BDBM578859 4-(aminomethyl)-6-(isothiazol-4- yl)phthalazin-1(2H)-one::US11479551, Example 4-2::US11492351, Example 4-2

SMILES NCc1n[nH]c(=O)c2ccc(cc12)-c1cnsc1

InChI Key InChIKey=LMCPTHXQJRIIJO-UHFFFAOYSA-N

Data  6 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 578859   

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

US Patent
LigandPNGBDBM578859(US11492351, Example 4-2 | 4-(aminomethyl)-6-(isoth...)
Affinity DataIC50: 490nMAssay 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
In Depth
Date in BDB:
1/20/2023
Entry Details
US Patent

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

US Patent
LigandPNGBDBM578859(US11492351, Example 4-2 | 4-(aminomethyl)-6-(isoth...)
Affinity DataIC50: 490nMAssay 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
In Depth
Date in BDB:
12/30/2022
Entry Details
US Patent

TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM578859(US11492351, Example 4-2 | 4-(aminomethyl)-6-(isoth...)
Affinity DataIC50: 710nMAssay 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
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM578859(US11492351, Example 4-2 | 4-(aminomethyl)-6-(isoth...)
Affinity DataIC50: 1.16E+4nMAssay Description:Inhibition of human PRMT5 co-complexed with MEP50 in absence of MTA using biotin labelled histone H4 peptide (1 to15) as substrate assessed as inhibi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

US Patent
LigandPNGBDBM578859(US11492351, Example 4-2 | 4-(aminomethyl)-6-(isoth...)
Affinity DataIC50: 1.38E+4nMAssay 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
In Depth
Date in BDB:
1/20/2023
Entry Details
US Patent

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

US Patent
LigandPNGBDBM578859(US11492351, Example 4-2 | 4-(aminomethyl)-6-(isoth...)
Affinity DataIC50: 1.38E+4nMAssay 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
In Depth
Date in BDB:
12/30/2022
Entry Details
US Patent