Medicinal Chemistry & Hit to Lead
Sirius offer fast, high quality Plate-Based assays for Medicinal Chemistry and Hit to Lead stages of drug development. We also offer consultancy where we will work with your chemists to provide context for the physicochemical data and training in the understanding of the parameters.
Objectives:
- Assays designed for 10mM DMSO stocks
- Analysis of large batches of compounds
- Fast turnaround
- Straightforward, standardised assay conditions
Assays Available:
Detailed Assay Information:
Plate Based pKa
Available under aqueous or cosolvent conditions.
pKas are screened using a fast pH/UV hybrid method. Any UV active pKas between 2 and 12 are detected.
Turbidity detection can identify compounds which precipitate.
Requires:
- 150ul of 10mM DMSO stock, or enough solid to create the stock ourselves.
- Client to select required condition (aqueous or cosolvent) in advance.
Delivers:
- Table of pKa results (failures due to precipitation or no UV absorption are indicated)
- Method overview
- Distribution of Species plots for all successful samples
- Molar absorption plots for UV active species of successful samples
Plate Based logD
LogD screening at a fixed pH's of 2.5, 4.5 and 7.4, with a HPLC approach using octanol coated columns.
Requires:
- 150ul of 10mM DMSO stock, or enough solid to create the stock ourselves.
Delivers:
- Table of logD results at specified pH values
- Chromatograms
- Method overview
Plate Based Stability
Compounds are screened for stability at low pH (2.0) and high pH (12.0).
Requires
- 150ul of 10mM DMSO stock, or enough solid to create the stock ourselves.
- Client to select required conditions in advance (i.e. low pH, high pH, and timeframe)
Delivers
- Table of observations (i.e. compound is unstable or not under the specified conditions)
- UV spectra of any species detected
Plate Based PAMPA Permeability
Measures rate of passage of a compound through a lipid/alkane membrane. Uses 96 well plates of compound stocks. pH can be adjusted between pH 3 and pH 10. Compound concentration in both Acceptor and Donor layers assayed using UV absorbance.
Requires:
- 150ul of 10mM DMSO stock, or enough solid to create the stock ourselves.
- Client to choose pH conditions and membrane type
Delivers:
- Table of Permeability results
- Membrane retention
- pH vs Permeability plot (if more than one pH studied)
Plate Based Surface Activity
Surface Tension measured using the Delta-8 in 96 well plate format.
Requires
- 150ul of 10mM DMSO stock, or enough solid to create the stock ourselves.
Delivers
- Surface Tension
- CMC (Critical Micelle Concentration)
- TSA (Total Surface Area)
- Air/Water Partition Coefficient
Plate Based Phospholipidosis Screen
Compounds are screened for risk of Phospholipidosis induction using PLDScreen on the Delta-8.
Requires
- 150ul of 10mM DMSO stock, or enough solid to create the stock ourselves.
Delivers
- Surface Tension
- CMC
- Phospholipidosis risk assessment
To use the service, simply fill in a sample submittal form:
Click here for plate based assay submittal formLatest Sirius Posters Available for download
01.08.09
Our latest posters, including Solubility & Dissolution measurements in excipients and FaSSIF/FeSSIF media and high throughput pKa measurements, are available for download.
New Scientific Paper Published
07.12.09
New paper from Sirius explains how our solubility measurements work, and introduces new methods for evaluating supersaturation.
PhysChem Forum 8
23.03.10
Sirius are sponsors and exhibitors at the next PhysChem Forum being held at Pfizer in Sandwich, UK.
ADMET Europe 2010
08.04.10
Sirius will be exhibiting and speaking at ADMET Europe 2010 in Munich. Visit us on booth #12.