T0901317 [Ligand Id: 2755] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL62136 (T0901317) |
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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: 2402, 2403] [UniProtKB: P49768, P49810, Q8WW43, Q92542, Q96BI3, Q9NZ42] | ||||||||
| 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 | |||||||