Medicinal Chemistry & Hit to Lead

Plate Based pK_a

Available under aqueous or cosolvent conditions.

pK_as are screened using a fast pH/UV hybrid method. Any UV active pK_as 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