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Human Kinases Annotated Library

Human Kinases Annotated Library Human Kinases Annotated Library Human Kinases Annotated Library Human Kinases Annotated Library Human Kinases Annotated Library
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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.
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