Synonyms: KYH-1872 | PROTAC 26 [PMID: 37567174]
Compound class:
Synthetic organic
Comment: This compound is a PROTAC [2]. It has a target warhead that is a multikinase inhibitor (YHJ1039 [1,3]) linked to a short peptide (PPPMAGG) based on the C-terminal domain of the kelch domain containing 2 (KLHDC2) substrate selenoprotein K (SelK), to engage the KLHDC2 ubiquitin E3 ligase.
![]() Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Cho H, Shin I, Yoon H, Jeon E, Lee J, Kim Y, Ryu S, Song C, Kwon NH, Moon Y et al.. (2021)
Identification of Thieno[3,2-d]pyrimidine Derivatives as Dual Inhibitors of Focal Adhesion Kinase and FMS-like Tyrosine Kinase 3. J Med Chem, 64 (16): 11934-11957. [PMID:34324343] |
2. Kim Y, Seo P, Jeon E, You I, Hwang K, Kim N, Tse J, Bae J, Choi HS, Hinshaw SM et al.. (2023)
Targeted kinase degradation via the KLHDC2 ubiquitin E3 ligase. Cell Chem Biol, 30 (11): 1414-1420.e5. [PMID:37567174] |
3. Ryu SS, Gadbois GE, Tao AJ, Fram BJ, Jiang J, Boyle B, Donovan KA, Krupnick NM, Berry BC, Bhunia D et al.. (2021)
Synthesis and structure-activity relationships of targeted protein degraders for the understudied kinase NEK9. Current Research in Chemical Biology, 1: 100008. DOI: 10.1016/j.crchbi.2021.100008 |