885270-73-5Relevant articles and documents
Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe
Paulson, Carolyn N.,Guan, Xianghong,Ayoub, Alex M.,Chan, Alice,Karim, Rezaul M.,Pomerantz, William C.K.,Sch?nbrunn, Ernst,Georg, Gunda I.,Hawkinson, Jon E.
, p. 1223 - 1229 (2018)
Several chemical probes have been developed for use in fluorescence polarization screening assays to aid in drug discovery for the bromodomain and extra-terminal domain (BET) proteins. However, few of those have been characterized in the literature. We ha
Differential BET Bromodomain Inhibition by Dihydropteridinone and Pyrimidodiazepinone Kinase Inhibitors
Karim, Rezaul Md,Bikowitz, Melissa J.,Chan, Alice,Zhu, Jin-Yi,Grassie, Dylan,Becker, Andreas,Berndt, Norbert,Gunawan, Steven,Lawrence, Nicholas J.,Sch?nbrunn, Ernst
, p. 15772 - 15786 (2021/11/16)
BRD4 and other members of the bromodomain and extraterminal (BET) family of proteins are promising epigenetic targets for the development of novel therapeutics. Among the reported BRD4 inhibitors are dihydropteridinones and benzopyrimidodiazepinones origi
BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
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Page/Page column 241-242, (2017/05/02)
Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.
POTENT DUAL BRD4-KINASE INHIBITORS AS CANCER THERAPEUTICS
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Page/Page column 130, (2016/04/26)
Disclosed herein are compounds that are inhibitors of BRD4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BRD4 are also disclosed. In certain aspects, disclosed are compounds of Formula I-IV.
PYRAZOLE PYRAZINE AMINE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREWITH
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Page/Page column 123, (2009/09/04)
Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure:Formula (I). Wherein Q and R1-R3 are as defined herein, compositions comprising an effective amount of a Pyrazole Pyrazine Amine Compound and methods for treating or preventing inflammatory conditions, immunological conditions, cancer, neurodegenerative diseases, age-related diseases, cardiovascular diseases and metabolic conditions, or conditions treatable or preventable by inhibition of an IKK, or an IKK pathway, comprising administering an effective amount of a Pyrazole Pyrazine Amine Compound to a patient in need thereof.
NOVEL CHEMICAL COMPOUNDS
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, (2008/06/13)
This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.
NOVEL CHEMICAL COMPOUNDS
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Page/Page column 74, (2010/11/25)
This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with hYAK3 activity.