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Case Studies
Hit Identification to 3 Compounds in the Clinic and 6 Development Candidates
UK-based small molecule drug discovery company Focus on identifying novel treatments of inflammatory respiratory diseases,…
Journal Papers
Design and synthesis of a potent, highly selective, orally bioavailable, retinoic acid receptor alpha agonist
Earl Clarke, Christopher I Jarvis, Maria B Goncalves, …
News
Sygnature Discovery’s Head Quarters is nominated for RICS Awards 2018
On the 26th of February 2018, in Nottingham, UK, an esteemed milestone was reached as…
Technical Notes
Caco-2 Permeability
The human colon epithelial cancer cell line, Caco-2, is used as a model of human intestinal absorption of drugs. This model is suitable to test compound suitability for oral dosing, predict intestinal permeability and investigate drug efflux.
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.
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