GW3965 [Ligand Id: 2754] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL59030 (GW3965)
  • Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
  • This target only has 0 pki data point
  • 0
1 CHEMBL59030_lig_chart_1 LXR-alpha Human
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  • Liver X receptor-β/LXR-beta in Human [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055]
  • This target only has 1 pki data point
  • 8.66
2 CHEMBL59030_lig_chart_2 LXR-beta Human
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  • Pregnane X receptor in Human [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
  • This target only has 1 pki data point
  • 5.7
3 CHEMBL59030_lig_chart_3 Pregnane X receptor Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
ChEMBL Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRalpha ligand binding domain B 6.63 pIC50 235 nM IC50 J. Med. Chem. (2008) 51: 5758-5765 [PMID:18800767]
ChEMBL Displacement of [3H]T-0901317 from human LXR alpha receptor B 7 pIC50 100 nM IC50 J. Med. Chem. (2006) 49: 6151-6154 [PMID:17034119]
ChEMBL Displacement of [3H]TO901317 from human recombinant LXRalpha expressed in Escherichia coli by flashplate method B 7 pIC50 100 nM IC50 J. Med. Chem. (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL Antagonist activity at LXRalpha ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay B 7 pIC50 100 nM IC50 J. Med. Chem. (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL Agonist activity at LXRalpha (unknown origin) B 5.89 pEC50 1300 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 5.89 pEC50 1300 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 1274-1278 [PMID:25677664]
ChEMBL Agonist activity at human LXRalpha by Gal4 assay B 5.95 pEC50 1128 nM EC50 J. Med. Chem. (2016) 59: 3264-3271 [PMID:26990539]
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 6.1 pEC50 794.33 nM EC50 J. Med. Chem. (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay B 6.18 pEC50 660 nM EC50 J. Med. Chem. (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL Agonist activity at LXRalpha LBD by HTRF cofactor peptide recruitment assay F 6.44 pEC50 367 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 6.44 pEC50 367 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 4442-4446 [PMID:17587573]
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 6.51 pEC50 310 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at LXRalpha ligand binding domain by FRET based SRC1 recruitment assay B 6.55 pEC50 280 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at human LXRalpha assessed as association of SRC1 to LXRalpha ligand binding domain by FRET based cell-free ligand sensing assay B 6.7 pEC50 200 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 5617-5621 [PMID:19717304]
GtoPdb - - 6.7 pEC50 - - - J Med Chem (2002) 45: 1963-6 [PMID:11985463]
ChEMBL Effective concentration in LXR alpha-Gal4 receptor gene assay B 6.72 pEC50 190 nM EC50 J. Med. Chem. (2002) 45: 1963-1966 [PMID:11985463]
ChEMBL Agonist activity at LXRalpha by FRET assay F 6.76 pEC50 175 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 1097-1100 [PMID:19167885]
ChEMBL Ligand-dependent recruitment of steroid receptor co-activator 1 (SRC1) to Liver X receptor-alpha B 6.9 pEC50 125 nM EC50 J. Med. Chem. (2002) 45: 1963-1966 [PMID:11985463]
ChEMBL Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay F 7.01 pEC50 97 nM EC50 J. Med. Chem. (2007) 50: 4255-4259 [PMID:17665897]
ChEMBL Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRalpha (Liver X receptor) B 7.1 pEC50 80 nM EC50 J. Med. Chem. (2005) 48: 5419-5422 [PMID:16107141]
ChEMBL Activity at human LXRalpha by Gal4 transactivation assay B 7.18 pEC50 66 nM EC50 J. Med. Chem. (2007) 50: 4255-4259 [PMID:17665897]
ChEMBL Binding affinity to human LXRalpha B 7.66 pEC50 22 nM EC50 J. Med. Chem. (2016) 59: 3264-3271 [PMID:26990539]
Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055]
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 8.66 pKi 2.2 nM Ki Eur J Med Chem (2019) 178: 458-467 [PMID:31202993]
ChEMBL Antagonist activity at LXRbeta ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay B 7.4 pIC50 39.81 nM IC50 J. Med. Chem. (2010) 53: 3412-3416 [PMID:20345102]
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 [3H]T-0901317 from human LXR beta receptor B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2006) 49: 6151-6154 [PMID:17034119]
ChEMBL Displacement of [3H]TO901317 from human recombinant LXRbeta expressed in Escherichia coli by flashplate method B 7.92 pIC50 12 nM IC50 J. Med. Chem. (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assay B 8.1 pIC50 7.94 nM IC50 J. Med. Chem. (2010) 53: 3412-3416 [PMID:20345102]
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 6.3 pEC50 501.19 nM EC50 J. Med. Chem. (2010) 53: 3412-3416 [PMID:20345102]
ChEMBL Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay B 6.38 pEC50 420 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 1274-1278 [PMID:25677664]
ChEMBL Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay F 6.39 pEC50 410 nM EC50 J. Med. Chem. (2006) 49: 6151-6154 [PMID:17034119]
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 Agonist activity at human LXRbeta by Gal4 assay B 6.41 pEC50 390 nM EC50 J. Med. Chem. (2016) 59: 3264-3271 [PMID:26990539]
ChEMBL Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay B 6.51 pEC50 310 nM EC50 J. Med. Chem. (2008) 51: 7161-7168 [PMID:18973288]
ChEMBL Agonist activity at recombinant human LXRbeta-LBD expressed in Escherichia coli BL21 (DE3) assessed as peptide D22 recruitment fluorescence polarization binding assay B 6.54 pEC50 289 nM EC50 Eur J Med Chem (2019) 178: 458-467 [PMID:31202993]
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 6.89 pEC50 130 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at LXRbeta ligand binding domain by FRET based SRC1 recruitment assay B 7.11 pEC50 78 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 2009-2012 [PMID:19264481]
ChEMBL Agonist activity at human LXRbeta assessed as association of SRC1 to LXRbeta ligand binding domain by FRET based cell-free ligand sensing assay B 7.4 pEC50 40 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 5617-5621 [PMID:19717304]
ChEMBL Agonist activity at LXRbeta LBD by HTRF cofactor peptide recruitment assay F 7.46 pEC50 35 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 7.46 pEC50 35 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 4442-4446 [PMID:17587573]
GtoPdb - - 7.52 pEC50 - - - J Med Chem (2002) 45: 1963-6 [PMID:11985463]
ChEMBL Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay F 7.57 pEC50 27 nM EC50 J. Med. Chem. (2007) 50: 4255-4259 [PMID:17665897]
ChEMBL Agonist activity at LXRbeta by FRET assay F 7.6 pEC50 25 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 1097-1100 [PMID:19167885]
ChEMBL Effective concentration for Steroid receptor coactivator-1 (SRC1) recruitment to human LXRbeta (Liver X receptor) B 7.7 pEC50 20 nM EC50 J. Med. Chem. (2005) 48: 5419-5422 [PMID:16107141]
ChEMBL Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay F 7.82 pEC50 15 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 7.82 pEC50 15 nM EC50 Bioorg. Med. Chem. Lett. (2007) 17: 3473-3479 [PMID:17416521]
ChEMBL Binding to human LXRbeta B 8.3 pEC50 5 nM EC50 J. Med. Chem. (2016) 59: 3264-3271 [PMID:26990539]
ChEMBL Activity at human LXRbeta by Gal4 transactivation assay B 8.4 pEC50 4 nM EC50 J. Med. Chem. (2007) 50: 4255-4259 [PMID:17665897]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Binding affinity to PXR by scintillation proximity binding assay B 5.7 pKi 2000 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 5617-5621 [PMID:19717304]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]