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Technical Notes
Chemical Stability
Explore drug stability assessment under physiological conditions using Sygnature's chemical stability assay. Learn about its significance in understanding molecule lability and potential impacts on biological data and pharmacokinetics.
Technical Notes
P450 / CYP Inhibition
Discover P450/CYP inhibition & drug interactions. Assess CYP isoforms, predict co-administered drug risks. Reliable screening with Sygnature.
Technical Notes
Hepatocyte Metabolic Stability
The liver is the major site of drug metabolism in the body, with well over…
Technical Notes
Microsomal Clearance and Stability
Discover the significance of hepatic drug metabolism through microsomal clearance studies. Sygnature offers NADPH-based Phase I assays and combined Phase I/Phase II assays for comprehensive metabolism insights. Gain compound ranking and predict in vivo hepatic clearance. Validated with species-specific controls, get accurate mean intrinsic clearance and half-life measurements.
Technical Notes
Plasma Protein Binding
Streamlined Plasma Protein Binding Assessment Using Rapid Equilibrium Dialysis In drug development, understanding plasma protein…
Technical Notes
Plasma and Blood Stability
Improve in vivo PK studies by evaluating chemical stability in plasma. Our assay measures molecule stability in mouse, rat & human plasma, aiding compound prioritisation. Explore species differences. Proven positive & negative control compounds.
Case Studies
Fragment-based hit discovery for the epigenetic target, BRD3
Fragment-based drug discovery allows a wide section of chemical space to be interrogated with a relatively small but diverse library of small molecules.
Journal Papers
Correction: Conformationally restricted benzothienoazepine respiratory syncytial virus inhibitors: their synthesis, structural analysis and biological activities
Euan A F Fordyce, S Fraser Hunt, Damien Crepin, Stuart T Onions, Guillaume F Parra, Chris J Sleigh, John King-Underwood, Harry Finch, John…
Journal Papers
Combinatorial Biophysical Approach: FTSA and SPR for Small Molecule Ligand and PAIN Identification
Biophysical dual method: FTSA and SPR for drug discovery. Explore ligands and PAINs, gain insights on affinity values and compound binding.
Journal Papers
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile
Hunt, H. J., Belanoff, J.K., Golding, E., Gourdet, B., Phillips, T., Swift, D., Thomas, J., Unitt,…
Journal Papers
The Identification of the Clinical Candidate
The Identification of the Clinical Candidate (R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1Hpyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134):– A Selective Glucocorticoid Receptor (GR) Antagonist Hunt,…
Journal Papers
Thermal Shift as an Entropy Driven Effect
Redhead M, Satchell R, McCarthy C, Pollack S, Unitt J. Biochemistry. 2017 Nov 28;56(47):6187-6199 Abstract…
Journal Papers
Surface Plasmon Resonance for Small Molecule Ligand Analysis
From the book « Biophysical Techniques in Drug Discovery », Chapter 7, Pages 170 – 207 Editor: Angeles…
Technical Notes
MDCK-WT/MDR1 Permeability
Wild-type MDCK (Madin-Darby canine kidney) cells, when transfected with either the Multidrug Resistance gene-1 (MDR1;…
Technical Notes
Time Dependent Inhibition
Explore Time-Dependent Inhibition (TDI) & Drug Interactions with Sygnature's CYP450 Assay. Predict IC50 Shift & Enzyme Dynamics.
Technical Notes
Parallel Artificial Membrane Permeability Assay (PAMPA)
Enhance drug development using PAMPA assay for permeability assessment. Rapid, accurate, and high-throughput method. Sygnature's advanced approach with Corning's pre-coated plate system. LC-MS/MS readouts and precise calibration curve ensure reliable results. Caffeine and Famotidine controls included.
Journal Papers
FKBP5 mRNA Expression is a Biomarker for GR Antagonism
Developing a qPCR assay to monitor mifepristone's effectiveness in Cushing's syndrome patients.
Journal Papers
Tools, techniques, organisation and culture of the CADD group at Sygnature Discovery
St-Gallay SA, Sambrook-Smith CP. J Comput Aided Mol Des. 2017 Mar;31(3):305-308. Computer-aided drug design encompasses a…
Journal Papers
Diastereoselective Synthesis of Highly Substituted, Amino- and Pyrrolidino-Tetrahydrofurans as Lead-Like Molecular Scaffolds
Dr. Steven M. Wales, Dr. Elena G. Merisor, Dr. Holly V. Adcock, Dr. Christopher A. Pearce, Dr. Ian R.
Journal Papers
Evaluation of the Biological Activity of Compounds: Techniques and Mechanism of Action Studies
Dougall, I. C,  Unitt, J. Abstract The first step in the biological assessment of compounds synthesized…
Journal Papers
Fluorescent Thermal Shift Assays for Identifying Small Molecule Ligands
Andrew D. Scott Abstract Fluorescent thermal shift assay (FTSA; also known as ThermoFluor, differential scanning…
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