Crelux and Zobio have executed their first fragment-based screening projects from a jointly established platform.
One of the first targets, which will be made accessible to customers, was Pim1, a kinase that has been implicated in the progression of several haematological malignancies.
In addition to the off-the-shelf data on Pim1, tailor made fragment-based screening projects are available for customers upon request.
The joint technology platform combines Zobio's target immobilised NMR screening (TINS) technology with Crelux's kinase crystallography platform.
In the first campaign Pim1 was screened by TINS using Zobio's fragment library, hits were assessed in an in vitro kinase assay and the top 50 hits have been soaked into protein crystals.
A total of 37 out of the 50 fragments showed defined binding modes.
Together with this high hit rate, the structural diversity within this group generated multiple points for optimisation and proved the power of this technology combination.
Crelux has used its structural biology platform to solve more than 270 crystal and co-crystal structures for pharma and biotech companies.
This platform encompasses all steps - from target cloning and expression all the way to high-throughput protein crystallisation and in-house X-ray crystallography.
Zobio provides fragment discovery and characterisation services to the pharmaceutical and biotech industries.
Offering sensitivity and reliability, TINS has been used to discovery diverse, efficient ligands for a variety of targets including kinases, protein-protein interactions, viral targets and membrane proteins.
