Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T76723 | Target Info | |||
| Target Name | Protein arginine methyltransferase 3 (PRMT3) | ||||
| Synonyms |
Protein arginine N-methyltransferase 3; Heterogeneous nuclear ribonucleoprotein methyltransferase-like protein 3; HRMT1L3
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| Target Type | Literature-reported Target | ||||
| Gene Name | PRMT3 | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 18 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 = 74000 nM
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[1] | |||
| 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
|
[2] | |||
| 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
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[2] | |||
| Compound Name |
1-(1,2,3-Benzothiadiazol-6-yl)-3-(cyclohexylmethyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325168; BDBM50427752
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| Activity |
IC50 ~ 50000 nM
|
[3] | |||
| Compound Name |
1-Isoquinolin-6-yl-1-methyl-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4064464; BDBM50247379
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| Activity |
IC50 ~ 50000 nM
|
[4] | |||
| 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 = 54000 nM
|
[1] | |||
| Compound Name |
1-(2H-Benzotriazol-5-yl)-3-(2-cyclohexylethyl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325444; BDBM50427765
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| 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 |
1-(2-Cyclohexylethyl)-3-(1H-indazol-5-yl)urea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325446; BDBM50427763
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
1-(1,2,3-Benzothiadiazol-6-yl)-3-cyano-2-(2-cyclohexylethyl)guanidine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325161; BDBM50427759
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| Compound Name |
N-[5-(2-Cyclohexylethyl)-1H-1,2,4-triazol-3-yl]-1,2,3-benzothiadiazol-6-amine
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325162; BDBM50427758
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| 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-(1,3-Benzothiazol-6-yl)-3-(2-cyclohexylethyl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325443; BDBM50427766
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|
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
3-(1,2,3-Benzothiadiazol-6-ylamino)-4-(2-cyclohexylethylamino)cyclobut-3-ene-1,2-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325448; BDBM50427761
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| Activity |
IC50 ~ 100000 nM
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[3] | |||
| 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
|
[6] | |||
| Compound Name |
3-(1,2,3-Benzothiadiazol-6-ylamino)-4-(phenacylamino)cyclobut-3-ene-1,2-dione
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325160; BDBM50427760
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|
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
1-(2-Cyclohexylethyl)-3-(1H-indazol-6-yl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325445; BDBM50427764
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
1-(2-Cyclohexylethyl)-3-(2-oxo-3H-1,3-benzoxazol-6-yl)urea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2325447; BDBM50427762
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 2 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-Methyl-2-(4-methylpiperidin-1-yl)ethanamine
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|
Investigative | Compound Info | ||
| Synonyms |
N-Methyl-N-[2-(4-methylpiperidin-1-yl)ethyl]amine; CHEMBL3780701; methyl[2-(4-methylpiperidin-1-yl)ethyl]amine; SCHEMBL16020344; CTK5H0152; DTXSID40655710; CHEMBRDG-BB 4013122; ALBB-014424; 3123AF; BDBM50158097; MFCD08691570; ZINC32445502; AKOS000257122; DA-18430; FT-0724284; N-Methyl-2-(4-methyl-1-piperidinyl)ethanamine; Y-4242; N-Methyl-2-(4-methylpiperidin-1-yl)ethan-1-amine; N-Methyl-2-(4-methylpiperidin-1-yl)ethanamine, AldrichCPR
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| Activity |
IC50 > 500000 nM
|
[7] | |||
| 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 > 1000000 nM
|
[7] | |||
| 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 | Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1). Medchemcomm. 2016 Sep 1;7(9):1793-1796. | ||||
| REF 3 | Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors. J Med Chem. 2013 Mar 14;56(5):2110-24. | ||||
| REF 4 | Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). J Med Chem. 2018 Feb 8;61(3):1204-1217. | ||||
| 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 | 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 7 | Discovery of a Potent Class I Protein Arginine Methyltransferase Fragment Inhibitor. J Med Chem. 2016 Feb 11;59(3):1176-83. | ||||
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