bexarotene [Ligand Id: 2807] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1023 (Bexarotene, LG-100069, LG100069, LGD-1069, LGD1069, NSC-747528, Targretin, Targretine)
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  • Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
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  • Retinoid X receptor-α/Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2/Retinoic acid receptor RXR-alpha in Human [ChEMBL: CHEMBL3885613] [GtoPdb: 610630] [UniProtKB: P19793P43354]
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  • Retinoic acid receptor-α/Retinoic acid receptor alpha in Human [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
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  • Retinoic acid receptor-β/Retinoic acid receptor beta in Human [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
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  • Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
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  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
  • Retinoid X receptor-α/Retinoid X receptor alpha in Mouse [ChEMBL: CHEMBL3084] [GtoPdb: 610] [UniProtKB: P28700]
  • Retinoid X receptor-α/Retinoid X receptor alpha in Rat [ChEMBL: CHEMBL4431] [GtoPdb: 610] [UniProtKB: Q05343]
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  • Retinoid X receptor-β/Retinoid X receptor beta in Human [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
  • Retinoid X receptor-β/Retinoid X receptor beta in Mouse [ChEMBL: CHEMBL4047] [GtoPdb: 611] [UniProtKB: P28704]
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  • Retinoid X receptor-γ/Retinoid X receptor gamma in Human [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
  • Retinoid X receptor-γ/Retinoid X receptor gamma in Mouse [ChEMBL: CHEMBL4402] [GtoPdb: 612] [UniProtKB: P28705]
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  • Retinoid X receptor-α/Peroxisome proliferator-activated receptor-γ/RXR alpha/PPAR gamma in Human [ChEMBL: CHEMBL2111394] [GtoPdb: 610595] [UniProtKB: P19793P37231]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP26A1/Cytochrome P450 26A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5141] [GtoPdb: 1366] [UniProtKB: O43174]
ChEMBL Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase B 4.87 pIC50 13500 nM IC50 J Med Chem (2016) 59: 2579-2595 [PMID:26918322]
CYP26B1/Cytochrome P450 26B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3713687] [GtoPdb: 1367] [UniProtKB: Q9NR63]
ChEMBL Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase B 5.23 pIC50 5900 nM IC50 J Med Chem (2016) 59: 2579-2595 [PMID:26918322]
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
ChEMBL Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay B 6.71 pEC50 196 nM EC50 Bioorg Med Chem Lett (2017) 27: 1193-1198 [PMID:28169169]
Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055]
ChEMBL Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay B 6.36 pEC50 434 nM EC50 Bioorg Med Chem Lett (2017) 27: 1193-1198 [PMID:28169169]
Retinoid X receptor-α/Nuclear receptor related 1/Nuclear receptor subfamily 4 group A member 2/Retinoic acid receptor RXR-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3885613] [GtoPdb: 610630] [UniProtKB: P19793P43354]
GtoPdb - - 7.4 pIC50 - - - Curr Pharm Des (2000) 6: 25-58 [PMID:10637371];
J Med Chem (1999) 42: 742-50 [PMID:10052980];
J Med Chem (1994) 37: 2930-41 [PMID:8071941]
ChEMBL Agonist activity at Renilla luciferase/GFP2-tagged RXRalpha/Nurr1 (unknown origin) expressed in HEK293T cells by BRET2 assay B 8 pEC50 10 nM EC50 J Med Chem (2016) 59: 1232-1238 [PMID:26820900]
ChEMBL Inhibition of Nurr1-RXRalpha in HEK293T cells by BRET assay B 8.3 pEC50 5.01 nM EC50 J Med Chem (2021) 64: 9592-9638 [PMID:34251209]
Retinoic acid receptor-α/Retinoic acid receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2055] [GtoPdb: 590] [UniProtKB: P10276]
ChEMBL Inhibition of [3H]-ATRA binding to baculovirus expressed retinoid receptor RAR alpha B 6 pKd >1000 nM Kd J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Inhibition of [3H]ATRA binding to baculovirus expressed Retinoic acid receptor RAR alpha B 5.26 pKi 5453 nM Ki J Med Chem (1999) 42: 742-750 [PMID:10052980]
ChEMBL Inhibition of [3H]ATRA binding to RAR alpha receptor B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (1997) 7: 2747-2752
ChEMBL Inhibition of [3H]ATRA binding to retinoic acid receptor RAR alpha B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (1997) 7: 2393-2398
ChEMBL Selective activity towards retinoic acid receptor-alpha B 6.74 pKi 180 nM Ki J Med Chem (1997) 40: 4222-4234 [PMID:9435893]
ChEMBL Effective concentration against retinoid receptor isoform (RAR alpha) expressed in CV-1 cells B 5 pEC50 >10000 nM EC50 J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Agonist activity at RARaplha (unknown origin) B 5 pEC50 >10000 nM EC50 J Med Chem (2018) 61: 2166-2210 [PMID:28850227]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR alpha F 8.22 pEC50 6 nM EC50 J Med Chem (1999) 42: 742-750 [PMID:10052980]
Retinoic acid receptor-β/Retinoic acid receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2008] [GtoPdb: 591] [UniProtKB: P10826]
ChEMBL Inhibition of [3H]ATRA binding to baculovirus expressed retinoid receptor RAR beta B 6 pKd >1000 nM Kd J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Inhibition of [3H]ATRA binding to baculovirus expressed Retinoic acid receptor RAR beta B 5.27 pKi 5353 nM Ki J Med Chem (1999) 42: 742-750 [PMID:10052980]
ChEMBL Inhibition of [3H]ATRA binding to RAR beta receptor B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (1997) 7: 2747-2752
ChEMBL Inhibition of [3H]ATRA binding to retinoic acid receptor RAR beta B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (1997) 7: 2393-2398
ChEMBL Binding affinity towards cRAR-beta-2 receptor by displacing 1.1 nM 3[H]-9-cis-RA B 6.1 pKi >800 nM Ki Bioorg Med Chem Lett (1997) 7: 2313-2318
ChEMBL Binding affinity towards cRAR-beta-2 receptor by displacing 0.82 nM 3[H]all-trans-RA B 6.26 pKi >550 nM Ki Bioorg Med Chem Lett (1997) 7: 2313-2318
ChEMBL Selective activity towards retinoic acid receptor-beta B 7.3 pKi 50 nM Ki J Med Chem (1997) 40: 4222-4234 [PMID:9435893]
ChEMBL Effective concentration against retinoid receptor isoform (RAR beta) expressed in CV-1 cells B 5 pEC50 >10000 nM EC50 J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Agonist activity at RARbeta (unknown origin) B 5 pEC50 >10000 nM EC50 J Med Chem (2018) 61: 2166-2210 [PMID:28850227]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR beta F 6.55 pEC50 282 nM EC50 J Med Chem (1999) 42: 742-750 [PMID:10052980]
Retinoic acid receptor-γ/Retinoic acid receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2003] [GtoPdb: 592] [UniProtKB: P13631]
ChEMBL Tested for binding affinity against [3H]-ATRA binding to retinoid receptor isoform (RAR gamma) expressed in baculovirus B 6 pKd >1000 nM Kd J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Inhibition of [3H]-ATRA binding to baculovirus expressed Retinoic acid receptor RAR gamma B 5.49 pKi 3206 nM Ki J Med Chem (1999) 42: 742-750 [PMID:10052980]
ChEMBL Inhibition of [3H]ATRA binding to RAR gamma receptor B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (1997) 7: 2747-2752
ChEMBL Inhibition of [3H]-ATRA binding to Retinoic acid receptor RAR gamma B 6 pKi >1000 nM Ki Bioorg Med Chem Lett (1997) 7: 2393-2398
ChEMBL Selective activity towards retinoic acid receptor-gamma B 6.89 pKi 130 nM Ki J Med Chem (1997) 40: 4222-4234 [PMID:9435893]
ChEMBL Effective concentration against retinoid receptor isoform (RAR gamma) expressed in CV-1 cells B 5 pEC50 >10000 nM EC50 J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Agonist activity at RARgamma (unknown origin) B 5 pEC50 >10000 nM EC50 J Med Chem (2018) 61: 2166-2210 [PMID:28850227]
ChEMBL Transcriptional activation in CV-1 cells expressing Retinoic acid receptor RAR gamma F 6.19 pEC50 648 nM EC50 J Med Chem (1999) 42: 742-750 [PMID:10052980]
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
ChEMBL Agonist activity at human RXR-alpha-ligand binding domain homodimers assessed as coactivator recruitment by measuring GRIP1 binding to receptor by isothermal titration calorimetry B 5.72 pKd 1890 nM Kd J Med Chem (2014) 57: 5370-5380 [PMID:24801499]
ChEMBL Binding affinity to human RXRalpha LBD after 15 mins by isothermal titration calorimetry assay B 5.8 pKd 1590 nM Kd J Med Chem (2015) 58: 7763-7774 [PMID:26331194]
ChEMBL Binding affinity to recombinant RXRalpha (unknown origin) by isothermal titration calorimetry B 6.68 pKd 210 nM Kd J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL Dissociation constant for binding to Retinoic acid receptor RXR-alpha B 7.44 pKd 36 nM Kd Bioorg Med Chem Lett (2002) 12: 2607-2609 [PMID:12182871]
ChEMBL Ability to bind directly to Retinoic acid receptor RXR-alpha was evaluated in a competitive binding assay. B 7.44 pKd 36 nM Kd J Med Chem (1995) 38: 3146-3155 [PMID:7636877]
ChEMBL Binding affinity to human RXRalpha ligand binding domain by fluorescence assay B 7.59 pKd 26 nM Kd Bioorg Med Chem (2014) 22: 178-185 [PMID:24359708]
ChEMBL Binding affinity to human RXR-alpha-ligand binding domain homodimers by fluorescence quenching method B 7.59 pKd 26 nM Kd J Med Chem (2014) 57: 5370-5380 [PMID:24801499]
ChEMBL Inhibition of [3H]9-cis-RA binding to baculovirus expressed retinoid receptor RXR alpha B 7.85 pKd 14 nM Kd J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Displacement of CU-6PMN from human RXRalpha LBD incubated for 2 hrs by fluorescence based assay B 6.42 pKi 379 nM Ki J Med Chem (2019) 62: 8809-8818 [PMID:31483660]
ChEMBL Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr in presence of compound by fluorescence polarization assay B 6.46 pKi 350 nM Ki ACS Med Chem Lett (2021) 12: 1024-1029 [PMID:34141088]
ChEMBL Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr in presence of compound by [3H]9-Cis retinoic acid assay B 6.7 pKi 201 nM Ki ACS Med Chem Lett (2021) 12: 1024-1029 [PMID:34141088]
ChEMBL Displacement of 9-cis-[11,12-3H]-retinoic acid from human RXRalpha LBD incubated for overnight by scintillation counting method B 6.82 pKi 150 nM Ki J Med Chem (2019) 62: 8809-8818 [PMID:31483660]
ChEMBL Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-alpha in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay B 7.44 pKi 36 nM Ki J Med Chem (1999) 42: 742-750 [PMID:10052980]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR alpha B 7.44 pKi 36 nM Ki Bioorg Med Chem Lett (1997) 7: 2393-2398
ChEMBL Displacement of [3H]9-cis-retinoic acid form human RXRalpha expressed in human Caco-2 cells after 16 hrs B 7.68 pKi 21 nM Ki J Med Chem (2009) 52: 5950-5966 [PMID:19791803]
ChEMBL Selective activity towards retinoid X receptor-alpha B 7.8 pKi 16 nM Ki J Med Chem (1997) 40: 4222-4234 [PMID:9435893]
ChEMBL Inhibition of [3H]9-cis-RA binding to RXR alpha receptor B 7.85 pKi 14 nM Ki Bioorg Med Chem Lett (1997) 7: 2747-2752
ChEMBL Binding affinity to human RXRalpha-LBD (224 to 462 residues) expressed in Escherichia coli BL21(DE3) incubated for 1 hr in presence of compound by fluorescence polarization assay B 6.2 pIC50 632 nM IC50 ACS Med Chem Lett (2021) 12: 1024-1029 [PMID:34141088]
GtoPdb - - 7.4 pIC50 - - - Curr Pharm Des (2000) 6: 25-58 [PMID:10637371];
J Med Chem (1999) 42: 742-50 [PMID:10052980];
J Med Chem (1994) 37: 2930-41 [PMID:8071941]
ChEMBL Transactivation of human RXRalpha transfected in human 293 cells after 48 hrs by dual-luciferase reporter gene assay B 6.83 pEC50 149 nM EC50 Bioorg Med Chem Lett (2013) 23: 3891-3895 [PMID:23707260]
ChEMBL Agonist activity at RXRalpha LBD (unknown origin) expressed in CV1 cells B 6.93 pEC50 118 nM EC50 J Med Chem (2015) 58: 7763-7774 [PMID:26331194]
ChEMBL Agonist activity at human recombinant Gal4-tagged RXRalpha expressed in human Caco-2 cells assessed as receptor homodimerization after 24 hrs by mammalian two hybrid assay F 7.28 pEC50 52 nM EC50 J Med Chem (2009) 52: 5950-5966 [PMID:19791803]
ChEMBL Effective concentration against Retinoic acid receptor RXR-alpha B 7.38 pEC50 42 nM EC50 J Med Chem (1995) 38: 3368-3383 [PMID:7650690]
ChEMBL Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay B 7.4 pEC50 40 nM EC50 J Med Chem (2014) 57: 5370-5380 [PMID:24801499]
ChEMBL Effective concentration against retinoid receptor isoform (RXR alpha) expressed in CV-1 cells B 7.48 pEC50 33 nM EC50 J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Agonist activity at RXRalpha (unknown origin) B 7.48 pEC50 33 nM EC50 J Med Chem (2021) 64: 9592-9638 [PMID:34251209]
ChEMBL Agonist activity RXRalpha (unknown origin) B 7.48 pEC50 33 nM EC50 J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL Agonist activity at human RXRalpha expressed in African green monkey CV1 cells B 7.48 pEC50 33 nM EC50 Medchemcomm (2018) 9: 1289-1292 [PMID:30151082]
ChEMBL Agonist activity at RXRaplha (unknown origin) B 7.48 pEC50 33 nM EC50 J Med Chem (2018) 61: 2166-2210 [PMID:28850227]
ChEMBL Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha F 7.48 pEC50 33 nM EC50 Bioorg Med Chem Lett (1997) 7: 2747-2752
ChEMBL Inhibition of RXRalpha in HEK293T cells by BRET assay B 7.5 pEC50 31.62 nM EC50 J Med Chem (2021) 64: 9592-9638 [PMID:34251209]
ChEMBL Agonist activity at histidine-tagged ligand binding domain of human RXRalpha expressed in Escherichia coli BL21 (DE3) by luciferase reporter gene assay B 7.5 pEC50 31.62 nM EC50 J Med Chem (2016) 59: 1232-1238 [PMID:26820900]
ChEMBL Agonist activity at Renilla luciferase/GFP2-tagged RXRalpha homodimer (unknown origin) expressed in HEK293T cells by BRET2 assay B 7.5 pEC50 31.62 nM EC50 J Med Chem (2016) 59: 1232-1238 [PMID:26820900]
ChEMBL Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-alpha F 7.55 pEC50 28 nM EC50 J Med Chem (1999) 42: 742-750 [PMID:10052980]
ChEMBL Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR alpha F 7.55 pEC50 28 nM EC50 Bioorg Med Chem Lett (1997) 7: 2393-2398
ChEMBL Ability to activate gene expression at Retinoic acid receptor RXR-alpha was evaluated in a cotransfection assay. B 7.55 pEC50 28 nM EC50 J Med Chem (1995) 38: 3146-3155 [PMID:7636877]
ChEMBL Agonist activity at human RXRalpha LBD expressed in African green monkey COS1 cells incubated for 24 hrs by luciferase reporter gene assay B 7.66 pEC50 22 nM EC50 J Med Chem (2019) 62: 8809-8818 [PMID:31483660]
ChEMBL Agonist activity at human RXRalpha expressed in African green monkey COS1 cells harboring CRBP2-tk-luc reporter incubated for 18 hrs by steady-glo luciferase reporter gene assay B 7.7 pEC50 20 nM EC50 Bioorg Med Chem Lett (2019) 29: 1891-1894 [PMID:31160175]
ChEMBL Agonist activity at RXRalpha (unknown origin) expressed in COS1 cells incubated for 18 hrs by luciferase reporter gene assay B 7.7 pEC50 20 nM EC50 ACS Med Chem Lett (2015) 6: 334-338 [PMID:25815156]
ChEMBL Agonist activity at RXRalpha transfected in human COS1 cells after 18 hrs by luciferase reporter gene transactivation assay F 7.7 pEC50 20 nM EC50 ACS Med Chem Lett (2010) 1: 521-525 [PMID:24900241]
ChEMBL Agonist activity at RXRalpha by luciferase reporter gene assay F 7.7 pEC50 19.8 nM EC50 Bioorg Med Chem Lett (2010) 20: 5139-5142 [PMID:20656484]
ChEMBL Agonist activity at human RXRalpha LBD by cell based luciferase reporter gene assay F 8.57 pEC50 2.7 nM EC50 J Med Chem (2011) 54: 788-808 [PMID:21218783]
Retinoid X receptor-α/Retinoid X receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3084] [GtoPdb: 610] [UniProtKB: P28700]
ChEMBL Transactivation of Gal4-LBD fused mouse RXRalpha (218 to 467) transfected in african green monkey CV1 cells assessed as luciferase activity at after 6 hrs by Dual-light chemiluminescent assay B 7.4 pEC50 40 nM EC50 Eur J Med Chem (2009) 44: 2434-2446 [PMID:19216008]
Retinoid X receptor-α/Retinoid X receptor alpha in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4431] [GtoPdb: 610] [UniProtKB: Q05343]
ChEMBL Agonist activity at RXRalpha in rat RK3E cells assessed as transcriptional activation by luciferase reporter gene assay B 7.4 pEC50 40 nM EC50 Bioorg Med Chem (2014) 22: 178-185 [PMID:24359708]
Retinoid X receptor-β/Retinoid X receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1870] [GtoPdb: 611] [UniProtKB: P28702]
ChEMBL Inhibition of [3H]9-cis-RA binding to RXR beta receptor B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (1997) 7: 2747-2752
ChEMBL Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-beta in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay B 7.68 pKi 21 nM Ki J Med Chem (1999) 42: 742-750 [PMID:10052980]
ChEMBL Selective activity towards retinoid X receptor-beta B 8.23 pKi 5.9 nM Ki J Med Chem (1997) 40: 4222-4234 [PMID:9435893]
GtoPdb - - 7.7 pIC50 - - - Curr Pharm Des (2000) 6: 25-58 [PMID:10637371];
J Med Chem (1999) 42: 742-50 [PMID:10052980];
J Med Chem (1994) 37: 2930-41 [PMID:8071941]
ChEMBL Effective concentrations against Retinoic acid receptor RXR-beta B 6.95 pEC50 112 nM EC50 J Med Chem (1995) 38: 3368-3383 [PMID:7650690]
ChEMBL Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-beta F 7.6 pEC50 25 nM EC50 J Med Chem (1999) 42: 742-750 [PMID:10052980]
ChEMBL Agonist activity at human RXRbeta expressed in African green monkey CV1 cells B 7.62 pEC50 24 nM EC50 Medchemcomm (2018) 9: 1289-1292 [PMID:30151082]
ChEMBL Agonist activity RXRbeta (unknown origin) B 7.62 pEC50 24 nM EC50 J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL Agonist activity at RXRbeta (unknown origin) B 7.62 pEC50 24 nM EC50 J Med Chem (2021) 64: 9592-9638 [PMID:34251209]
ChEMBL Agonist activity at RXRbeta (unknown origin) B 7.62 pEC50 24 nM EC50 J Med Chem (2018) 61: 2166-2210 [PMID:28850227]
ChEMBL Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta F 7.62 pEC50 24 nM EC50 Bioorg Med Chem Lett (1997) 7: 2747-2752
Retinoid X receptor-β/Retinoid X receptor beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4047] [GtoPdb: 611] [UniProtKB: P28704]
ChEMBL Binding affinity to Retinoic acid receptor RXR-beta was determined in a competitive binding assay. B 7.68 pKd 21 nM Kd J Med Chem (1995) 38: 3146-3155 [PMID:7636877]
ChEMBL Inhibition of [3H]9-cis-RA binding to baculovirus expressed retinoid receptor RXR beta B 7.68 pKd 21 nM Kd J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Inhibition of [3H]-9-cis-RA binding to Retinoid X receptor RXR beta B 7.68 pKi 21 nM Ki Bioorg Med Chem Lett (1997) 7: 2393-2398
ChEMBL Ability to activate gene expression at Retinoic acid receptor RXR-beta was evaluated in a cotransfection assay. B 7.6 pEC50 25 nM EC50 J Med Chem (1995) 38: 3146-3155 [PMID:7636877]
ChEMBL Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR beta F 7.6 pEC50 25 nM EC50 Bioorg Med Chem Lett (1997) 7: 2393-2398
ChEMBL Effective concentration against retinoid receptor isoform (RXR beta) expressed in CV-1 cells B 7.62 pEC50 24 nM EC50 J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
Retinoid X receptor-γ/Retinoid X receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2004] [GtoPdb: 612] [UniProtKB: P48443]
ChEMBL Binding affinity towards Retinoic acid receptor RXR-gamma B 7.12 pKi 75 nM Ki Bioorg Med Chem Lett (1997) 7: 2313-2318
ChEMBL Inhibition of [3H]9-cis-RA binding to RXR gamma receptor B 7.54 pKi 29 nM Ki Bioorg Med Chem Lett (1997) 7: 2747-2752
ChEMBL Binding affinity towards recombinantly expressed Retinoic acid receptor RXR-gamma in baculoviral system, by using 5 nM [3H]targretin in a competitive binding assay B 7.54 pKi 29 nM Ki J Med Chem (1999) 42: 742-750 [PMID:10052980]
ChEMBL Selective activity towards retinoid X receptor-gamma B 8.08 pKi 8.3 nM Ki J Med Chem (1997) 40: 4222-4234 [PMID:9435893]
GtoPdb - - 7.54 pIC50 - - - Curr Pharm Des (2000) 6: 25-58 [PMID:10637371];
J Med Chem (1999) 42: 742-50 [PMID:10052980];
J Med Chem (1994) 37: 2930-41 [PMID:8071941]
ChEMBL Effective concentrations against Retinoic acid receptor RXR-gamma B 6.91 pEC50 122 nM EC50 J Med Chem (1995) 38: 3368-3383 [PMID:7650690]
ChEMBL Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma F 7.6 pEC50 25 nM EC50 Bioorg Med Chem Lett (1997) 7: 2747-2752
ChEMBL Agonist activity at RXRgamma (unknown origin) B 7.6 pEC50 25 nM EC50 J Med Chem (2018) 61: 2166-2210 [PMID:28850227]
ChEMBL Agonist activity at RXRgamma (unknown origin) B 7.6 pEC50 25 nM EC50 J Med Chem (2021) 64: 9592-9638 [PMID:34251209]
ChEMBL Agonist activity at human RXRgamma expressed in African green monkey CV1 cells B 7.6 pEC50 25 nM EC50 Medchemcomm (2018) 9: 1289-1292 [PMID:30151082]
ChEMBL Agonist activity RXRgamma (unknown origin) B 7.6 pEC50 25 nM EC50 J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL Transcriptional activity was evaluated in CV-1 cells transfected with expression vector for Retinoic acid receptor RXR-gamma F 7.7 pEC50 20 nM EC50 J Med Chem (1999) 42: 742-750 [PMID:10052980]
Retinoid X receptor-γ/Retinoid X receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4402] [GtoPdb: 612] [UniProtKB: P28705]
ChEMBL Binding affinity to Retinoic acid receptor RXR-gamma was evaluated in a competitive binding assay. B 7.54 pKd 29 nM Kd J Med Chem (1995) 38: 3146-3155 [PMID:7636877]
ChEMBL Inhibition of [3H]9-cis-RA binding to baculovirus expressed retinoid receptor RXR gamma B 7.54 pKd 29 nM Kd J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Inhibition of [3H]9-cis-RA binding to Retinoid X receptor RXR gamma B 7.54 pKi 29 nM Ki Bioorg Med Chem Lett (1997) 7: 2393-2398
ChEMBL Effective concentration against retinoid receptor isoform (RXR gamma) expressed in CV-1 cells B 7.6 pEC50 25 nM EC50 J Med Chem (1994) 37: 2930-2941 [PMID:8071941]
ChEMBL Ability to activate gene expression at Retinoic acid receptor RXR-gamma was evaluated in a cotransfection assay. B 7.7 pEC50 20 nM EC50 J Med Chem (1995) 38: 3146-3155 [PMID:7636877]
ChEMBL Effective potency in transcriptional activation assay in CV-1 cells expressing Retinoid X receptor RXR gamma B 7.7 pEC50 20 nM EC50 Bioorg Med Chem Lett (1997) 7: 2393-2398
Retinoid X receptor-α/Peroxisome proliferator-activated receptor-γ/RXR alpha/PPAR gamma in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111394] [GtoPdb: 610595] [UniProtKB: P19793P37231]
GtoPdb Measured using a TR-FRET competitive displacement assay. - 5.52 pIC50 ~3000 nM IC50 PPAR Res (2015) 2015: 254560 [PMID:26451138]
ChEMBL Displacement of CU-6PMN from human PPARgamma-LBD (206 to 477 residues)/human RXRalpha-LBD (224 to 462 residues) heterodimer incubated for 30 mins by fluorospectrometer B 6.41 pIC50 389 nM IC50 ACS Med Chem Lett (2023) 14: 291-296 [PMID:36923911]
GtoPdb - - 7.4 pIC50 - - - Curr Pharm Des (2000) 6: 25-58 [PMID:10637371];
J Med Chem (1999) 42: 742-50 [PMID:10052980];
J Med Chem (1994) 37: 2930-41 [PMID:8071941]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]