BDBM578831 2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin-6-yl)-1-methyl-1H- pyrazol-5-yl)-6-methoxybenzonitrile::US11479551, Example 4-107::US11492351, Example 4-107

SMILES COc1cccc(-c2c(cnn2C)-c2ccc3c(c2)c(CN)n[nH]c3=O)c1C#N

InChI Key InChIKey=OBJJGGPWWQFRHU-UHFFFAOYSA-N

Data  9 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 9 hits for monomerid = 578831   

TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  0.5nMAssay Description:The assay uses purified human, PRMT5 enzyme to convert S-adenosyl-L-[methyl-3H]methionine plus histone H4 L-arginine to S-adenosyl-L-homocysteine plu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  37nMAssay Description:The assay uses purified human, PRMT5 enzyme to convert S-adenosyl-L-[methyl-3H]methionine plus histone H4 L-arginine to S-adenosyl-L-homocysteine plu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  760nMAssay Description:The assay uses purified human, PRMT5 enzyme to convert S-adenosyl-L-[methyl-3H]methionine plus histone H4 L-arginine to S-adenosyl-L-homocysteine plu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  0.5nMAssay Description:The assay uses purified human, PRMT5 enzyme to convert S-adenosyl-L-[methyl-3H]methionine plus histone H4 L-arginine to S-adenosyl-L-homocysteine plu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50: >1.00E+4nMAssay Description:Inhibition of PRMT5 methyltransferase activity in human HCT-116 cells expressing wild type MTAP assessed as inhibition of PRMT5- mediated SDMA modifi...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  760nMAssay Description:The assay uses purified human, PRMT5 enzyme to convert S-adenosyl-L-[methyl-3H]methionine plus histone H4 L-arginine to S-adenosyl-L-homocysteine plu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  1.00E+3nMAssay Description:Inhibition of MTA-bound human PRMT5 co-complexed with MEP50 using biotin labelled histone H4 peptide (1 to 15) as substrate assessed as inhibition of...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  62nMAssay Description:Inhibition of PRMT5 methyltransferase activity in MTAP knockout human HCT-116 cells assessed as inhibition of PRMT5- mediated SDMA modification level...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM578831(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  37nMAssay Description:The assay uses purified human, PRMT5 enzyme to convert S-adenosyl-L-[methyl-3H]methionine plus histone H4 L-arginine to S-adenosyl-L-homocysteine plu...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent