Compile Data Set for Download or QSAR
maximum 50k data
Found 19 Enz. Inhib. hit(s) for PDB: 1OSV
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  361nMpH: 7.2 T: 2°CAssay Description:To evaluate FXR activity of compounds, COS1 (ATCC) cells were transfected with hFXR expression plasmid, mouse retinoid X receptor expression plasmid,...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  10nMAssay Description:Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferas...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  98nMAssay Description:Binding affinity to FXR assessed as ligand-dependent SRC1 recruitment by FRET based co-activator assayMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  85nMAssay Description:Agonist activity at FXR (unknown origin) by reporter gene assayMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  9.90E+4nMAssay Description:Agonist activity at FXR (unknown origin) by coactivator recruitment assayMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  160nMAssay Description:Agonist activity at human FXR expressed in human HeLa cells assessed as receptor activation by BSEP promoter-driven firefly luciferase reporter gene ...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  160nMAssay Description:Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  200nMAssay Description:Agonist activity at human GST-fused FXR LBD assessed as coactivator interaction with receptor ligand binding domain by Alphascreen assayMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  99nMAssay Description:Effective concentration against Farnesoid X receptor (FXR)More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  90nMAssay Description:Binding affinity for human Farnesoid X receptor in FRET assayMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  99nMAssay Description:Activation of human farnesoid X receptorMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  99nMAssay Description:Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assayMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  550nMAssay Description:The assay utilizes non-human mammalian cells, CHO (Chinese hamster ovary) cells engineered to express human NR1H4 protein (referred to as FXR). Repor...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  550nMAssay Description:The potency and efficacy of the compounds of the invention on TGR5 receptor was evaluated using in vitro assays which carried out using the express k...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  100nMAssay Description:Agonist activity at FXR (unknown origin) assessed as recruitment of SRC1 peptide to FXR by FRET assayMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  42nMAssay Description:Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferas...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  550nMAssay Description:Determination of a ligand mediated Gal4 promoter driven transactivation to quantify ligand binding mediated activation of FXR. FXR Reporter Assay kit...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  180nMAssay Description:Agonist activity at recombinant human GST-tagged FXR LBD (193 to 472 residues) expressed in baculovirus-infected insect cells assessed as recruitment...More data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
University Di Perugia

LigandPNGBDBM21675((4R)-4-[(1S,2S,5R,7S,8R,9R,10S,11S,14R,15R)-8-ethy...)
Affinity DataEC50:  99nMAssay Description:Binding affinity for Farnesoid X Receptor (FXR)More data for this Ligand-Target Pair