Kinase Library

Designed for discovery of novel protein kinase inhibitors

64 960 compounds

Protein kinase inhibitors (PKI) represent an important and still emerging class of targeted therapeutic agents. It is difficult to overestimate the role of protein kinase inhibitors in modern anticancer and immune-oncology therapy. Almost 70 kinase inhibitors have received KNS-64960-4-Z-10 approval, with majority being approved for the treatment of different cancers, and about 200 kinase-targeted drugs are in clinical phase trials.

Request

In order, to bring New Chemistry into this well-explored drug discovery field we carefully designed our Kinase targeted Library. The library is available in pre-plated format and can be promptly delivered in any custom formats. You can receive multiple benefits in the hit follow-up stages and lead optimization by using our Kinase Library:

  • Hit confirmation support and hit expansion from dry stock of over 3M compounds.
  • Straightforward and low-cost analogs synthesis through REAL Database technology.
  • Hit-to-lead project support provided in timely manner with broad capabilities available on-site.

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

Typical Formats

Catalog No.
Compounds
Amount
Format
Price

Catalog No.

KNS-64960-4-Z-10

Compounds

64 960
51 plates

Amount

4 µL of 10 mM DMSO solutions

Plates and formats

1536-well acoustic LDV plates, Labcyte #LP-0400,
first and last four columns empty,
1280 compounds per plate

Price

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Catalog No.

KNS-64960-10-Y-10

Compounds

64 960
203 plates

Amount

10 µL of 10 mM DMSO solutions

Plates and formats

384-well acoustic LDV plates, Labcyte #LP-0200,
first and last two columns empty,
320 compounds per plate

Price

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Catalog No.

KNS-64960-50-X-10

Compounds

64 960
203 plates

Amount

25 µL of 10 mM DMSO solutions

Plates and formats

384-well plates, Greiner #784201,
first and last two columns empty,
320 compounds per plate

Price

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Catalog No.

KNS-64960

Compounds

64 960

Amount

Custom

Plates and formats

Any custom format

Price

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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 design. We also introduced carefully selected compounds that were similar to known drugs.

Hinge Binders 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

Molecular properties

Kinase Libraries

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