Target
Oxysterols receptor LXR-beta [154-461]
Ligand
BDBM19993
Substrate
BDBM19993
Meas. Tech.
LXR Binding Assay and hLXR beta Reporter Assay
pH
7.4±n/a
Temperature
277.15±n/a K
IC50
10±n/a nM
EC50
16±n/a nM
Comments
Efficacy=100% in transfected hLXRbeta reporter cell line assay.
Citation
 Hu, BCollini, MUnwalla, RMiller, CSinghaus, RQuinet, ESavio, DHalpern, ABasso, MKeith, JClerin, VChen, LResmini, CLiu, QYFeingold, IHuselton, CAzam, FFarnegardh, MEnroth, CBonn, TGoos-Nilsson, AWilhelmsson, ANambi, PWrobel, J Discovery of phenyl acetic acid substituted quinolines as novel liver X receptor agonists for the treatment of atherosclerosis. J Med Chem 49:6151-4 (2006) [PubMed]  Article
Target
Name:
Oxysterols receptor LXR-beta [154-461]
Synonyms:
Liver X Receptor beta (LXR-beta) | Nuclear orphan receptor LXR-beta | Nuclear receptor NER | Nuclear receptor subfamily 1 group H member 2 | Oxysterols receptor LXR-beta | Ubiquitously-expressed nuclear receptor
Type:
Receptor
Mol. Mass.:
34695.52
Organism:
Homo sapiens (Human)
Description:
LXR beta ligand binding domain (amino acid residues 154-461) with an N-terminal biotinylation tag expressed in E.coli, was used for the binding assays.
Residue:
308
Sequence:
MREQCVLSEEQIRKKKIRKQQQQQESQSQSQSPVGPQGSSSSASGPGASPGGSEAGSQGSGEGEGVQLTAAQELMIQQLVAAQLQCNKRSFSDQPKVTPWPLGADPQSRDARQQRFAHFTELAIISVQEIVDFAKQVPGFLQLGREDQIALLKASTIEIMLLETARRYNHETECITFLKDFTYSKDDFHRAGLQVEFINPIFEFSRAMRRLGLDDAEYALLIAINIFSADRPNVQEPGRVEALQQPYVEALLSYTRIKRPQDQLRFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVH
  
Inhibitor
Name:
BDBM19993
Synonyms:
CHEMBL62136 | N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide | T 0901317 | T0901317 | TO-901317 | US10543183, Compound TO901317 | US10669296, Compound TO901317 | US10945978, Compound 1 | [3H]T0901317
Type:
Small organic molecule
Emp. Form.:
C17H12F9NO3S
Mol. Mass.:
481.333
SMILES:
OC(c1ccc(cc1)N(CC(F)(F)F)S(=O)(=O)c1ccccc1)(C(F)(F)F)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM19993
Synonyms:
CHEMBL62136 | N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide | T 0901317 | T0901317 | TO-901317 | US10543183, Compound TO901317 | US10669296, Compound TO901317 | US10945978, Compound 1 | [3H]T0901317
Type:
Small organic molecule
Emp. Form.:
C17H12F9NO3S
Mol. Mass.:
481.333
SMILES:
OC(c1ccc(cc1)N(CC(F)(F)F)S(=O)(=O)c1ccccc1)(C(F)(F)F)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: