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Compile Data Set for Download or QSAR

Found 31 hits Enz. Inhib. hit(s) with Target = 'PRMT5/MEP50 complex'   
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
PRMT5/MEP50 complex


(Homo sapiens (Human))
BDBM50089221
PNG
(CHEMBL3577854)
Show SMILES CCNC(=O)NCCSC[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cnc2c(N)ncnc12
Show InChI InChI=1S/C15H23N7O4S/c1-2-17-15(25)18-3-4-27-5-8-10(23)11(24)14(26-8)22-7-21-9-12(16)19-6-20-13(9)22/h6-8,10-11,14,23-24H,2-5H2,1H3,(H2,16,19,20)(H2,17,18,25)/t8-,10-,11-,14-/m1/s1
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n/an/an/a 2.50E+4n/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Binding affinity to human full length PRMT5-MEP50 complex by Surface plasmon resonance method


ACS Med Chem Lett 6: 408-12 (2015)


Article DOI: 10.1021/ml500467h
BindingDB Entry DOI: 10.7270/Q2Q81FSZ
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50431676
PNG
(CHEMBL2349526)
Show SMILES N[C@@H](CCSC[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cc(Br)c2c(N)ncnc12)C(O)=O
Show InChI InChI=1S/C15H20BrN5O5S/c16-6-3-21(13-9(6)12(18)19-5-20-13)14-11(23)10(22)8(26-14)4-27-2-1-7(17)15(24)25/h3,5,7-8,10-11,14,22-23H,1-2,4,17H2,(H,24,25)(H2,18,19,20)/t7-,8+,10+,11+,14+/m0/s1
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1.15E+3n/an/an/an/an/an/an/an/a



EntreMed Inc.

Curated by ChEMBL


Assay Description
Inhibition of PRMT5 (unknown origin) using [3H]SAM after 1 hr by scintillation proximity assay


Bioorg Med Chem 21: 1787-94 (2013)


Article DOI: 10.1016/j.bmc.2013.01.049
BindingDB Entry DOI: 10.7270/Q24F1S41
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223126
PNG
(P5i-7)
Show SMILES NC(=S)N\N=C\c1ccc(o1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C12H10ClN3OS/c13-9-3-1-8(2-4-9)11-6-5-10(17-11)7-15-16-12(14)18/h1-7H,(H3,14,16,18)/b15-7+
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n/an/a 720n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM8460
PNG
(5-{[5-(4-chlorophenyl)furan-2-yl]methylidene}-2-su...)
Show SMILES Clc1ccc(cc1)-c1ccc(C=C2C(=O)NC(=S)NC2=O)o1
Show InChI InChI=1S/C15H9ClN2O3S/c16-9-3-1-8(2-4-9)12-6-5-10(21-12)7-11-13(19)17-15(22)18-14(11)20/h1-7H,(H2,17,18,19,20,22)
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n/an/a 6.70E+4n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223127
PNG
(2-((5-phenylfuran-2-yl)methylene)hydrazinecarboxam...)
Show SMILES NC(=O)N\N=C\c1ccc(o1)-c1ccccc1
Show InChI InChI=1S/C12H11N3O2/c13-12(16)15-14-8-10-6-7-11(17-10)9-4-2-1-3-5-9/h1-8H,(H3,13,15,16)/b14-8+
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n/an/a 1.20E+4n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223128
PNG
(2-((5-(3-fluorophenyl)furan-2-yl)methylene)hydrazi...)
Show SMILES NC(=O)N\N=C\c1ccc(o1)-c1cccc(F)c1
Show InChI InChI=1S/C12H10FN3O2/c13-9-3-1-2-8(6-9)11-5-4-10(18-11)7-15-16-12(14)17/h1-7H,(H3,14,16,17)/b15-7+
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n/an/a 1.40E+4n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223129
PNG
(2-((5-(4-fluorophenyl)furan-2-yl)methylene)hydrazi...)
Show SMILES NC(=O)N\N=C\c1ccc(o1)-c1ccc(F)cc1
Show InChI InChI=1S/C12H10FN3O2/c13-9-3-1-8(2-4-9)11-6-5-10(18-11)7-15-16-12(14)17/h1-7H,(H3,14,16,17)/b15-7+
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n/an/a 1.20E+4n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223130
PNG
(2-((5-(4-nitrophenyl)furan-2-yl)methylene)hydrazin...)
Show SMILES NC(=O)N\N=C\c1ccc(o1)-c1ccc(cc1)[N+]([O-])=O
Show InChI InChI=1S/C12H10N4O4/c13-12(17)15-14-7-10-5-6-11(20-10)8-1-3-9(4-2-8)16(18)19/h1-7H,(H3,13,15,17)/b14-7+
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n/an/a 1.80E+4n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223131
PNG
(2-((5-(4-methoxyphenyl)furan-2-yl)methylene)hydraz...)
Show SMILES COc1ccc(cc1)-c1ccc(\C=N\NC(N)=O)o1
Show InChI InChI=1S/C13H13N3O3/c1-18-10-4-2-9(3-5-10)12-7-6-11(19-12)8-15-16-13(14)17/h2-8H,1H3,(H3,14,16,17)/b15-8+
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n/an/a 2.10E+3n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223132
PNG
(2-((5-(4-aminophenyl)furan-2-yl)methylene)hydrazin...)
Show SMILES NC(=O)N\N=C\c1ccc(o1)-c1ccc(N)cc1
Show InChI InChI=1S/C12H12N4O2/c13-9-3-1-8(2-4-9)11-6-5-10(18-11)7-15-16-12(14)17/h1-7H,13H2,(H3,14,16,17)/b15-7+
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n/an/a 4.00E+4n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223133
PNG
(2-((5-(2-amino-4-chlorophenyl)furan-2-yl)methylene...)
Show SMILES NC(=O)N\N=C\c1ccc(o1)-c1ccc(Cl)cc1N
Show InChI InChI=1S/C12H11ClN4O2/c13-7-1-3-9(10(14)5-7)11-4-2-8(19-11)6-16-17-12(15)18/h1-6H,14H2,(H3,15,17,18)/b16-6+
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n/an/a 1.30E+4n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223134
PNG
(2-((4′-chloro-[1,1′-biphenyl]-3-yl)met...)
Show SMILES NC(=O)N\N=C\c1cccc(c1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C14H12ClN3O/c15-13-6-4-11(5-7-13)12-3-1-2-10(8-12)9-17-18-14(16)19/h1-9H,(H3,16,18,19)/b17-9+
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n/an/a 3.80E+3n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223135
PNG
(2-((5-(4-chlorophenyl)pyridin-3-yl)methylene)hydra...)
Show SMILES NC(=O)N\N=C\c1cncc(c1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C13H11ClN4O/c14-12-3-1-10(2-4-12)11-5-9(6-16-8-11)7-17-18-13(15)19/h1-8H,(H3,15,18,19)/b17-7+
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n/an/a 6.90E+3n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM223136
PNG
(2-((6-(4-chlorophenyl)pyridin-2-yl)methylene)hydra...)
Show SMILES NC(=O)N\N=C\c1cccc(n1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C13H11ClN4O/c14-10-6-4-9(5-7-10)12-3-1-2-11(17-12)8-16-18-13(15)19/h1-8H,(H3,15,18,19)/b16-8+
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n/an/a 3.50E+3n/an/an/an/an/an/a



Sichuan University



Assay Description
All in vitro enzymatic assays were carried out by Shanghai ChemPartner Co. (998 Halei Road, Pudong New Area, Shanghai, 201203, China). To measure the...


Chem Biol Drug Des 89: 585-598 (2017)


Article DOI: 10.1111/cbdd.12881
BindingDB Entry DOI: 10.7270/Q21V5CTR
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50388602
PNG
(FURAMIDINE)
Show SMILES NC(=N)c1ccc(cc1)-c1ccc(o1)-c1ccc(cc1)C(N)=N
Show InChI InChI=1S/C18H16N4O/c19-17(20)13-5-1-11(2-6-13)15-9-10-16(23-15)12-3-7-14(8-4-12)18(21)22/h1-10H,(H3,19,20)(H3,21,22)
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n/an/a 1.66E+5n/an/an/an/an/an/a



The University of Georgia

Curated by ChEMBL


Assay Description
Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 min...


J Med Chem 57: 2611-22 (2014)


Article DOI: 10.1021/jm401884z
BindingDB Entry DOI: 10.7270/Q2ZW1NFB
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50007728
PNG
(CHEMBL424121 | DB867)
Show SMILES NC(=N)c1ccc(cc1)-c1ccc(o1)-c1ccc(nc1)C(N)=N
Show InChI InChI=1S/C17H15N5O/c18-16(19)11-3-1-10(2-4-11)14-7-8-15(23-14)12-5-6-13(17(20)21)22-9-12/h1-9H,(H3,18,19)(H3,20,21)
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n/an/a 1.86E+5n/an/an/an/an/an/a



The University of Georgia

Curated by ChEMBL


Assay Description
Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 min...


J Med Chem 57: 2611-22 (2014)


Article DOI: 10.1021/jm401884z
BindingDB Entry DOI: 10.7270/Q2ZW1NFB
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50210461
PNG
((stilbamidine)4-[2-[4-amino(imino)methylphenyl]-(E...)
Show SMILES NC(=N)c1ccc(\C=C\c2ccc(cc2)C(N)=N)cc1
Show InChI InChI=1S/C16H16N4/c17-15(18)13-7-3-11(4-8-13)1-2-12-5-9-14(10-6-12)16(19)20/h1-10H,(H3,17,18)(H3,19,20)/b2-1+
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n/an/a 4.41E+4n/an/an/an/an/an/a



The University of Georgia

Curated by ChEMBL


Assay Description
Inhibition of HA-tagged recombinant PRMT5 (unknown origin) expressed in HEK293T cells using [3H]SAM and histone H4 (1 to 20) as substrate after 8 min...


J Med Chem 57: 2611-22 (2014)


Article DOI: 10.1021/jm401884z
BindingDB Entry DOI: 10.7270/Q2ZW1NFB
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50051117
PNG
(CHEMBL3318285)
Show SMILES COc1cc2nc(nc(NCCCCCN3CCCC3)c2cc1OC)N1CCCC1
Show InChI InChI=1S/C23H35N5O2/c1-29-20-16-18-19(17-21(20)30-2)25-23(28-14-8-9-15-28)26-22(18)24-10-4-3-5-11-27-12-6-7-13-27/h16-17H,3-15H2,1-2H3,(H,24,25,26)
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n/an/a>1.00E+5n/an/an/an/an/an/a



University of North Carolina at Chapel Hill

Curated by ChEMBL


Assay Description
Inhibition of PRMT5 (unknown origin) assessed as incorporation of tritium-labeled methyl group to lysine or arginine residues of peptide substrate by...


J Med Chem 57: 6822-33 (2014)


Article DOI: 10.1021/jm500871s
BindingDB Entry DOI: 10.7270/Q2J9681Q
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50070950
PNG
(CHEMBL3409562)
Show SMILES CCCCN1\C(=C\C=C(/Br)\C=C\C2=[N+](CCCC)c3ccc(Br)cc3C2(C)C)C(C)(C)c2cc(Br)ccc12
Show InChI InChI=1S/C33H40Br3N2/c1-7-9-19-37-28-15-11-24(35)21-26(28)32(3,4)30(37)17-13-23(34)14-18-31-33(5,6)27-22-25(36)12-16-29(27)38(31)20-10-8-2/h11-18,21-22H,7-10,19-20H2,1-6H3/q+1
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n/an/a 3.54E+4n/an/an/an/an/an/a



The University of Georgia

Curated by ChEMBL


Assay Description
Displacement of [3H]-SAM from recombinant His6-tagged PRMT5 (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 methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50070951
PNG
(CHEMBL3409558)
Show SMILES C(CN1\C(Sc2c1ccc1ccccc21)=C\C=C\c1sc2c(ccc3ccccc23)[n+]1CCCc1ccccc1)Cc1ccccc1
Show InChI InChI=1S/C43H37N2S2/c1-3-14-32(15-4-1)18-12-30-44-38-28-26-34-20-7-9-22-36(34)42(38)46-40(44)24-11-25-41-45(31-13-19-33-16-5-2-6-17-33)39-29-27-35-21-8-10-23-37(35)43(39)47-41/h1-11,14-17,20-29H,12-13,18-19,30-31H2/q+1
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n/an/a 7.04E+3n/an/an/an/an/an/a



The University of Georgia

Curated by ChEMBL


Assay Description
Displacement of [3H]-SAM from recombinant His6-tagged PRMT5 (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 methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50070952
PNG
(CHEMBL3409555)
Show SMILES CCCCN1\C(Sc2ccc(Br)cc12)=C\C=C\c1sc2ccc(Br)cc2[n+]1CCCC
Show InChI InChI=1S/C25H27Br2N2S2/c1-3-5-14-28-20-16-18(26)10-12-22(20)30-24(28)8-7-9-25-29(15-6-4-2)21-17-19(27)11-13-23(21)31-25/h7-13,16-17H,3-6,14-15H2,1-2H3/q+1
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n/an/a 8.36E+3n/an/an/an/an/an/a



The University of Georgia

Curated by ChEMBL


Assay Description
Displacement of [3H]-SAM from recombinant His6-tagged PRMT5 (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 methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50070953
PNG
(CHEMBL3409550)
Show SMILES CC1(C)\C(=C/C=C/C2=[N+](CCCc3ccccc3)c3ccc4ccccc4c3C2(C)C)N(CCCc2ccccc2)c2ccc3ccccc3c12
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 1.40E+3n/an/an/an/an/an/a



The University of Georgia

Curated by ChEMBL


Assay Description
Displacement of [3H]-SAM from recombinant His6-tagged PRMT5 (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 methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50089221
PNG
(CHEMBL3577854)
Show SMILES CCNC(=O)NCCSC[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cnc2c(N)ncnc12
Show InChI InChI=1S/C15H23N7O4S/c1-2-17-15(25)18-3-4-27-5-8-10(23)11(24)14(26-8)22-7-21-9-12(16)19-6-20-13(9)22/h6-8,10-11,14,23-24H,2-5H2,1H3,(H2,16,19,20)(H2,17,18,25)/t8-,10-,11-,14-/m1/s1
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n/an/a>5.00E+4n/an/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Inhibition of human full length PRMT5 expressed in Sf9 cells


ACS Med Chem Lett 6: 408-12 (2015)


Article DOI: 10.1021/ml500467h
BindingDB Entry DOI: 10.7270/Q2Q81FSZ
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50009672
PNG
(AdoHcy | CHEMBL418052 | S-(5'-adenosyl)-L-homocyst...)
Show SMILES N[C@@H](CCSC[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cnc2c(N)ncnc12)C(O)=O
Show InChI InChI=1S/C14H20N6O5S/c15-6(14(23)24)1-2-26-3-7-9(21)10(22)13(25-7)20-5-19-8-11(16)17-4-18-12(8)20/h4-7,9-10,13,21-22H,1-3,15H2,(H,23,24)(H2,16,17,18)/t6-,7+,9+,10+,13+/m0/s1
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n/an/a>5.00E+4n/an/an/an/an/an/a



University of Toronto

Curated by ChEMBL


Assay Description
Inhibition of human full length PRMT5 expressed in Sf9 cells


ACS Med Chem Lett 6: 408-12 (2015)


Article DOI: 10.1021/ml500467h
BindingDB Entry DOI: 10.7270/Q2Q81FSZ
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50130929
PNG
(CHEMBL3633189)
Show SMILES NC(=N)c1ccc(Nc2ncnc(Nc3ccc(cc3)C#N)c2[N+]([O-])=O)cc1
Show InChI InChI=1S/C18H14N8O2/c19-9-11-1-5-13(6-2-11)24-17-15(26(27)28)18(23-10-22-17)25-14-7-3-12(4-8-14)16(20)21/h1-8,10H,(H3,20,21)(H2,22,23,24,25)
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n/an/a>1.00E+5n/an/an/an/an/an/a



Sichuan University

Curated by ChEMBL


Assay Description
Inhibition of PRMT5 (unknown origin) using biotinylated histone H4-derived peptide as substrate after 60 mins by AlphaLISA assay


Bioorg Med Chem Lett 25: 5449-53 (2015)


Article DOI: 10.1016/j.bmcl.2015.06.095
BindingDB Entry DOI: 10.7270/Q2R2136F
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50387477
PNG
(CHEMBL2047477)
Show SMILES CCn1c2cccc3cccc(c23)\c1=C\[CH+]\C=c1/n(CC)c2cccc3cccc1c23
Show InChI InChI=1S/C29H25N2/c1-3-30-24(22-14-5-10-20-12-7-18-26(30)28(20)22)16-9-17-25-23-15-6-11-21-13-8-19-27(29(21)23)31(25)4-2/h5-19H,3-4H2,1-2H3/q+1/b24-16-,25-17-
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n/an/a 9.10E+3n/an/an/an/an/an/a



Georgia State University

Curated by ChEMBL


Assay Description
Inhibition of His6X-tagged PRMT5 expressed in Escherichia coli BL21(DE3) cells using [14C]-S-adenosyl-L-methionine and histone H4 peptide after 8 min...


Eur J Med Chem 54: 647-59 (2012)


Article DOI: 10.1016/j.ejmech.2012.06.017
BindingDB Entry DOI: 10.7270/Q2XD12R6
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50400778
PNG
(CHEMBL2204995)
Show SMILES CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc2n(ncc12)C(C)C)-c1ccnc(c1)N1CCN(C)CC1
Show InChI InChI=1S/C31H39N7O2/c1-6-7-23-14-21(4)35-31(40)26(23)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)22-8-9-32-29(17-22)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)
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n/an/a>1.00E+5n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of PRMT5 using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins


ACS Med Chem Lett 3: 1091-1096 (2012)


Article DOI: 10.1021/ml3003346
BindingDB Entry DOI: 10.7270/Q2NK3G60
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50400781
PNG
(CHEMBL2204997)
Show SMILES CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc2n(ncc12)C(C)C)-c1ccc(nc1)N1CCN(C)CC1
Show InChI InChI=1S/C31H39N7O2/c1-6-7-22-14-21(4)35-31(40)26(22)18-33-30(39)25-15-24(16-28-27(25)19-34-38(28)20(2)3)23-8-9-29(32-17-23)37-12-10-36(5)11-13-37/h8-9,14-17,19-20H,6-7,10-13,18H2,1-5H3,(H,33,39)(H,35,40)
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n/an/a>1.00E+5n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of PRMT5 using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins


ACS Med Chem Lett 3: 1091-1096 (2012)


Article DOI: 10.1021/ml3003346
BindingDB Entry DOI: 10.7270/Q2NK3G60
More data for this
Ligand-Target Pair
PRMT5/MEP50 complex


(Homo sapiens (Human))
BDBM225230
PNG
(EED226)
Show SMILES CS(=O)(=O)c1ccc(cc1)-c1cnc(NCc2ccco2)n2cnnc12
Show InChI InChI=1S/C17H15N5O3S/c1-26(23,24)14-6-4-12(5-7-14)15-10-19-17(22-11-20-21-16(15)22)18-9-13-3-2-8-25-13/h2-8,10-11H,9H2,1H3,(H,18,19)
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n/an/a>1.00E+5n/an/an/an/an/an/a



Novartis Institutes for BioMedical Research



Assay Description
All HMT reactions were performed as described previously [Nasveschuk et al., ACS Med. Chem. Lett., 5:378-383].


Nat Chem Biol 13: 381-388 (2017)


Article DOI: 10.1038/nchembio.2304
BindingDB Entry DOI: 10.7270/Q2S75F64
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50400779
PNG
(CHEMBL2204998)
Show SMILES CC(C)n1ncc2c(cc(cc12)-c1ccc(nc1)N1CCN(C)CC1)C(=O)NCc1c(C)cc(C)[nH]c1=O
Show InChI InChI=1S/C29H35N7O2/c1-18(2)36-26-14-22(21-6-7-27(30-15-21)35-10-8-34(5)9-11-35)13-23(25(26)17-32-36)28(37)31-16-24-19(3)12-20(4)33-29(24)38/h6-7,12-15,17-18H,8-11,16H2,1-5H3,(H,31,37)(H,33,38)
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n/an/a>1.00E+5n/an/an/an/an/an/a



TBA

Curated by ChEMBL


Assay Description
Inhibition of PRMT5 using histone H3 as substrate preincubated for 10 mins followed by addition of [3H]SAM and incubated for 60 mins


ACS Med Chem Lett 3: 1091-1096 (2012)


Article DOI: 10.1021/ml3003346
BindingDB Entry DOI: 10.7270/Q2NK3G60
More data for this
Ligand-Target Pair
Protein arginine methyltransferase 5 (PRMT5)


(Homo sapiens (Human))
BDBM50431676
PNG
(CHEMBL2349526)
Show SMILES N[C@@H](CCSC[C@H]1O[C@H]([C@H](O)[C@@H]1O)n1cc(Br)c2c(N)ncnc12)C(O)=O
Show InChI InChI=1S/C15H20BrN5O5S/c16-6-3-21(13-9(6)12(18)19-5-20-13)14-11(23)10(22)8(26-14)4-27-2-1-7(17)15(24)25/h3,5,7-8,10-11,14,22-23H,1-2,4,17H2,(H,24,25)(H2,18,19,20)/t7-,8+,10+,11+,14+/m0/s1
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n/an/a 2.30E+3n/an/an/an/an/an/a



EntreMed Inc.

Curated by ChEMBL


Assay Description
Inhibition of PRMT5 (unknown origin) using [3H]SAM after 1 hr by scintillation proximity assay


Bioorg Med Chem 21: 1787-94 (2013)


Article DOI: 10.1016/j.bmc.2013.01.049
BindingDB Entry DOI: 10.7270/Q24F1S41
More data for this
Ligand-Target Pair