The Chemical Probes Portal
The Chemical Probes Portal is an online open access catalog of annotated small molecule inhibitors, agonists and other chemical tools for biological research and preclinical drug discovery. Annotations for are extensive and distinguish between activity in cells and model organisms. Probe records also include ratings and commentary from our Scientific Advisory Board, which consists of known experts in medicinal chemistry, chemical biology, pharmacology and related fields.
Description
More detailed information about this field from each metasource.
The Chemical Probes Portal is an online open access catalog of annotated small molecule inhibitors, agonists and other chemical tools for biological research and preclinical drug discovery. Annotations for are extensive and distinguish between activity in cells and model organisms. Probe records also include ratings and commentary from our Scientific Advisory Board, which consists of known experts in medicinal chemistry, chemical biology, pharmacology and related fields.
metasource: Fairsharing.orgversion: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
The Chemical Probes Portal is an online open access catalog of annotated small molecule inhibitors, agonists and other chemical tools for biological research and preclinical drug discovery. Annotations for are extensive and distinguish between activity in cells and model organisms.
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
Webpage:
http://www.chemicalprobes.orgWebpage
More detailed information about this field from each metasource.
http://www.chemicalprobes.org
metasource: Fairsharing.orgversion: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
https://new.chemicalprobes.org/
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
Licence:
Name: Creative Commons Attribution-ShareAlike 3.0 Unported (CC BY-SA 3.0)Licence name
More detailed information about this field from each metasource.
Creative Commons Attribution-ShareAlike 3.0 Unported (CC BY-SA 3.0)
metasource: Fairsharing.orgversion: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
CC
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
Licence URL
More detailed information about this field from each metasource.
https://creativecommons.org/licenses/by-sa/3.0/
metasource: Fairsharing.orgversion: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
metasource: re3data.org
version: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
Publications:
Publications
More detailed information about this field from each metasource.
The promise and peril of chemical probes
PMID: 26196764
metasource: Fairsharing.org
version: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
Publications
More detailed information about this field from each metasource.
The promise and peril of chemical probes
PMID: 26196764
metasource: Fairsharing.org
version: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
-
The promise and peril of chemical probes
PubMed citations: 268.
268 articles citing: The promise and peril of chemical probes
Optimization of the 4-anilinoquin(az)oline scaffold as epidermal growth factor receptor (EGFR) inhibitors for chordoma utilizing a toxicology profiling assay platform. PMID:35896603
Development of Small-Molecule Fluorescent Probes Targeting Enzymes. PMID:35889374
A conversation on using chemical probes to study protein function in cells and organisms. PMID:35790718
Evaluation of a Selective Chemical Probe Validates That CK2 Mediates Neuroinflammation in a Human Induced Pluripotent Stem Cell-Derived Mircroglial Model. PMID:35774866
Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses. PMID:35723434
canSAR chemistry registration and standardization pipeline. PMID:35643512
Phenotypic drug discovery: recent successes, lessons learned and new directions. PMID:35637317
On the Study of Deubiquitinases: Using the Right Tools for the Job. PMID:35625630
Bioluminescent Zebrafish Transplantation Model for Drug Discovery. PMID:35559262
Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. PMID:35484434
AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery. PMID:35475262
opnMe.com: a digital initiative for sharing tools with the biomedical research community. PMID:35459938
Lysine methyltransferase inhibitors: where we are now. PMID:35441141
Use of AD Informer Set compounds to explore validity of novel targets in Alzheimer's disease pathology. PMID:35434254
Identification of 4-Anilinoquin(az)oline as a Cell-Active Protein Kinase Novel 3 (PKN3) Inhibitor Chemotype. PMID:35403825
The emerging role of mass spectrometry-based proteomics in drug discovery. PMID:35351998
Triterpenoids as Reactive Oxygen Species Modulators of Cell Fate. PMID:35312315
Target 2035 - update on the quest for a probe for every protein. PMID:35211674
Image-Based Annotation of Chemogenomic Libraries for Phenotypic Screening. PMID:35209227
Structure-Based Design of a Chemical Probe Set for the 5-HT5A Serotonin Receptor. PMID:35195401
Discovery of Potent Peptidomimetic Antagonists for Heterochromatin Protein 1 Family Proteins. PMID:35036738
Host kinase CSNK2 is a target for inhibition of pathogenic β-coronaviruses including SARS-CoV-2. PMID:35018375
Drugging Fuzzy Complexes in Transcription. PMID:34993233
Gains from no real PAINS: Where 'Fair Trial Strategy' stands in the development of multi-target ligands. PMID:34900527
Exploration of Aberrant E3 Ligases Implicated in Alzheimer's Disease and Development of Chemical Tools to Modulate Their Function. PMID:34867205
Apoptolidin family glycomacrolides target leukemia through inhibition of ATP synthase. PMID:34857958
Understanding the ancillary ligand effect on luminescent cyclometalated Ir(III) complex as a reporter for 2-acetylaminofluorene DNA(AAF-dG) adduct. PMID:34843001
Small-molecule antagonism of the interaction of the RAGE cytoplasmic domain with DIAPH1 reduces diabetic complications in mice. PMID:34818060
A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization. PMID:34782742
Targeting Cullin-RING E3 Ubiquitin Ligase 4 by Small Molecule Modulators. PMID:34604860
Computational Prediction of Chemical Tools for Identification and Validation of Synthetic Lethal Interaction Networks. PMID:34590285
Emerging therapeutic opportunities for integrin inhibitors. PMID:34535788
Rational design of ASCT2 inhibitors using an integrated experimental-computational approach. PMID:34507995
Enhancer of Zeste Homolog 2 (EZH2) Contributes to Rod Photoreceptor Death Process in Several Forms of Retinal Degeneration and Its Activity Can Serve as a Biomarker for Therapy Efficacy. PMID:34502238
Chemogenomics for drug discovery: clinical molecules from open access chemical probes. PMID:34458810
Will the chemical probes please stand up? PMID:34447939
Functional interrogation and therapeutic targeting of protein tyrosine phosphatases. PMID:34431504
Towards the sustainable discovery and development of new antibiotics. PMID:34426795
Human carboxylesterases and fluorescent probes to image their activity in live cells. PMID:34355180
Efficient Entropy-Driven Inhibition of Dipeptidyl Peptidase III by Hydroxyethylene Transition-State Peptidomimetics. PMID:34314529
The PROTACtable genome. PMID:34285415
Targeting Small GTPases and Their Prenylation in Diabetes Mellitus. PMID:34236862
A critical overview of computational approaches employed for COVID-19 drug discovery. PMID:34212944
Metal-binding effects of sirtuin inhibitor sirtinol. PMID:34177214
Identification of β-strand mediated protein-protein interaction inhibitors using ligand-directed fragment ligation. PMID:34163995
Remodelin Is a Cryptic Assay Interference Chemotype That Does Not Inhibit NAT10-Dependent Cytidine Acetylation. PMID:34141066
The right tools for the job: the central role for next generation chemical probes and chemistry-based target deconvolution methods in phenotypic drug discovery. PMID:34124668
Tryptophan scanning mutagenesis as a way to mimic the compound-bound state and probe the selectivity of allosteric inhibitors in cells. PMID:34123282
Insights on Targeting Small Molecules to the Mitochondrial Matrix and the Preparation of MitoB and MitoP as Exomarkers of Mitochondrial Hydrogen Peroxide. PMID:34118033
Development and biological applications of sulfur-triazole exchange (SuTEx) chemistry. PMID:34095850
Crowdsourced mapping of unexplored target space of kinase inhibitors. PMID:34083538
Functionalized Scout Fragments for Site-Specific Covalent Ligand Discovery and Optimization. PMID:34056091
Pharmacological inhibition of PI5P4Kα/β disrupts cell energy metabolism and selectively kills p53-null tumor cells. PMID:34001596
Opportunities and challenges in translational science. PMID:33982407
Exploiting vulnerabilities of SWI/SNF chromatin remodelling complexes for cancer therapy. PMID:33941852
Transcriptome screening followed by integrated physicochemical and structural analyses for investigating RNA-mediated berberine activity. PMID:33784402
Impact of structural biologists and the Protein Data Bank on small-molecule drug discovery and development. PMID:33744282
Protein arginine methylation: from enigmatic functions to therapeutic targeting. PMID:33742187
Inhibitors of cullin-RING E3 ubiquitin ligase 4 with antitumor potential. PMID:33602808
Nuisance compounds in cellular assays. PMID:33592188
Online informatics resources to facilitate cancer target and chemical probe discovery. PMID:33479663
Pseudoreplication in physiology: More means less. PMID:33464305
Evaluating and evolving a screening library in academia: the St Jude approach. PMID:33453364
The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. PMID:33429995
The histone methyltransferase inhibitor A-366 enhances hemoglobin expression in erythroleukemia cells upon co-exposure with chemical inducers in culture. PMID:33407944
Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK. PMID:33291717
From Phenotypic Hit to Chemical Probe: Chemical Biology Approaches to Elucidate Small Molecule Action in Complex Biological Systems. PMID:33287212
A Single-Stranded DNA-Encoded Chemical Library Based on a Stereoisomeric Scaffold Enables Ligand Discovery by Modular Assembly of Building Blocks. PMID:33240760
canSAR: update to the cancer translational research and drug discovery knowledgebase. PMID:33219674
A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation. PMID:33215924
Improving target assessment in biomedical research: the GOT-IT recommendations. PMID:33199880
Open Targets Platform: supporting systematic drug-target identification and prioritisation. PMID:33196847
The Dark Kinase Knowledgebase: an online compendium of knowledge and experimental results of understudied kinases. PMID:33079988
Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease. PMID:33028810
Comment on: Food for Bone: Evidence for a Role for Delta-Tocotrienol in the Physiological Control of Osteoblast Migration. Int. J. Mol. Sci. 2020, 21, 4661. PMID:32932718
Inducers of the endothelial cell barrier identified through chemogenomic screening in genome-edited hPSC-endothelial cells. PMID:32759214
Gini Coefficients as a Single Value Metric to Define Chemical Probe Selectivity. PMID:32568503
Discovering and validating cancer genetic dependencies: approaches and pitfalls. PMID:32561862
Pharmacological Inhibition of Soluble Epoxide Hydrolase as a New Therapy for Alzheimer's Disease. PMID:32488482
An exon skipping screen identifies antitumor drugs that are potent modulators of pre-mRNA splicing, suggesting new therapeutic applications. PMID:32469945
Anti-Inflammatory Properties of Chemical Probes in Human Whole Blood: Focus on Prostaglandin E2 Production. PMID:32435199
Transcription Factor Inhibition: Lessons Learned and Emerging Targets. PMID:32359481
Phenotypic Screening of Chemical Libraries Enriched by Molecular Docking to Multiple Targets Selected from Glioblastoma Genomic Data. PMID:32243127
Critical Assessment of Targeted Protein Degradation as a Research Tool and Pharmacological Modality. PMID:32222318
Development of 2-(4-pyridyl)-benzimidazoles as PKN2 chemical tools to probe cancer. PMID:32085971
Natural products as modulators of eukaryotic protein secretion. PMID:32067014
Click Chemistry in Proteomic Investigations. PMID:32059777
Synthesis and Biological Validation of a Harmine-Based, Central Nervous System (CNS)-Avoidant, Selective, Human β-Cell Regenerative Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase A (DYRK1A) Inhibitor. PMID:32003560
Characterization of the Menin-MLL Interaction as Therapeutic Cancer Target. PMID:31947537
In Depth Analysis of Kinase Cross Screening Data to Identify CAMKK2 Inhibitory Scaffolds. PMID:31941153
Getting a handle on chemical probes of chomatin readers. PMID:31920100
Activity-Based Sensing for Site-Specific Proteomic Analysis of Cysteine Oxidation. PMID:31869209
Towards the Development of an In vivo Chemical Probe for Cyclin G Associated Kinase (GAK). PMID:31698822
Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation. PMID:31631011
Cytosolic delivery of inhibitory antibodies with cationic lipids. PMID:31611380
R-BIND: An Interactive Database for Exploring and Developing RNA-Targeted Chemical Probes. PMID:31589399
Covalent-Allosteric Inhibitors to Achieve Akt Isoform-Selectivity. PMID:31584233
Nonparametric Analysis of Thermal Proteome Profiles Reveals Novel Drug-binding Proteins. PMID:31582558
Chemical proteomics reveals target selectivity of clinical Jak inhibitors in human primary cells. PMID:31578349
BAX, BAK, and BOK: A Coming of Age for the BCL-2 Family Effector Proteins. PMID:31570337
Microglial Drug Targets in AD: Opportunities and Challenges in Drug Discovery and Development. PMID:31507408
Ubiquitin C-Terminal Hydrolase L1: Biochemical and Cellular Characterization of a Covalent Cyanopyrrolidine-Based Inhibitor. PMID:31449350
Leveraging Atropisomerism to Obtain a Selective Inhibitor of RET Kinase with Secondary Activities toward EGFR Mutants. PMID:31424197
Discovery and Characterization of a Cellular Potent Positive Allosteric Modulator of the Polycomb Repressive Complex 1 Chromodomain, CBX7. PMID:31422906
Cytotoxic unsaturated electrophilic compounds commonly target the ubiquitin proteasome system. PMID:31285509
A fast and specific fluorescent probe for thioredoxin reductase that works via disulphide bond cleavage. PMID:31227705
A chemoprobe tracks its target. PMID:31101661
Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor. PMID:31097999
A Medicinal Chemist's Perspective on Transitioning from Industry to Academic Drug Discovery. PMID:31097980
Pharmacological Modulation of Transcriptional Coregulators in Cancer. PMID:31078321
Phenotypic Screening Combined with Machine Learning for Efficient Identification of Breast Cancer-Selective Therapeutic Targets. PMID:31056464
Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery. PMID:31027189
A chemical toolbox for the study of bromodomains and epigenetic signaling. PMID:31015424
Validation and Invalidation of Chemical Probes for the Human N-myristoyltransferases. PMID:31006618
Bromodomain inhibition of the coactivators CBP/EP300 facilitate cellular reprogramming. PMID:30962627
Cheminformatics Tools for Analyzing and Designing Optimized Small-Molecule Collections and Libraries. PMID:30956147
Systematic computational identification of promiscuity cliff pathways formed by inhibitors of the human kinome. PMID:30915709
CRISPR/Cas9 - An evolving biological tool kit for cancer biology and oncology. PMID:30911676
Targeting the Small GTPase Superfamily through Their Regulatory Proteins. PMID:30869179
SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK). PMID:30768268
Mapping biologically active chemical space to accelerate drug discovery. PMID:30710133
Assembly of Divalent Ligands and Their Effect on Divalent Binding to Pseudomonas aeruginosa Lectin LecA. PMID:30681333
EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology. PMID:30616481
A chemical biology toolbox to study protein methyltransferases and epigenetic signaling. PMID:30604761
canSAR: update to the cancer translational research and drug discovery knowledgebase. PMID:30496479
Open Targets Platform: new developments and updates two years on. PMID:30462303
Selective Inhibitors of a Human Prolyl Hydroxylase (OGFOD1) Involved in Ribosomal Decoding. PMID:30427558
A chemical genetic screen reveals that iminosugar inhibitors of plant glucosylceramide synthase inhibit root growth in Arabidopsis and cereals. PMID:30401902
Cutting Edge Therapeutic Insights Derived from Molecular Biology of Pediatric High-Grade Glioma and Diffuse Intrinsic Pontine Glioma (DIPG). PMID:30340362
Data-Driven Exploration of Selectivity and Off-Target Activities of Designated Chemical Probes. PMID:30249057
Drug Target Commons 2.0: a community platform for systematic analysis of drug-target interaction profiles. PMID:30219839
Chemical Instability and Promiscuity of Arylmethylidenepyrazolinone-Based MDMX Inhibitors. PMID:30216042
Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity. PMID:30170319
Insights into the development of chemical probes for RNA. PMID:30102391
Developing Small-Molecule Inhibitors of HECT-Type Ubiquitin Ligases for Therapeutic Applications: Challenges and Opportunities. PMID:30088849
A new quinoline-based chemical probe inhibits the autophagy-related cysteine protease ATG4B. PMID:30076329
ALARM NMR for HTS triage and chemical probe validation. PMID:30034947
Targeting Pim Kinases and DAPK3 to Control Hypertension. PMID:30033129
Modulating the masters: chemical tools to dissect CBP and p300 function. PMID:30025258
Reconciling Selectivity Trends from a Comprehensive Kinase Inhibitor Profiling Campaign with Known Activity Data. PMID:30023860
New 1,2-Dihydropyridine-Based Fluorophores and Their Applications as Fluorescent Probes. PMID:30023792
Facile target validation in an animal model with intracellularly expressed monobodies. PMID:30013062
Modeling Small-Molecule Reactivity Identifies Promiscuous Bioactive Compounds. PMID:29990427
High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2. PMID:29945974
New tools for evaluating protein tyrosine sulfation: tyrosylprotein sulfotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors. PMID:29934490
The Endocannabinoid Reuptake Inhibitor WOBE437 Is Orally Bioavailable and Exerts Indirect Polypharmacological Effects via Different Endocannabinoid Receptors. PMID:29910713
Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery. PMID:29877628
Remarkable Progress with Small-Molecule Modulation of TRPC1/4/5 Channels: Implications for Understanding the Channels in Health and Disease. PMID:29865154
Dissecting the role of the tubulin code in mitosis. PMID:29804676
RNA-modifying proteins as anticancer drug targets. PMID:29773918
Optimization of a "bump-and-hole" approach to allele-selective BET bromodomain inhibition. PMID:29732121
Dissecting the Contributions of Cooperating Gene Mutations to Cancer Phenotypes and Drug Responses with Patient-Derived iPSCs. PMID:29681544
Donated chemical probes for open science. PMID:29676732
Data Mining and Computational Modeling of High-Throughput Screening Datasets. PMID:29671272
Chemical probes and drug leads from advances in synthetic planning and methodology. PMID:29651105
Proteostasis in Huntington's disease: disease mechanisms and therapeutic opportunities. PMID:29620053
The role of ZA channel water-mediated interactions in the design of bromodomain-selective BET inhibitors. PMID:29605436
Challenges in validating candidate therapeutic targets in cancer. PMID:29417929
Fluorescence anisotropy imaging in drug discovery. PMID:29410158
Atropisomerism in medicinal chemistry: challenges and opportunities. PMID:29380622
High-throughput screen for compounds that modulate neurite growth of human induced pluripotent stem cell-derived neurons. PMID:29361516
Targeted NUDT5 inhibitors block hormone signaling in breast cancer cells. PMID:29343827
DNA-Encoded Chemical Libraries: A Selection System Based on Endowing Organic Compounds with Amplifiable Information. PMID:29328784
Drug Target Commons: A Community Effort to Build a Consensus Knowledge Base for Drug-Target Interactions. PMID:29276046
CRISPR Approaches to Small Molecule Target Identification. PMID:29261286
Objective, Quantitative, Data-Driven Assessment of Chemical Probes. PMID:29249694
Defining Metabolic and Nonmetabolic Regulation of Histone Acetylation by NSAID Chemotypes. PMID:29240439
Seven Year Itch: Pan-Assay Interference Compounds (PAINS) in 2017-Utility and Limitations. PMID:29202222
Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement. PMID:29174542
Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors. PMID:29170024
Assay interference and off-target liabilities of reported histone acetyltransferase inhibitors. PMID:29142305
The SGC beyond structural genomics: redefining the role of 3D structures by coupling genomic stratification with fragment-based discovery. PMID:29118096
Structure-based drug design: aiming for a perfect fit. PMID:29118091
Reproducibility of science: Fraud, impact factors and carelessness. PMID:29079076
Chemical Proteomics for Target Discovery of Head-to-Tail Cyclized Mini-Proteins. PMID:29075625
Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action. PMID:29043777
Report and Application of a Tool Compound Data Set. PMID:29035535
Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation. PMID:29018234
Combined CRISPRi/a-Based Chemical Genetic Screens Reveal that Rigosertib Is a Microtubule-Destabilizing Agent. PMID:28985505
Modulators of 14-3-3 Protein-Protein Interactions. PMID:28968506
SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models. PMID:28890935
Developing antineoplastic agents that target peroxisomal enzymes: cytisine-linked isoflavonoids as inhibitors of hydroxysteroid 17-beta-dehydrogenase-4 (HSD17B4). PMID:28868548
More Haste, Less Speed: Could Public-Private Partnerships Advance Cellular Immunotherapies? PMID:28861415
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel-Lindau (VHL) E3 Ubiquitin Ligase: Structure-Activity Relationships Leading to the Chemical Probe (2S,4R)-1-((S)-2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298). PMID:28853884
Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations. PMID:28790404
Progress towards a public chemogenomic set for protein kinases and a call for contributions. PMID:28767711
Probes &Drugs portal: an interactive, open data resource for chemical biology. PMID:28753599
Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening. PMID:28714473
Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology. PMID:28697345
Chemical genetics and strigolactone perception. PMID:28690842
Chemical modulators for epigenome reader domains as emerging epigenetic therapies for cancer and inflammation. PMID:28689146
Opportunities and challenges in phenotypic drug discovery: an industry perspective. PMID:28685762
Structural Characterization of Maize SIRK1 Kinase Domain Reveals an Unusual Architecture of the Activation Segment. PMID:28603531
Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake. PMID:28584105
Curcumin May (Not) Defy Science. PMID:28523093
Fluorescent Probes and Selective Inhibitors for Biological Studies of Hydrogen Sulfide- and Polysulfide-Mediated Signaling. PMID:28443673
Epigenetic assays for chemical biology and drug discovery. PMID:28439316
The Ecstasy and Agony of Assay Interference Compounds. PMID:28435522
An open source pharma roadmap. PMID:28419094
Benzoisoquinolinediones as Potent and Selective Inhibitors of BRPF2 and TAF1/TAF1L Bromodomains. PMID:28402630
The Ecstasy and Agony of Assay Interference Compounds. PMID:28386587
Inhibitors of Protein Methyltransferases and Demethylases. PMID:28338320
Non-kinase targets of protein kinase inhibitors. PMID:28280261
Structural insight into inhibitors of flavin adenine dinucleotide-dependent lysine demethylases. PMID:28277979
Arylmethylamino steroids as antiparasitic agents. PMID:28211535
Establishing a reliable framework for harnessing the creative power of the scientific crowd. PMID:28199324
Applications of chemogenomic library screening in drug discovery. PMID:28104905
Chemical probes targeting epigenetic proteins: Applications beyond oncology. PMID:28080202
Cellular analysis of the action of epigenetic drugs and probes. PMID:28071961
Broad-Spectrum Kinase Profiling in Live Cells with Lysine-Targeted Sulfonyl Fluoride Probes. PMID:28051857
Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen. PMID:28004573
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors. PMID:28001384
Rational Design of Small Molecules Targeting Oncogenic Noncoding RNAs from Sequence. PMID:27993012
Discovery of a PCAF Bromodomain Chemical Probe. PMID:27966810
A Dormant Microbial Component in the Development of Preeclampsia. PMID:27965958
A Versatile Method to Determine the Cellular Bioavailability of Small-Molecule Inhibitors. PMID:27935314
Adaptive Resistance to an Inhibitor of Chromosomal Instability in Human Cancer Cells. PMID:27829147
Targeting AMPK for the Alleviation of Pathological Pain. PMID:27812984
Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. PMID:27811928
Loss-of-function genetic tools for animal models: cross-species and cross-platform differences. PMID:27795562
Characterization of Hedgehog Acyltransferase Inhibitors Identifies a Small Molecule Probe for Hedgehog Signaling by Cancer Cells. PMID:27779865
Potent and selective bivalent inhibitors of BET bromodomains. PMID:27775716
Design and characterization of bivalent BET inhibitors. PMID:27775715
Structural features and inhibitors of bromodomains. PMID:27769355
Enhancer of Zeste Homolog 2 Inhibition Stimulates Bone Formation and Mitigates Bone Loss Caused by Ovariectomy in Skeletally Mature Mice. PMID:27758858
A High-Throughput Screening-Compatible Strategy for the Identification of Inositol Pyrophosphate Kinase Inhibitors. PMID:27736936
Oligosaccharyltransferase inhibition induces senescence in RTK-driven tumor cells. PMID:27694802
The emerging role of lysine methyltransferase SETD8 in human diseases. PMID:27688818
Glycogen Synthase Kinase 3β Promotes the Endocytosis of Transferrin in the African Trypanosome. PMID:27626104
Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain. PMID:27595327
Dual action antifungal small molecule modulates multidrug efflux and TOR signaling. PMID:27571477
CZ415, a Highly Selective mTOR Inhibitor Showing in Vivo Efficacy in a Collagen Induced Arthritis Model. PMID:27563401
Non-Substrate Based, Small Molecule Inhibitors of the Human Isoprenylcysteine Carboxyl Methyltransferase. PMID:27547295
Inhibition of mTOR-kinase destabilizes MYCN and is a potential therapy for MYCN-dependent tumors. PMID:27438153
Studying epigenetic complexes and their inhibitors with the proteomics toolbox. PMID:27437033
Chemical genetics approaches for selective intervention in epigenetics. PMID:27423045
Unveiling (-)-Englerin A as a Modulator of L-Type Calcium Channels. PMID:27391219
Sensitivity and engineered resistance of myeloid leukemia cells to BRD9 inhibition. PMID:27376689
Chromodomain Ligand Optimization via Target-Class Directed Combinatorial Repurposing. PMID:27356154
Chemical probes for methyl lysine reader domains. PMID:27348158
Structure-Guided Discovery of Selective Antagonists for the Chromodomain of Polycomb Repressive Protein CBX7. PMID:27326334
The arsenal of pathogens and antivirulence therapeutic strategies for disarming them. PMID:27313446
Badapple: promiscuity patterns from noisy evidence. PMID:27239230
Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy. PMID:27222667
Counting on natural products for drug design. PMID:27219696
Tubulin is a molecular target of the Wnt-activating chemical probe. PMID:27207629
Selectivity on-target of bromodomain chemical probes by structure-guided medicinal chemistry and chemical biology. PMID:27193077
Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk. PMID:27159579
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit. PMID:27115555
Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2. PMID:27075367
CETSA screening identifies known and novel thymidylate synthase inhibitors and slow intracellular activation of 5-fluorouracil. PMID:27010513
Beyond PAINs: Chemotype Sensitivity of Protein Methyltransferases in Screens. PMID:26985291
Characterizing the Covalent Targets of a Small Molecule Inhibitor of the Lysine Acetyltransferase P300. PMID:26985290
Preclinical Data on Efficacy of 10 Drug-Radiation Combinations: Evaluations, Concerns, and Recommendations. PMID:26947881
Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. PMID:26914985
Docking Screens for Novel Ligands Conferring New Biology. PMID:26913380
Decoupling Activation of Heme Biosynthesis from Anaerobic Toxicity in a Molecule Active in Staphylococcus aureus. PMID:26890615
DREADDs for Neuroscientists. PMID:26889809
Deciphering the true antiproliferative target of an MK2 activation inhibitor in glioblastoma. PMID:26821065
Small Molecule Inhibitors of Protein Arginine Methyltransferases. PMID:26789238
A Multilayer Network Approach for Guiding Drug Repositioning in Neglected Diseases. PMID:26735851
A Cell Biologist's Field Guide to Aurora Kinase Inhibitors. PMID:26732741
Hitting the target. PMID:26624797
Chemical modulators of ribosome biogenesis as biological probes. PMID:26575239
How to Triage PAINS-Full Research. PMID:26496388
Corrigendum: The promise and peril of chemical probes. PMID:26485080
Investigating Apoptozole as a Chemical Probe for HSP70 Inhibition. PMID:26458144
Tackling reproducibility in academic preclinical drug discovery. PMID:26388229
Tags:
Tags
More detailed information about this field from each metasource.
drug
metasource: Fairsharing.org
version: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
probe
metasource: Fairsharing.org
version: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
protein interaction
metasource: Fairsharing.org
version: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
target
metasource: Fairsharing.org
version: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
biochemical studies
metasource: re3data.org
version: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
biomedical research
metasource: re3data.org
version: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
chemical biology
metasource: re3data.org
version: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
drug discovery
metasource: re3data.org
version: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
medicinal chemistry
metasource: re3data.org
version: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
pharmacology
metasource: re3data.org
version: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
protein interactions
metasource: re3data.org
version: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
Tags
More detailed information about this field from each metasource.
drug
metasource: Fairsharing.orgversion: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
probe
metasource: Fairsharing.orgversion: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
protein interaction
metasource: Fairsharing.orgversion: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
target
metasource: Fairsharing.orgversion: FAIRsharing.org: The Chemical Probes Portal; The Chemical Probes Portal; DOI: https://doi.org/10.25504/FAIRsharing.yrkkbt; Last edited: April 26, 2021, 4:05 p.m.; Last accessed: Jan 03 2022 7:08 p.m.
biochemical studies
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
biomedical research
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
chemical biology
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
drug discovery
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
medicinal chemistry
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
pharmacology
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
protein interactions
metasource: re3data.orgversion: re3data.org: The Chemical Probes Portal; editing status 2021-09-29; re3data.org - Registry of Research Data Repositories. http://doi.org/10.17616/R3NF86 last accessed: 2022-11-04
drug probe protein interaction target biochemical studies biomedical research chemical biology drug discovery medicinal chemistry pharmacology protein interaction
Need help integrating and/or managing biomedical data?