Target and Its Patented Drug(s)
Target General Information | Top | ||||
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Target ID | T17036 | Target Info | |||
Target Name | Lysine-specific demethylase 4E (KDM4E) | ||||
Synonyms | Lysine-specific demethylase 4D-like; KDM4DL; KDM4D-like protein | ||||
Target Type | Patented-recorded Target | ||||
Gene Name | KDM4E | ||||
Biochemical Class | Paired donor oxygen oxidoreductase | ||||
UniProt ID |
Patent(s) and the Corresponding Patented Drug(s) | Top | ||||
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World Intellectual Property Organization (WIPO) | |||||
Patent ID | WO2010043866 | ||||
Title | Histone Lysine Demethylase Inhibitors. | ||||
Abstract | The invention provides a compound which is an iV-oxalylglycine derivative of formula (I): a hydroxamic acid derivative of formula (II): or a heteroaryl derivative of fomula (III): wherein n; Z1; Z2; Y1; Y2; A; p; X1; X2; m; R4; B; R5; R6; R7; R8; R9; X3; R10; R11 and R12 are as defined herein, or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of the human 2-oxoglutarate-dependant JMJD2 subfamily of histone demethylases, in particular JMJD2E. Such inhibitors are useful in changing the epigenetic state of cells resulting in the inhibition / activation of chromatin remodelling, multiple gene activation / deactivation, and in treating cancer and other conditions characterised by undesirable cellular proliferation, and psychiatric disorders including depression. | ||||
Applicant(s) | Isis Innovation Limited | ||||
Representative Drug(s) | D0O9WS | Drug Info | IC50 = 300 nM | Click to Show More | [1] |
2 | D06ZPF | Drug Info | IC50 = 600 nM | [1] | |
3 | D0D0WU | Drug Info | IC50 = 1100 nM | [1] | |
4 | D03EOJ | Drug Info | IC50 = 5400 nM | [1] | |
5 | D0OR0K | Drug Info | IC50 = 7900 nM | [1] | |
6 | D0WC4Z | Drug Info | IC50 = 8600 nM | [1] | |
7 | D0P7ZY | Drug Info | IC50 = 11700 nM | [1] | |
8 | D0C8CI | Drug Info | IC50 = 14700 nM | [1] | |
9 | D0L7HC | Drug Info | IC50 = 14700 nM | [1] | |
10 | D0YF2M | Drug Info | IC50 = 14800 nM | [1] | |
11 | D0LU7U | Drug Info | IC50 = 16600 nM | [1] | |
12 | D06MHK | Drug Info | IC50 = 20100 nM | [1] | |
13 | D0P5MY | Drug Info | IC50 = 37100 nM | [1] | |
United States Patent and Trademark Office (USPTO) | |||||
Patent ID | US20130123344 | ||||
Title | of Health and Human Services. Method of Preventing or Treating Viral Infection with Compounds That Inhibit Jmjd2 Proteins. | ||||
Representative Drug(s) | D00VLQ | Drug Info | IC50 = 840 to 12000 nM | Click to Show More | [1] |
2 | D03TPE | Drug Info | IC50 = 840 to 12000 nM | [1] | |
3 | D08KYP | Drug Info | IC50 = 840 to 12000 nM | [1] | |
4 | D0P8YL | Drug Info | IC50 = 840 to 12000 nM | [1] | |
5 | D0VS3A | Drug Info | IC50 = 840 to 12000 nM | [1] | |
Patent ID | US20130137720 | ||||
Title | Histone Demethylase Inhibitors and Methods for Using The Same. | ||||
Representative Drug(s) | D09NCT | Drug Info | IC50 = 5900 nM | [1] |
References | Top | ||||
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REF 1 | KDM4 histone demethylase inhibitors for anti-cancer agents: a patent review.Expert Opin Ther Pat. 2015 Feb;25(2):135-44. |
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