Identification of 4‐Anilinoquin(az)oline as a Cell‐Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype**
Why is this work in the frame?
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No Canadian affiliation. An affiliation-only frame — the usual design — would never have seen this work. It is one of the works that make the case for inverting the frame.
The three-model screen
all 1,000 screened works →All three models called this out of scope.
Medicinal chemistry identification of a PKN3 kinase inhibitor chemotype.
The work identifies a protein kinase inhibitor for cancer research, not a study of research.
Medicinal chemistry identification of a PKN3 inhibitor chemotype; domain drug discovery.
Abstract
Abstract Deep annotation of a library of 4‐anilinoquin(az)olines led to the identification of 7‐iodo‐ N ‐(3,4,5‐trimethoxyphenyl)quinolin‐4‐amine 16 as a potent inhibitor (IC 50 =14 nM) of Protein Kinase Novel 3 (PKN3) with micromolar activity in cells. Compound 16 is a potential tool compound to study the cell biology of PKN3 and its role in pancreatic and prostate cancer and T‐cell acute lymphoblastic leukemia. These 4‐anilinoquin(az)olines may also be useful tools to uncover the therapeutic potential of PKN3 inhibition in a broad range of diseases.
Stored with the screening record, where it is evidence for the labels above.
The record
- Venue
- ChemMedChem
- Topic
- Protein Kinase Regulation and GTPase Signaling
- Field
- Biochemistry, Genetics and Molecular Biology
- Canadian institutions
- —
- Funders
- National Center for Advancing Translational SciencesNational Institute of Diabetes and Digestive and Kidney DiseasesUniversity of North Carolina at Chapel HillNational Institutes of HealthCanada Foundation for InnovationInnovative Medicines InitiativeWellcome Trust
- Keywords
- ChemotypeKinaseChemistryProtein kinase inhibitorIdentification (biology)Protein kinase ABiochemistryCancer researchBiologyComputational biology
- Has abstract in OpenAlex
- yes