| Kinase Library |
6084 compounds
For cherry-picking
Update: 2020-07 |
ASINEX facilitates the discovery of novel kinase inhibitors by providing access to
our advanced collection of small molecules, fragments and macrocycles. The efficacy
of our compounds has been validated through in silico modeling and in vitro
on-target and phenotypic profiling. This is paralleled with 20+ years of medicinal
chemistry expertise, delivering designs with outstanding ADMET and PK properties,
optimizing chances in hit to candidate development. F
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| Kinase Type II Inhibitors |
2376 compounds
For cherry-picking
Update: 2020-07 |
ASINEX has designed molecules that could act as Type-II Kinase ligands using a
proprietary computational algorithm.
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SL#015
Ser-Thr Kinases |
80 compounds
Pre-Plated Set
Release: 2016 |
ASINEX has designed molecules that in vitro target a number of Ser-Thr Kinases
including Aurora A, Aurora B, Haspin, and B-Raf.
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SL#026
IRAK4 inhibitors |
80 compounds
Pre-Plated Set
Release: 2016 |
ASINEX has created a series of IRAK4-oriented compounds by combining the IRAK4 hinge
binding motif with proprietary natural product-like fragments. Several compounds
from this library were screened against IRAK4 kinase in vitro and showed sub-uM
IC50. Sunitinib was also included in the library as a reference
compound.
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SL#046
EGFR, PDGFR alpha & beta inhibitors |
80 compounds
Pre-Plated Set
Release: 2016 |
Screening of the ASINEX BioDesign Libraries has revealed a number of potent (IC50
< 1µM) inhibitors of EGFR and PDGFRɑ/β . This library is a useful starting point
for kinase-oriented research and drug discovery.
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SL#073
CNS Kinase - DLK (MAP3K12) |
80 compounds
Pre-Plated Set
Release: 2017 |
80 analogs of the reported hits have been included in this library. |
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SL#074
PKCε translocation inhibitors |
80 compounds
Pre-Plated Set
Release: 2017 |
ATP-competitive inhibitors of the PKC family show a lack of desired selectivity. In
order to identify a selective inhibitor of PKCε signaling, research pointed to a
molecule that can disrupt the PKCε/RACK2 interaction.
A series of
thienoquinolines was shown to prevent the PKCε/RACK2 interaction at low uM
concentrations. Initial hits originated from the Asinex collections; analogs of the
reported hits were included in this library.
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SL#082
p38 Inhibitors for
anti-Inflammatory Drug Discovery |
80 compounds
Pre-Plated Set
Release: 2018 |
A number of natural product and synthetic inhibitors of p38 kinase family has been
reported showing a promising anti-inflammatory activity in several models. However,
low specificity, low efficacy, and high toxicity of known candidates, creates an
unmet need for novel agents.
Using a proprietary library design platform ASINEX
has created molecules that in vitro target p38a in a range of therapeutically
relevant concentrations.
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