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TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 579105BDBM579105(US11492351, Example 16-8 | 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 Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 415557BDBM415557(US10428104, Example 88)
Affinity DataKi:  0.0200nMAssay Description:Inhibition of PRMT5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50597886BDBM50597886(CHEMBL5180177)
Affinity DataKi:  0.0200nMAssay Description:Binding affinity to PRMT5 (unknown origin) assessed as inhibition constantMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandChemical structure of BindingDB Monomer ID 50462572BDBM50462572(CHEMBL4249337)
Affinity DataIC50: 0.130nMAssay Description:Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50597880BDBM50597880(CHEMBL5203719)
Affinity DataIC50: 0.130nMAssay Description:Inhibition of PRMT5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50462572BDBM50462572(CHEMBL4249337)
Affinity DataIC50: 0.140nMAssay Description:Inhibition of PRMT5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50462572BDBM50462572(CHEMBL4249337)
Affinity DataIC50: 0.140nMAssay Description:Inhibition of full-length human N-terminal FLAG-tagged PRMT5 expressed in Sf9 insect cells using histone H2A as peptide after 120 mins in presence of...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
LigandChemical structure of BindingDB Monomer ID 50523646BDBM50523646(CHEMBL4541714)
Affinity DataIC50: 0.160nMAssay Description:Inhibition of PRMT5 in human A549 cells assessed as reduction in sDMA production after 48 hrs by Hoechst Stain/HCS CellMask Deep Red Stain based immu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50523629BDBM50523629(CHEMBL4564327)
Affinity DataIC50: 0.160nMAssay Description:Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50523642BDBM50523642(CHEMBL4539612)
Affinity DataIC50: 0.200nMAssay Description:Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 533479BDBM533479(US11220524, Example 86-B | (Z)-7-((1R,2S,3R,4S)-4-...)
Affinity DataIC50: 0.200nMAssay Description:Compounds were solubilized, and 3-fold diluted in 100% DMSO. These diluted compounds were further diluted in the assay buffer (50 mM Tris-HCl, pH 8.5...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/14/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 533464BDBM533464(US11220524, Example 105 | (E)-7-((2R,3R,4S,5S)-5-(...)
Affinity DataIC50: 0.200nMAssay Description:Compounds were solubilized, and 3-fold diluted in 100% DMSO. These diluted compounds were further diluted in the assay buffer (50 mM Tris-HCl, pH 8.5...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/14/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 515298BDBM515298(US11098059, Example 6 | US11098059, Example 2)
Affinity DataIC50: 0.210nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 515310BDBM515310(US11098059, Example 14)
Affinity DataIC50: 0.240nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50523646BDBM50523646(CHEMBL4541714)
Affinity DataIC50: 0.25nMAssay Description:Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50462572BDBM50462572(CHEMBL4249337)
Affinity DataIC50: 0.25nMAssay Description:Inhibition of PRMT5 in human A549 cells assessed as reduction in sDMA production after 48 hrs by Hoechst Stain/HCS CellMask Deep Red Stain based immu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandChemical structure of BindingDB Monomer ID 515307BDBM515307(US11098059, Example 11 | 6'-(1-cyclopropyl-1H-1,2,...)
Affinity DataIC50: 0.290nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 533440BDBM533440(US11220524, Example 81 | (2R,3S,4R,5R)-2-((R)-(3,4...)
Affinity DataIC50: 0.300nMAssay Description:Compounds were solubilized, and 3-fold diluted in 100% DMSO. These diluted compounds were further diluted in the assay buffer (50 mM Tris-HCl, pH 8.5...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/14/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 515299BDBM515299(US11098059, Example 7 | US11098059, Example 3)
Affinity DataIC50: 0.310nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 50523655BDBM50523655(CHEMBL4577464)
Affinity DataIC50: 0.320nMAssay Description:Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 533482BDBM533482(US11220524, Example 87-B | (Z)-7-((1R,2S,3R,4S)-4-...)
Affinity DataIC50: 0.330nMAssay Description:Compounds were solubilized, and 3-fold diluted in 100% DMSO. These diluted compounds were further diluted in the assay buffer (50 mM Tris-HCl, pH 8.5...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/14/2022
Entry Details
US Patent

TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50238541BDBM50238541(CHEMBL4092336)
Affinity DataIC50: 0.330nMAssay Description:Inhibition of PRMT5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandChemical structure of BindingDB Monomer ID 515323BDBM515323(US11098059, Example 27 | 6-(hexahydro-3,6- epimino...)
Affinity DataIC50: 0.350nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 515309BDBM515309(US11098059, Example 13)
Affinity DataIC50: 0.360nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50523641BDBM50523641(CHEMBL4543007)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of PRMT5 in human A549 cells assessed as reduction in sDMA production after 48 hrs by Hoechst Stain/HCS CellMask Deep Red Stain based immu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 50523643BDBM50523643(CHEMBL4454890)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of full-length human N-terminal FLAG-tagged PRMT5/full length N-terminal His6-tagged MEP50 (unknown origin) expressed in baculovirus infec...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 515306BDBM515306(US11098059, Example 10 | 6-(1-cyclopropyl-1H-1,2,4...)
Affinity DataIC50: 0.400nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50597881BDBM50597881(CHEMBL5187591)
Affinity DataIC50: 0.400nMAssay Description:Inhibition of PRMT5 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/22/2023
Entry Details
PubMed
LigandChemical structure of BindingDB Monomer ID 533414BDBM533414(US11220524, Example 66 | 7-((2R,3R,4S,5R)-5-((R)-(...)
Affinity DataIC50: 0.400nMAssay Description:Compounds were solubilized, and 3-fold diluted in 100% DMSO. These diluted compounds were further diluted in the assay buffer (50 mM Tris-HCl, pH 8.5...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/14/2022
Entry Details
US Patent

TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50637554BDBM50637554(CHEMBL5560909)
Affinity DataIC50: 0.420nMAssay Description:Inhibition of PRMT5 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50637320BDBM50637320(CHEMBL5559161)
Affinity DataIC50: 0.420nMAssay Description:Inhibition of PRMT5 (unknown origin) by HotSpot profiling analysisMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In Depth
Date in BDB:
10/11/2025
Entry Details
PubMed
TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50612685BDBM50612685(CHEMBL5283866)
Affinity DataIC50: 0.420nMAssay Description:Inhibition of human PRMT5 by fluorescence-based SAHH-coupled assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
LigandChemical structure of BindingDB Monomer ID 515321BDBM515321(US11098059, Example 25 | 2-((R)-2-hydroxy-2-((S)- ...)
Affinity DataIC50: 0.440nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 515305BDBM515305(US11098059, Example 9 | 6-(1-cyclopropyl-1H-1,2,4-...)
Affinity DataIC50: 0.470nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 515319BDBM515319(US11098059, Example 23)
Affinity DataIC50: 0.5nMAssay Description:In this assay, the potency (IC50) of each compound was determined from a twenty-point (1:2 serial dilution; top compound concentration of 100000 nM) ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578831BDBM578831(US11492351, Example 4-107 | 2-(4-(4-(aminomethyl)-...)
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
In Depth
Date in BDB:
12/30/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578895BDBM578895(US11492351, Example 4-78 | 4-(aminomethyl)-6-(5-(2...)
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
In Depth
Date in BDB:
12/30/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578819BDBM578819(US11492351, Example 4-100 | US11479551, Example 4-...)
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
In Depth
Date in BDB:
1/20/2023
Entry Details
US Patent

TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 50566330BDBM50566330(CHEMBL4874774)
Affinity DataEC50: <0.5nMAssay Description:Inhibition of PRMT5 (unknown origin) assessed as inhibition of symmetric dimethylation of arginine incubated for 3 days by fluorescence based cellula...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2022
Entry Details Article
PubMed
LigandChemical structure of BindingDB Monomer ID 435525BDBM435525(US10570140, Example 12 | (2R,3S,4R,5R)-2-(((2-amin...)
Affinity DataIC50: 0.5nMAssay Description:Compounds were solubilized and 3-fold diluted in 100% DMSO. These diluted compounds were further diluted in the assay buffer (50 mM Tris-HCl, pH 8.5,...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2020
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578821BDBM578821(US11492351, Example 4-101 | 2-(4-(4-(aminomethyl)-...)
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
In Depth
Date in BDB:
1/20/2023
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578819BDBM578819(US11492351, Example 4-100 | US11479551, Example 4-...)
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
In Depth
Date in BDB:
12/30/2022
Entry Details
US Patent

TargetProtein arginine N-methyltransferase 5(Human)
Mirati Therapeutics

Curated by ChEMBL
LigandChemical structure of BindingDB Monomer ID 435525BDBM435525(US10570140, Example 12 | (2R,3S,4R,5R)-2-(((2-amin...)
Affinity DataIC50: 0.5nMAssay Description:Compounds were solubilized and 3-fold diluted in 100% DMSO. These diluted compounds were further diluted in the assay buffer (50 mM Tris-HCl, pH 8.5,...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/16/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578823BDBM578823(US11492351, Example 4-103 | 2-(4-(4-(aminomethyl)-...)
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
In Depth
Date in BDB:
1/20/2023
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 435525BDBM435525(US10570140, Example 12 | (2R,3S,4R,5R)-2-(((2-amin...)
Affinity DataIC50: 0.5nMAssay Description:Compounds were solubilized and 3-fold diluted in 100% DMSO. These diluted compounds were further diluted in the assay buffer (50 mM Tris-HCl, pH 8.5,...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/3/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578821BDBM578821(US11492351, Example 4-101 | 2-(4-(4-(aminomethyl)-...)
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
In Depth
Date in BDB:
12/30/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578825BDBM578825(US11492351, Example 4-104 | 2-(4-(4-(aminomethyl)-...)
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
In Depth
Date in BDB:
1/20/2023
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578823BDBM578823(US11492351, Example 4-103 | 2-(4-(4-(aminomethyl)-...)
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
In Depth
Date in BDB:
12/30/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578825BDBM578825(US11492351, Example 4-104 | 2-(4-(4-(aminomethyl)-...)
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
In Depth
Date in BDB:
12/30/2022
Entry Details
US Patent

LigandChemical structure of BindingDB Monomer ID 578829BDBM578829(US11492351, Example 4-106 | 2-(4-(4-(aminomethyl)-...)
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
In Depth
Date in BDB:
1/20/2023
Entry Details
US Patent

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