Synonyms: compound 21 [WO2021053495A1]
Compound class:
Synthetic organic
Comment: This compound is a bifunctional degrader of the cardiac-specific kinase TNNI3K protein, that is claimed in patent WO2021053495A1 [1]. It's kinase binding domain is derived from the quinazoline TNNI3K inhibitor GSK114 [2], and it contains a cereblon binding ligand to promote association with the protein-degrading E3 ubiquitin ligase complex.
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Bioactivity Comments |
This compound is designed to promote the targeted degradation of the TNNI3K protein, as an alternative to small molecule enzyme inhibitors. The IC50 (reduction in protein level by 50%) for TNNI3K degradation by this degrader is 350 nM in vitro [1]. |