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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB (change energy unit to kcal/mol)

Found 6 hits in this display   

TargetHistone-lysine N-methyltransferase SMYD3(Homo sapiens (Human))
Epizyme

Curated by ChEMBL
LigandPNGBDBM378462(6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluo...)
Affinity DataKi:  1.10nMAssay Description:Non-competitive inhibition of full length N-terminal His-tagged SMYD3 (1 to 428 residues) (unknown origin) expressed in Escherichia coli using varyin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase SMYD3(Homo sapiens (Human))
Epizyme

Curated by ChEMBL
LigandPNGBDBM378462(6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluo...)
Affinity DataKi:  1.20nMAssay Description:Non-competitive inhibition of full length N-terminal His-tagged SMYD3 (1 to 428 residues) (unknown origin) expressed in Escherichia coli using fixed ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase SMYD3(Homo sapiens (Human))
Epizyme

Curated by ChEMBL
LigandPNGBDBM378462(6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluo...)
Affinity DataIC50:  3nMAssay Description:Inhibition of full length N-terminal His-tagged SMYD3 (1 to 428 residues) (unknown origin) expressed in Escherichia coli using N-terminal GST-tagged ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistone-lysine N-methyltransferase SMYD3(Homo sapiens (Human))
Epizyme

Curated by ChEMBL
LigandPNGBDBM378462(6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluo...)
Affinity DataIC50:  3.54nMAssay Description:The assays were all performed in a buffer consisting of 25 mM Tris-Cl pH 8.0, 1 mM TCEP, 0.005% BSG, and 0.005% Tween 20, prepared on the day of use....More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetHistone-lysine N-methyltransferase SMYD3(Homo sapiens (Human))
Epizyme

Curated by ChEMBL
LigandPNGBDBM378462(6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluo...)
Affinity DataIC50:  36nMAssay Description:Inhibition of human SMYD3 expressed in HEK293T/17 cells using FLAG-tagged MEKK2 as substrate incubated for 30 mins in low air flow area followed by i...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetN-lysine methyltransferase SMYD2(Homo sapiens (Human))
Epizyme

Curated by ChEMBL
LigandPNGBDBM378462(6-chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluo...)
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of SMYD2 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed