Target Poor or Non Binder(s) Information

Target General Information

Target ID

T82665

Target Info

Target Name

Protein arginine methyltransferase 5 (PRMT5)

Synonyms

Shk1 kinase-binding protein 1 homolog; SKB1Hs; SKB1 homolog; SKB1; Protein arginine N-methyltransferase 5; Jak-binding protein 1; JBP1; IBP72; Histone-arginine N-methyltransferase PRMT5; HRMT1L5; 72 kDa ICln-binding protein

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Target Type

Clinical trial Target

Gene Name

PRMT5

Biochemical Class

Methyltransferase

UniProt ID

O14744

Poor Binders of This Target (in total, 16 binders)

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Compound Name

(L-)-S-adenosyl-L-homocysteine

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Investigative

Compound Info

Synonyms

S-Adenosyl-L-homocysteine; S-adenosylhomocysteine; S-adenosyl-L-homocysteine; 979-92-0; AdoHcy; S-(5'-adenosyl)-L-homocysteine; adenosylhomocysteine; Formycinylhomocysteine; Adenosyl-L-homocysteine; S-(5'-deoxyadenosin-5'-yl)-L-homocysteine; 2-S-adenosyl-L-homocysteine; 5'-Deoxy-S-adenosyl-L-homocysteine; S-adenosyl-homocysteine; S-Adenosyl Homocysteine; L-S-Adenosylhomocysteine; L-Homocysteine, S-(5'-deoxyadenosin-5'-yl)-; adenosylhomo-cys; adenosyl-homo-cys; UNII-8K31Q2S66S; (S)-5'-(S)-(3-Amino-3-carboxypropyl)-5'-thioadenosine; BRN 5166233; SAH; S-Adenosylhomocysteine; S-Adenosyl-L-Homocysteine

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Activity

IC50 ~ 50000 nM

[1]

Compound Name

GSK343

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Investigative

Compound Info

Synonyms

compound 6 [PMID 24900432]; GSK 343

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Activity

IC50 ~ 100000 nM

[2]

Compound Name

1-[(2R)-3-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-4-phenylpyridin-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3981583; SCHEMBL15835837

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Activity

EC50 ~ 50000 nM

[3]

Compound Name

1-[3-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-4-(2-methylphenyl)piperazin-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3943447; SCHEMBL15835836; BDBM310194; US10150758, Compound 10

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Activity

EC50 ~ 50000 nM

[3]

Compound Name

N-[(3-Bromophenyl)methyl]-1-[2-(methylamino)ethyl]piperidin-4-amine

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Investigative

Compound Info

Synonyms

CHEMBL4062667

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Activity

IC50 ~ 50000 nM

[4]

Compound Name

1-[(2S)-3-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-4-phenylpyridin-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3933246; SCHEMBL15908701

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Activity

EC50 ~ 50000 nM

[3]

Compound Name

1-[3-(3,4-Dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]-4-(2-fluorophenyl)piperazin-2-one

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Investigative

Compound Info

Synonyms

CHEMBL3940784; SCHEMBL15823498

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Activity

EC50 ~ 50000 nM

[3]

Compound Name

N-Benzyl-1-[2-(methylamino)ethyl]piperidin-4-amine

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Investigative

Compound Info

Synonyms

CHEMBL4099850

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Activity

IC50 ~ 50000 nM

[4]

Compound Name

1-(2-((((2S,3S,4R,5R)-5-(6-Amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)thio)ethyl)-3-ethylurea

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Investigative

Compound Info

Synonyms

DS-437; CHEMBL3577854; EX-A3697; BDBM50089221; HY-124131; CS-0084441

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Activity

IC50 ~ 50000 nM

[1]

Compound Name

6,7-Dimethoxy-2-(pyrrolidin-1-yl)-N-(5-(pyrrolidin-1-yl)pentyl)quinazolin-4-amine

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Investigative

Compound Info

Synonyms

UNC0379; UNC-0379; CHEMBL3318285; UNC 0379; 6,7-Dimethoxy-2-pyrrolidin-1-yl-N-(5-pyrrolidin-1-ylpentyl)quinazolin-4-amine; C23H35N5O2; CS-3345; HY-12335; SCHEMBL22568439; AOB6365; EX-A461; SYN5081; BCP10429; KS-00000T5A; 3362AH; BDBM50051117; MFCD28167817; s7570; ZINC98214604; AKOS025404942; UNC 0379;UNC-0379; CCG-268809; SB19349; NCGC00384189-06; NCGC00384189-10; AK174945; AS-16447; DA-43617; B8009; FT-0699830; A14320; UNC0379 trifluoroacetate salt, >=98% (HPLC)

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Activity

IC50 ~ 100000 nM

[5]

Compound Name

N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indazole-4-carboxamide

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Investigative

Compound Info

Synonyms

GSK926; CHEMBL2204998; SCHEMBL2590353; BDBM50400779

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Activity

IC50 ~ 100000 nM

[2]

Compound Name

N'-[[2-(2-Chlorophenyl)sulfanylphenyl]methyl]-N'-methylethane-1,2-diamine

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Investigative

Compound Info

Synonyms

CHEMBL4094513

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Activity

IC50 ~ 100000 nM

[6]

Compound Name

N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[6-(4-methylpiperazin-1-yl)pyridin-3-yl]-1-propan-2-ylindazole-4-carboxamide

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Investigative

Compound Info

Synonyms

CHEMBL2204997; SCHEMBL12180659; BDBM50400781

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Activity

IC50 ~ 100000 nM

[2]

Compound Name

4-[[6-(4-Cyanoanilino)-5-nitropyrimidin-4-yl]amino]benzenecarboximidamide

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Investigative

Compound Info

Synonyms

CHEMBL3633189; BDBM50130929

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Activity

IC50 ~ 100000 nM

[7]

Compound Name

Furamidine

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Investigative

Compound Info

Synonyms

Benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis-; UNII-08GH1YF0RA; 08GH1YF0RA; Furamidine Dihydrochloride; 73819-26-8 (free base); DB75;NSC 305831; 4-[5-(4-carbamimidoylphenyl)furan-2-yl]benzenecarboximidamide; NSC305831; 2,5-bis(4-amidinophenyl)furan; NSC-305831; DB 75; 4,4'-(2,5-Furandiyl)bis(benzenecarboximidamide); BRN 1435532; Furandiamidine; WR 199385; NCIStruc1_001694; NCIStruc2_001468; 5-18-07-00177 (Beilstein Handbook Reference); CHEMBL24057; SCHEMBL549198; CTK5A3496; ZINC26213; DTXSID00224264; 2,5-Bis(4-amidinophenyl)-furan; BDBM50388602; CCG-37385; NCGC00014688; NCI305831; AKOS030254780; HY-110137A; 4,4'-(Furan-2,5-diyl)dibenzimidamide; NCGC00014688-02; NCGC00014688-03; NCGC00014688-06; NCGC00097791-01; NCGC00097791-02; NCI60_002601; CS-0058706; Benzenecarboximidamide, 4,4'-(2,5-furandiyl)bis-, dihydrochloride; Benzenecarboximidamide,4,4'-(2,5-furandiyl)bis-, dihydrochloride (9CI)

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Activity

IC50 = 166000 nM

[8]

Compound Name

5-[5-(4-Carbamimidoylphenyl)furan-2-yl]pyridine-2-carboximidamide

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Investigative

Compound Info

Synonyms

CHEMBL424121; DB867; SCHEMBL5492310; BDBM50007728

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Activity

IC50 = 186000 nM

[8]

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Non Binders of This Target (in total, 3 non binders)

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Compound Name

Pentamidine

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Approved

Compound Info

Synonyms

Lomidine; Nebupent; PENTAM; PNT; Pentacarinat; Pentamide; Pentamidin; Pentamidina; Pentamidinum; Pneumopent; PENTAMIDINE ISETHIONATE; Pentamidina [DCIT]; Pentamidine isetionate; Pentamidine mesylate; MB 800; Pentam 300; Lomidine (TN); MB-800; Nebupent (as isethionate); Pentacarinat (as isethionate); Pentam 300 (as isethionate); Pentamidine (INN); Pentamidinum [INN-Latin]; RP-2512; Nebupent (*Isethionate); Pentacarinat (*Isethionate); Pentam 300 (*Isethionate); Pentamidine Isethionate 2-Hydroxy-Ethanesulfonic Acid;Pentamidine [INN:BAN:DCF]; RP 2512 (*Isethionate); P,p'-(Pentamethylenedioxy)bis[benzamidine]; P,p'-(Pentamethylenedioxy)dibenzamidine; P,p'-(Pentamethylene-dioxy)bis-benzamidine; Benzenecarboximidamide, 4,4'-(1,5-pentanediylbis(oxy))bis-(9CI); 1,3-BIS(4-AMIDINOPHENOXY)PENTANE; 4, 4'-Diamidinodiphenoxypentane; 4,4'-(1,5-Pentanediylbis(oxy))bis-benzenecarboximidamide; 4,4'-(Pentamethylenedioxy)dibenzamide; 4,4'-(Pentamethylenedioxy)dibenzamidine; 4,4'-Diamidino-.alpha.,.omega.-diphenoxypentane; 4,4'-Diamidinodiphenoxypentane; 4,4'-[pentane-1,5-diylbis(oxy)]dibenzenecarboximidamide; 4-[5-(4-Carbamimidoylphenoxy)pentoxy]benzenecarboximidamide

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Activity

IC50 = 582000 nM

[9]

Compound Name

Hexamidine

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Investigative

Compound Info

Synonyms

Hexamidina; Hexamidinum; UNII-3483C2H13H; CHEMBL25105; 4,4'-(1,6-Hexanediylbis(oxy))bis-benzenecarboximidamide; 3483C2H13H; 4,4'-[hexane-1,6-diylbis(oxy)]dibenzenecarboximidamide; Hexamidinum [INN-Latin]; Hexamidina [INN-Spanish]; CHEMBL494852; Hexamidine [INN:BAN:DCF]; 4-[6-(4-carbamimidoylphenoxy)hexoxy]benzenecarboximidamide; Hexamidine[antipeptic]; Hexamidine (INN/BAN); 4-[6-(4-carbamimidoylphenoxy)hexoxy]benzamidine; SCHEMBL144738; 1,6-Di(4-amidinophenoxy)hexane; DTXSID60191524; 4,4'[1,6-HEXANEDIYLBIS(OXY)]BISBENZENECARBOXIMIDAMIDE; Benzenecarboximidamide, 4,4'-(1,6-hexanediylbis(oxy))bis-; ZINC1705403; BDBM50015234; STL483397; 1,6-Di (4-amidinophenoxy)-n-hexane; DB03808; FT-0700701; FT-0700706; D07206; Q250360; 4-[6-(4-Carbamimidoyl-phenoxy)-hexyloxy]-benzamidine; 4,4'-[hexane-1,6-diylbis(oxy)]di(benzene-1-carboximidamide); 4,4''''[1,6-HEXANEDIYLBIS(OXY)]BISBENZENECARBOXIMIDAMIDE; 4-{6-[4-amino(imino)methylphenoxy]hexyloxy}phenyl-iminomethanamine; 4-{6-[4-ammino(imino)methylphenoxy]hexyloxy}phenyl-iminomethanammine

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Activity

IC50 = 357000 nM

[9]

Compound Name

Stilbamidine

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Investigative

Compound Info

Synonyms

Diamidino stilbene; 4,4'-Diamidinostilbene; Benzamidine, 4,4'-vinylenedi-; UNII-ST31IIO5EW; 4,4'-Stilbenedicarboxamidine; BA 2652; ST31IIO5EW; CHEMBL142304; Stilbamidinum; NSC-35605; Stilbamidine [BAN]; EINECS 204-519-5; BRN 3206434; Stilbamidin; 4-09-00-03639 (Beilstein Handbook Reference); SCHEMBL208655; ZINC2079; NCI35605; BDBM50210461; CCG-36712; HY-U00007; CS-6597; 4,4''-(ethene-1,2-diyl)dibenzimidamide; 4,4'-(1,2-Ethanediyl)bisbenzenecarboximidamide; Benzenecarboximidamide, 4,4'-(1,2-ethenediyl)bis-; Q27289385; 4-((E)-2-{4-[(Z)-amino(imino)methyl]phenyl}vinyl)benzenecarboximidamide

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Activity

IC50 = 712000 nM

[9]

References

Top

REF 1

Discovery of a Dual PRMT5-PRMT7 Inhibitor. ACS Med Chem Lett. 2015 Mar 2;6(4):408-12.

REF 2

Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6.

REF 3

WO patent application no. 2014100764A2, METHODS OF INHIBITING PRMT5

REF 4

Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1). Medchemcomm. 2016 Sep 1;7(9):1793-1796.

REF 5

Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33.

REF 6

Development of Potent Type I Protein Arginine Methyltransferase (PRMT) Inhibitors of Leukemia Cell Proliferation. J Med Chem. 2017 Nov 9;60(21):8888-8905.

REF 7

Discovery and structure-activity analysis of 4-((5-nitropyrimidin-4-yl)amino)benzimidamide derivatives as novel protein arginine methyltransferase 1 (PRMT1) inhibitors. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5449-53.

REF 8

Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22.

REF 9

Discovery of Decamidine as a New and Potent PRMT1 Inhibitor. Medchemcomm. 2017 Feb 1;8(2):440-444.

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