Burger line Burger line Burger line
Logo Logo Logo
Burger line Burger line Burger line
Menu
Sign in
Sign in

Human Kinases Annotated Library

Format:
$11,160
Add to cart
Delivery:
Shipping to: · Change Shiptime: 1 week
Preferred format:
Desirable size of the custom library selection:
Amount:
Mg
  • Mg
  • uMol
Volume:

Description


Kinases are enzymatic proteins that phosphorylate other functional proteins

•Physiologically the kinase enzymatic activity can be modulated by
- Catalytic ATP site binders
- Allosteric binders that cause conformational changes within the catalytic ATP site

•Kinases are well recognized as important therapeutic targets for
- Oncology, e.g. cancer immunotherapy
- Inflammatory diseases, e.g. fibrosis, rheumatoid arthritis
- Cardiovascular system, e.g. cerebral vasospasm, pulmonary arterial hypertension

A unique collection of small molecule compounds with annotated activities for Kinases protein targets

  • Annotated activities : 249 kinase targets
  • Express Delivery : 640 compounds
  • Complete Version : 2585 compounds


Library Composition

Data sources of annotations : Pharos, ChEMBL 25, PubChem, PubMed, Current Patent Literature (CAS, Integrity)

IDNUMBER – ChemDiv Catalog ID (in some instances the same IDNUMBER might have multiple annotation entries due to multiple data sources or because having activity against multiple similar targets);

UNIPROT – SwissProt and ChEMBL Target accesion ID; 

Type – character of the measured activity;

Value – Active compounds selection criteria, included only compounds with reported activities < 5 µM;

pubmed_id – PubMed record entry; 

doi, patent_id – journal or patent reference to a publication of original data;  

For screening data extracted from PubChem, see column assay_description for entry names PUBCHEM_BIOASSAY

Example of Annotations - an Excel file structure


IDNUMBER

UNIPROT

Target Name

Type

Relation

Value

Units

pubmed_id

doi

patent_id

Target Description

assay_description

8008-7025

Q7L7X3

Serine/threonine-protein kinase TAO1

IC50

<

50

nM

US-20070208166-A1

Serine/threonine-protein kinase TAO1

Inhibition of human KIAA1361 kinase domain

5122-1774

P43250

G protein-coupled receptor kinase 6

IC50

=

1030

nM

US-20140309185-A1

G protein-coupled receptor kinase 6

Inhibition of human recombinant full-length GST-tagged human GRK6

0073-0059

O75460

Serine/threonine-protein kinase/endoribonuclease IRE1

IC50

=

170

nM

US-8614253-B2

Serine/threonine-protein kinase/endoribonuclease IRE1

In Vitro Enzyme Assays: IRE-1 alpha T1 RNase and RNase A assays

S553-1690

Q00535

Cyclin-dependent kinase 5

Ki

=

50.12

nM

Cyclin-dependent-like kinase 5

PUBCHEM_BIOASSAY: Navigating the Kinome.

Y031-8414

P50613

Cyclin-dependent kinase 7/ cyclin H

IC50

=

400

nM

20627564

10.1016/j.bmcl.2010.05.039

Cyclin-dependent kinase 7

Inhibition of human CDK7/Cyclin H/MAT1

L785-0049

P49336

CDK8/Cyclin C

IC50

=

9

nM

28231524

10.1016/j.ejmech.2017.02.020

Cyclin-dependent kinase 8

Inhibition of Alexa647 tracer binding to full length recombinant human His-tagged CDK8/Cyclin C

H025-3231

Q2M2I8

Adaptor-associated kinase

Kd

=

1200

nM

22037378

10.1038/nbt.1990

AP2-associated protein kinase 1

Binding constant for AAK1 kinase domain

8012-7305

Q5S007

Leucine-rich repeat serine/threonine-protein kinase 2

IC50

=

100

nM

28774425

10.1016/j.bmcl.2017.07.052

Leucine-rich repeat serine/threonine-protein kinase 2

Inhibition of LRRK2 (unknown origin) by HTRF assay

Publications


1.J Med Chem 2017 60(14):6337-6352. Discovery of Potent and Selective Inhibitors of Cdc2-Like Kinase 1 (CLK1) as a New Class of Autophagy Inducers. Sun QZ Lin GF Li LL Jin XT Huang LY Zhang G Yang W Chen K Xiang R Chen C Wei YQ Lu GW Yang SY.

2.Bioorg Med Chem Lett 2017 27(11):2617-2621. Developing DYRK inhibitors derived from the meridianins as a means of increasing levels of NFAT in the nucleus. Shaw SJ Goff DA Lin N Singh R Li W McLaughlin J Baltgalvis KA Payan DG Kinsella TM.

3.J Med Chem 2017 60(16):7099-7107. Optimization of Allosteric With-No-Lysine (WNK) Kinase Inhibitors and Efficacy in Rodent Hypertension Models. Yamada K Levell J Yoon T Kohls D Yowe D Rigel DF Imase H Yuan J Yasoshima K DiPetrillo K Monovich L Xu L Zhu M Kato M Jain M Idamakanti N Taslimi P Kawanami T Argikar UA Kunjathoor V Xie X Yagi YI Iwaki Y Robinson Z Park HM.

4.J. Med. Chem. 2015 58(3):1563-1568. A high-throughput screen reveals new small-molecule activators and inhibitors of pantothenate kinases. Sharma LK Leonardi R Lin W Boyd VA Goktug A Shelat AA Chen T Jackowski S Rock CO.

5.ACS Med. Chem. Lett. 2014 5(9):963-967. Hydroxybenzothiophene Ketones Are Efficient Pre-mRNA Splicing Modulators Due to Dual Inhibition of Dyrk1A and Clk1/4. Schmitt C Miralinaghi P Mariano M Hartmann RW Engel M.

6.J. Med. Chem. 2014 57(6):2755-2772. Protein kinase CK-1 inhibitors as new potential drugs for amyotrophic lateral sclerosis. Salado IG Redondo M Bello ML Perez C Liachko NF Kraemer BC Miguel L Lecourtois M Gil C Martinez A Perez DI.

7.Nat. Biotechnol. 2011 29(11):1046-1051. Comprehensive analysis of kinase inhibitor selectivity. Davis MI Hunt JP Herrgard S Ciceri P Wodicka LM Pallares G Hocker M Treiber DK Zarrinkar PP.

8.Bioorg. Med. Chem. Lett. 2011 21(13):4108-4114. Identification of new inhibitors of protein kinase R guided by statistical modeling. Bryk R Wu K Raimundo BC Boardman PE Chao P Conn GL Anderson E Cole JL Duffy NP Nathan C Griffin JH.

9.ACS Med. Chem. Lett. 2011 2(2):154-159. Synthesis and Structure-Activity Relationships of Benzothienothiazepinone Inhibitors of Protein Kinase D. Bravo-Altamirano K George KM Frantz MC Lavalle CR Tandon M Leimgruber S Sharlow ER Lazo JS Wang QJ Wipf P.
0 items in Cart
Cart Subtotal:
Go to cart
You will be able to Pay Online or Request a Quote
Catalog
Services
Company

We use "cookies*  to ensure the functionality of our website, recognise your browser or device, learn more about your interests, and provide you with essential features and services and for additional purposes, including:

Recognising you when you sign-in to use our services. This allows us to provide you with product recommendations, display personalised content, and provide other customised features and services.
Keeping track of your specified preferences. You may set your preferences through Your Account..
Keeping track of items stored in your shopping basket and personal cabinet.
Conducting research and diagnostics to improve ChemDiv’s content, products, and services.
Delivering content, including ads, relevant to your interests on ChemDiv’s site
Reporting. This allows us to measure and analyse the performance of our services.

By  cookies you give consent to the processing of your personal data, including transfer to third parties. Further information can be found in our privacy policy.

Accept all cookies