Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | 7.90 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline Curated by ChEMBL | Assay Description Displacement of [N-methyl-3H]T1317 from human biotinylated LXRbeta LBD after 3 hrs by LEAD seeker binding assay | J Med Chem 53: 3412-6 (2010) Article DOI: 10.1021/jm901797p BindingDB Entry DOI: 10.7270/Q2NP25P6 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta [154-461] (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB MMDB KEGG UniProtKB/SwissProt B.MOAD DrugBank GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | 12 | n/a | 310 | n/a | n/a | 7.4 | 4 |
Wyeth Research | Assay Description Binding reaction was initiated by adding a dilution series of test compound in tracer solution to LXR-coated flash plates. Each concentration of test... | J Med Chem 51: 7161-8 (2008) Article DOI: 10.1021/jm800799q BindingDB Entry DOI: 10.7270/Q2XW4H4G | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta [154-461] (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB MMDB KEGG UniProtKB/SwissProt B.MOAD DrugBank GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | 12 | n/a | 410 | n/a | n/a | 7.4 | 4 |
Wyeth Research | Assay Description Binding reaction was initiated by adding a dilution series of test compound in tracer solution to LXR-coated flash plates. Each concentration of test... | J Med Chem 49: 6151-4 (2006) Article DOI: 10.1021/jm0609566 BindingDB Entry DOI: 10.7270/Q20863KH | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | 23 | n/a | n/a | n/a | n/a | n/a | n/a |
GNF | Assay Description SPA assays were run in displacement mode using 30 nM [3H]-GW3965. Ligands were tested in 12-point dose-response curves starting at 20 uM. IC50 values... | J Med Chem 50: 4255-9 (2007) Article DOI: 10.1021/jm070453f BindingDB Entry DOI: 10.7270/Q2BK19N6 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | 30 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline Research and Development Curated by ChEMBL | Assay Description Displacement of [N-methyl-3H]GW0438 from human biotinylated LXRbeta ligand binding domain | J Med Chem 51: 5758-65 (2008) Article DOI: 10.1021/jm800612u BindingDB Entry DOI: 10.7270/Q28052FN | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | 40 | n/a | n/a | n/a | n/a | n/a | n/a |
GlaxoSmithKline Curated by ChEMBL | Assay Description Antagonist activity at LXRbeta ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cel... | J Med Chem 53: 3412-6 (2010) Article DOI: 10.1021/jm901797p BindingDB Entry DOI: 10.7270/Q2NP25P6 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 40 | n/a | n/a | n/a | n/a |
GlaxoSmithKline Curated by ChEMBL | Assay Description Agonist activity at human LXRbeta assessed as association of SRC1 to LXRbeta ligand binding domain by FRET based cell-free ligand sensing assay | Bioorg Med Chem Lett 19: 5617-21 (2009) Article DOI: 10.1016/j.bmcl.2009.08.036 BindingDB Entry DOI: 10.7270/Q20865CN | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 501 | n/a | n/a | n/a | n/a |
GlaxoSmithKline Curated by ChEMBL | Assay Description Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 b... | J Med Chem 53: 3412-6 (2010) Article DOI: 10.1021/jm901797p BindingDB Entry DOI: 10.7270/Q2NP25P6 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 420 | n/a | n/a | n/a | n/a |
Kowa Co., Ltd Curated by ChEMBL | Assay Description Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay | Bioorg Med Chem Lett 25: 1274-8 (2015) Article DOI: 10.1016/j.bmcl.2015.01.047 BindingDB Entry DOI: 10.7270/Q2CC12BH | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 400 | n/a | n/a | n/a | n/a |
Kowa Co., Ltd Curated by ChEMBL | Assay Description Agonist activity at LXRbeta (unknown origin) | Bioorg Med Chem Lett 25: 2668-74 (2015) Article DOI: 10.1016/j.bmcl.2015.04.080 BindingDB Entry DOI: 10.7270/Q2PN97CM | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 390 | n/a | n/a | n/a | n/a |
Vitae Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Agonist activity at human LXRbeta by Gal4 assay | J Med Chem 59: 3264-71 (2016) Article DOI: 10.1021/acs.jmedchem.5b02029 BindingDB Entry DOI: 10.7270/Q2XP76V7 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 5 | n/a | n/a | n/a | n/a |
Vitae Pharmaceuticals, Inc. Curated by ChEMBL | Assay Description Binding to human LXRbeta | J Med Chem 59: 3264-71 (2016) Article DOI: 10.1021/acs.jmedchem.5b02029 BindingDB Entry DOI: 10.7270/Q2XP76V7 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 130 | n/a | n/a | n/a | n/a |
AstraZeneca R&D Södertälje Curated by ChEMBL | Assay Description Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay | Bioorg Med Chem Lett 19: 2009-12 (2009) Article DOI: 10.1016/j.bmcl.2009.02.039 BindingDB Entry DOI: 10.7270/Q20C4VNS | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 78 | n/a | n/a | n/a | n/a |
AstraZeneca R&D Södertälje Curated by ChEMBL | Assay Description Agonist activity at LXRbeta ligand binding domain (unknown origin) by FRET based SRC1 recruitment assay | Bioorg Med Chem Lett 19: 2009-12 (2009) Article DOI: 10.1016/j.bmcl.2009.02.039 BindingDB Entry DOI: 10.7270/Q20C4VNS | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 35 | n/a | n/a | n/a | n/a |
Tanabe Research Laboratories USA | Assay Description Polyhistidine-tagged human LXR ligand-binding domain was mixed with the test compound, biotin-SRC1 peptide, streptavidin-allophycocyanin, and europiu... | Bioorg Med Chem Lett 17: 4442-6 (2007) Article DOI: 10.1016/j.bmcl.2007.06.017 BindingDB Entry DOI: 10.7270/Q2N58JQ9 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 25 | n/a | n/a | 7.5 | 22 |
GSK | Assay Description The LXR LiSA measures the ligand-dependent recruitment of a 25 amino acid fragment of the steroid receptor coactivator 1 (SRC1) to the ligand-binding... | Bioorg Med Chem Lett 19: 1097-100 (2009) Article DOI: 10.1016/j.bmcl.2009.01.004 BindingDB Entry DOI: 10.7270/Q28W3BMD | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 20 | n/a | n/a | 7.5 | 22 |
GlaxoSmithKline | Assay Description The LXR LiSA measures the ligand-dependent recruitment of a 25 amino acid fragment of the steroid receptor coactivator 1 (SRC1) to the ligand-binding... | J Med Chem 48: 5419-22 (2005) Article DOI: 10.1021/jm050532w BindingDB Entry DOI: 10.7270/Q26T0JXG | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB US Patent | n/a | n/a | n/a | n/a | 40 | n/a | n/a | n/a | n/a |
The Rockefeller University US Patent | Assay Description As used herein, reference to the activity of an LXR agonist at LXRα and LXRβ refer to the activity as measured using the ligand sensing ass... | US Patent US10543183 (2020) BindingDB Entry DOI: 10.7270/Q2JW8H8C | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Oxysterols receptor LXR-beta (249/249 = 100%)† (Homo sapiens (Human)) | BDBM19992 (2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methy...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE KEGG MMDB PC cid PC sid PDB UniChem Patents Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 27 | n/a | n/a | 7.2 | 37 |
GNF | Assay Description FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin... | J Med Chem 50: 4255-9 (2007) Article DOI: 10.1021/jm070453f BindingDB Entry DOI: 10.7270/Q2BK19N6 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) |