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Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases
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What this work says
Outgoing claims: the papers this work cites, builds on, or argues with.
inferredcites →https://doi.org/10.1002/9780470559277.ch130145openalex-snapshot
Chemiluminescent Nitrogen Detection (CLND) to Measure Kinetic Aqueous Solubility
inferredcites →https://doi.org/10.1016/c2009-0-05547-0openalex-snapshot
Handbook of Heterocyclic Chemistry
inferredcites →https://doi.org/10.1016/j.bmcl.2005.07.077openalex-snapshot
Structure–activity relationship study of novel necroptosis inhibitors
inferredcites →https://doi.org/10.1016/j.ceb.2009.12.003openalex-snapshot
Necroptosis as an alternative form of programmed cell death
inferredcites →https://doi.org/10.1016/j.cell.2008.12.004openalex-snapshot
Necroptosis: A Specialized Pathway of Programmed Necrosis
inferredcites →https://doi.org/10.1016/j.immuni.2011.08.014openalex-snapshot
The Adaptor Protein FADD Protects Epidermal Keratinocytes from Necroptosis In Vivo and Prevents Skin Inflammation
inferredcites →https://doi.org/10.1016/j.immuni.2011.09.020openalex-snapshot
RIP Kinase-Dependent Necrosis Drives Lethal Systemic Inflammatory Response Syndrome
inferredcites →https://doi.org/10.1016/j.immuni.2014.12.031openalex-snapshot
A20 Restricts Ubiquitination of Pro-Interleukin-1β Protein Complexes and Suppresses NLRP3 Inflammasome Activity
inferredcites →https://doi.org/10.1016/j.immuni.2016.06.007openalex-snapshot
RIPK1 and RIPK3 Kinases Promote Cell-Death-Independent Inflammation by Toll-like Receptor 4
inferredcites →https://doi.org/10.1016/j.str.2013.01.016openalex-snapshot
Structural Basis of RIP1 Inhibition by Necrostatins
inferredcites →https://doi.org/10.1021/ac961242dopenalex-snapshot
Chromatographic Hydrophobicity Index by Fast-Gradient RP-HPLC: A High-Throughput Alternative to log P/log D
inferredcites →https://doi.org/10.1021/acs.jmedchem.5b01898openalex-snapshot
DNA-Encoded Library Screening Identifies Benzo[ b ][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors
inferredcites →https://doi.org/10.1021/ja506518topenalex-snapshot
Stereoelectronic Effects Dictate Molecular Conformation and Biological Function of Heterocyclic Amides
inferredcites →https://doi.org/10.1021/ml400382popenalex-snapshot
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis
inferredcites →https://doi.org/10.1038/cdd.2012.90openalex-snapshot
TRAIL induces necroptosis involving RIPK1/RIPK3-dependent PARP-1 activation
inferredcites →https://doi.org/10.1038/cddis.2012.64openalex-snapshot
A novel role for RIP1 kinase in mediating TNFα production
inferredcites →https://doi.org/10.1038/cddiscovery.2015.9openalex-snapshot
Characterization of GSK′963: a structurally distinct, potent and selective inhibitor of RIP1 kinase
inferredcites →https://doi.org/10.1038/nature10273openalex-snapshot
FADD prevents RIP3-mediated epithelial cell necrosis and chronic intestinal inflammation
inferredcites →https://doi.org/10.1038/nature10400openalex-snapshot
Caspase-8 regulates TNF-α-induced epithelial necroptosis and terminal ileitis
inferredcites →https://doi.org/10.1038/nature13608openalex-snapshot
RIPK1 maintains epithelial homeostasis by inhibiting apoptosis and necroptosis
inferredcites →https://doi.org/10.1038/nature13706openalex-snapshot
RIPK1 ensures intestinal homeostasis by protecting the epithelium against apoptosis
inferredcites →https://doi.org/10.1038/nchembio.1938openalex-snapshot
The ins and outs of selective kinase inhibitor development
inferredcites →https://doi.org/10.1038/nchembio.211openalex-snapshot
Design, synthesis and selection of DNA-encoded small-molecule libraries
inferredcites →https://doi.org/10.1038/nchembio.83openalex-snapshot
Identification of RIP1 kinase as a specific cellular target of necrostatins
inferredcites →https://doi.org/10.1038/nchembio711openalex-snapshot
Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury
inferredcites →https://doi.org/10.1039/c2md20111aopenalex-snapshot
The developability of heteroaromatic and heteroaliphatic rings – do some have a better pedigree as potential drug molecules than others?
inferredcites →https://doi.org/10.1053/j.gastro.2014.03.049openalex-snapshot
A CD3-Specific Antibody Reduces Cytokine Production and Alters Phosphoprotein Profiles in Intestinal Tissues From Patients With Inflammatory Bowel Disease
inferredcites →https://doi.org/10.1097/shk.0b013e31820b2db1openalex-snapshot
The Dual Functions of Receptor Interacting Protein 1 in Fas-Induced Hepatocyte Death During Sepsis
inferredcites →https://doi.org/10.1126/science.1098231openalex-snapshot
A Small Molecule Smac Mimic Potentiates TRAIL- and TNFα-Mediated Cell Death
inferredcites →https://doi.org/10.4049/jimmunol.1400499openalex-snapshot
Cutting Edge: RIP1 Kinase Activity Is Dispensable for Normal Development but Is a Key Regulator of Inflammation in SHARPIN-Deficient Mice
What points at this work
Incoming claims: where this work appears in other papers’ reference lists and arguments.
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Randomized clinical study of safety, pharmacokinetics, and pharmacodynamics of RIPK 1 inhibitor GSK 2982772 in healthy volunteers
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Identification of an antibody‐based immunoassay for measuring direct target binding of RIPK 1 inhibitors in cells and tissues
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Second-generation DNA-encoded multiple display on a constant macrocyclic scaffold enabled by an orthogonal protecting group strategy
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Structure-based optimizations of a necroptosis inhibitor (SZM594) as novel protective agents of acute lung injury
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Antimony salt-promoted cyclization facilitating on-DNA syntheses of dihydroquinazolinone derivatives and its applications
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RIPK1 kinase and scaffold activities in tumor cell fate and therapy
inferred← citeshttps://doi.org/10.1016/j.chembiol.2020.03.016openalex-snapshot
Ferroptosis and Necroptosis in the Kidney
inferred← citeshttps://doi.org/10.1016/j.chembiol.2023.06.019openalex-snapshot
DELs enable the development of BRET probes for target engagement studies in cells
inferred← citeshttps://doi.org/10.1016/j.chembiol.2026.04.011openalex-snapshot
Kinetic control of macrophage death by PTM-turnover crosstalk in infection and inflammation
inferred← citeshttps://doi.org/10.1016/j.clim.2024.110313openalex-snapshot
Necroptosis and autoimmunity
inferred← citeshttps://doi.org/10.1016/j.compbiomed.2025.110324openalex-snapshot
Synthesis and characterization of a new Carbon-11 labeled positron emission tomography radiotracer for RIPK1 neuroimaging
inferred← citeshttps://doi.org/10.1016/j.drudis.2021.10.011openalex-snapshot
Targeting regulated cell death (RCD) with small-molecule compounds in cancer therapy: A revisited review of apoptosis, autophagy-dependent cell death and necroptosis
inferred← citeshttps://doi.org/10.1016/j.drudis.2026.104658openalex-snapshot
Targeting kinases with DNA-encoded libraries: current landscape and future directions
inferred← citeshttps://doi.org/10.1016/j.ejmech.2020.112652openalex-snapshot
An insight on medicinal attributes of 1,2,4-triazoles
inferred← citeshttps://doi.org/10.1016/j.ejmech.2020.113004openalex-snapshot
Design, synthesis, and biological evaluation of tetrahydroisoquinolines derivatives as novel, selective PDE4 inhibitors for antipsoriasis treatment
inferred← citeshttps://doi.org/10.1016/j.ejmech.2020.113030openalex-snapshot
Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors
inferred← citeshttps://doi.org/10.1016/j.ejmech.2021.113484openalex-snapshot
Structure-based bioisosterism design of thio-benzoxazepinones as novel necroptosis inhibitors
inferred← citeshttps://doi.org/10.1016/j.ejmech.2021.114036openalex-snapshot
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity
inferred← citeshttps://doi.org/10.1016/j.ejmech.2022.114345openalex-snapshot
Investigation on the chemical space of the substituted triazole thio-benzoxazepinone RIPK1 inhibitors
inferred← citeshttps://doi.org/10.1016/j.ejmech.2023.115190openalex-snapshot
Discovery of Sibiriline derivatives as novel receptor-interacting protein kinase 1 inhibitors
inferred← citeshttps://doi.org/10.1016/j.ejmech.2023.116076openalex-snapshot
Discovery of 4-amino-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one derivatives as potential receptor-interacting serine/threonine-protein kinase 1 (RIPK1) inhibitors
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116123openalex-snapshot
RIPK1 inhibitors: A key to unlocking the potential of necroptosis in drug development
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116269openalex-snapshot
Small-molecule agents for treating skin diseases
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116304openalex-snapshot
Scaffold hopping derived novel benzoxazepinone receptor-interacting protein kinase 1 (RIP1) inhibitors as anti-necroptosis agents: Anti-inflammatory effect in systemic inflammatory response syndrome (SIRS) and epilepsy
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116309openalex-snapshot
Structure-based approaches for the design of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d][1,2,3]triazoles as tubulin polymerization inhibitors
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116851openalex-snapshot
Design, synthesis, and preclinical evaluation of 11C/18F-labeled inhibitors for RIPK1 PET imaging
inferred← citeshttps://doi.org/10.1016/j.ejmech.2025.117451openalex-snapshot
Discovery of a potent and in vivo anti-inflammatory Efficacious, P2Y14R antagonist with a novel benzisoxazoles scaffold by DNA-encoded chemical library technology
inferred← citeshttps://doi.org/10.1016/j.ejmech.2025.117530openalex-snapshot
Discovery of phenylisoxazolidine analogs targeting receptor interacting protein kinase 1 with anti-inflammatory activity
inferred← citeshttps://doi.org/10.1016/j.ejmech.2025.118380openalex-snapshot
Discovery of benzothiazole derivatives as novel orally receptor-interacting protein kinase 1 (RIPK1) inhibitors for inflammatory disease therapy
inferred← citeshttps://doi.org/10.1016/j.ejmech.2026.118623openalex-snapshot
Small-molecule modulators of the necroptotic pathway: A medicinal chemistry perspective
inferred← citeshttps://doi.org/10.1016/j.ejmech.2026.118925openalex-snapshot
Design, synthesis and anti-necroptosis evaluation of RIPK1 inhibitors derived from sunitinib
inferred← citeshttps://doi.org/10.1016/j.ejmech.2026.119077openalex-snapshot
Structure-based optimization of GSK2982772-derived RIPK1 inhibitors reveals the dispensability of the methylene linker and identifies a potent anti-necroptosis candidate for further optimization
inferred← citeshttps://doi.org/10.1016/j.ejphar.2023.175840openalex-snapshot
A natural chalcone cardamonin inhibits necroptosis and ameliorates dextran sulfate sodium (DSS)-induced colitis by targeting RIPK1/3 kinases
inferred← citeshttps://doi.org/10.1016/j.ejphar.2024.176508openalex-snapshot
Protein phosphorylation and kinases: Potential therapeutic targets in necroptosis
inferred← citeshttps://doi.org/10.1016/j.exer.2024.110030openalex-snapshot
Necrostatin-1 protects corneal epithelial cells by inhibiting the RIPK1/RIPK3/MLKL cascade in a benzalkonium chloride-induced model of necroptosis
inferred← citeshttps://doi.org/10.1016/j.fct.2023.114069openalex-snapshot
Pazopanib ameliorates rotenone-induced Parkinsonism in rats by suppressing multiple regulated cell death mechanisms
inferred← citeshttps://doi.org/10.1016/j.intimp.2023.110400openalex-snapshot
Understanding necroptosis and its therapeutic target for intervertebral disc degeneration
inferred← citeshttps://doi.org/10.1016/j.intimp.2023.110603openalex-snapshot
Necroptosis in the sarcoma immune microenvironment: From biology to therapy
inferred← citeshttps://doi.org/10.1016/j.intimp.2025.116095openalex-snapshot
Ponicidin ameliorates Alzheimer's disease through dual inhibition of RIPK1-mediated neuroinflammation and necroptosis
inferred← citeshttps://doi.org/10.1016/j.intimp.2026.117076openalex-snapshot
Flavokawain C alleviates dextran sulphate sodium-induced colitis through suppressing necroptosis via blocking RIPK1-RIPK3-MLKL axis
inferred← citeshttps://doi.org/10.1016/j.jare.2021.12.002openalex-snapshot
Role of necroptosis in traumatic brain and spinal cord injuries
inferred← citeshttps://doi.org/10.1016/j.jcrc.2026.155696openalex-snapshot
Cell death mechanisms in sepsis-associated adaptive immune dysfunction
inferred← citeshttps://doi.org/10.1016/j.jdermsci.2020.06.001openalex-snapshot
RIPK1: A rising star in inflammatory and neoplastic skin diseases
inferred← citeshttps://doi.org/10.1016/j.jpha.2018.11.002openalex-snapshot
Methodology of drug screening and target identification for new necroptosis inhibitors
inferred← citeshttps://doi.org/10.1016/j.lfs.2021.119304openalex-snapshot
5-((7-Chloro-6-fluoro-1h-indol-3-yl) methyl)-3-methylimidazolidine-2,4-dione as a RIP1 inhibitor protects LPS/D-galactosamine-induced liver failure
inferred← citeshttps://doi.org/10.1016/j.lfs.2025.123871openalex-snapshot
Linking necroptosis with liver aging and chronic inflammation in hepatic pathology
inferred← citeshttps://doi.org/10.1016/j.medidd.2020.100075openalex-snapshot
Biologics vs. small molecules: Drug costs and patient access
inferred← citeshttps://doi.org/10.1016/j.molmed.2017.11.002openalex-snapshot
Checkpoints in TNF-Induced Cell Death: Implications in Inflammation and Cancer
inferred← citeshttps://doi.org/10.1016/j.molmed.2018.01.004openalex-snapshot
Inflammasome, Inflammation, and Tissue Homeostasis
inferred← citeshttps://doi.org/10.1016/j.molmed.2018.10.007openalex-snapshot
RIP Kinases in Liver Cell Death, Inflammation and Cancer
inferred← citeshttps://doi.org/10.1016/j.molmed.2023.10.001openalex-snapshot
Therapeutic potential of PANoptosis: innate sensors, inflammasomes, and RIPKs in PANoptosomes
inferred← citeshttps://doi.org/10.1016/j.nucmedbio.2022.04.006openalex-snapshot
Radiosynthesis and characterization of a carbon-11 PET tracer for receptor-interacting protein kinase 1
inferred← citeshttps://doi.org/10.1016/j.pharmthera.2021.107979openalex-snapshot
Novel insights into RIPK1 as a promising target for future Alzheimer’s disease treatment
inferred← citeshttps://doi.org/10.1016/j.phrs.2019.104439openalex-snapshot
Necroptosis signaling in liver diseases: An update
inferred← citeshttps://doi.org/10.1016/j.phrs.2020.105297openalex-snapshot
Necrostatin-1 and necroptosis inhibition: Pathophysiology and therapeutic implications
inferred← citeshttps://doi.org/10.1016/j.phymed.2025.156842openalex-snapshot
Natural diterpenoids in dermatology: Multifunctional roles and therapeutic potential for skin diseases
inferred← citeshttps://doi.org/10.1016/j.revmed.2022.06.005openalex-snapshot
Revue de la littérature sur les maladies auto-inflammatoires associées aux mutations du gène RIPK1
inferred← citeshttps://doi.org/10.1016/j.sbi.2023.102578openalex-snapshot
Navigating large chemical spaces in early-phase drug discovery
inferred← citeshttps://doi.org/10.1016/j.semcdb.2020.06.014openalex-snapshot
RIPK protein kinase family: Atypical lives of typical kinases
inferred← citeshttps://doi.org/10.1016/j.surg.2018.02.017openalex-snapshot
Inhibition of necroptosis attenuates lung injury and improves survival in neonatal sepsis
inferred← citeshttps://doi.org/10.1016/j.tcb.2022.05.008openalex-snapshot
The web of death: the expanding complexity of necroptotic signaling
inferred← citeshttps://doi.org/10.1016/j.tetlet.2017.05.001openalex-snapshot
Synthesis of ( S )-3-amino-benzo[ b ][1,4]oxazepin-4-one via Mitsunobu and S N Ar reaction for a first-in-class RIP1 kinase inhibitor GSK2982772 in clinical trials
inferred← citeshttps://doi.org/10.1016/j.tetlet.2017.08.020openalex-snapshot
Room-temperature synthesis of pharmaceutically important carboxylic acids bearing the 1,2,4-oxadiazole moiety
inferred← citeshttps://doi.org/10.1016/j.tibs.2026.05.005openalex-snapshot
Biochemistry at scale: Seeing both the forest and the trees
inferred← citeshttps://doi.org/10.1016/j.tips.2020.01.002openalex-snapshot
Inhibitors Targeting RIPK1/RIPK3: Old and New Drugs
inferred← citeshttps://doi.org/10.1016/j.tips.2021.04.001openalex-snapshot
Fragment-based drug design facilitates selective kinase inhibitor discovery
inferred← citeshttps://doi.org/10.1016/j.trsl.2025.11.002openalex-snapshot
Unraveling PANoptosis a key player in acute kidney injury and its clinical implications
inferred← citeshttps://doi.org/10.1016/j.yjmcc.2018.03.003openalex-snapshot
Necroptosis in cardiovascular disease - a new therapeutic target
inferred← citeshttps://doi.org/10.1016/j.yjmcc.2021.09.010openalex-snapshot
Programmed cell death in aortic aneurysm and dissection: A potential therapeutic target
inferred← citeshttps://doi.org/10.1021/acs.accounts.2c00778openalex-snapshot
Photochemical Methods Applied to DNA Encoded Library (DEL) Synthesis
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.0c00508openalex-snapshot
Condensation of DNA-Conjugated Imines with Homophthalic Anhydride for the Synthesis of Isoquinolones on DNA
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.1c00076openalex-snapshot
C–S Coupling of DNA-Conjugated Aryl Iodides for DNA-Encoded Chemical Library Synthesis
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.1c00363openalex-snapshot
Application of l -Threonine Aldolase to on-DNA Reactions
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.1c00567openalex-snapshot
DNA-Compatible Synthesis of α,β-Epoxyketones for DNA-Encoded Chemical Libraries
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.2c00340openalex-snapshot
DNA Compatible Oxidization and Amidation of Terminal Alkynes
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.2c00471openalex-snapshot
On-DNA Alkyne Iodination and Acetylenic Coupling as a Useful Tool for DEL Synthesis
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.3c00138openalex-snapshot
On-DNA Morita-Baylis-Hillman Reaction: Accessing Targeted Covalent Inhibitor Motifs in DNA-Encoded Libraries
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.3c00235openalex-snapshot
Enolate–Azide [3 + 2]-Cycloaddition Reaction Suitable for DNA-Encoded Library Synthesis
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.7b00292openalex-snapshot
Ruthenium Promoted On-DNA Ring-Closing Metathesis and Cross-Metathesis
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.7b00343openalex-snapshot
Selecting a DNA-Encoded Chemical Library against Non-immobilized Proteins Using a “Ligate–Cross-Link–Purify” Strategy
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.7b00416openalex-snapshot
DNA-Compatible Nitro Reduction and Synthesis of Benzimidazoles
inferred← citeshttps://doi.org/10.1021/acs.bioconjchem.9b00863openalex-snapshot
C–N Coupling of DNA-Conjugated (Hetero)aryl Bromides and Chlorides for DNA-Encoded Chemical Library Synthesis
inferred← citeshttps://doi.org/10.1021/acs.chemrev.0c00789openalex-snapshot
DNA-Encoded Chemistry: Drug Discovery from a Few Good Reactions
inferred← citeshttps://doi.org/10.1021/acs.jcim.4c00232openalex-snapshot
Building Block-Centric Approach to DNA-Encoded Library Design
inferred← citeshttps://doi.org/10.1021/acs.jcim.5c02584openalex-snapshot
Metadynamics Simulation Reveals Allosteric Communication Effects of the Flipping Process of the Atypical DLG Motif in RIPK1
inferred← citeshttps://doi.org/10.1021/acs.jcim.9b00729openalex-snapshot
Designing DNA Encoded Libraries of Diverse Products in a Focused Property Space
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.0c00452openalex-snapshot
Machine Learning on DNA-Encoded Libraries: A New Paradigm for Hit Finding
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.0c00523openalex-snapshot
High-Throughput Screening for the Discovery of Enzyme Inhibitors
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