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Kinase Library

Designed for discovery of novel protein kinase inhibitors

67 385 compounds

Protein kinase inhibitors (PKI) represent an important and still emerging class of targeted therapeutic agents. Kinases have proven their key role in modern anticancer and anti-inflammatory therapies. Kinases are probably the most convenient targets for drug development. More than 40 diverse kinase inhibitors are currently approved for treatment of different cancers, with another 150 kinase-targeted drugs undergoing clinical trials.

In spite of extensive studies and impressive achievements in kinase inhibitor development there is a strong interest in development of novel and more selective inhibitors, including but not limited to allosteric, covalent and bivalent ligands.

Based on numerous investigations and detailed structure analysis of known and most potent kinase inhibitors, we developed a complex MedChem-based approach to design our Kinase Library. All compounds are stored as dry materials and they can be acquired in diverse custom formats. Alternatively, we can promptly supply a copy of the pre-plated Kinase Library having 64 000 compounds, that can be also made in a customized ready-to-screen formats.

Using our kinase library for hit discovery you receive multiple benefits allowing you to save the time and cost in lead generation:

  • Hit resupply and hit expansion from dry stock of over 2.6 M compounds.
  • Straightforward and low-cost analogs synthesis through REAL Database technology.
  • Fully customized hit-to-lead project support provided in a timely manner with broad MedChem and ADMET/PK capabilities available on-site.

You have also an option to screen the library directly at Enamine. We will be happy to offer you discount on library cost depending on the collaboration scope.

Most popular library formats available for immediate supply

Item
Catalog #
# of compounds
# of plates
Amount
Plates and format

Item

1

Catalog #

KNS-64-Y-0

# of compounds

64 000

# of plates

200

Amount

Any applicable for 1 assay

Plates and format

384-well plates, 320 cpds per plate,
first two and last two columns empty

Item

2

Catalog #

KNS-64-Y-10

# of compounds

64 000

# of plates

200

Amount

10 µL of 10 mM
DMSO stock solutions

Plates and format

384-well plates, 320 cpds per plate,
first two and last two columns empty

Item

3

Catalog #

KNS-64-Y-50

# of compounds

64 000

# of plates

200

Amount

50 µL of 10 mM
DMSO solutions

Plates and format

384-well plates, 320 cpds per plate,
first two and last two columns empty

Library Design

In spite of extensive studies and impressive achievements in kinase inhibitor development there is a strong interest in development of novel and selective kinase inhibitors (including allosteric, covalent, bivalent) and subsequently qualitative kinases targeted libraries.

Our previous investigation and detailed structure analysis of known and most potent kinases’ inhibitors yielded the complex approach to design of unique kinase focused libraries. We used several approaches with proven record in development of known successful kinase inhibitors. Validated in silico screening along with selection of compounds bearing privileged scaffolds/moieties and bioisosteric core replacements were the key components of the dedicated deign. We also introduced carefully selected compounds that were similar to known drugs.

Hinge region directed sublibrary - 24 000 compounds

Well validated Cores with New Chemistry decoration

Pharmacophore & Shape similarity searches to the set of potent allosteric inhibitors

PD98059 (Allosteric inhibitor of MAPKK)

RS2 (allsoteric PDK1 inhibitor)

MK2206 (allosteric Akt-inhibitor)

Docking into allosteric kinases binding sites

Docking calculations into ATP-binding pocket

Kinase Libraries

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