Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
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| Target ID | T15797 | Target Info | |||
| Target Name | SET and MYND domain-containing protein 2 (SMYD2) | ||||
| Synonyms |
Nlysine methyltransferase SMYD2; N-lysine methyltransferase SMYD2; Lysine Nmethyltransferase 3C; Lysine N-methyltransferase 3C; KMT3C; Histone methyltransferase SMYD2; HSKMB; HSKM-B
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| Target Type | Preclinical Target | ||||
| Gene Name | SMYD2 | ||||
| Biochemical Class | Methyltransferase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 4 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
N-((1R,3r,5S)-8-((4-(Benzylamino)piperidin-1-yl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)-6-chloro-2-oxoindoline-5-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
EPZ-030456; CHEMBL3798468; SCHEMBL17591901; SCHEMBL17591904; SCHEMBL21489931; BDBM378459; US10266526, Compound 592
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| Activity |
IC50 ~ 50000 nM
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[1] | |||
| Compound Name |
6-Chloro-2-oxo-N-((1R,3r,5S)-8-(((1-(4,4,4-trifluorobutyl)piperidin-4-yl)methyl)sulfonyl)-8-azabicyclo[3.2.1]octan-3-yl)indoline-5-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
EPZ031686; EPZ-031686; CHEMBL3798741; SCHEMBL17591794; SCHEMBL17591795; SCHEMBL21490167; BDBM378462; EX-A1613; US10266526, Compound 595; ZINC521836533; CS-5775; HY-19324; A16375
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| Activity |
IC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
(2~{S})-5-[2-(3-Aminocarbonylphenyl)ethyl-[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl]amino]-2-azanyl-pentanoic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4067973; BDBM50247634; F0P
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| Activity |
IC50 = 62000 nM
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[2] | |||
| 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
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[3] | |||
| References | Top | ||||
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| REF 1 | Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor. ACS Med Chem Lett. 2015 Aug 27;7(2):134-8. | ||||
| REF 2 | Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT). J Med Chem. 2018 Feb 22;61(4):1541-1551. | ||||
| REF 3 | Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J Med Chem. 2014 Aug 14;57(15):6822-33. | ||||
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