T0901317 [Ligand Id: 2755] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL62136 (T0901317)
  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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  • Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
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  • RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398]
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  • RAR-related orphan receptor-β/Nuclear receptor ROR-beta in Human [ChEMBL: CHEMBL3091268] [GtoPdb: 599] [UniProtKB: Q92753]
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  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
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  • Liver X receptor-β in Human [GtoPdb: 601] [UniProtKB: P55055]
  • Liver X receptor-β/Oxysterols receptor LXR-beta in Mouse [ChEMBL: CHEMBL2417346] [GtoPdb: 601] [UniProtKB: Q60644]
  • Liver X receptor-β/Oxysterols receptor LXR-beta in Rat [ChEMBL: CHEMBL4105785] [GtoPdb: 601] [UniProtKB: Q62755]
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  • Retinoid X receptor-α/Liver X receptor-α/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha in Human [ChEMBL: CHEMBL3430879] [GtoPdb: 610602] [UniProtKB: P19793Q13133]
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  • Retinoid X receptor-α/Liver X receptor-β/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta in Human [ChEMBL: CHEMBL3430878] [GtoPdb: 610601] [UniProtKB: P19793P55055]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL Agonist activity at Gal4-fused FXR LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay B 5.28 pIC50 5300 nM IC50 J Med Chem (2019) 62: 4716-4730 [PMID:30964293]
ChEMBL Agonist activity at human FXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay B 5.47 pEC50 3400 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 1817-1820 [PMID:26905831]
ChEMBL Agonist activity at FXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay B 5.89 pEC50 1300 nM EC50 J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
ChEMBL Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay B 6 pEC50 1000 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 6604-6609 [PMID:24239186]
presenilin 1/presenilin 2/Gamma-secretase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094135] [GtoPdb: 24022403] [UniProtKB: P49768P49810Q8WW43Q92542Q96BI3Q9NZ42]
ChEMBL Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-40 formation LPECL assay B 4.4 pIC50 >40000 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 5428-5431 [PMID:17723298]
ChEMBL Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-38 formation by LPECL assay B 5.35 pIC50 4500 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 5428-5431 [PMID:17723298]
ChEMBL Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay B 5.44 pEC50 3600 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 5428-5431 [PMID:17723298]
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
ChEMBL Binding affinity to human LXRalpha-LBD by surface plasmon resonance B 7.03 pKd 92.4 nM Kd Bioorg. Med. Chem. Lett. (2013) 23: 4185-4190 [PMID:23769638]
ChEMBL Displacement of radiolabeled T0901317 from LXRalpha LBD (unknown origin) B 7.62 pKi 24 nM Ki Bioorg Med Chem Lett (2016) 26: 5044-5050 [PMID:27599745]
ChEMBL Displacement of [3H]T0901317 from human recombinant N-terminal biotinylated tagged LXRalpha ligand binding domain (197-447) expressed in Escherichia coli B 4.85 pIC50 14000 nM IC50 Bioorg. Med. Chem. (2009) 17: 3519-3527 [PMID:19394832]
ChEMBL Displacement of [3H]N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-methylbenzenesulfonamide from LXRalpa by scintillation proximity assay B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 2407-2410 [PMID:22406115]
ChEMBL Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRalpha ligand binding domain B 7.12 pIC50 75 nM IC50 J. Med. Chem. (2008) 51: 5758-5765 [PMID:18800767]
ChEMBL Agonist activity at Gal4-fused LXRalpha LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay B 7.3 pIC50 50 nM IC50 J Med Chem (2019) 62: 4716-4730 [PMID:30964293]
ChEMBL Binding affinity to LXRalpha by radioligand displacement assay B 7.52 pIC50 30 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 5231-5237 [PMID:16876993]
ChEMBL Binding affinity to human recombinant LXRalpha ligand binding domain B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2010) 53: 3296-3304 [PMID:20350005]
ChEMBL Displacement of [3H]T0901317 from human recombinant LXRalpha ligand binding domain B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. (2009) 17: 8086-8092 [PMID:19853462]
ChEMBL Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 689-693 [PMID:19962892]
ChEMBL Binding affinity at human LXRalpha B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 54-59 [PMID:18023179]
ChEMBL Displacement of [3H]T0901317 from LXRalpha ligand binding domain B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2903-2907 [PMID:20382019]
ChEMBL Displacement of [3H]T-0901317 from human LXR alpha receptor B 8 pIC50 10 nM IC50 J. Med. Chem. (2006) 49: 6151-6154 [PMID:17034119]
ChEMBL Displacement of [3H]T0901317 from human recombinant LXRalpha LBD B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 521-525 [PMID:20005711]
ChEMBL Displacement of [3H]T0901317 from human recombinant LXRalpha-LBD B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 209-212 [PMID:19932617]
ChEMBL Displacement of [3H]T0901317 from human recombinant LXRalpha LBD B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 526-530 [PMID:20006495]
ChEMBL Agonist activity at human LXR-alpha assessed as increase in recruitment of Trap 220/Drip2 coactivator peptide by TR-FRET assay F 5.84 pEC50 1430 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 4094-4099 [PMID:22579484]
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 6.03 pEC50 940 nM EC50 Bioorg Med Chem Lett (2017) 27: 1193-1198 [PMID:28169169]
ChEMBL Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay B 6.28 pEC50 530 nM EC50 J Nat Prod (2019) 82: 1558-1564 [PMID:31095389]
ChEMBL Agonist activity at LXRalpha (unknown origin) B 6.3 pEC50 500 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 2668-2674 [PMID:25998501]
ChEMBL Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay B 6.31 pEC50 490 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 1274-1278 [PMID:25677664]
ChEMBL Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay B 6.31 pEC50 490 nM EC50 Bioorg. Med. Chem. (2016) 24: 3436-3446 [PMID:27283790]
ChEMBL Agonist activity at human LXRalpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay B 6.4 pEC50 400 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 1817-1820 [PMID:26905831]
ChEMBL Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay B 6.43 pEC50 373 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 6604-6609 [PMID:24239186]
ChEMBL Agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay B 6.43 pEC50 370 nM EC50 J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
ChEMBL Agonist activity at GAL4-tagged human LXRalpha assessed as receptor activation expressed in African green monkey CV1 cells by luciferase reporter gene assay B 6.44 pEC50 359 nM EC50 Bioorg Med Chem Lett (2018) 28: 85-93 [PMID:29233651]
ChEMBL Agonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay B 6.54 pEC50 290 nM EC50 Bioorg. Med. Chem. (2014) 22: 2799-2808 [PMID:24702856]
ChEMBL Agonist activity at GAL4-fused LXR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay B 6.6 pEC50 250 nM EC50 MedChemComm (2013) 4: 764-776
ChEMBL Transactivation of LXRalpha by luciferase reporter gene assay F 6.6 pEC50 250 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 5231-5237 [PMID:16876993]
ChEMBL Agonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay B 6.68 pEC50 210 nM EC50 ACS Med. Chem. Lett. (2015) 6: 902-907 [PMID:26288691]
ChEMBL Agonist activity at Homo sapiens (human) LXRalpha expressed in HepG2 cells assessed as transactivation of CYP7A1 gene expression after 48 hr by luciferase reporter gene assay B 6.72 pEC50 190 nM EC50 Med Chem Res (2013) 22: 3270-3281
ChEMBL Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay F 6.77 pEC50 170 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 521-525 [PMID:20005711]
ChEMBL Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay B 6.85 pEC50 140 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 689-693 [PMID:19962892]
ChEMBL Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay B 6.85 pEC50 140 nM EC50 J. Med. Chem. (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay F 6.87 pEC50 135 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 54-59 [PMID:18023179]
ChEMBL Agonist activity at human LXRalpha ligand binding domain (205-448) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay B 6.87 pEC50 135 nM EC50 Bioorg. Med. Chem. (2009) 17: 3519-3527 [PMID:19394832]
ChEMBL Agonist activity at LXR alpha (unknown origin) by Alpha Screen assay B 6.92 pEC50 120 nM EC50 MedChemComm (2019) 10: 1412-1419
ChEMBL Agonist activity at human LXRalpha-LBD assessed as recruitment of co-activator peptide after 2 hrs by TR-FRET assay B 7.04 pEC50 91.1 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 4185-4190 [PMID:23769638]
ChEMBL Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay F 7.07 pEC50 85 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Effective concentration in LXR alpha-Gal4 receptor gene assay B 7.07 pEC50 85 nM EC50 J. Med. Chem. (2002) 45: 1963-1966 [PMID:11985463]
ChEMBL Agonist activity at LXRalpha ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay B 7.2 pEC50 63.1 nM EC50 J. Med. Chem. (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL Ligand-dependent recruitment of steroid receptor co-activator 1 (SRC1) to Liver X receptor-alpha B 7.22 pEC50 60 nM EC50 J. Med. Chem. (2002) 45: 1963-1966 [PMID:11985463]
ChEMBL Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRalpha (Liver X receptor) B 7.26 pEC50 55 nM EC50 J. Med. Chem. (2005) 48: 5419-5422 [PMID:16107141]
GtoPdb - - 7.3 pEC50 - - - Genes Dev (2000) 14: 2831-8 [PMID:11090131]
ChEMBL Agonist activity LXRalpha (unknown origin) B 7.3 pEC50 50 nM EC50 J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL Agonist activity LXRalpha (unknown origin) B 7.3 pEC50 50 nM EC50 J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL Agonist activity at human LXRalpha receptor after 1 hr by HTRF cofactor recruitment assay F 7.4 pEC50 40 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 4442-4446 [PMID:17587573]
ChEMBL Agonist activity at LXRalpha LBD by HTRF cofactor peptide recruitment assay F 7.4 pEC50 40 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 3473-3479 [PMID:17416521]
ChEMBL Agonist activity at human LXRalpha expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay B 7.52 pEC50 30 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 3914-3920 [PMID:26238323]
ChEMBL Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay B 7.55 pEC50 28 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 372-377 [PMID:25435151]
ChEMBL Agonist activity at LXRalpha (unknown origin) expressed in human HepG2 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay B 7.7 pEC50 20 nM EC50 J. Med. Chem. (2016) 59: 3489-3498 [PMID:27011007]
ChEMBL Activity against LXR alpha transiently transfected in HEK293 cells B 8 pEC50 10 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 1638-1642 [PMID:16386417]
ChEMBL Agonist activity at LXRalpha ligand binding domain by FRET based SRC1 recruitment assay B 8 pEC50 10 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at human LXRalpha expressed in HEK293 cells co-expressing CMX-beta-galactosidase incubated for 16 hrs by luciferase reporter gene assay B 8.22 pEC50 6 nM EC50 Bioorg Med Chem Lett (2018) 28: 796-801 [PMID:29398545]
ChEMBL Agonist activity at LXRalpha by TR-FRET assay F 8.49 pEC50 3.2 nM EC50 J. Med. Chem. (2011) 54: 788-808 [PMID:21218783]
Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055]
ChEMBL Binding affinity to human LXRbeta-LBD by surface plasmon resonance B 6.99 pKd 103 nM Kd Bioorg. Med. Chem. Lett. (2013) 23: 4185-4190 [PMID:23769638]
ChEMBL Binding affinity to recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as inhibitory constant incubated for 30 mins by fluorescence polarization binding assay B 7.38 pKi 41.3 nM Ki Eur J Med Chem (2019) 178: 458-467 [PMID:31202993]
ChEMBL Displacement of radiolabeled T0901317 from LXRbeta LBD (unknown origin) B 7.77 pKi 17 nM Ki Bioorg Med Chem Lett (2016) 26: 5044-5050 [PMID:27599745]
ChEMBL Displacement of [3H]T0901317 from human recombinant N-terminal biotinylated tagged LXRbeta ligand binding domain (154-461) expressed in Escherichia coli B 5.05 pIC50 9000 nM IC50 Bioorg. Med. Chem. (2009) 17: 3519-3527 [PMID:19394832]
ChEMBL Displacement of [3H]N-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl)-N-methylbenzenesulfonamide from LXRbeta by scintillation proximity assay B 7 pIC50 100 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 2407-2410 [PMID:22406115]
ChEMBL Binding affinity to LXRbeta by radioligand displacement assay B 7.15 pIC50 70 nM IC50 Bioorg. Med. Chem. Lett. (2006) 16: 5231-5237 [PMID:16876993]
ChEMBL Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRbeta ligand binding domain B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2008) 51: 5758-5765 [PMID:18800767]
ChEMBL Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assay B 7.7 pIC50 19.95 nM IC50 J. Med. Chem. (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL Displacement of [3H]T0901317 from human recombinant LXRbeta-LBD B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 209-212 [PMID:19932617]
ChEMBL Displacement of [3H]T0901317 from human recombinant LXRbeta LBD B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 526-530 [PMID:20006495]
ChEMBL Displacement of [3H]T0901317 from human recombinant LXRbeta LBD B 7.89 pIC50 13 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 521-525 [PMID:20005711]
ChEMBL Displacement of [3H]T-0901317 from human LXR beta receptor B 8 pIC50 10 nM IC50 J. Med. Chem. (2006) 49: 6151-6154 [PMID:17034119]
ChEMBL Binding affinity at human LXRbeta B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 54-59 [PMID:18023179]
ChEMBL Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 689-693 [PMID:19962892]
ChEMBL Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL Displacement of [3H]T0901317 from human recombinant LXRbeta ligand binding domain B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. (2009) 17: 8086-8092 [PMID:19853462]
ChEMBL Displacement of [3H]T0901317 from LXRbeta ligand binding domain B 8.05 pIC50 9 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 2903-2907 [PMID:20382019]
ChEMBL Binding affinity to human recombinant LXRbeta ligand binding domain B 8.05 pIC50 9 nM IC50 J. Med. Chem. (2010) 53: 3296-3304 [PMID:20350005]
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 6.1 pEC50 800 nM EC50 Bioorg Med Chem Lett (2017) 27: 1193-1198 [PMID:28169169]
ChEMBL Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay B 6.39 pEC50 410 nM EC50 Bioorg. Med. Chem. (2016) 24: 3436-3446 [PMID:27283790]
ChEMBL Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay B 6.39 pEC50 410 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 1274-1278 [PMID:25677664]
ChEMBL Agonist activity at LXRbeta (unknown origin) B 6.4 pEC50 400 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 2668-2674 [PMID:25998501]
ChEMBL Transactivation of LXRbeta by luciferase reporter gene assay F 6.52 pEC50 300 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 5231-5237 [PMID:16876993]
ChEMBL Agonist activity at human LXRbeta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay B 6.64 pEC50 230 nM EC50 Bioorg. Med. Chem. Lett. (2016) 26: 1817-1820 [PMID:26905831]
ChEMBL Agonist activity at GAL4-tagged human LXRbeta assessed as receptor activation expressed in African green monkey CV1 cells by luciferase reporter gene assay B 6.7 pEC50 198 nM EC50 Bioorg Med Chem Lett (2018) 28: 85-93 [PMID:29233651]
ChEMBL Agonist activity at human LXRbeta ligand binding domain (219-462) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay B 6.75 pEC50 178 nM EC50 Bioorg. Med. Chem. (2009) 17: 3519-3527 [PMID:19394832]
ChEMBL Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay F 6.75 pEC50 178 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 54-59 [PMID:18023179]
ChEMBL Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay B 6.77 pEC50 170 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 689-693 [PMID:19962892]
ChEMBL Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay B 6.77 pEC50 170 nM EC50 J. Med. Chem. (2010) 53: 3296-3304 [PMID:20350005]
ChEMBL Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay B 6.77 pEC50 170 nM EC50 J. Med. Chem. (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay B 6.77 pEC50 170 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2903-2907 [PMID:20382019]
ChEMBL Agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay B 6.8 pEC50 160 nM EC50 J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
ChEMBL Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay B 6.81 pEC50 156 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 6604-6609 [PMID:24239186]
ChEMBL Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay B 6.85 pEC50 140 nM EC50 J. Med. Chem. (2010) 53: 3296-3304 [PMID:20350005]
ChEMBL Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay B 6.85 pEC50 140 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 372-377 [PMID:25435151]
ChEMBL Agonist activity at human Gal4-LBD fused LXRbeta LBD expressed in Huh7 cells by transient transactivation assay F 6.87 pEC50 135 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 521-525 [PMID:20005711]
ChEMBL Agonist activity at human LXRbeta expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay B 6.89 pEC50 130 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 3914-3920 [PMID:26238323]
ChEMBL Agonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay B 6.92 pEC50 120 nM EC50 Bioorg. Med. Chem. (2014) 22: 2799-2808 [PMID:24702856]
ChEMBL Agonist activity at human LXR-beta assessed as increase in recruitment of Trap 220/D22 coactivator peptide by TR-FRET assay F 6.96 pEC50 110 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 4094-4099 [PMID:22579484]
ChEMBL Agonist activity at human LXRbeta-LBD assessed as recruitment of co-activator peptide after 2 hrs by TR-FRET assay B 6.99 pEC50 102.6 nM EC50 Bioorg. Med. Chem. Lett. (2013) 23: 4185-4190 [PMID:23769638]
ChEMBL Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay B 7 pEC50 100 nM EC50 J. Med. Chem. (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL Antagonist activity at human LXRbeta by transient transfection assay F 7 pEC50 100 nM EC50 Bioorg. Med. Chem. (2007) 15: 2156-2166 [PMID:17215127]
ChEMBL Agonist activity at human LXRbeta expressed in HEK293 cells by luciferase reporter gene assay B 7.07 pEC50 85 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 5265-5267 [PMID:25305688]
ChEMBL Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay F 7.12 pEC50 75 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay B 7.18 pEC50 66 nM EC50 ACS Med. Chem. Lett. (2015) 6: 902-907 [PMID:26288691]
ChEMBL Agonist activity at LXR beta (unknown origin) by Alpha Screen assay B 7.22 pEC50 60 nM EC50 MedChemComm (2019) 10: 1412-1419
ChEMBL Agonist activity at human LXRalpha in HEK293 cells assessed as Gal4 transactivation F 7.28 pEC50 53 nM EC50 J. Med. Chem. (2010) 53: 3296-3304 [PMID:20350005]
GtoPdb - - 7.3 pEC50 - - - Genes Dev (2000) 14: 2831-8 [PMID:11090131]
ChEMBL Agonist activity LXRbeta (unknown origin) B 7.3 pEC50 50 nM EC50 J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL Agonist activity LXRbeta (unknown origin) B 7.3 pEC50 50 nM EC50 J Med Chem (2019) 62: 2112-2126 [PMID:30702885]
ChEMBL Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRbeta (Liver X receptor) B 7.52 pEC50 30 nM EC50 J. Med. Chem. (2005) 48: 5419-5422 [PMID:16107141]
ChEMBL Agonist activity at human LXRbeta expressed in HEK293 cells co-expressing CMX-beta-galactosidase incubated for 16 hrs by luciferase reporter gene assay B 7.68 pEC50 21 nM EC50 Bioorg Med Chem Lett (2018) 28: 796-801 [PMID:29398545]
ChEMBL Agonist activity at LXRbeta (unknown origin) expressed in human H4 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay B 7.7 pEC50 20 nM EC50 J. Med. Chem. (2016) 59: 3489-3498 [PMID:27011007]
ChEMBL Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation F 7.72 pEC50 19 nM EC50 J. Med. Chem. (2010) 53: 3296-3304 [PMID:20350005]
ChEMBL Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay F 7.8 pEC50 16 nM EC50 Bioorg. Med. Chem. (2009) 17: 8086-8092 [PMID:19853462]
ChEMBL Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay F 7.8 pEC50 16 nM EC50 J. Med. Chem. (2006) 49: 6151-6154 [PMID:17034119]
ChEMBL Agonist activity at LXRbeta LBD by HTRF cofactor peptide recruitment assay F 7.82 pEC50 15 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 3473-3479 [PMID:17416521]
ChEMBL Agonist activity at human LXRbeta receptor after 1 hr by HTRF cofactor recruitment assay F 7.82 pEC50 15 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 4442-4446 [PMID:17587573]
ChEMBL Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay F 7.96 pEC50 11 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 4442-4446 [PMID:17587573]
ChEMBL Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay F 7.96 pEC50 11 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 3473-3479 [PMID:17416521]
ChEMBL Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assay B 8.1 pEC50 8 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at LXRbeta by TR-FRET assay F 8.33 pEC50 4.7 nM EC50 J. Med. Chem. (2011) 54: 788-808 [PMID:21218783]
RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398]
ChEMBL Displacement of 25-[3H]hydroxycholesterol from GST-tagged ROR alpha ligand binding domain (unknown origin) expressed in Escherichia coli BL21 gold (DE3) cells by radioligand competition assay B 6.88 pKi 132 nM Ki MedChemComm (2013) 4: 764-776
ChEMBL Binding affinity to RORa (unknown origin) by radioligand binding assay B 6.88 pKi 132 nM Ki J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
GtoPdb - - 6.88 pKi 132 nM Ki Mol Pharmacol (2010) 77: 228-36 [PMID:19887649]
ChEMBL Inverse agonist activity at human ROR-alpha1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay