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.
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 4.4M 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
Kinase Library is available for supply in various pre-plated formats, including the following most popular ones:
Catalog No.
KNS-64-0-Z-10
Compounds
64 960
51 plates
Amount
≤ 300 nL of 10 mM of DMSO solutions
Plates and formats
1536-well Echo LDV microplates, first and last four columns empty, 1280 compounds per plate
Price
Catalog No.
KNS-64-10-Y-10
Compounds
64 960
203 plates
Amount
≤ 10 µL of 10 mM DMSO solutions
Plates and formats
384-well, Echo Qualified LDV microplates #001-12782 (LP-0200), first and last two columns empty, 320 compounds per plate
Price
Catalog No.
KNS-64-50-Y-10
Compounds
64 960
203 plates
Amount
50 μL of 10 mM DMSO solutions
Plates and formats
384-well, Greiner Bio-One plates #781280, first and last two columns empty, 320 compounds per plate
Price
Catalog No.
Library & follow-up package
Plates and formats
KNS-64-10-Y-10 screening library 64 960 cmpds, hit resupply, analogs from 4.4M+ stock and synthesis from REAL Space
Price
*We will be happy to provide our library in any other most convenient for your project format. Please select among the following our standard microplates: Greiner Bio-One 781270, 784201, 781280, 651201 or Echo Qualified 001-12782 (LP-0200), 001-14555 (PP-0200), 001-6969 (LP-0400), C52621 or send your preferred labware. Compounds pooling can be provided upon request.
Download SD files
Library code: HBL-24
Version: 16 March 2021
24 000 compounds
sublibrary of KNS-64960
Library code: ALK-4
Version: 17 February 2022
4 800 compounds
sublibrary of KNS-64960
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
