BDBM579030 2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin-6-yl)-1-methyl-1H- pyrazol-5-yl)benzo[b]thiophene-3- carbonitrile::US11479551, Example 4-242::US11492351, Example 4-242

SMILES Cn1ncc(c1-c1sc2ccccc2c1C#N)-c1ccc2c(c1)c(CN)n[nH]c2=O

InChI Key InChIKey=RDTXSYQRBOBLFV-UHFFFAOYSA-N

Data  7 IC50

PDB links: 1 PDB ID matches this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 7 hits for monomerid = 579030   

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

US Patent
LigandPNGBDBM579030(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  102nMAssay 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 sidPDB
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM579030(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  102nMAssay 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 sidPDB
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579030(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  5nMAssay 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 sidPDB
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579030(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50: >1.00E+3nMAssay Description:Inhibition of PRMT5 methyltransferase activity in human HCT-116 cells expressing wild type MTAP assessed as inhibition of PRMT5-mediated SDMA modific...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579030(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  37nMAssay Description:Inhibition of PRMT5 (unknown origin) using H2A and 3H-SAM as substrates preincubated for 20 mins followed by substrate addition incubated for 60 mins...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sidPDB
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579030(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50:  5nMAssay 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 sidPDB
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579030(2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin...)
Affinity DataIC50: >1.00E+3nMAssay 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 sidPDB