ArticleACS medicinal chemistry letters2015
Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Article in ACS medicinal chemistry letters, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
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The trial behind it
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Who cites it
27 citing papers in PubMed.
- Brain Permeable SGK1 Inhibitors: A Promising Therapeutic Strategy for Neurodegenerative Diseases.Journal of medicinal chemistry · 2026Article
- Advantages of PROTACs in achieving selective degradation of homologous protein families.Beilstein journal of organic chemistry · 2026Review
- Discovery of a brain penetrant SGK1 inhibitor using a ligand- and structure-based virtual screening methodology.Journal of enzyme inhibition and medicinal chemistry · 2025Article
- Decoding the role of glucocorticoid-regulated kinase 1 in Alzheimer's disease: a promising path toward novel therapeutic strategies.Inflammopharmacology · 2025Review
- Unraveling the Potential of SGK1 in Osteoporosis: From Molecular Mechanisms to Therapeutic Targets.Biomolecules · 2025Review
- Distinct phases of cellular signaling revealed by time-resolved protein synthesis.Nature chemical biology · 2024Article
- AGC kinase inhibitors regulate STING signaling through SGK-dependent and SGK-independent mechanisms.Cell chemical biology · 2023Article
- An overview of PROTACs: a promising drug discovery paradigm.Molecular biomedicine · 2022Review
- Identification of Novel Inhibitors Targeting SGK1 via Ensemble-Based Virtual Screening Method, Biological Evaluation and Molecular Dynamics Simulation.International journal of molecular sciences · 2022Article
- Ontogeny and Vulnerabilities of Drug-Tolerant Persisters in HER2+ Breast Cancer.Cancer discovery · 2022Article
- Serum and glucocorticoid-regulated kinase 1: Structure, biological functions, and its inhibitors.Frontiers in pharmacology · 2022Review
- Serum- and glucocorticoid-inducible kinase 1 activity in ventral tegmental area dopamine neurons regulates cocaine conditioned place preference but not cocaine self-administration.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2021Article
- PROTACs to address the challenges facing small molecule inhibitors.European journal of medicinal chemistry · 2021Review
- Serum and Glucocorticoid-Inducible Kinase 1 (SGK1) in NSCLC Therapy.Pharmaceuticals (Basel, Switzerland) · 2020Review
- The prospect of serum and glucocorticoid-inducible kinase 1 (SGK1) in cancer therapy: a rising star.Therapeutic advances in medical oncology · 2020Review
- Design and Characterization of SGK3-PROTAC1, an Isoform Specific SGK3 Kinase PROTAC Degrader.ACS chemical biology · 2019Article
- Rapid and Reversible Knockdown of Endogenously Tagged Endosomal Proteins via an Optimized HaloPROTAC Degrader.ACS chemical biology · 2019Article
- Identification, structure modification, and characterization of potential small-molecule SGK3 inhibitors with novel scaffolds.Acta pharmacologica Sinica · 2018Article
- Serum and glucocorticoid inducible protein kinases (SGKs): a potential target for cancer intervention.Acta pharmaceutica Sinica. B · 2018Review
- Modification of Boc-Protected CAN508 via Acylation and Suzuki-Miyaura Coupling.Molecules (Basel, Switzerland) · 2018Article
Corrections and comments
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Authors and funding
12 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
From a virtual screening starting point, inhibitors of the serum and glucocorticoid regulated kinase 1 were developed through a combination of classical medicinal chemistry and library approaches. This resulted in highly active small molecules with nanomolar activity and a good overall in vitro and ADME profile. Furthermore, the compounds exhibited unusually high kinase and off-target selectivity due to their rigid structure.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.