ChemDiv’s team of trained and highly experienced scientists is proud to offer unparalleled expertise in developing and accommodating assays for HTS format and designing orthogonal assays for early identification and removal of false positive hits from further costly follow up processes. Not being limited to a third party libraries for screening and by offering our proprietary focused discovery sub-libraries assembled from the ChemDiv’s ever-growing collection of 1.5 million small molecules, being synthesized based on unique ideas of novel templates, provides tremendous benefits for high throughput hit hunting. Unique design of these sublibraries provides a very robust way for early mini-SAR analysis for identification and confirmation of hit series, which then become seed templates for hit expansion, hit-to-lead exploration, and medicinal chemistry lead optimization.

A robust screening platform encompassing automated liquid handling and multimode signal detection equipment have been assembled at ChemDiv to be able to provide access to screening assays for multiplicity of targets, such as receptors, enzymes, signaling pathways etc., which play major role in different therapeutics areas (oncology, immunology, CNS, metabolic diseases).

We have assembled a robust screening infrastructure to be able to work with targets of major therapeutics areas. Our technical park of Discovery Division includes:

Equipment

• Liquid Handling
  • Biomek 2000,
  • Biomek NX,
  • Biomek FX work station
  • 96/384-well plate readers;
    • FLIPR-Tetra (Molecular Devices)
    • Microbeta PLUS 1450 (PerkinElmer),
    • scintillation counters;
    • Victor2V and Victor 3 multimode;
    • SpectraMax Plus 96/384;
    • Mach III (Tomtec) 96-well cell harvester;
    • Beckman and GUAVA 96/384 well format Flow Cytometers.

Readout capabilities

• Luminescence: Reporter genes; ELISAs;
• Fluorescence: FLINT, FRET, TR-FRET, FP, GFP; ELISAs
• Radio-Isotope: Receptor assays (ligand-binding/competition), SPA, metabolic enzymes

Absorbance: OD, ABS spectra

Ready to deploy assays

• In vitro assays:
  • FLIPR (cytoplasmic and mitochondrial calcium),
  • LANCE (cytoplasmic cAMP/cGMP),
  • ELISA,
  • Western,
  • Kinase activity, Enzymatic activity
• Cell Assays:
  • cell growth,
  • cell cycle analysis,
  • apoptosis/necrosis,
  • in vitro chemoinvasion,
  • high content high throughput microscopy
• Molecular and Cell Biology:
  • Custom Expression / Reporter Constructs;
  • Transient/stable transfection.
  • Cell lines and primary cultures;

Please contact our team at chemdiv@chemdiv.com to discuss your specific needs and application.

ChemDiv has assembled a robust high throughput screening platform encompassing automated liquid handling and multimode signal detection equipment for assays to be ran in up to 1536-well plate formats. Multimode reading capability provides access to screening assays with multiplicity of targets, such as receptors, enzymes, signaling pathways etc. that play a major role in different therapeutics areas (oncology, immunology, CNS, metabolic diseases).

ChemDiv offers logistics and compound handling support to High Throughput Screening (HTS) performed at our facilities, which substantially reduces time and eliminates costs associated with compounds shipments and plate preparations. Decades of stellar experience of being a worldwide manufacturer and supplier of chemical libraries to drug discovery institutions, uniquely positions ChemDiv, with its logistics infrastructure, to be able to backtrack every hit to its specific QC data for the original compound on the plate. Our proprietary focused discovery sub-libraries assembled from the ChemDiv’s ever-growing collection of 1.5 million small molecules, being synthesized based on novel templates ideas, provide tremendous benefits for high throughput hit hunting in terms of both potential hit novelty and follow up synthetic hit expansion. Unique design of these sublibraries provides a very robust way for early chemoinformatics-based identification and confirmation of hit compounds with immediate mini-SAR cluster analyses offering seed scaffolds, or starting points, for hit expansion, hit-to-lead exploration, and medicinal chemistry lead optimization.

We have assembled a robust screening infrastructure to be able to work with targets of major therapeutics areas. Our technical park of Discovery Division includes:

Equipment

• Liquid Handling
  • Biomek 2000,
  • Biomek NX,
  • Biomek FX work station
  • 96/384-well plate readers;
    • FLIPR-Tetra (Molecular Devices)
    • Microbeta PLUS 1450 (PerkinElmer),
    • scintillation counters;
    • Victor2V and Victor 3 multimode;
    • SpectraMax Plus 96/384;
    • Mach III (Tomtec) 96-well cell harvester;
    • Beckman and GUAVA 96/384 well format Flow Cytometers.

Readout capabilities

• Luminescence: Reporter genes; ELISAs;
• Fluorescence: FLINT, FRET, TR-FRET, FP, GFP; ELISAs
• Radio-Isotope: Receptor assays (ligand-binding/competition), SPA, metabolic enzymes

Absorbance: OD, ABS spectra

Ready to deploy assays

• In vitro assays:
  • FLIPR (cytoplasmic and mitochondrial calcium),
  • LANCE (cytoplasmic cAMP/cGMP),
  • ELISA,
  • Western,
  • Kinase activity, Enzymatic activity
• Cell Assays:
  • cell growth,
  • cell cycle analysis,
  • apoptosis/necrosis,
  • in vitro chemoinvasion,
  • high content high throughput microscopy
• Molecular and Cell Biology:
  • Custom Expression / Reporter Constructs;
  • Transient/stable transfection.
  • Cell lines and primary cultures;

Custom Assay Development (per Clients’ specification)

Please contact our team at chemdiv@chemdiv.com to discuss your specific needs and application.

ChemDiv is a leading provider of ADME/T molecular screening and development programs. We offer standardized and custom programs, led by experienced PhD-level scientific staff, backed up by processes that deliver fast cycle times. ChemDiv Inc. provides a range of in vitro ADME/T assays to evaluate and improve metabolism, bioavailability, pharmacology, and toxicology characteristics of screening compounds during early stages of hit expansion and lead optimization. Our researchers develop, validate, and apply different modern methods for the early ADME/T molecular screening of potential drugs under development.

PHYSICOCHEMICAL PROFILING

• cLogP, polar surface area, and other physchem parameters;
• Solubility in Aqueous Solutions with different pH;
• PAMPA (Parallel Artificial Membrane Permeability Assay);
• CACO2 permeability (basal-apical/apical-basal)

BIOCHEMICAL PROFILING


• Plasma protein equilibrium binding (different species)
• CYP Inhibition/ CYP induction
• Microsomal metabolism
• Metabolites identification

CELL-BASED TOX PROFILING

• Cytotoxic Effects
• Cytostatic Effects
• hERG inhibition
• Cell growth kinetics
• Apoptosis induction

In vivo DMPK

• PK (IV/PO) in different species
• Efficacy models
• PK/PD in same animals

Please contact our team at chemdiv@chemdiv.com to discuss your specific needs and application.

The cornerstone of ChemDiv’s in vitro pharmacology is a broad expertise in target-specific molecular interactions coupled with state-of-the-art technology platforms. Our team of scientists with extensive industrial experience, supports the in vitro pharmacological characterization of screening compounds as part of hit identification, hit expansion, lead series identification, and lead optimization processes with emphasis on novelty to generate target-relevant high-quality data and New Chemical Entity in a short turnaround time.

The Company’s offering includes:

• Development of biochemical and cell-based functional assays
• Secondary and tertiary characterization of screening hits
• Compound characterization as part of hit-to-lead and lead optimization programs
• Design and synthesis of novel small molecule entities in a target-relevant space
• Design and implementation of target-relevant screening cascades
• Potency and selectivity assessment
• Mode-of-action studies (e.g. competitive vs. allosteric, reversible vs. non-reversible etc.)
• Translational assays (rodents, primates, or humans)
• Disease-relevant primary and engineered cells
• Surrogate ADME assessment (such as solubility, microsomal stability, CYP inhibition, plasma protein binding, CACO-2 permeability)
• Pharmacokinetics and Pharmacokinetics/Pharmacodynamics in rodents

More than 15 years of screening compound profiling campaigns at ChemDiv yielded hundreds of assays developed and executed in different formats: from Low Throughput to Mid and High Throughput. The in vitro Pharmacology is part of ChemDiv’s integrated lead finding and optimization projects as well as is frequently used to support discovery chemistry projects that are executed in labs of ChemDiv’s customers.

Please contact our team at chemdiv@chemdiv.com to discuss your specific needs and application.

Testing drug candidates in in vivo animal settings is still necessary step in the process of discovery chemistry to understand the candidate behavior in the whole organism, starting from bioavailability and going through pharmacokinetics, organ exposure, pharmacodynamics, efficacy in a disease models, and to a potential toxicity of either the compound itself or its metabolite(s).

ChemDiv’s in vivo pharmacology team consists of highly experienced scientists with extensive pharmaceutical and biotechnology backgrounds. ChemDiv has state-of-the art animal facility equipped to house immune-compromised animals, rodents with genetically modified disease specific background and access to other facilities housing other species including dogs and monkeys. All experimental procedures involving animals have been implemented according to US, EU, and RF animal welfare laws.

ChemDiv offers in vivo pharmacology services in accordance with customer’s-designed protocols supporting its discovery chemistry needs on flexible basis: from delivering standalone studies to taking over responsibility for planning and executing the in vivo pharmacology strategy in a frame of integrated discovery chemistry program.

ChemDiv offers high-quality in vivo services including efficiency and tolerability studies, in a wide range of therapeutic areas.

Please contact our team at chemdiv@chemdiv.com to discuss your specific needs and application.