ArticleACS medicinal chemistry letters2013
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed.
- Benchmarking 3D Structure-Based Molecule Generators.Journal of chemical information and modeling · 2025Article
- Recent Advancements in the Synthesis of α-fluoroalkylated Azine-derived Heterocycles through Direct Fluorination.Current organic synthesis · 2024Article
- Conformational Selectivity of ITK Inhibitors: Insights from Molecular Dynamics Simulations.Journal of chemical information and modeling · 2023Article
- Article
- Structure-based molecular modeling in SAR analysis and lead optimization.Computational and structural biotechnology journal · 2021Review
- Synthesis of aminopyrazole analogs and their evaluation as CDK inhibitors for cancer therapy.Bioorganic & medicinal chemistry letters · 2018Article
- Identification of inactive conformation-selective interleukin-2-inducible T-cell kinase (ITK) inhibitors based on second-harmonic generation.FEBS open bio · 2018Article
- Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.The Journal of biological chemistry · 2015Article
- Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.The Journal of biological chemistry · 2013Article
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Authors and funding
19 authors.
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Abstract
Inhibition of Itk potentially constitutes a novel, nonsteroidal treatment for asthma and other T-cell mediated diseases. In-house kinase cross-screening resulted in the identification of an aminopyrazole-based series of Itk inhibitors. Initial work on this series highlighted selectivity issues with several other kinases, particularly AurA and AurB. A template-hopping strategy was used to identify a series of aminobenzothiazole Itk inhibitors, which utilized an inherently more selective hinge binding motif. Crystallography and modeling were used to rationalize the observed selectivity. Initial exploration of the SAR around this series identified potent Itk inhibitors in both enzyme and cellular assays.
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