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Compile Data Set for Download or QSAR

Found 69 hits Enz. Inhib. hit(s) with Target = 'Protein arginine N-methyltransferase 8'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM178103
PNG
(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Show SMILES CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN
Show InChI InChI=1S/C17H25N3O/c1-13(2)21-16-6-4-14(5-7-16)17-11-19-10-15(17)12-20(3)9-8-18/h4-7,10-11,13,19H,8-9,12,18H2,1-3H3
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1.30n/a 5n/an/an/an/an/an/a



University of Toronto



Assay Description
In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...


ACS Chem Biol 11: 772-81 (2016)


Article DOI: 10.1021/acschembio.5b00839
BindingDB Entry DOI: 10.7270/Q2765D4H
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM178102
PNG
(N1-Methyl-N1-((4-(3-(trifluoromethyl)phenyl)-1H-py...)
Show SMILES CN(CCN)Cc1c[nH]cc1-c1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C15H18F3N3/c1-21(6-5-19)10-12-8-20-9-14(12)11-3-2-4-13(7-11)15(16,17)18/h2-4,7-9,20H,5-6,10,19H2,1H3
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17n/a 42n/an/an/an/an/an/a



University of Toronto



Assay Description
In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...


ACS Chem Biol 11: 772-81 (2016)


Article DOI: 10.1021/acschembio.5b00839
BindingDB Entry DOI: 10.7270/Q2765D4H
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM178101
PNG
(N1-Methyl-N1-((5-(3-(trifluoromethyl)phenyl)-2H-1,...)
Show SMILES CN(CCN)Cc1n[nH]nc1-c1cccc(c1)C(F)(F)F
Show InChI InChI=1S/C13H16F3N5/c1-21(6-5-17)8-11-12(19-20-18-11)9-3-2-4-10(7-9)13(14,15)16/h2-4,7H,5-6,8,17H2,1H3,(H,18,19,20)
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1.50E+3n/a 3.00E+3n/an/an/an/an/an/a



University of Toronto



Assay Description
In brief, the tritiated S-adenosyl-L-methionine (3HSAM, PerkinElmer Life Sciences) was used as the donor of methyl group. The (3H) methylated biotin ...


ACS Chem Biol 11: 772-81 (2016)


Article DOI: 10.1021/acschembio.5b00839
BindingDB Entry DOI: 10.7270/Q2765D4H
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50243294
PNG
(CHEMBL4094513)
Show SMILES CN(CCN)Cc1ccccc1Sc1ccccc1Cl
Show InChI InChI=1S/C16H19ClN2S/c1-19(11-10-18)12-13-6-2-4-8-15(13)20-16-9-5-3-7-14(16)17/h2-9H,10-12,18H2,1H3
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n/an/a 1.10n/an/an/an/an/an/a



Zhejiang Sci-Tech University

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin) incubated for 15 mins followed by substrate addition measured after 60 mins by AlphaLisa method


J Med Chem 60: 8888-8905 (2017)


Article DOI: 10.1021/acs.jmedchem.7b01134
BindingDB Entry DOI: 10.7270/Q27D2XHK
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095355
PNG
(CHEMBL3589029)
Show SMILES CN(CCN)Cc1cn[nH]c1-c1ccc(Oc2ccccc2)cc1
Show InChI InChI=1S/C19H22N4O/c1-23(12-11-20)14-16-13-21-22-19(16)15-7-9-18(10-8-15)24-17-5-3-2-4-6-17/h2-10,13H,11-12,14,20H2,1H3,(H,21,22)
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n/an/a 2n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM178103
PNG
(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Show SMILES CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN
Show InChI InChI=1S/C17H25N3O/c1-13(2)21-16-6-4-14(5-7-16)17-11-19-10-15(17)12-20(3)9-8-18/h4-7,10-11,13,19H,8-9,12,18H2,1-3H3
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n/an/a 4n/an/an/an/an/an/a



Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin) using biotinylated histone H4 (1 to 24 residues) as substrate in presence of [3H]SAM by scintillation proximity ...


J Med Chem 62: 5414-5433 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00297
BindingDB Entry DOI: 10.7270/Q289199B
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM178103
PNG
(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Show SMILES CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN
Show InChI InChI=1S/C17H25N3O/c1-13(2)21-16-6-4-14(5-7-16)17-11-19-10-15(17)12-20(3)9-8-18/h4-7,10-11,13,19H,8-9,12,18H2,1-3H3
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n/an/a 4n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of PRMT8 (unknown origin) by scintillation proximity assay


Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c02160
BindingDB Entry DOI: 10.7270/Q20V8HN0
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM178103
PNG
(MS023 (Compound 3) | N1-((4-(4-isopropoxyphenyl)-1...)
Show SMILES CC(C)Oc1ccc(cc1)-c1c[nH]cc1CN(C)CCN
Show InChI InChI=1S/C17H25N3O/c1-13(2)21-16-6-4-14(5-7-16)17-11-19-10-15(17)12-20(3)9-8-18/h4-7,10-11,13,19H,8-9,12,18H2,1-3H3
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n/an/a 4n/an/an/an/an/an/a



Icahn School of Medicine at Mount Sinai

Curated by ChEMBL


Assay Description
Inhibition of human PRMT8 assessed as inhibition of methylation activity using biotin-labeled peptide as substrate and [3H]-SAM by scintillation prox...


J Med Chem 59: 9124-9139 (2016)


Article DOI: 10.1021/acs.jmedchem.6b01033
BindingDB Entry DOI: 10.7270/Q2028TGJ
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095354
PNG
(CHEMBL3589030)
Show SMILES CC(C)Oc1ccc(cc1Cl)-c1[nH]ncc1CN(C)CCN
Show InChI InChI=1S/C16H23ClN4O/c1-11(2)22-15-5-4-12(8-14(15)17)16-13(9-19-20-16)10-21(3)7-6-18/h4-5,8-9,11H,6-7,10,18H2,1-3H3,(H,19,20)
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n/an/a 7n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095432
PNG
(CHEMBL3589026)
Show SMILES CC(C)Oc1ccc(cc1)-c1[nH]ncc1CN(C)CCN
Show InChI InChI=1S/C16H24N4O/c1-12(2)21-15-6-4-13(5-7-15)16-14(10-18-19-16)11-20(3)9-8-17/h4-7,10,12H,8-9,11,17H2,1-3H3,(H,18,19)
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n/an/a 10n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095356
PNG
(CHEMBL3589028)
Show SMILES CC(C)Cc1ccc(cc1)-c1[nH]ncc1CN(C)CCN
Show InChI InChI=1S/C17H26N4/c1-13(2)10-14-4-6-15(7-5-14)17-16(11-19-20-17)12-21(3)9-8-18/h4-7,11,13H,8-10,12,18H2,1-3H3,(H,19,20)
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n/an/a 10n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095353
PNG
(CHEMBL3589031)
Show SMILES CNCCN(C)Cc1cn[nH]c1-c1ccc(OC(C)C)c(Cl)c1
Show InChI InChI=1S/C17H25ClN4O/c1-12(2)23-16-6-5-13(9-15(16)18)17-14(10-20-21-17)11-22(4)8-7-19-3/h5-6,9-10,12,19H,7-8,11H2,1-4H3,(H,20,21)
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n/an/a 10n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095357
PNG
(CHEMBL3589027)
Show SMILES CNCCN(C)Cc1cn[nH]c1-c1ccc(OC(C)C)cc1
Show InChI InChI=1S/C17H26N4O/c1-13(2)22-16-7-5-14(6-8-16)17-15(11-19-20-17)12-21(4)10-9-18-3/h5-8,11,13,18H,9-10,12H2,1-4H3,(H,19,20)
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n/an/a 14n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095347
PNG
(CHEMBL3589037)
Show SMILES CNCCN(C)Cc1cn[nH]c1-c1cc(OCCC2CCCCC2)cc(c1)C(F)(F)F
Show InChI InChI=1S/C23H33F3N4O/c1-27-9-10-30(2)16-19-15-28-29-22(19)18-12-20(23(24,25)26)14-21(13-18)31-11-8-17-6-4-3-5-7-17/h12-15,17,27H,3-11,16H2,1-2H3,(H,28,29)
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n/an/a 21n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095352
PNG
(CHEMBL3589032)
Show SMILES CNCCN(C)Cc1cnn(C)c1-c1ccc(OC(C)C)c(Cl)c1
Show InChI InChI=1S/C18H27ClN4O/c1-13(2)24-17-7-6-14(10-16(17)19)18-15(11-21-23(18)5)12-22(4)9-8-20-3/h6-7,10-11,13,20H,8-9,12H2,1-5H3
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n/an/a 22n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095351
PNG
(CHEMBL3589033)
Show SMILES CCC(CO)Oc1ccc(cc1)-c1[nH]ncc1CN(C)CCNC
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n/an/a 22n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095348
PNG
(CHEMBL3589036)
Show SMILES CNCCN(C)Cc1cn[nH]c1-c1cc(OCCc2ccccc2)cc(c1)C(F)(F)F
Show InChI InChI=1S/C23H27F3N4O/c1-27-9-10-30(2)16-19-15-28-29-22(19)18-12-20(23(24,25)26)14-21(13-18)31-11-8-17-6-4-3-5-7-17/h3-7,12-15,27H,8-11,16H2,1-2H3,(H,28,29)
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n/an/a 23n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095433
PNG
(CHEMBL3589913)
Show SMILES CCOc1ccc(cc1)-c1[nH]ncc1CN(C)CCNC
Show InChI InChI=1S/C16H24N4O/c1-4-21-15-7-5-13(6-8-15)16-14(11-18-19-16)12-20(3)10-9-17-2/h5-8,11,17H,4,9-10,12H2,1-3H3,(H,18,19)
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n/an/a 28n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095442
PNG
(CHEMBL3589038)
Show SMILES CNCCN(C)Cc1cn[nH]c1-c1cc(OC(CO)CC(C)C)cc(c1)C(F)(F)F
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n/an/a 44n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095350
PNG
(CHEMBL3589034)
Show SMILES CNCCN(C)Cc1cn[nH]c1-c1ccc(OC(CO)C(C)C)cc1
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n/an/a 55n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095435
PNG
(CHEMBL3590417)
Show SMILES CNCCN(C)Cc1n[nH]cc1-c1ccc(Oc2ccccc2C(=O)NC)cc1
Show InChI InChI=1S/C22H27N5O2/c1-23-12-13-27(3)15-20-19(14-25-26-20)16-8-10-17(11-9-16)29-21-7-5-4-6-18(21)22(28)24-2/h4-11,14,23H,12-13,15H2,1-3H3,(H,24,28)(H,25,26)
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n/an/a 65n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095434
PNG
(CHEMBL3589912)
Show SMILES CN(CCN)Cc1cn[nH]c1-c1ccc(F)cc1
Show InChI InChI=1S/C13H17FN4/c1-18(7-6-15)9-11-8-16-17-13(11)10-2-4-12(14)5-3-10/h2-5,8H,6-7,9,15H2,1H3,(H,16,17)
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n/an/a 67n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095349
PNG
(CHEMBL3589035)
Show SMILES CC(C)Oc1c(Cl)cc(cc1C(F)(F)F)-c1c[nH]nc1CN(C)CCN
Show InChI InChI=1S/C17H22ClF3N4O/c1-10(2)26-16-13(17(19,20)21)6-11(7-14(16)18)12-8-23-24-15(12)9-25(3)5-4-22/h6-8,10H,4-5,9,22H2,1-3H3,(H,23,24)
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n/an/a 70n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50511923
PNG
(CHEMBL4463793)
Show SMILES CN(CCN)Cc1c[nH]cc1-c1cccc(NC(=O)C=C)c1
Show InChI InChI=1S/C17H22N4O/c1-3-17(22)20-15-6-4-5-13(9-15)16-11-19-10-14(16)12-21(2)8-7-18/h3-6,9-11,19H,1,7-8,12,18H2,2H3,(H,20,22)
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n/an/a 110n/an/an/an/an/an/a



Icahn School of Medicine at Mount Sinai

Curated by ChEMBL


Assay Description
Inhibition of human PRMT8 using [3H]SAM as donor and [3H]methylated biotin-labeled peptide as substrate by scintillation proximity assay


J Med Chem 63: 5477-5487 (2020)


Article DOI: 10.1021/acs.jmedchem.0c00406
BindingDB Entry DOI: 10.7270/Q2BG2S9V
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50511921
PNG
(CHEMBL4544587)
Show SMILES CCC(=O)Nc1cccc(c1)-c1c[nH]cc1CN(C)CCN
Show InChI InChI=1S/C17H24N4O/c1-3-17(22)20-15-6-4-5-13(9-15)16-11-19-10-14(16)12-21(2)8-7-18/h4-6,9-11,19H,3,7-8,12,18H2,1-2H3,(H,20,22)
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n/an/a 130n/an/an/an/an/an/a



Icahn School of Medicine at Mount Sinai

Curated by ChEMBL


Assay Description
Inhibition of human PRMT8 using [3H]SAM as donor and [3H]methylated biotin-labeled peptide as substrate by scintillation proximity assay


J Med Chem 63: 5477-5487 (2020)


Article DOI: 10.1021/acs.jmedchem.0c00406
BindingDB Entry DOI: 10.7270/Q2BG2S9V
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095438
PNG
(CHEMBL3589042)
Show SMILES CNCCN(C)Cc1c[nH]nc1-c1ccc(Oc2cccc(c2)C(=O)N(C)C)cc1
Show InChI InChI=1S/C23H29N5O2/c1-24-12-13-28(4)16-19-15-25-26-22(19)17-8-10-20(11-9-17)30-21-7-5-6-18(14-21)23(29)27(2)3/h5-11,14-15,24H,12-13,16H2,1-4H3,(H,25,26)
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n/an/a 179n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095441
PNG
(CHEMBL3589039)
Show SMILES CNCCN(C)Cc1c[nH]nc1-c1ccc(O[C@H]2C[C@@H](C2)OCCC2CCOCC2)cc1 |r,wU:17.17,wD:19.22,(9.1,4.97,;7.93,4.58,;7.61,3.08,;6.15,2.59,;5.83,1.08,;6.75,.26,;4.37,.6,;4.06,-.91,;5.09,-2.05,;4.31,-3.38,;2.81,-3.06,;2.67,-1.54,;1.33,-.77,;1.33,.77,;,1.54,;-1.33,.77,;-2.67,1.54,;-4,.77,;-4.35,-.7,;-5.84,-.3,;-5.45,1.19,;-7.17,-1.07,;-8.5,-.31,;-9.84,-1.08,;-11.17,-.31,;-12.51,-1.08,;-13.84,-.31,;-13.84,1.23,;-12.51,2,;-11.17,1.23,;-1.33,-.77,;,-1.54,)|
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Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095436
PNG
(CHEMBL3589043)
Show SMILES CNCCN(C)Cc1n[nH]cc1-c1ccc(Oc2cccc(c2)C(=O)N(C)C)cc1
Show InChI InChI=1S/C23H29N5O2/c1-24-12-13-28(4)16-22-21(15-25-26-22)17-8-10-19(11-9-17)30-20-7-5-6-18(14-20)23(29)27(2)3/h5-11,14-15,24H,12-13,16H2,1-4H3,(H,25,26)
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n/an/a 347n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095440
PNG
(CHEMBL3589040)
Show SMILES CN(CCN)Cc1c[nH]nc1-c1ccc(OCCCN2CCOCC2)cc1
Show InChI InChI=1S/C20H31N5O2/c1-24(9-7-21)16-18-15-22-23-20(18)17-3-5-19(6-4-17)27-12-2-8-25-10-13-26-14-11-25/h3-6,15H,2,7-14,16,21H2,1H3,(H,22,23)
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Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50194758
PNG
(CHEMBL3970878)
Show SMILES CNCCN1CCC(CC1)OCc1cccc(c1)-c1ccccc1
Show InChI InChI=1S/C21H28N2O/c1-22-12-15-23-13-10-21(11-14-23)24-17-18-6-5-9-20(16-18)19-7-3-2-4-8-19/h2-9,16,21-22H,10-15,17H2,1H3
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Icahn School of Medicine at Mount Sinai

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin) assessed as inhibition of methylation activity measured after 3 hrs using [3H]-SAM by scintillation proximity as...


J Med Chem 59: 9124-9139 (2016)


Article DOI: 10.1021/acs.jmedchem.6b01033
BindingDB Entry DOI: 10.7270/Q2028TGJ
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
CHEMBL5266562
PNG
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Citation and Details
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50598021
PNG
(CHEMBL5191769)
Show SMILES COC(=O)c1cc(O)c2cc(NC(=O)NCCCCNC(=N)NCCC[C@H]3O[C@H]([C@H](O)[C@@H]3O)n3cnc4c(N)ncnc34)ccc2c1 |r|
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n/an/a 1.41E+3n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00252
BindingDB Entry DOI: 10.7270/Q2DF6W8F
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50095439
PNG
(CHEMBL3589041)
Show SMILES CN(CCN)Cc1c[nH]nc1-c1ccc(cc1)N1CCN(CC1)C(=O)Cc1ccccc1
Show InChI InChI=1S/C25H32N6O/c1-29(12-11-26)19-22-18-27-28-25(22)21-7-9-23(10-8-21)30-13-15-31(16-14-30)24(32)17-20-5-3-2-4-6-20/h2-10,18H,11-17,19,26H2,1H3,(H,27,28)
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n/an/a 1.50E+3n/an/an/an/an/an/a



Epizyme, Inc.

Curated by ChEMBL


Assay Description
Inhibition of N-terminal GST tagged full-length human PRMT8 expressed in Escherichia coli (BL21(DE3) pre-incubated for 30 mins before addition of a [...


ACS Med Chem Lett 6: 655-9 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00071
BindingDB Entry DOI: 10.7270/Q20003V2
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50194756
PNG
(CHEMBL3961701)
Show SMILES CNCCN1CCC(CC1)OCc1ccccc1
Show InChI InChI=1S/C15H24N2O/c1-16-9-12-17-10-7-15(8-11-17)18-13-14-5-3-2-4-6-14/h2-6,15-16H,7-13H2,1H3
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n/an/a 1.60E+3n/an/an/an/an/an/a



Icahn School of Medicine at Mount Sinai

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin) assessed as inhibition of methylation activity measured after 3 hrs using [3H]-SAM by scintillation proximity as...


J Med Chem 59: 9124-9139 (2016)


Article DOI: 10.1021/acs.jmedchem.6b01033
BindingDB Entry DOI: 10.7270/Q2028TGJ
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50070953
PNG
(CHEMBL3409550)
Show SMILES [Br-].CC1(C)\C(=C/C=C/C2=[N+](CCCc3ccccc3)c3ccc4ccccc4c3C2(C)C)N(CCCc2ccccc2)c2ccc3ccccc3c12 |c:7|
Show InChI InChI=1S/C49H49N2/c1-48(2)44(50(34-16-22-36-18-7-5-8-19-36)42-32-30-38-24-11-13-26-40(38)46(42)48)28-15-29-45-49(3,4)47-41-27-14-12-25-39(41)31-33-43(47)51(45)35-17-23-37-20-9-6-10-21-37/h5-15,18-21,24-33H,16-17,22-23,34-35H2,1-4H3/q+1
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n/an/a 1.74E+3n/an/an/an/an/an/a



The University of Georgia

Curated by ChEMBL


Assay Description
Displacement of [3H]-SAM from recombinant His6-tagged PRMT8 (unknown origin) expressed in Escherichia coli BL21(DE3) incubated for 5 mins prior to H4...


J Med Chem 58: 1228-43 (2015)


Article DOI: 10.1021/jm501452j
BindingDB Entry DOI: 10.7270/Q29S1SQN
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50194772
PNG
(CHEMBL3955728)
Show SMILES CNCCN1CCC(CC1)OCc1cccc(F)c1
Show InChI InChI=1S/C15H23FN2O/c1-17-7-10-18-8-5-15(6-9-18)19-12-13-3-2-4-14(16)11-13/h2-4,11,15,17H,5-10,12H2,1H3
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n/an/a 1.85E+3n/an/an/an/an/an/a



Icahn School of Medicine at Mount Sinai

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin) assessed as inhibition of methylation activity measured after 3 hrs using [3H]-SAM by scintillation proximity as...


J Med Chem 59: 9124-9139 (2016)


Article DOI: 10.1021/acs.jmedchem.6b01033
BindingDB Entry DOI: 10.7270/Q2028TGJ
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50598022
PNG
(CHEMBL5173678)
Show SMILES COC(=O)c1cc(O)c2cc(NC(=O)NCCCCNC(=N)NC\C=C\[C@H]3O[C@H]([C@H](O)[C@@H]3O)n3cnc4c(N)ncnc34)ccc2c1 |r|
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n/an/a 1.95E+3n/an/an/an/an/an/a


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Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00252
BindingDB Entry DOI: 10.7270/Q2DF6W8F
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50158094
PNG
(CHEMBL3780926)
Show SMILES NCCN1CCC(Cc2ccccc2)CC1
Show InChI InChI=1S/C14H22N2/c15-8-11-16-9-6-14(7-10-16)12-13-4-2-1-3-5-13/h1-5,14H,6-12,15H2
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n/an/a 2.10E+3n/an/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Inhibition of human PRMT8 using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity as...


J Med Chem 59: 1176-83 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01772
BindingDB Entry DOI: 10.7270/Q2SF2Z11
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50525201
PNG
(CHEMBL4463124)
Show SMILES CNC[C@@H](O)CN1CCc2c(C1)cccc2OCc1ccc(cc1)-c1nccs1 |r|
Show InChI InChI=1S/C23H27N3O2S/c1-24-13-20(27)15-26-11-9-21-19(14-26)3-2-4-22(21)28-16-17-5-7-18(8-6-17)23-25-10-12-29-23/h2-8,10,12,20,24,27H,9,11,13-16H2,1H3/t20-/m1/s1
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n/an/a 3.70E+3n/an/an/an/an/an/a



Chinese Academy of Sciences

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin) preincubated for 15 mins followed by substrate addition and measured after 60 mins by AlphaLisa assay


J Med Chem 62: 5414-5433 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00297
BindingDB Entry DOI: 10.7270/Q289199B
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50598018
PNG
(CHEMBL5180108)
Show SMILES COC(=O)c1cc(O)c2ccc(NC(=O)NCCCCCCNC(=N)NC[C@H]3O[C@H]([C@H](O)[C@@H]3O)n3cnc4c(N)ncnc34)cc2c1 |r|
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n/an/a 3.82E+3n/an/an/an/an/an/a


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Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00252
BindingDB Entry DOI: 10.7270/Q2DF6W8F
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50598019
PNG
(CHEMBL5186617)
Show SMILES COC(=O)c1cc(O)c2cc(NC(=O)NCCCCCCCNC(=N)NC[C@H]3O[C@H]([C@H](O)[C@@H]3O)n3cnc4c(N)ncnc34)ccc2c1 |r|
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n/an/a 5.84E+3n/an/an/an/an/an/a


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Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00252
BindingDB Entry DOI: 10.7270/Q2DF6W8F
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50598017
PNG
(CHEMBL5206272)
Show SMILES COC(=O)c1cc(O)c2cc(NC(=O)NCCCCCNC(=N)NC[C@H]3O[C@H]([C@H](O)[C@@H]3O)n3cnc4c(N)ncnc34)ccc2c1 |r|
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n/an/a 5.87E+3n/an/an/an/an/an/a


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Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00252
BindingDB Entry DOI: 10.7270/Q2DF6W8F
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50598020
PNG
(CHEMBL5202088)
Show SMILES COC(=O)c1cc(O)c2cc(NC(=O)NCCCCNC(=N)NCC[C@H]3O[C@H]([C@H](O)[C@@H]3O)n3cnc4c(N)ncnc34)ccc2c1 |r|
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n/an/a 6.00E+3n/an/an/an/an/an/a


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Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00252
BindingDB Entry DOI: 10.7270/Q2DF6W8F
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50532871
PNG
(CHEMBL4470484)
Show SMILES CN(CCN)Cc1ccccc1
Show InChI InChI=1S/C10H16N2/c1-12(8-7-11)9-10-5-3-2-4-6-10/h2-6H,7-9,11H2,1H3
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n/an/a 6.00E+3n/an/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin)


J Med Chem 59: 6838-47 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00668
BindingDB Entry DOI: 10.7270/Q2445QZC
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50532871
PNG
(CHEMBL4470484)
Show SMILES CN(CCN)Cc1ccccc1
Show InChI InChI=1S/C10H16N2/c1-12(8-7-11)9-10-5-3-2-4-6-10/h2-6H,7-9,11H2,1H3
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n/an/a 6.00E+3n/an/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin)


J Med Chem 59: 6838-47 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00668
BindingDB Entry DOI: 10.7270/Q2445QZC
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50158095
PNG
(CHEMBL3780444)
Show SMILES CNCCN(C)C
Show InChI InChI=1S/C5H14N2/c1-6-4-5-7(2)3/h6H,4-5H2,1-3H3
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CHEMBL
MCE
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UniChem

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Article
PubMed
n/an/a 7.00E+3n/an/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Inhibition of human PRMT8 using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity as...


J Med Chem 59: 1176-83 (2016)


Article DOI: 10.1021/acs.jmedchem.5b01772
BindingDB Entry DOI: 10.7270/Q2SF2Z11
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50550091
PNG
(CHEMBL4648477)
Show SMILES NC(=N)c1ccc(Nc2ccc(cc2)-c2cc3ccc(cc3[nH]2)C(N)=N)cc1
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n/an/a 8.20E+3n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of recombinant His-tagged human PRMT8 expressed in Escherichia coli BL21 (DE3) using biotin-labeled histone H4-20 peptide as substrate inc...


Citation and Details

Article DOI: 10.1039/d0md00259c
BindingDB Entry DOI: 10.7270/Q29P3583
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50598015
PNG
(CHEMBL5199380)
Show SMILES COC(=O)c1cc(O)c2cc(NC(=O)NCCCNC(=N)NC[C@H]3O[C@H]([C@H](O)[C@@H]3O)n3cnc4c(N)ncnc34)ccc2c1 |r|
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n/an/a 8.29E+3n/an/an/an/an/an/a


TBA



Citation and Details

Article DOI: 10.1021/acs.jmedchem.2c00252
BindingDB Entry DOI: 10.7270/Q2DF6W8F
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50532860
PNG
(CHEMBL4445795)
Show SMILES CNCCN1CCCC1
Show InChI InChI=1S/C7H16N2/c1-8-4-7-9-5-2-3-6-9/h8H,2-7H2,1H3
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UniChem
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PubMed
n/an/a 1.00E+4n/an/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin)


J Med Chem 59: 6838-47 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00668
BindingDB Entry DOI: 10.7270/Q2445QZC
More data for this
Ligand-Target Pair
Protein arginine N-methyltransferase 8


(Homo sapiens (Human))
BDBM50532860
PNG
(CHEMBL4445795)
Show SMILES CNCCN1CCCC1
Show InChI InChI=1S/C7H16N2/c1-8-4-7-9-5-2-3-6-9/h8H,2-7H2,1H3
PDB

UniProtKB/SwissProt

GoogleScholar
AffyNet 
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PC cid
PC sid
UniChem
Article
PubMed
n/an/a 1.00E+4n/an/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Inhibition of PRMT8 (unknown origin)


J Med Chem 59: 6838-47 (2016)


Article DOI: 10.1021/acs.jmedchem.6b00668
BindingDB Entry DOI: 10.7270/Q2445QZC
More data for this
Ligand-Target Pair
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