BDBM291687 N-((5-Fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methylpyridin-3-yl)-[1,2,4]triazolo[4,3-c]pyrimidin-5-amine::US11207325, Example 2::US9580437, Example 2
SMILES Cc1ncccc1-c1cnc(NCc2c3CCOc3ccc2F)n2cnnc12
InChI Key InChIKey=XLIBABIFOBYHSV-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 29 hits for monomerid = 291687
TargetAlpha-2A adrenergic receptor(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 9.60E+3nMAssay Description:Agonist activity at adrenergic receptor alpha2a (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 5.90nMAssay Description:Binding affinity to his tagged EED (1 to 441 residues) (unknown origin) incubated for 20 mins in presence of biotinylated H3K27me3 peptide (19 to 33 ...More data for this Ligand-Target Pair
Affinity DataKd: 0.400nMAssay Description:Inhibition of EED (unknown origin) assessed dissociation constantMore data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of EED (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 60nMAssay Description:Inhibition of EED (unknown origin) by alpha screen binding assayMore data for this Ligand-Target Pair
Affinity DataKd: 0.400nMAssay Description:Binding affinity to EED (unknown origin) assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of EED (unknown origin)More data for this Ligand-Target Pair
Affinity DataIC50: 1.80E+4nMAssay Description:Inhibition of CYP3A5 in human liver microsomes by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 1.80E+4nMAssay Description:Inhibition of CYP2C9 human liver microsomes using diclofenac as substrate incubated for 15 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 1.80E+4nMAssay Description:Inhibition of CYP2D6 human liver microsomes using bufuralol as substrate incubated for 15 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 1.80E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 10 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of hERG potassium channel in HEK293 cells by Q-patch clamp assayMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of hERG potassium channel in HEK293 cells by manual patch clamp assayMore data for this Ligand-Target Pair
TargetSynaptic vesicular amine transporter(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 1.80E+3nMAssay Description:Inhibition of vesicular monoamine transporter 2 (unknown origin)More data for this Ligand-Target Pair
TargetMuscarinic acetylcholine receptor M2(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 8.90E+3nMAssay Description:Agonist activity at muscarinic M2 receptor (unknown origin)More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 5.90nMpH: 8.0Assay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
TargetcAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Novartis Institutes For Biomedical Research
Curated by ChEMBL
Affinity DataIC50: 6.40E+3nMAssay Description:Inhibition of human Phosphodiesterase 4DMore data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using bufuralol as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 5nMAssay Description:Inhibition of EED in human G-401 cells assessed as reduction in H3K27 trimethylation incubated for 48 hrs by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 4.80nMAssay Description:Inhibition of EED in human G-401 cells assessed as reduction in H3K27 trimethylation incubated for 48 hrs by HTRF assayMore data for this Ligand-Target Pair
Affinity DataIC50: 2.60nMAssay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Affinity DataIC50: 8.90nMAssay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair
Affinity DataIC50: 5.90nMAssay Description:To assess the compounds potency in the EED-H3K27Me3 competition binding assay, compounds were serially diluted 3-fold in DMSO to obtain a total of tw...More data for this Ligand-Target Pair
Affinity DataIC50: 4.5nMAssay Description:Inhibition of biotinylated H3K27me3 peptide (19 to 33 residues) binding to His-tagged EED (1 to 441 residues) (unknown origin) incubated for 30 mins ...More data for this Ligand-Target Pair
Affinity DataKd: 400nMAssay Description:Binding affinity to EED (unknown origin) assessed as dissociation constant by SPR analysisMore data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 2.60nMAssay Description:Cell lysates were transferred to the wells of a 384-well plate and the final volume was adjusted to 50 μL per well with PBS. The plate was seale...More data for this Ligand-Target Pair
TargetHistone-lysine N-methyltransferase EZH2/Polycomb protein EED/Polycomb protein SUZ12(Human)
Novartis
US Patent
Novartis
US Patent
Affinity DataIC50: 8.90nMpH: 8.0Assay Description:Representative compounds of the present disclosure were serially and separately diluted 3-fold in DMSO to obtain a total of eight or twelve concentra...More data for this Ligand-Target Pair