Compile Data Set for Download or QSAR
Report error Found 21 Enz. Inhib. hit(s) for PDB: 4X63
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataKd:  1.10E+4nMAssay Description:Binding affinity to MTA-bound human PRMT5 assessed as dissociation constant by SPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 9nMAssay Description:Inhibition of PRMT5 in human Z138 cells assessed as reduction in symmetrical dimethylation of arginine containing substrate using SmD3 as substrate i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 22nMAssay Description:Inhibition of full length recombinant human FLAG-tagged PRMT5/full length recombinant human His6-tagged MEP50 expressed in baculovirus infected Sf9 i...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/27/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 22nMAssay Description:Inhibition of PRMT5 human PRMT5 using [3H]-SAM as substrate by radioactive methylation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 22nMAssay Description:Inhibition of PRMT5 (unknown origin) by biochemical assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/25/2023
Entry Details
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 22nMAssay Description:Inhibition of human full length FLAG-tagged PRMT5/human His6-tagged MEP50 expressed in baculovirus-infected Sf9 cells assessed as reduction in tritiu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/23/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 22nMAssay Description:Inhibition of human recombinant PRMT5/MEP50 expressed in 293-F cells using histone 4 peptide as substrate after 90 mins in presence of [3H]SAM by aut...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 22nMAssay Description:Inhibition of PRMT5 (unknown origin) using H4R3 as substrate by HTRF assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 30nMAssay Description:Inhibition of human PRMT5/MEP50 assessed as reduction in methyltransferase activity using histone 4 peptide as substrate in presence of [3H]SAM incub...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 47nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues) /human N-terminal His-tagged MEP50 (2 to end residues) expressed in ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/19/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 47nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues)/human N-terminal His-tagged MEP50 (2 to end residues) expressed in H...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 47nMAssay Description:Inhibition of recombinant human N-terminal FLAG-tagged PRMT5 (2 to end residues)/human N-terminal His-tagged MEP50 (2 to end residues) expressed in H...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/26/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 60nMAssay 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
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 85nMAssay Description:General Procedure for PRMT5/MEP50 AlphaLISA Enzyme Inhibitory Assays: Assays were performed in the buffer consisting of 50 mM Tris, pH 8.5, 5 mM MgCl...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/14/2023
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Epizyme

US Patent
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/26/2021
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/20/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Epizyme

US Patent
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Epizyme

US Patent
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/15/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Epizyme

US Patent
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 100nMAssay Description:The assays were all performed in a buffer consisting of 20 mM Bicine (pH=7.6), 1 mM TCEP, 0.005% BSG, and 0.002% Tween20, prepared on the day of use....More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/12/2018
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 110nMAssay 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
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM177922(US9675614, 166 | US10307413, Compound 337 | US1039...)
Affinity DataIC50: 1.00E+5nMAssay Description:Displacement of fluorophore-labeled RIOK1 from human PRMT5/WDR77 hetero octameric complex expressed in Sf9 cells by competition fluorescence polariza...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)