BDBM579105 US11479551, Example 16-7::US11479551, Example 16-8::US11492351, Example 16-8

SMILES Cn1ncc(c1-c1c(F)c(Cl)cc(OC2CC2)c1C#N)-c1ccc2c(c1)c(CN)n[nH]c2=O

InChI Key InChIKey=BZKIOORWZAXIBA-UHFFFAOYSA-N

Data  12 IC50  2 Kd

  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 14 hits for monomerid = 579105   

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

US Patent
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  7.07E+3nMAssay 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 DepthDetails US Patent
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  77nMAssay 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 DepthDetails US Patent
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  7.07E+3nMAssay 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 DepthDetails US Patent
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  77nMAssay 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 DepthDetails US Patent
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  6nMAssay 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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  6nMAssay 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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  653nMAssay 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
In DepthDetails PubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  653nMAssay 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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50: >5.50E+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
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataKd:  0nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant in presence of MTA by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataKd:  0.00900nMAssay Description:Binding affinity to human PRMT5 assessed as dissociation constant in presence of SAM by SPR analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMethylosome protein 50/Protein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

US Patent
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  410nMAssay Description:Inhibition of PRMT5/MEP50 (unknown origin) using Histone H2A as substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  8nMAssay 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
In DepthDetails PubMed
TargetProtein arginine N-methyltransferase 5(Homo sapiens (Human))
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM579105(US11479551, Example 16-7 | US11479551, Example 16-...)
Affinity DataIC50:  8nMAssay 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
In DepthDetails ArticlePubMed