about
Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834Structure-Guided Design of Group I Selective p21-Activated Kinase InhibitorsChemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Windowp21-activated kinase inhibitorsp21-Activated kinase inhibitors: a patent reviewRate-Determining and Rate-Limiting Steps in the Clearance and Excretion of a Potent and Selective p21-Activated Kinase Inhibitor: A Case Study of Rapid Hepatic Uptake and Slow Elimination in Rat.Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.Recent progress on nuclear receptor RORγ modulators.RORγ antagonists and inverse agonists: a patent review.Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell-associated damage in IFNα-driven lupus nephritis.Inhibitors of p21-activated kinases (PAKs).Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.Learning Medicinal Chemistry Absorption, Distribution, Metabolism, Excretion, and Toxicity (ADMET) Rules from Cross-Company Matched Molecular Pairs Analysis (MMPA).Streamlined Total Synthesis of Uncialamycin and Its Application to the Synthesis of Designed Analogues for Biological Investigations.Synthesis of Fused Imidazole-Containing Ring Systems via Dual Oxidative Amination of C(sp(3))-H Bonds.A simple in vitro assay for assessing the reactivity of nitrile containing compounds.Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats.NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.Discovery of GDC-0853, a Potent, Selective, and Non-Covalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors.Synthesis of (+)-crocacin D and simplified bioactive analogues.Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition.Single electron transfer (SET) activity of the dialkyl-amido sodium zincate [(TMEDA)·Na(μ-TMP)(μ-tBu)Zn(tBu)] towards TEMPO and chalconeOptimized arylomycins are a new class of Gram-negative antibioticsRemote functionalisation via sodium alkylamidozincate intermediates: access to unusual fluorenone and pyridyl ketone reactivity patternsCopper/TEMPO catalysed synthesis of nitriles from aldehydes or alcohols using aqueous ammonia and with air as the oxidantDiethylphosphine oxide (DEPO): high-yielding and facile preparation of indolones in waterTotal synthesis and stereochemistry of uncialamycinProtecting group free, stereocontrolled synthesis of β-halo-enamidesFast and efficient one step synthesis of dienamidesStep-economic synthesis of (+)-crocacin C: a concise crotylboronation/[3,3]-sigmatropic rearrangement approachPharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitorsScaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing KinaseLogD Contributions of Substituents Commonly Used in Medicinal ChemistryHippo pathway inhibition by blocking the YAP/TAZ-TEAD interface: a patent reviewThe kinase IRAK4 promotes endosomal TLR and immune complex signaling in B cells and plasmacytoid dendritic cells
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P50
description
researcher ORCID ID = 0000-0002-6408-8246
@en
wetenschapper
@nl
name
James J Crawford
@ast
James J Crawford
@en
James J Crawford
@es
James J Crawford
@nl
type
label
James J Crawford
@ast
James J Crawford
@en
James J Crawford
@es
James J Crawford
@nl
prefLabel
James J Crawford
@ast
James J Crawford
@en
James J Crawford
@es
James J Crawford
@nl
P106
P1153
57202296166
7401850669
P31
P496
0000-0002-6408-8246