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 against human LXRalpha expressed in human HEK293T cells co-expressing CMX-GAL4N-hLXRalpha incubated for 24 hrs by reporter gene assay | B | 6.59 | pEC50 | 260 | nM | EC50 | Bioorg Med Chem (2022) 66: 116792-116792 [PMID:35576658] |
| ChEMBL | Agonist activity at LXRalpha (unknown origin) transfected in HEK293T cells incubated for 20 hrs by luciferase reporter assay | B | 6.6 | pEC50 | 250 | nM | EC50 | J Med Chem (2023) 66: 752-765 [PMID:36539349] |
| 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 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 | 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 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 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 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 [PMID:31673308] |
| 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 | 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 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 | 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 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 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 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 hyodeoxycholicacid-based fluorescent tracer from recombinant human LXRbeta LBD (215 to 461 residues) expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins under shaking condition and measured after 30 mins by fluorescence polarization assay | B | 7.38 | pKi | 41.3 | nM | Ki | Eur J Med Chem (2020) 194: 112240-112240 [PMID:32248003] |
| 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-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 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 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 against human LXRbeta expressed in human HEK293T cells co-expressing CMX-GAL4N-hLXRbeta incubated for 24 hrs by reporter gene assay | B | 6.59 | pEC50 | 260 | nM | EC50 | Bioorg Med Chem (2022) 66: 116792-116792 [PMID:35576658] |
| 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 LXRbeta (unknown origin) transfected in HEK293T cells incubated for 20 hrs by luciferase reporter assay | B | 6.66 | pEC50 | 220 | nM | EC50 | J Med Chem (2023) 66: 752-765 [PMID:36539349] |
| 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 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 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 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 | 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 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 | 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 [PMID:31673308] |
| 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 | 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 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 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 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 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 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 human LXR-beta | B | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2016) 59: 9201-9214 [PMID:27652492] |
| 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 | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem (2014) 22: 2799-2808 [PMID:24702856] |
| ChEMBL | Inhibition of human RORalpha1 expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | Bioorg Med Chem (2018) 26: 4493-4501 [PMID:30077610] |
| ChEMBL | Inverse agonist activity at RORalpha (unknown origin) by M1H assay | B | 5.3 | pIC50 | >5011.87 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Inverse agonist activity at Gal4-fused RORalpha LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2019) 62: 4716-4730 [PMID:30964293] |
| ChEMBL | Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | Medchemcomm (2013) 4: 764-776 |
| ChEMBL | Inhibition of RORa (unknown origin) assessed as inhibition of coactivator recruitment by GAL4-nuclear receptor LBD assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| ChEMBL | Inhibition of human GAL4-fused RORalpha LBD transfected in HEK293T cell measured after 24 hrs by luciferase reporter assay | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2018) 61: 10976-10995 [PMID:30010338] |
| ChEMBL | Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | B | 5.3 | pEC50 | 5000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6604-6609 [PMID:24239186] |
| ChEMBL | Agonist activity at RoRa (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay | B | 5.3 | pEC50 | 5000 | nM | EC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| RAR-related orphan receptor-β/Nuclear receptor ROR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091268] [GtoPdb: 599] [UniProtKB: Q92753] | ||||||||
| ChEMBL | Inverse agonist activity at recombinant N-terminally GST-tagged RORbeta ligand binding domain (unknown origin) expressed in Escherichia coli incubated for 1 hr by FRET assay | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Inverse agonist activity at RORbeta (unknown origin) by M1H assay | B | 5.3 | pIC50 | >5011.87 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | B | 5.22 | pEC50 | 6000 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6604-6609 [PMID:24239186] |
| ChEMBL | Agonist activity at RoRb (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay | B | 5.22 | pEC50 | 6000 | nM | EC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449] | ||||||||
| GtoPdb | - | - | 7.29 | pKi | 51 | nM | Ki | Mol Pharmacol (2010) 77: 228-36 [PMID:19887649] |
| ChEMBL | Displacement of 25-[3H]hydroxycholesterol from GST-tagged ROR gamma (unknown origin) by radioligand competition assay | B | 7.29 | pKi | 51 | nM | Ki | Medchemcomm (2013) 4: 764-776 |
| ChEMBL | Binding affinity to RORc (unknown origin) by radioligand binding assay | B | 7.29 | pKi | 51 | nM | Ki | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| ChEMBL | Inverse agonist activity at human ROR-gamma1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay | B | 5.19 | pIC50 | 6500 | nM | IC50 | Bioorg Med Chem (2014) 22: 2799-2808 [PMID:24702856] |
| ChEMBL | Inhibition of human RORgamma1 expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 5.36 | pIC50 | 4400 | nM | IC50 | Bioorg Med Chem (2018) 26: 4493-4501 [PMID:30077610] |
| ChEMBL | Antagonist activity at full-length RORgamma (unknown origin) expressed in 293T cells after 24 hrs by luciferase reporter gene assay | B | 5.46 | pIC50 | 3500 | nM | IC50 | Eur J Med Chem (2014) 78: 431-441 [PMID:24704616] |
| ChEMBL | Inverse agonist activity at human RORgamma transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1817-1820 [PMID:26905831] |
| ChEMBL | Antagonist activity at human His6-tagged RORgamma ligand binding domain (262 to 507 aa) assessed as inhibition of SRC1-4 co-activator peptide recruitment by luminescence-based AlphaScreen assay | B | 5.7 | pIC50 | 2010 | nM | IC50 | Eur J Med Chem (2014) 78: 431-441 [PMID:24704616] |
| ChEMBL | Inhibition of human GAL4-fused RORgamma LBD transfected in HEK293T cell measured after 24 hrs by luciferase reporter assay | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2018) 61: 10976-10995 [PMID:30010338] |
| ChEMBL | Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay | B | 5.77 | pIC50 | 1700 | nM | IC50 | Medchemcomm (2013) 4: 764-776 |
| ChEMBL | Inhibition of RORc (unknown origin) assessed as inhibition of coactivator recruitment by GAL4-nuclear receptor LBD assay | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| ChEMBL | Inhibition of human GAL4-fused RORgammat LBD transfected in HEK293T cell measured after 24 hrs by by dual-glo luciferase assay | B | 6.09 | pIC50 | 810 | nM | IC50 | J Med Chem (2022) 65: 592-615 [PMID:34957834] |
| ChEMBL | Antagonist activity at Gal4-fused RORgamma (unknown origin) expressed in 293T cells after 24 hrs by luciferase reporter gene assay | B | 6.27 | pIC50 | 540 | nM | IC50 | Eur J Med Chem (2014) 78: 431-441 [PMID:24704616] |
| ChEMBL | Inverse agonist activity at RORgammaT (unknown origin) by M1H assay | B | 6.3 | pIC50 | 501.19 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Inverse agonist activity at Gal4-fused RORgamma LBD (unknown origin) expressed in 293T cells measured after 24 hrs by dual-luciferase reporter gene assay | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2019) 62: 4716-4730 [PMID:30964293] |
| ChEMBL | Inverse agonist activity at human recombinant N-terminally 6xHis-tagged RORgamma ligand binding domain (unknown origin) expressed in Escherichia coli incubated for 1 hr by FRET assay | B | 6.5 | pIC50 | 316.23 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5265-5267 [PMID:25305688] |
| ChEMBL | Inhibition of human APC-labeled RORgammat LBD (262 to 518 residues) transfected in Escherichia coli BL21 (DE3) assessed as biotinylated SRC recruitment incubated for 1 hr by dual FRET assay | B | 6.62 | pIC50 | 238 | nM | IC50 | J Med Chem (2022) 65: 592-615 [PMID:34957834] |
| ChEMBL | Inverse agonist activity at recombinant human GST-tagged ROR-gamma receptor ligand binding domain assessed as inhibition of receptor and co-activator TRAP220 interaction by FRET assay | B | 6.69 | pIC50 | 204 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2459-2463 [PMID:27080181] |
| ChEMBL | Displacement of [3H2]-25-hydroxycholesterol from N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system after 3 hrs by scintillation counting analysis | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 6604-6609 [PMID:24239186] |
| ChEMBL | Binding affinity to RORgamma (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| ChEMBL | Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | B | 6.33 | pEC50 | 463 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6604-6609 [PMID:24239186] |
| ChEMBL | Agonist activity at RoRc (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay | B | 6.34 | pEC50 | 460 | nM | EC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| ChEMBL | Inverse agonist activity at Gal4-tagged human RORgammat ligand binding domain expressed in human Jurkat cells by native IL17 promoter driven luciferase reporter gene assay | B | 6.48 | pEC50 | 333 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 85-93 [PMID:29233651] |
| ChEMBL | Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis | B | 7.27 | pEC50 | 54 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6604-6609 [PMID:24239186] |
| ChEMBL | Inverse agonist activity at human RoRc-LBD fusion protein with GST expressed in BL-21 (BL3) cells assessed as SRC1 coactivator peptide recruitment | B | 7.27 | pEC50 | 54 | nM | EC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| Liver X receptor-β in Human [GtoPdb: 601] [UniProtKB: P55055] | ||||||||
| GtoPdb | - | - | 7.3 | pEC50 | - | - | - | Genes Dev (2000) 14: 2831-8 [PMID:11090131] |
| Liver X receptor-β/Oxysterols receptor LXR-beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417346] [GtoPdb: 601] [UniProtKB: Q60644] | ||||||||
| ChEMBL | Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression | F | 7.57 | pEC50 | 27 | nM | EC50 | Bioorg Med Chem (2009) 17: 8086-8092 [PMID:19853462] |
| Liver X receptor-β/Oxysterols receptor LXR-beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105785] [GtoPdb: 601] [UniProtKB: Q62755] | ||||||||
| ChEMBL | Transactivation of rat LXRbeta expressed in HEK293FT cells measured after 14 to 18 hrs by dual-luciferase reporter gene assay | B | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2019) 29: 1330-1335 [PMID:30952591] |
| Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| ChEMBL | Displacement of [N-methyl-3H]GW0438X from human PXR | B | 7.4 | pIC50 | 39.81 | nM | IC50 | Bioorg Med Chem (2007) 15: 2156-2166 [PMID:17215127] |
| ChEMBL | Displacement of BODIPY FL vindoline from GST-tagged human PXR LBD incubated for 60 mins by TR-FRET assay | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2021) 64: 1733-1761 [PMID:33497575] |
| ChEMBL | Inhibition of BODIPY FL vindoline binding to recombinant human GST-tagged PXR LBD (111 to 434 residues) expressed in baculovirus infected insect cells incubated for 1 mins under shaking condition followed by 60 mins under dark condition by TR-FRET assay | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (2022) 65: 16829-16859 [PMID:36480704] |
| ChEMBL | Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 6.57 | pEC50 | 270 | nM | EC50 | Bioorg Med Chem Lett (2016) 26: 1817-1820 [PMID:26905831] |
| ChEMBL | Agonist activity at VP16-fused human PXR expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay | B | 6.92 | pEC50 | 120 | nM | EC50 | Bioorg Med Chem (2018) 26: 4493-4501 [PMID:30077610] |
| ChEMBL | Agonist activity at PXR (unknown origin) by AlphaScreen assay | B | 7.3 | pEC50 | 50 | nM | EC50 | ACS Med Chem Lett (2019) 10: 677-681 [PMID:30996817] |
| ChEMBL | Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | B | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 6604-6609 [PMID:24239186] |
| ChEMBL | Agonist activity at PXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay | B | 7.44 | pEC50 | 36 | nM | EC50 | J Med Chem (2014) 57: 5871-5892 [PMID:24502334] |
| ChEMBL | Agonist activity at His-tagged PXR-LBD/SRC-1p (unknown origin) expressed in Escherichia coli BL21(DE3) by coactivator recruitment based Alpha-screen assay | B | 7.82 | pEC50 | 15 | nM | EC50 | J Med Chem (2020) 63: 3701-3712 [PMID:32160459] |
| ChEMBL | Antagonist activity at human PXR by transient transfection assay | F | 7.9 | pEC50 | 12.59 | nM | EC50 | Bioorg Med Chem (2007) 15: 2156-2166 [PMID:17215127] |
| Retinoid X receptor-α/Liver X receptor-α/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-alpha in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430879] [GtoPdb: 610, 602] [UniProtKB: P19793, Q13133] | ||||||||
| ChEMBL | Binding affinity to His-LXRalpha/FLAG-RXRalpha (unknown origin) by FITC-labeled T0901317 based fluorescence polarization assay | B | 6.64 | pKi | 230 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 3914-3920 [PMID:26238323] |
| ChEMBL | Binding affinity to LXRalpha-RXRalpha heterodimer (unknown origin) expressed in insect cells by scintillation proximity assay | B | 7.51 | pKi | 31 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 372-377 [PMID:25435151] |
| GtoPdb | - | - | 7.3 | pEC50 | - | - | - | Genes Dev (2000) 14: 2831-8 [PMID:11090131] |
| Retinoid X receptor-α/Liver X receptor-β/Retinoic acid receptor RXR-alpha/oxysterols receptor LXR-beta in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430878] [GtoPdb: 610, 601] [UniProtKB: P19793, P55055] | ||||||||
| ChEMBL | Binding affinity to His-LXRbeta/FLAG-RXRalpha (unknown origin) by FITC-labeled T0901317 based fluorescence polarization assay | B | 6.66 | pKi | 220 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 3914-3920 [PMID:26238323] |
| ChEMBL | Binding affinity to LXRbeta-RXRalpha heterodimer (unknown origin) expressed in insect cells by scintillation proximity assay | B | 7.59 | pKi | 26 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 372-377 [PMID:25435151] |
| GtoPdb | - | - | 7.3 | pEC50 | - | - | - | Genes Dev (2000) 14: 2831-8 [PMID:11090131] |
| ChEMBL | Agonist activity at human RXRalpha/LXRbeta expressed in HEK293 cells measured after 20 hrs by dual luciferase reporter gene assay | B | 9.97 | pEC50 | 0.11 | nM | EC50 | Eur J Med Chem (2020) 194: 112240-112240 [PMID:32248003] |
ChEMBL data shown on this page come from version 35:
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]
