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LigandPNGBDBM19992(2-{3-[3-({[2-chloro-3-(trifluoromethyl)phenyl]meth...)
Affinity DataEC50:  97nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM20131(5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-[(2,4...)
Affinity DataEC50:  2.30E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20132((2R)-5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-...)
Affinity DataEC50:  1.60E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20133(2-(2,3-dimethoxyphenyl)-5-(4-fluorophenyl)-3-[(2,4...)
Affinity DataEC50:  1.40E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20134(2-(2,3-dimethoxyphenyl)-5-(4-methylphenyl)-3-[(2,4...)
Affinity DataEC50:  1.40E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20135(5-(4-chlorophenyl)-2-(2-methoxyphenyl)-3-[(2,4,6-t...)
Affinity DataEC50:  180nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20136(2-(4-fluoro-2-methoxyphenyl)-5-(4-fluorophenyl)-3-...)
Affinity DataEC50:  70nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20137(2-[2-(difluoromethoxy)phenyl]-5-(4-fluorophenyl)-3...)
Affinity DataEC50:  1.90E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20138(5-(4-chlorophenyl)-2-(2,2-difluoro-2H-1,3-benzodio...)
Affinity DataEC50:  3.90E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20139(5-(4-fluorophenyl)-2-(2-methoxypyridin-3-yl)-3-[(2...)
Affinity DataEC50:  400nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20140(5-(4-chlorophenyl)-3-[(2,4-difluorophenyl)carbonyl...)
Affinity DataEC50:  6.70E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20141(5-(3,4-difluorophenyl)-2-(2,3-dimethoxyphenyl)-3-[...)
Affinity DataEC50:  1.50E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20142(3-[(3,5-difluorophenyl)carbonyl]-2-(2,3-dimethoxyp...)
Affinity DataEC50:  2.10E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20143(2-(2,3-dimethoxyphenyl)-3-[(5-fluoro-2-methylpheny...)
Affinity DataEC50:  2.40E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20144(3-[(2,6-difluoro-4-methoxyphenyl)carbonyl]-2-(2,3-...)
Affinity DataEC50:  900nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20145(3-[(4-bromo-2,6-difluorophenyl)carbonyl]-2-(2,3-di...)
Affinity DataEC50:  900nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20146(2-(2,3-dimethoxyphenyl)-5-(4-fluorophenyl)-3-[(2,4...)
Affinity DataEC50:  700nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM19992(2-{3-[3-({[2-chloro-3-(trifluoromethyl)phenyl]meth...)
Affinity DataEC50:  27nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM20131(5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-[(2,4...)
Affinity DataEC50:  300nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20132((2R)-5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-...)
Affinity DataEC50:  67nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20133(2-(2,3-dimethoxyphenyl)-5-(4-fluorophenyl)-3-[(2,4...)
Affinity DataEC50:  76nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20134(2-(2,3-dimethoxyphenyl)-5-(4-methylphenyl)-3-[(2,4...)
Affinity DataEC50:  200nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20147(5-(3,4-dichlorophenyl)-2-(2,3-dimethoxyphenyl)-3-[...)
Affinity DataEC50: >1.00E+4nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20135(5-(4-chlorophenyl)-2-(2-methoxyphenyl)-3-[(2,4,6-t...)
Affinity DataEC50:  35nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20148(5-(4-chlorophenyl)-2-(3-methoxyphenyl)-3-[(2,4,6-t...)
Affinity DataEC50:  3.70E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20136(2-(4-fluoro-2-methoxyphenyl)-5-(4-fluorophenyl)-3-...)
Affinity DataEC50:  6nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20149(5-(4-chlorophenyl)-2-[2-(trifluoromethoxy)phenyl]-...)
Affinity DataEC50:  3.40E+3nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20137(2-[2-(difluoromethoxy)phenyl]-5-(4-fluorophenyl)-3...)
Affinity DataEC50:  150nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20138(5-(4-chlorophenyl)-2-(2,2-difluoro-2H-1,3-benzodio...)
Affinity DataEC50:  800nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20139(5-(4-fluorophenyl)-2-(2-methoxypyridin-3-yl)-3-[(2...)
Affinity DataEC50:  210nMpH: 7.2 T: 2°CAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20150(5-(4-fluorophenyl)-2-(2-methoxyphenyl)-2-methyl-3-...)
Affinity DataEC50:  4.00E+3nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20151(5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-[(2-f...)
Affinity DataEC50:  7.70E+3nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20140(5-(4-chlorophenyl)-3-[(2,4-difluorophenyl)carbonyl...)
Affinity DataEC50:  980nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20152(2-(2,3-dimethoxyphenyl)-5-(4-fluorophenyl)-3-[(2,3...)
Affinity DataEC50:  970nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20153(2-(2,3-dimethoxyphenyl)-5-(4-fluorophenyl)-3-[(2,4...)
Affinity DataEC50:  600nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20141(5-(3,4-difluorophenyl)-2-(2,3-dimethoxyphenyl)-3-[...)
Affinity DataEC50:  560nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20142(3-[(3,5-difluorophenyl)carbonyl]-2-(2,3-dimethoxyp...)
Affinity DataEC50:  470nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20154(3-[(3-chlorophenyl)carbonyl]-2-(2,3-dimethoxypheny...)
Affinity DataEC50:  250nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20143(2-(2,3-dimethoxyphenyl)-3-[(5-fluoro-2-methylpheny...)
Affinity DataEC50:  140nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20144(3-[(2,6-difluoro-4-methoxyphenyl)carbonyl]-2-(2,3-...)
Affinity DataEC50:  170nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20145(3-[(4-bromo-2,6-difluorophenyl)carbonyl]-2-(2,3-di...)
Affinity DataEC50:  160nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20146(2-(2,3-dimethoxyphenyl)-5-(4-fluorophenyl)-3-[(2,4...)
Affinity DataEC50:  81nMAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20155((2S)-5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-...)
Affinity DataAssay 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...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20155((2S)-5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-...)
Affinity DataAssay 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...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20155((2S)-5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-...)
Affinity DataAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM20155((2S)-5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-...)
Affinity DataAssay Description:FRET-based co-activator recruitment assay measures agonist activities in a 384-well plate format. Reaction mixture containing His-tagged hLXR, biotin...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPolycomb protein EED(Human)
Novartis Institutes For Biomedical Research

Curated by ChEMBL
LigandPNGBDBM50259900(CHEMBL4101947)
Affinity DataKd:  3.20E+4nMAssay Description:Binding affinity to human methionine-13Cepsilon-methyl labeled PRC2-EED (76 to 441 residues) expressed in Escherichia coli BL21 (DE3) by 2D NMR metho...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetHepatocyte growth factor receptor(Human)
Novartis

US Patent
LigandPNGBDBM100728(US8507676, 78)
Affinity DataIC50: 0.400nMAssay Description:The kinase assay is based on the LanthaScreen technology. LanthaScreen is the detection of Time-Resolved Fluorescence Resonance Energy Transfer (TR-...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetHepatocyte growth factor receptor(Human)
Novartis

US Patent
LigandPNGBDBM100726(US8507676, 77-S)
Affinity DataIC50: 0.480nMAssay Description:The kinase assay is based on the LanthaScreen technology. LanthaScreen is the detection of Time-Resolved Fluorescence Resonance Energy Transfer (TR-...More data for this Ligand-Target Pair
In DepthDetails
US Patent

TargetHepatocyte growth factor receptor(Human)
Novartis

US Patent
LigandPNGBDBM163169(US9062045, 8)
Affinity DataIC50: 1nMAssay Description:The kinase assay is based on the LanthaScreen technology. LanthaScreen is the detection of Time-Resolved Fluorescence Resonance Energy Transfer (TR-F...More data for this Ligand-Target Pair
In DepthDetails
US Patent

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