List of works by Ajit Jadhav

12-lipoxygenase activity plays an important role in PAR4 and GPVI-mediated platelet reactivity

scientific article published on 20 June 2013

3-substituted indole inhibitors against Francisella tularensis FabI identified by structure-based virtual screening

scientific article published on July 2013

4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth

scientific article

A 1,536-well-based kinetic HTS assay for inhibitors of Schistosoma mansoni thioredoxin glutathione reductase

scientific article published on August 2008

A Comparative Study of Target Engagement Assays for HDAC1 Inhibitor Profiling

scientific article published on 29 October 2019

A High-Content Assay Enables the Automated Screening and Identification of Small Molecules with Specific ALDH1A1-Inhibitory Activity.

scientific article

A High-Throughput Screen Identifies 2,9-Diazaspiro[5.5]Undecanes as Inducers of the Endoplasmic Reticulum Stress Response with Cytotoxic Activity in 3D Glioma Cell Models

scientific article

A comprehensive strategy to discover inhibitors of the translesion synthesis DNA polymerase κ

scientific article

A fluorescence-based high throughput assay for the determination of small molecule-human serum albumin protein binding

scientific article

A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().

scientific article

A grid algorithm for high throughput fitting of dose-response curve data

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A high throughput fluorescence polarization assay for inhibitors of the GoLoco motif/G-alpha interaction

scientific article

A high throughput screen identifies potent and selective inhibitors to human epithelial 15-lipoxygenase-2

scientific article

A high-throughput approach for identification of novel general anesthetics

scientific article

A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein

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A high-throughput screen for aggregation-based inhibition in a large compound library

scientific article published on 21 April 2007

A high-throughput small molecule screen identifies synergism between DNA methylation and Aurora kinase pathways for X reactivation

scientific article

A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety

scientific article

A miniaturized glucocorticoid receptor translocation assay using enzymatic fragment complementation evaluated with qHTS.

scientific article published on August 2008

A miniaturized screen for inhibitors of Jumonji histone demethylases

scientific article

A novel P300 inhibitor reverses DUX4-mediated global histone H3 hyperacetylation, target gene expression, and cell death

scientific article published on 11 September 2019

A potent and selective inhibitor targeting human and murine 12/15-LOX.

scientific article

A quantitative high-throughput screen for modulators of IL-6 signaling: a model for interrogating biological networks using chemical libraries

scientific article

A quantitative high-throughput screen identifies potential epigenetic modulators of gene expression

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A robotic platform for quantitative high-throughput screening

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A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses.

scientific article

A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells

scientific article

A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase

scientific article

Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes

scientific article

AlphaScreen-Based Assays: Ultra-High-Throughput Screening for Small-Molecule Inhibitors of Challenging Enzymes and Protein-Protein Interactions

scientific article

Anxiolytic Drug FGIN-1-27 Ameliorates Autoimmunity by Metabolic Reprogramming of Pathogenic Th17 Cells

scientific article published on 28 February 2020

Are hERG channel blockers also phospholipidosis inducers?

scientific article published on 20 June 2013

Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays

scientific article published on 6 October 2017

Biochemical and Cellular Characterization and Inhibitor Discovery of Pseudomonas aeruginosa 15-Lipoxygenase

scientific article

Biochemical assays for the discovery of TDP1 inhibitors

scientific article

Cell Lysate-Based AlphaLISA Deubiquitinase Assay Platform for Identification of Small Molecule Inhibitors

scientific article

Characterization of chemical libraries for luciferase inhibitory activity

scientific article

Chemical Control of a CRISPR-Cas9 Acetyltransferase.

scientific article

Complementarity Between a Docking and a High-Throughput Screen in Discovering New Cruzain Inhibitors

scientific article

Compound Management for Quantitative High-Throughput Screening

scientific article

Compound cytotoxicity profiling using quantitative high-throughput screening

scientific article

Comprehensive Mechanistic Analysis of Hits from High-Throughput and Docking Screens against β-Lactamase

scientific article

Connecting Neuronal Cell Protective Pathways and Drug Combinations in a Huntington's Disease Model through the Application of Quantitative Systems Pharmacology.

scientific article published on 19 December 2017

Correction: A High-Content Assay Enables the Automated Screening and Identification of Small Molecules with Specific ALDH1A1-Inhibitory Activity.

scientific article published on 15 May 2018

Covalent small molecule inhibitors of Ca(2+)-bound S100B.

scientific article

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).

scientific article

Discovery and lead identification of quinazoline-based BRD4 inhibitors

scientific article published on 31 August 2018

Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1)

scientific article published on 24 July 2015

Discovery of Orally Bioavailable, Quinoline-based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity.

scientific article published on 16 May 2018

Discovery of a 2,4-Diamino-7-aminoalkoxyquinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

scientific article

Discovery of a novel dual fungal CYP51/human 5-lipoxygenase inhibitor: implications for anti-fungal therapy

scientific article (publication date: 2013)

Discovery of a novel general anesthetic chemotype using high-throughput screening

scientific article

Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase

scientific article

Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.

scientific article

Disrupting malaria parasite AMA1-RON2 interaction with a small molecule prevents erythrocyte invasion

scientific article

Diverse small molecule inhibitors of human apurinic/apyrimidinic endonuclease APE1 identified from a screen of a large public collection

scientific article

Drug-based modulation of endogenous stem cells promotes functional remyelination in vivo

scientific article

Dual-fluorophore quantitative high-throughput screen for inhibitors of BRCT-phosphoprotein interaction

scientific article

Erratum: Quantitative high throughput screening using a primary human three-dimensional organotypic culture predicts in vivo efficacy

scientific article published on 3 February 2016

Exploratory analysis of kinetic solubility measurements of a small molecule library

scientific article

First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis

scientific article published on 03 August 2017

Fluorescence polarization assays in high-throughput screening and drug discovery: a review

scientific article published on 28 April 2016

Fluorescence spectroscopic profiling of compound libraries

scientific article

Fluorescent protein-based cellular assays analyzed by laser-scanning microplate cytometry in 1536-well plate format

scientific article

Fragment-Based Discovery of a Regulatory Site in Thioredoxin Glutathione Reductase Acting as “Doorstop” for NADPH Entry

scientific article published on 11 June 2018

Genomic and protein expression analysis reveals flap endonuclease 1 (FEN1) as a key biomarker in breast and ovarian cancer

scientific article

High-affinity inhibitors of human NAD-dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of inhibition and structure-activity relationships

scientific article

High-throughput 1,536-well fluorescence polarization assays for α(1)-acid glycoprotein and human serum albumin binding

scientific article

High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells

scientific article

High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe

scientific article

High-throughput screen identifies cyclic nucleotide analogs that inhibit prostatic acid phosphatase

scientific article

High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2

scientific article published in Journal of Biological Chemistry

Highly predictive and interpretable models for PAMPA permeability

scientific article published on 31 December 2016

Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB

scientific article

Identification and characterization of inhibitors of human apurinic/apyrimidinic endonuclease APE1

scientific article

Identification of Activators of Human Fumarate Hydratase by Quantitative High-Throughput Screening

scientific article published on 14 September 2019

Identification of novel PARP inhibitors using a cell-based TDP1 inhibitory assay in a quantitative high-throughput screening platform

scientific article

Identification of phosphotyrosine mimetic inhibitors of human tyrosyl-DNA phosphodiesterase I by a novel AlphaScreen high-throughput assay

scientific article

Inhibition of DNA glycosylases via small molecule purine analogs

scientific article

Inhibition of thioredoxin reductase 1 by porphyrins and other small molecules identified by a high-throughput screening assay

scientific article

Inhibitors of the Menin-Mixed Lineage Leukemia (MLL) Interaction

scientific article published on 10 May 2013

Inhibitors of the apurinic/apyrimidinic endonuclease 1 (APE1)/nucleophosmin (NPM1) interaction that display anti-tumor properties

scientific article published on 11 April 2015

Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.

scientific article published on 14 March 2018

Integration of pro-inflammatory cytokines, 12-lipoxygenase and NOX-1 in pancreatic islet beta cell dysfunction

scientific article

Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy.

scientific article published in February 2018

KDM4/JMJD2 Histone Demethylase Inhibitors Block Prostate Tumor Growth by Suppressing the Expression of AR and BMYB-Regulated Genes

scientific article

KDM5 histone demethylases repress immune response via suppression of STING

scientific article published on 06 August 2018

Kinetic, Mutational, and Structural Studies of the Venezuelan Equine Encephalitis Virus Nonstructural Protein 2 Cysteine Protease

scientific article

Large-Scale Screening and Identification of Novel Ebola Virus and Marburg Virus Entry Inhibitors

scientific article

Lecithin:Cholesterol Acyltransferase Activation by Sulfhydryl-Reactive Small Molecules: Role of Cysteine-31.

scientific article published on 02 June 2017

Microfluidic Mobility Shift Profiling of Lysine Acetyltransferases Enables Screening and Mechanistic Analysis of Cellular Acetylation Inhibitors.

scientific article published on October 2015

Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol

scientific article published on 27 November 2018

NCATS Inxight Drugs: a comprehensive and curated portal for translational research

scientific article published on 14 October 2021

Novel Phenotypic Outcomes Identified for a Public Collection of Approved Drugs from a Publicly Accessible Panel of Assays

scientific article

Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond

scientific article (publication date: July 2016)

Optimization and validation of two miniaturized glucocerebrosidase enzyme assays for high throughput screening

scientific article published in December 2008

Oxadiazole 2-oxides are toxic to the human hookworm, Ancylostoma ceylanicum, however glutathione reductase is not the primary target

scientific article

Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold

scientific article published on 21 August 2017

Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor

scientific article published on 10 June 2013

Pharos: Collating protein information to shed light on the druggable genome

scientific article

Platelet 12-LOX is essential for FcγRIIa-mediated platelet activation

scientific article

Potent and selective inhibitors of human reticulocyte 12/15-lipoxygenase as anti-stroke therapies

scientific article

Preparation of FRET reporters to support chemical probe development

scientific article published on 20 August 2010

Protein kinase C regulation of 12-lipoxygenase-mediated human platelet activation

scientific article published on 9 December 2011

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines

scientific article

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

scientific article

Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease

scientific article

Quantitative high throughput screening using a primary human three-dimensional organotypic culture predicts in vivo efficacy.

scientific article published on 5 February 2015

Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing

scientific article published on 19 December 2017

Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade

scientific article

Quantitative high-throughput screening identifies cytoprotective molecules that enhance SUMO conjugation via the inhibition of SUMO-specific protease (SENP)2.

scientific article published on 16 November 2017

Quantitative high-throughput screening: a titration-based approach that efficiently identifies biological activities in large chemical libraries

scientific article

Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells

scientific article

Selective inhibition of 12-lipoxygenase protects islets and beta cells from inflammatory cytokine-mediated beta cell dysfunction

scientific article

Sharing and community curation of mass spectrometry data with Global Natural Products Social Molecular Networking

scientific article (publication date: 9 August 2016)

Streamlined system for purifying and quantifying a diverse library of compounds and the effect of compound concentration measurements on the accurate interpretation of biological assay results

scientific article

Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds

scientific article published on 13 July 2016

Structural insight into exosite binding and discovery of novel exosite inhibitors of botulinum neurotoxin serotype A through in silico screening

scientific article

Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis

scientific article published on October 2009

Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors

scientific article published on 04 December 2013

Suppression of the FOXM1 transcriptional programme via novel small molecule inhibition

scientific article

Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase

scientific article published on 13 August 2013

Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase

scientific article published on 06 January 2014

Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer

scientific article

Synthesis, biological evaluation, and structure-activity relationships of a novel class of apurinic/apyrimidinic endonuclease 1 inhibitors

scientific article

Targeting human apurinic/apyrimidinic endonuclease 1 (APE1) in phosphatase and tensin homolog (PTEN) deficient melanoma cells for personalized therapy

scientific article

Targeting the JMJD2 histone demethylases to epigenetically control herpesvirus infection and reactivation from latency

scientific article published on January 2013

The NCATS BioPlanet - An Integrated Platform for Exploring the Universe of Cellular Signaling Pathways for Toxicology, Systems Biology, and Chemical Genomics

The NCGC pharmaceutical collection: a comprehensive resource of clinically approved drugs enabling repurposing and chemical genomics

scientific article

The pilot phase of the NIH Chemical Genomics Center

scientific article

Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease

scientific article

Unexplored therapeutic opportunities in the human genome.

scientific article published on 23 February 2018

Varied Role of Ubiquitylation in Generating MHC Class I Peptide Ligands.

scientific article published on 31 March 2017

Weighted feature significance: a simple, interpretable model of compound toxicity based on the statistical enrichment of structural features

scientific article published on 04 October 2009