Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T12837 | Target Info | |||
| Target Name | Histone-arginine methyltransferase CARM1 (CARM1) | ||||
| Synonyms |
Protein arginine N-methyltransferase 4; PRMT4; Histonearginine methyltransferase CARM1; Coactivatorassociated arginine methyltransferase 1; Coactivator-associated arginine methyltransferase 1
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| Target Type | Literature-reported Target | ||||
| Gene Name | CARM1 | ||||
| Biochemical Class | Methyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 20 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
GSK343
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Investigative | Compound Info | ||
| Synonyms |
compound 6 [PMID 24900432]; GSK 343
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| Activity |
IC50 = 128000 nM
|
[1] | |||
| Compound Name |
1-[3-[[(1S,2R,3S,4R)-4-(6-Aminopurin-9-yl)-2,3-dihydroxycyclopentyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3087501; SCHEMBL16424780; BDBM50443020
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| Compound Name |
1-[3-[[(1R,2R,3S,4R)-4-(6-Aminopurin-9-yl)-2,3-dihydroxycyclopentyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3087503; SCHEMBL16424848; BDBM50443018
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| Activity |
Ki ~ 50000 nM
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[2] | |||
| Compound Name |
1-[3-[[(3R,4S,5R)-3-(6-Aminopurin-9-yl)-4,5-dihydroxycyclopenten-1-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3087502; SCHEMBL16424776; BDBM50443019
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| Compound Name |
2-[3-[[(2S)-2-Aminopropanoyl]amino]phenyl]-N-benzyl-5-(trifluoromethyl)pyrazole-3-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL1162995
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
(S)-1-(4-((2-Aminopropanamido)methyl)phenyl)-N-benzyl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL479037; BDBM50262983
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
1-(2-(((S)-2-Aminopropanamido)methyl)phenyl)-N-benzyl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL517366; BDBM50262984
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
5'-[(3-{[(4-Tert-Butylphenyl)carbamoyl]amino}propyl)(Propan-2-Yl)amino]-5'-Deoxyadenosine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2171169; SCHEMBL9970132; BDBM50396980; ZINC95557720; Q27458098
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| Activity |
Ki ~ 50000 nM
|
[2] | |||
| Compound Name |
(2S)-2-Amino-5-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(methylamino)purin-9-yl]oxolan-2-yl]methyl-(2-iodoethyl)amino]pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2172427; BDBM50396017
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| Activity |
IC50 ~ 100000 nM
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[4] | |||
| Compound Name |
(2s)-2-Azanyl-4-[[(2s,3s,4r,5r)-5-[6-(Methylamino)purin-9-Yl]-3,4-Bis(Oxidanyl)oxolan-2-Yl]methylsulfanyl]butanoic Acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2171174; Methyl-SAH; SCHEMBL9058595; BDBM50396981; S-(N6-Methyladenosyl)-L-homocysteine; Q27466742
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| Activity |
Ki ~ 100000 nM
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[5] | |||
| Compound Name |
(2S)-2-Amino-5-[[(2R,3S,4R,5R)-5-[6-(benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl-(2-iodoethyl)amino]pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2169918; BDBM50396016
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| Activity |
IC50 ~ 100000 nM
|
[4] | |||
| 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
|
[1] | |||
| Compound Name |
1-(4-Tert-butylphenyl)-3-[3-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(prop-2-enylamino)purin-9-yl]oxolan-2-yl]methyl-propan-2-ylamino]propyl]urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2171171; BDBM50396978
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| Activity |
Ki ~ 100000 nM
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[5] | |||
| Compound Name |
1-[3-[[(2R,3S,4R,5R)-5-[6-(Benzylamino)purin-9-yl]-3,4-dihydroxyoxolan-2-yl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2171172; BDBM50396977
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
1-(4-Tert-butylphenyl)-3-[3-[[(2R,3S,4R,5R)-3,4-dihydroxy-5-[6-(methylamino)purin-9-yl]oxolan-2-yl]methyl-propan-2-ylamino]propyl]urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2171170; BDBM50396979
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| Activity |
Ki ~ 100000 nM
|
[5] | |||
| Compound Name |
2-Hydroxy-5-{[4-(4-methoxy-3-methylphenyl)-1,3-thiazol-2-yl]amino}benzoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4128513; Oprea1_203261; ZINC955929; BDBM50271657; STK024442; AKOS001673438; MCULE-8723917637; SR-01000111406; SR-01000111406-1
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| Activity |
IC50 ~ 100000 nM
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[6] | |||
| Compound Name |
Methyl 2-[[2-[(6-methoxy-1H-benzimidazol-2-yl)sulfanyl]acetyl]amino]benzoate
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Investigative | Compound Info | ||
| Synonyms |
PRMT5-IN-C17; ZINC00659298; ChemDiv1_002844; Oprea1_645106; CHEMBL4092336; HMS595B06; ZINC5455374; STK346078; AKOS000421473; AKOS000830714; MCULE-9755352312; AG-690/12869587; SR-01000429953; SR-01000429953-1; Z16078172; methyl 2-({[(5-methoxy-1H-benzimidazol-2-yl)sulfanyl]acetyl}amino)benzoate; methyl 2-({[(6-methoxy-1H-benzimidazol-2-yl)sulfanyl]acetyl}amino)benzoate; methyl 2-{2-[(6-methoxy-1H-1,3-benzodiazol-2-yl)sulfanyl]acetamido}benzoate
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| Activity |
IC50 ~ 100000 nM
|
[7] | |||
| Compound Name |
(2Z)-1-Ethyl-2-[(E)-3-(1-ethylbenzo[cd]indol-1-ium-2-yl)prop-2-enylidene]benzo[cd]indole;iodide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2047477
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| Activity |
IC50 = 100000 nM
|
[8] | |||
| Compound Name |
(2R)-2-Amino-N-ethylpropanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3781841; SCHEMBL12955470; ZINC4206147; BDBM50158087; AKOS017426894
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| Activity |
IC50 = 105000 nM
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[9] | |||
| 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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|
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| Activity |
IC50 = 116000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 3 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| 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 > 400000 nM
|
[10] | |||
| 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 = 400000 nM
|
[10] | |||
| 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 > 400000 nM
|
[10] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | 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 2 | Synthesis, Activity and Metabolic Stability of Non-Ribose Containing Inhibitors of Histone Methyltransferase DOT1L. Medchemcomm. 2013 May 1;4(5):822-826. | ||||
| REF 3 | Pyrazole inhibitors of coactivator associated arginine methyltransferase 1 (CARM1). Bioorg Med Chem Lett. 2008 Aug 1;18(15):4438-41. | ||||
| REF 4 | Oncoepigenomics: making histone lysine methylation count. Eur J Med Chem. 2012 Oct;56:179-94. | ||||
| REF 5 | Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L. J Med Chem. 2012 Sep 27;55(18):8066-74. | ||||
| REF 6 | Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations. Bioorg Med Chem Lett. 2018 May 15;28(9):1476-1483. | ||||
| REF 7 | Potent, Selective, and Cell Active Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor Developed by Structure-Based Virtual Screening and Hit Optimization. J Med Chem. 2017 Jul 27;60(14):6289-6304. | ||||
| REF 8 | Synthesis and evaluation of carbocyanine dyes as PRMT inhibitors and imaging agents. Eur J Med Chem. 2012 Aug;54:647-59. | ||||
| REF 9 | Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor. J Med Chem. 2016 Feb 11;59(3):1176-83. | ||||
| REF 10 | Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22. | ||||
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