BDBM21724 3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(1-methylethyl)isoxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid::3-[(E)-2-(2-chloro-4-{[3-(2,6-dichlorophenyl)-5-(propan-2-yl)-1,2-oxazol-4-yl]methoxy}phenyl)ethenyl]benzoic acid::CHEMBL318457::GW-4064
SMILES CC(C)c1onc(c1COc1ccc(\C=C\c2cccc(c2)C(O)=O)c(Cl)c1)-c1c(Cl)cccc1Cl
InChI Key InChIKey=BYTNEISLBIENSA-MDZDMXLPSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 56 hits for monomerid = 21724
Affinity DataEC50: 70nMpH: 7.2 T: 2°CAssay Description:Compounds were screened for agonist/antagonist activity on FXR-GAL4 chimeric receptors in transiently transfected HEK-293 cells. The EC50/IC50 values...More data for this Ligand-Target Pair
3D Structure (crystal)Affinity DataEC50: 400nMAssay Description:Agonist activity at human FXR transfected in CHO-K1 cells coexpressed with beta-galactosidase incubated for 3 to 16 hrs by PathHunter chemiluminescen...More data for this Ligand-Target Pair
Affinity DataEC50: 65nMAssay Description:The cell-based assay measures the ligand-mediated luminescense resulting from FXR-induced transcription of a luciferase reporter. FXR and the lucifer...More data for this Ligand-Target Pair
Affinity DataIC50: 64nM EC50: 900nMpH: 8.0 T: 2°CAssay Description:Binding affinity (IC50) was evaluated using scintillation proximity assay with radiolabeled ligand and biotinylated receptor. Because the scintillant...More data for this Ligand-Target Pair
Affinity DataIC50: 20nMAssay Description:Antagonist activity at human GST-tagged FXR after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 15nMAssay Description:Agonist activity at FXR (unknown origin) by coactivator recruitment assayMore data for this Ligand-Target Pair
Affinity DataEC50: 900nMAssay Description:Agonist activity at FXR (unknown origin) by reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 35nMAssay Description:Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assayMore data for this Ligand-Target Pair
Affinity DataEC50: 20nMAssay Description:Agonist activity at human GST-fused FXR LBD assessed as cofactor peptide interaction with receptor ligand binding domain by FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 1.50E+4nMAssay Description:Agonist activity at FXR (unknown origin) by coactivator recruitment assayMore data for this Ligand-Target Pair
Affinity DataEC50: 900nMAssay Description:Agonist activity at FXR (unknown origin) by reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 26nMAssay Description:Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 65nMAssay Description:Agonist activity at FXR (unknown origin) transfected into african green monkey CV1 cells assessed as ligand-mediated transcription by luciferase repo...More data for this Ligand-Target Pair
Affinity DataEC50: 59nMAssay Description:Agonist activity at FXR (unknown origin) assessed as ligand-mediated interaction of the SRC1 peptide with protein LBD by FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 510nMAssay 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
Affinity DataEC50: 59nMAssay Description:Agonist activity at human FXR assessed as SRC1 peptide interaction with receptor ligand binding domain by FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 65nMAssay Description:Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assayMore data for this Ligand-Target Pair
Affinity DataEC50: 20nMAssay Description:Agonist activity at GST-tagged FXR LBD (187 to 472 residues) (unknown origin) assessed as FXR interaction with b-CPSSHSSLTERHKILHRLLQEGSPS-COOH by FR...More data for this Ligand-Target Pair
Affinity DataEC50: 20nMAssay Description:Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid as...More data for this Ligand-Target Pair
Affinity DataEC50: 59nMAssay Description:Induction of SRC1 coactivator peptide binding to ligand binding domain of human FXR by FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 65nMAssay Description:Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cellsMore data for this Ligand-Target Pair
Affinity DataEC50: 30nMAssay Description:Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct r...More data for this Ligand-Target Pair
Affinity DataIC50: 112nMAssay Description:Displacement of radioligand from human FXR by scintillation proximity assayMore data for this Ligand-Target Pair
Affinity DataEC50: 910nMAssay Description:Agonist activity at Gal4-fused human FXR by luciferase reporter gene transactivation assayMore data for this Ligand-Target Pair
Affinity DataEC50: 59nMAssay Description:Agonist activity at human FXR LBD assessed as SRC1 peptide recruitment by FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 65nMAssay Description:Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expressionMore data for this Ligand-Target Pair
Affinity DataEC50: 59nMAssay Description:Agonist activity at human amino-terminal polyhistidine-tagged FXR alpha LBD (amino acids 237 to 472) assessed as cofactor peptide SRC-1 interaction w...More data for this Ligand-Target Pair
Affinity DataEC50: 65nMAssay Description:Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 15nMAssay Description:Ligand dependent recruitment of SRC1(676-700) peptide to human Farnesoid X-activated receptor by fluorescence resonance energy transfer assayMore data for this Ligand-Target Pair
Affinity DataEC50: 37nMAssay Description:Effective concentration against Farnesoid X receptor (FXR)More data for this Ligand-Target Pair
Affinity DataEC50: 70nMAssay Description:Activation of human farnesoid X receptorMore data for this Ligand-Target Pair
Affinity DataEC50: 15nMAssay Description:Agonist activity at FXRMore data for this Ligand-Target Pair
Affinity DataEC50: 753nMAssay Description:Binding affinity to human GTS-tagged FXR LBD using fluorescein-tagged SRC2-2 after 30 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 373nMAssay Description:Binding affinity to human GTS-tagged FXR LBD using fluorescein-tagged SRC2-2 after 20 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 317nMAssay Description:Binding affinity to human GTS-tagged FXR LBD using fluorescein-tagged SRC2-2 after 15 mins by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 45nMAssay Description:Agonist activity at human FXR assessed as recruitment of SRC1 peptide by TR-FRET assayMore data for this Ligand-Target Pair
Affinity DataEC50: 70nMAssay Description:Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 19nMAssay Description:Agonist activity at recombinant human GST-tagged FXR ligand binding domain (193 to 472 residues) expressed in baculovirus infected insect cells asses...More data for this Ligand-Target Pair
Affinity DataEC50: 373nMAssay Description:Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 220nMAssay Description:Agonist activity at recombinant His-tagged human FXR ligand binding domain assessed as SRC-1 coactivator recruitment after 4 hrs by luminescence anal...More data for this Ligand-Target Pair
Affinity DataEC50: 95nMAssay 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
Affinity DataEC50: 15nMAssay Description:Agonist activity at FXR (unknown origin)More data for this Ligand-Target Pair
Affinity DataEC50: 90nMAssay Description:Agonist activity at FXR (unknown origin) by cell based assayMore data for this Ligand-Target Pair
Affinity DataEC50: 70nMAssay Description:Agonist activity FXR (unknown origin)More data for this Ligand-Target Pair
Affinity DataEC50: 70nMAssay Description:Agonist activity FXR (unknown origin)More data for this Ligand-Target Pair
Affinity DataEC50: 20nMAssay Description:Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase rep...More data for this Ligand-Target Pair
Affinity DataIC50: >1.00E+4nMAssay Description:Antagonist activity at human VDR transfected in HEK293T cells measured after 24 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 13nMAssay Description:Agonist activity at human FXR expressed in human HuH7 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
Affinity DataEC50: 90nMAssay Description:Activation of human FXR LBD expressed in HEK293T cells assessed as induction of receptor activation incubated for 12 to 14 hrs by luciferase reporter...More data for this Ligand-Target Pair
Affinity DataEC50: 12nMAssay Description:Agonist activity at human FXR expressed in HEK293 cells measured after 18 hrs by steady-glo luciferase reporter gene assayMore data for this Ligand-Target Pair