Most of ArisPharma chemists are Ph.D.'s with post doctoral and previous industrial experience. Our scientists are very adept at designing new synthetic routes to target molecules as well as working on various scales. Together with our talented staff, we have all the tools necessary to support your medicinal chemistry needs, such as advanced analytical instrumentation (NMR, LC-MS, HPLCs), preparative HPLC, etc. ArisPharma has a proven track record in this area, from synthesis of analogs on milligram scale to the semi-scale up of lead compounds.

Our mission is to ensure customer's research success by delivering creative solutions based on effective communication and services at a competitive price without compromising the quality and IP.

We provide services in the following areas:

We provide custom synthesis of various building blocks, reference compounds and novel molecules, ranging from a few milligrams, to kilograms quantities. Our highly efficient and professional project management group and chemistry team hold the key to our consistent success: We care about customers' concerns and requirement, and try our best to meet the challenges.

Special Technologies
 

Acylation	Amidation	Asymmetric Synthesis	Bromination
Chlorination	Coupling Reaction	Diazotization	Esterification
Fluorination	Hydrosilylation	Hydrogenation
Reduction	Oxidation	Ring closure	Resolution

ArisPharma offers FTE scientists (Ph.D, MS.-level chemists) to our customers for lead optimization, scale up synthesis and process R&D. Our hard working and experienced chemists can save you time and minimize the risk and costs in the early stages of your projects.
We will do our utmost to keep our customers' information confidential and to give complete guarantee for IP protection.

In silico drug discovery service using molecule modeling software and virtual screening against public or in-house libraries to generate hits
1.Hits to leads expansion using structure- or ligand-based design
2.QSAR evaluation to predict physicochemical properties
3.Closely cooperate with clients to design and provide compounds needed to optimize hits

Virtual screening is computational screening of small-molecule libraries using the three-dimensional structure of a target protein or the chemical structure of known active compounds. Softwares are used to match each small-molecule compound in the library to a binding site in the target protein or to the structure of a known active compound. Scoring function is selected to produce a ranked list of compounds predicted to bind to the target protein or mimic the active compound. Softwares include Shrodinger suite, MOE, Autodock, DOCK etc.

ArisPharma provides virtual screening of drug-like compounds and fragment libraries. These include the in-house drug-like compounds, NCI library (~265,000 compounds) and libraries of commercially available compounds (>20 million compounds). Virtual screening can usually be completed in a few weeks. Hits generated can be purchased or synthesized by us.
 

1. Protein Structure Modeling
Proteins without NMR or crystallography data can obtain a model of its 3D structure via comparative or homology modeling, which takes advantage of the known structures of homologous proteins. ArisPharma provides protein structure modeling services and offers guidance to make decisions about the suitability of models for virtual screening and other applications.

 

2. Ligand Binding Site Identification
ArisPharma provides methods for the identification of ligand binding sites in protein structures. Identifying the likely binding sites is useful to guide virtual screening, mutagenesis experiments etc. Hits will be generated using structure-based design with crystallography or NMR data of target protein, or with a homology model.
Example: Heat Shock Protein 70 binding site identification, homology model, inhibitor design and hit optimization.

Rational design of the allosteric pocket ligands. (a,b) The homology-modeled hHsp70 structure led to the identification of a novel allosteric pocket (shown in green) located in the N-terminal domain of human Hsp70

ArisPharma helps to identify tool compounds with known bioactivities for target validation. This will generate SAR data for compound identified in virtual or physical small-molecule screens. We use software QSAR evaluation to predict physicochemical properties. ArisPharma also provides services to identify small molecules that are similar to existing hits or new compounds

ArisPharma provides full medicinal chemistry services. We offer hit-to-lead and lead optimization services to our pharmaceutical and biotechnology clients. We couple our expertise in tackling complex biologically relevant compounds with our deep understanding of medicinal chemistry to help drive projects toward the clinic for our clients.

1. Expert advice on chemistry and overall project strategy for library design and synthesis
2. Designing library with (bio-) Isosteric replacement, hit fragmentation, fragment linking, fragment
expansion, pharmacophore hopping etc.
3. Synthetic route design, optimization and scale-up chemistry
4. Scaffold and custom building-block synthesis based on client / our designs
5. Hit to lead and lead optimization to furnish preclinical candidates
6. Scaffold-hopping for IP extensions

Example: First round hit to lead optimization (from covalent to non-covalent inhibitors)
 

ArisPharma delivers optimized solutions for custom labeling, assay development and implementation, reagent supply and training service. Bio-chemical tools design and synthesis are utilized to support biological assay development in various drug discovery stages.

FITC-derivatized Poloxamer with Purity Analyzed by CAD (charged aerosol detection)

 

Chemical Structure of Poloxamer

 

 

Equipments available in the Lab:

.Hydrogenator
.Parr reactors
.semi-scale up glass reactors
.Heidolph Laborota 20 20 liter Rotavapor
.Biotage Microwave reactor
.Varian 400 MHz NMR
.Agilent 1100 and Shimadzu HPLCs
.prep HPLC
.Waters LC-MS's.
.Buchi Syncore reactor system