |
DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
DNA-binding transcription activator activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that activates or increases transcription of specific gene sets transcribed by RNA polymerase II. [GOC:aruk, GOC:txnOH-2018, PMID:20737563, PMID:27145859] |
nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
nuclear receptor binding | molecular function | Binding to a nuclear receptor protein. Nuclear receptor proteins are DNA-binding transcription factors which are regulated by binding to a ligand. [PMID:7776974] |
sequence-specific double-stranded DNA binding | molecular function | Binding to double-stranded DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA, e.g. promotor binding or rDNA binding. [GOC:dos, GOC:sl] |
RNA polymerase II cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018] |
Located In
This protein is located in 3 target(s):
Target | Category | Definition |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
nuclear body | cellular component | Extra-nucleolar nuclear domains usually visualized by confocal microscopy and fluorescent antibodies to specific proteins. [GOC:ma, PMID:10330182] |
intermediate filament cytoskeleton | cellular component | Cytoskeletal structure made from intermediate filaments, typically organized in the cytosol as an extended system that stretches from the nuclear envelope to the plasma membrane. Some intermediate filaments run parallel to the cell surface, while others traverse the cytosol; together they form an internal framework that helps support the shape and resilience of the cell. [ISBN:0716731363] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 2 target(s):
Target | Category | Definition |
transcription regulator complex | cellular component | A protein complex that is capable of associating with DNA by direct binding, or via other DNA-binding proteins or complexes, and regulating transcription. [GOC:jl] |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
Involved In
This protein is involved in 12 target(s):
Target | Category | Definition |
regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
xenobiotic metabolic process | biological process | The chemical reactions and pathways involving a xenobiotic compound, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:cab2, GOC:krc] |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
steroid metabolic process | biological process | The chemical reactions and pathways involving steroids, compounds with a 1,2,cyclopentanoperhydrophenanthrene nucleus. [ISBN:0198547684] |
positive regulation of gene expression | biological process | Any process that increases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
intracellular receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to a receptor located within a cell. [GOC:bf, GOC:mah] |
xenobiotic catabolic process | biological process | The chemical reactions and pathways resulting in the breakdown of a xenobiotic compound, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
xenobiotic transport | biological process | The directed movement of a xenobiotic into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. A xenobiotic is a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:go_curators, GOC:krc] |
positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
cell differentiation | biological process | The cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732] |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |