TargetOxysterols receptor LXR-beta/Retinoic acid receptor RXR-alpha(Human)
Sun Yat-Sen University
Curated by ChEMBL
Sun Yat-Sen University
Curated by ChEMBL
Affinity DataEC50: 0.228nMAssay Description:Agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assayMore data for this Ligand-Target Pair
3D Structure (crystal)TargetOxysterols receptor LXR-alpha/Retinoic acid receptor RXR-alpha(Human)
Sun Yat-Sen University
Curated by ChEMBL
Sun Yat-Sen University
Curated by ChEMBL
Affinity DataEC50: 0.401nMAssay Description:Agonist activity at human RXRalpha/LXRalpha expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 1.5nMAssay Description:Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alphaMore data for this Ligand-Target Pair
Affinity DataKd: 1.5nMAssay Description:Dissociation constant for Retinoid X receptor alphaMore data for this Ligand-Target Pair
Affinity DataKi: 2.20nMAssay Description:Binding affinity to recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as inhibitory constant incubated for 30 mins by f...More data for this Ligand-Target Pair
Affinity DataKi: 2.20nMAssay Description:Displacement of hyodeoxycholicacid-based fluorescent tracer from recombinant human LXRbeta LBD (215 to 461 residues) expressed in Escherichia coli BL...More data for this Ligand-Target Pair
Affinity DataKd: 3nMAssay Description:Inhibition of binding to human Retinoic acid receptor RXR DEF domainMore data for this Ligand-Target Pair
Affinity DataEC50: 4nMAssay Description:Agonist activity at human RXR-alphaMore data for this Ligand-Target Pair
Affinity DataEC50: 5nMAssay Description:Binding to human LXRbetaMore data for this Ligand-Target Pair
Affinity DataEC50: 6nMAssay Description:Agonist activity at human RXR-alpha expressed in U2OS cells by PathHunter assayMore data for this Ligand-Target Pair
Affinity DataEC50: 6nMAssay Description:Effective concentration against Retinoic acid receptor RXR-alphaMore data for this Ligand-Target Pair
Affinity DataIC50: 7.90nMAssay Description:Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 8nMAssay Description:Inhibition of [3H]targretin binding to Retinoid X receptor RXR alphaMore data for this Ligand-Target Pair
Affinity DataKd: 8nMAssay Description:Transcriptional activation in CV-1 cells expressing human Retinoid X receptor RXR-alphaMore data for this Ligand-Target Pair
Affinity DataKd: 8nMAssay Description:Inhibition of [3H]-9-cis RA binding to Retinoid X receptor RXR gammaMore data for this Ligand-Target Pair
Affinity DataKi: 8.40nMAssay Description:Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR alphaMore data for this Ligand-Target Pair
Affinity DataKd: 9nMAssay Description:Compound was tested for functional activity in CV-1 cells transfected with an expression vector for retinoid X receptor alpha using transactivation a...More data for this Ligand-Target Pair
Affinity DataEC50: 10nMAssay Description:Agonist activity at human RXRalpha expressed in HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataIC50: 12nM EC50: 310nMpH: 7.4 T: 2°CAssay Description:Binding reaction was initiated by adding a dilution series of test compound in tracer solution to LXR-coated flash plates. Each concentration of test...More data for this Ligand-Target Pair
Affinity DataIC50: 12nM EC50: 410nMpH: 7.4 T: 2°CAssay Description:Binding reaction was initiated by adding a dilution series of test compound in tracer solution to LXR-coated flash plates. Each concentration of test...More data for this Ligand-Target Pair
Affinity DataKi: 12nMAssay Description:Agonistic activity towards retinoid X receptor-alphaMore data for this Ligand-Target Pair
Affinity DataKd: 13nMAssay Description:Inhibition of [3H]9-cis-retinoic acid binding to baculovirus expressed retinoic acid receptor RXR-alphaMore data for this Ligand-Target Pair
Affinity DataEC50: 13nMAssay Description:Transcriptional activation for RXR alpha receptorMore data for this Ligand-Target Pair
Affinity DataEC50: 13nMAssay Description:Transcriptional activation of Retinoid X receptor RXR alphaMore data for this Ligand-Target Pair
Affinity DataEC50: 13nMAssay Description:Effective concentration against RXR-alpha receptorMore data for this Ligand-Target Pair
Affinity DataKd: 14nMAssay Description:Binding affinity to human RXR-alpha-ligand binding domain homodimers by fluorescence quenching methodMore data for this Ligand-Target Pair
Affinity DataKd: 16nMAssay Description:Binding affinity to human RXRalpha LBD (T225 to T462 residues) by fluorescence quenching assayMore data for this Ligand-Target Pair
Affinity DataEC50: 20nMpH: 7.5 T: 2°CAssay Description:The LXR LiSA measures the ligand-dependent recruitment of a 25 amino acid fragment of the steroid receptor coactivator 1 (SRC1) to the ligand-binding...More data for this Ligand-Target Pair
Affinity DataIC50: 23nMAssay Description:SPA assays were run in displacement mode using 30 nM [3H]-GW3965. Ligands were tested in 12-point dose-response curves starting at 20 uM. IC50 values...More data for this Ligand-Target Pair
Affinity DataEC50: 25nMpH: 7.5 T: 2°CAssay Description:The LXR LiSA measures the ligand-dependent recruitment of a 25 amino acid fragment of the steroid receptor coactivator 1 (SRC1) to the ligand-binding...More data for this Ligand-Target Pair
Affinity DataEC50: 26nMAssay Description:Agonist activity at RXRalpha-LBD (unknown origin) assessed as transactivation by measuring increase in fluorescein-labelled coactivator PGC-1alpha pe...More data for this Ligand-Target Pair
Affinity DataEC50: 27nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
Affinity DataIC50: 29nMAssay Description:Inhibition of [3H]9-cis-retinoic acid binding to human retinoid X receptor alpha ligand-binding domain expressed in Escherichia coliMore data for this Ligand-Target Pair
Affinity DataIC50: 30nMAssay Description:Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRbeta ligand binding domainMore data for this Ligand-Target Pair
Affinity DataKd: 32nMAssay Description:Dissociation constant for binding to Retinoid X receptor alphaMore data for this Ligand-Target Pair
Affinity DataIC50: 32nMAssay Description:Binding affinity against retinoic Acid X alpha receptor using [3H]- -9-cis-Retinoic Acid in competitive binding assayMore data for this Ligand-Target Pair
Affinity DataEC50: 35nMAssay Description:Polyhistidine-tagged human LXR ligand-binding domain was mixed with the test compound, biotin-SRC1 peptide, streptavidin-allophycocyanin, and europiu...More data for this Ligand-Target Pair
Affinity DataEC50: 40nMAssay Description:As used herein, reference to the activity of an LXR agonist at LXRα and LXRβ refer to the activity as measured using the ligand sensing ass...More data for this Ligand-Target Pair
Affinity DataIC50: 40nMAssay Description:Antagonist activity at LXRbeta ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cel...More data for this Ligand-Target Pair
Affinity DataEC50: 40nMAssay Description:Agonist activity at human LXRbeta assessed as association of SRC1 to LXRbeta ligand binding domain by FRET based cell-free ligand sensing assayMore data for this Ligand-Target Pair
Affinity DataEC50: 40nMAssay Description:As used herein, reference to the activity of an LXR agonist at LXRα and LXRβ refer to the activity as measured using the ligand sensing ass...More data for this Ligand-Target Pair
Affinity DataKd: 50nMAssay Description:Dissociation constant for binding to Retinoic acid receptor RXR-alphaMore data for this Ligand-Target Pair
Affinity DataEC50: 78nMAssay Description:Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assayMore data for this Ligand-Target Pair
Affinity DataIC50: 82nMAssay Description:Inhibition of [3H]-ATRA binding to mouse Retinoic acid receptor RXR alphaMore data for this Ligand-Target Pair
Affinity DataEC50: 100nMAssay Description:Binding affinity against retinoic Acid X alpha receptors co-transfected into CV-1 cellsMore data for this Ligand-Target Pair
Affinity DataEC50: 100nMAssay Description:Transcriptional activation of Retinoid X receptor RXR alphaMore data for this Ligand-Target Pair
Affinity DataEC50: 100nMAssay Description:Agonist activity for retinoic acid receptor RXR alpha in transcriptional activation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 110nMAssay Description:Agonist activity at RXR-alpha in rat R3KE cells infected with oncogene KLF4-ER assessed as inhibition of KLF4-mediated oncogenic transformationMore data for this Ligand-Target Pair
Affinity DataEC50: 120nMAssay Description:Agonist activity at RXRalpha in rat RK3E cells assessed as transcriptional activation by luciferase reporter gene assayMore data for this Ligand-Target Pair
