ArticleACS medicinal chemistry letters2015
Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Abstract read
In one paragraph
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.
0numbers the graph read from it
0cells of the map it votes in
27citing papers in PubMed
–field-weighted citation impact
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
27 citing papers in PubMed.
- Hydroxysafflor Yellow A improves diabetic nephropathy by inhibiting PI3K/AKT/mTOR pathway based on a multidimensional study.Frontiers in medicine · 2026Article
- Article
- The power of DNA-encoded chemical libraries in the battle against drug-resistant bacteria.RSC advances · 2025Review
- ATP-competitive inhibitors of PI3K enzymes demonstrate an isoform selective dual action by controlling membrane binding.The Biochemical journal · 2024Article
- Structure-based pharmacophore modeling and DFT studies of Indian Ocean-derived red algal compounds as PI3Kα inhibitors.Molecular diversity · 2024Article
- Structural insights into the interaction of three Y-shaped ligands with PI3Kα.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- Opportunities for Expanding Encoded Chemical Diversification and Improving Hit Enrichment in mRNA-Displayed Peptide Libraries.Chembiochem : a European journal of chemical biology · 2022Review
- PI3K inhibitors are finally coming of age.Nature reviews. Drug discovery · 2021Review
- DNA-Encoded Library Hit Confirmation: Bridging the Gap Between On-DNA and Off-DNA Chemistry.ACS medicinal chemistry letters · 2021Article
- DNA-Encoded Chemistry: Drug Discovery from a Few Good Reactions.Chemical reviews · 2021Review
- Stereo- and regiodefined DNA-encoded chemical libraries enable efficient tumour-targeting applications.Nature chemistry · 2021Article
- Considerations for Achieving Maximized DNA Recovery in Solid-Phase DNA-Encoded Library Synthesis.ACS combinatorial science · 2020Article
- Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.Journal of medicinal chemistry · 2020Article
- DNA-Encoded Libraries: Aryl Fluorosulfonates as Versatile Electrophiles Enabling Facile On-DNA Suzuki, Sonogashira, and Buchwald Reactions.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2019Article
- DNA Barcoding a Complete Matrix of Stereoisomeric Small Molecules.Journal of the American Chemical Society · 2019Article
- Accelerating the Throughput of Affinity Mass Spectrometry-Based Ligand Screening toward a G Protein-Coupled Receptor.Analytical chemistry · 2019Article
- DNA-Compatible [3 + 2] Nitrone-Olefin Cycloaddition Suitable for DEL Syntheses.Organic letters · 2019Article
- Structural Determinants of Isoform Selectivity in PI3K Inhibitors.Biomolecules · 2019Review
- Insights into the mechanism of the PIK3CA E545K activating mutation using MD simulations.Scientific reports · 2018Article
- DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information.Annual review of biochemistry · 2018Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
21 authors.
Hongfang YangMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Patricia F MedeirosMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Kaushik RahaComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Patricia ElkinsComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Kenneth E LindMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Ruth LehrComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Nicholas D AdamsComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Joelle L BurgessComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Stanley J SchmidtComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Steven D KnightComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Kurt R AugerComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Michael D SchaberComputational and Structural Chemistry, Platform Technology and Science, Biological Reagents and Assay Development, Platform Technology and Science, Oncology Research, and Screening and Compound Profiling, Platform Technology and Science, GlaxoSmithKline , 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
G Joseph FranklinMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Yun DingMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Jennifer L DeLoreyMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Paolo A CentrellaMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Sibongile MataruseMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Steven R SkinnerMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Matthew A ClarkMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
John W CuozzoMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Ghotas EvindarMDR (Molecular Discovery Research) Boston, Platform Technology and Science, GlaxoSmithKline , 830 Winter Street, Waltham, Massachusetts 02451, United States.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In the search of PI3K p110α wild type and H1047R mutant selective small molecule leads, an encoded library technology (ELT) campaign against the desired target proteins was performed which led to the discovery of a selective chemotype for PI3K isoforms from a three-cycle DNA encoded library. An X-ray crystal structure of a representative inhibitor from this chemotype demonstrated a unique binding mode in the p110α protein.
Indexed as
ELTEncoded Library technologyp110αPI3K p110α (H1047R)PI3Kα
Identifiers
What OpenQuestion holds
Textmetadata
Read underepoch 390
Registered trials
None linked
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.