Visit With BellBrook Labs at Discovery On Target 2018

Discovery on Target 2018
BellBrook Labs will exhibit and present posters at the upcoming Discovery on Target conference in Boston, MA. At the event BellBrook will demonstrate applications for its suite of high throughput screening tools, including residence time determination, methyltransferase activity measurement, studying ectonucleotidase enzymes, screening for kinase inhibitors, and more! Discovery on Target 2018 Sheraton Boston Hotel
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A Guide to Measuring Drug-Target Residence Times with Biochemical Assays

Residence Time Guide
Learn How to Determine Drug-Target Residence Times with Biochemical Assays in this Free Guide Drug-target residence time has become a critical component in the discovery of new therapeutics. BellBrook Labs has recently published a guide to help describe the use of a proven “jump-dilution” method along with BellBrook’s Transcreener Assay platform to help streamline efforts
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New Posters from DOT 2017

Poster Presentations A Homogenous, High Throughput Assay to Measure Guanine Nucleotide Exchange Factor Activity Using Transcreener® GDP Assay Guanine nucleotide exchange factors (GEFs) positively regulate Rho GTPases by accelerating GDP dissociation to allow formation of the active, GTP-bound complex. Development of inhibitors that specifically disrupt GEF action on a target Rho GTPase may be a
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Sialyltransferases: Sugar Makes the Medicine Go Down?

Glycan structures decorate a wide variety of cell types—dotting the surface of blood cells, linked to lipid moieties on neurons, and studding the membrane of tumor cells. These carbohydrate structures create a cellular language that is translated by binding partners, eliciting specific downstream effects. And for some cancers, the effects can be devastating.   Consider
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Ectonucleotidases: An Outside Chance for Drug Development

Sometimes, the most intriguing cellular processes happen outside of the cell. Case in point: purinergic signaling pathways, in which extracellular receptors sense levels of purines in the extracellular milieu. The result? A wide array of effects on neuronal signaling, vascular tone, thrombosis, and immune function. But what controls the level of extracellular purines? Enter ectonucleotidases:
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New Publication: HTS Method for Measuring Drug Residence Time

View our latest publication, “A High-Throughput Method for Measuring Drug Residence Time Using the Transcreener® ADP2 Assay” in SLAS Discovery. Inhibitor residence times are increasingly being used to prioritize molecules early in lead discovery programs. Current methods for determining residence time are low-throughput or require the synthesis of labeled ligands. Our goal was to create
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Targeting Phosphodiesterase 4B for Cognitive Disorders

Cognitive dysfunction, including loss of core functions such as memory, learning and reasoning occurs in many psychiatric disorders, and impairs the quality of life for millions of older adults suffering from dementia. As there is no single cause, treatments vary. However the few drugs that are available, most of which boost neurotransmitter levels, are not
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Jump-Starting Residence Time Assays

New Case Study: Determination of Inhibitor Residence Times for a Phosphodiesterase using the Transcreener® AMP2/GMP2 FP Assay Analysis of inhibitor residence times is increasingly being incorporated into lead development efforts because longer engagement with the target can result in improved efficacy, increased therapeutic window and reduced side effects. BellBrook Labs scientist, Meera Kumar, recently used
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Overcoming the Blood-Brain Barrier: Increasing Access for Therapeutic Agents

The blood-brain barrier (BBB), a layer of endothelial cells lining the blood vessels leading to the brain, is one of the brain’s greatest assets.  Responsible for determining what molecules are allowed to cross from the bloodstream into the brain, the BBB protects the brain from the invasion of infectious and toxic agents. However, this barrier
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Ensuring Assay Success: The Right Plate Makes All The Difference

Transcreener® HTS Assays rely on direct immunodetection of nucleotides with a far-red readout in a simple mix-and-read format.  The assays are available in three different detection modes, fluorescence polarization (FP), fluorescence intensity (FI), and time-resolved Forster resonance energy transfer (TR-FRET).  A good microplate reader and the right choice of plates to differentiate specific signal versus
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