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Human Phosphatases Annotated Library

Human Phosphatases Annotated Library Human Phosphatases Annotated Library Human Phosphatases Annotated Library Human Phosphatases Annotated Library
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Description


•Phosphatases are enzymatic proteins that dephosphorylate other functional proteins

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

•Phosphatases are interesting therapeutic targets for

-Oncology, e.g. cancer immunotherapy
-Metabolic diseases, e.g. diabetes, obesity
-Infections, e.g. antibacterial, antiviral


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

  • Annotated activities : 25 phosphatase targets
  • Express Delivery : 160 compounds
  • Complete Version : 225 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

H025-3231

O14976

Serine/threonine-protein kinase GAK

Kd

=

2700

nM

22037378

10.1038/nbt.1990

Cyclin-G-associated kinase

Binding constant for GAK kinase domain

Y203-7358

P34913

Epoxide hydratase

IC50

=

700

nM

19746975

10.1021/jm9005302

Bifunctional epoxide hydrolase 2

Displacement of rhodamine-labeled probe from human soluble epoxide hydrolase by fluorescence polarization assay

7547-4118

P05186

Alkaline phosphatase tissue-nonspecific isozyme

IC50

=

1130

nM

19821572

10.1021/jm900383s

Alkaline phosphatase tissue-nonspecific isozyme

Inhibition of TNAP transfected in african green monkey COS1 cells by colorimetric assay

4032-1302

Q13822

Autotaxin

IC50

=

56

nM

20536182

10.1021/jm1005012

Ectonucleotide pyrophosphatase/phosphodiesterase family member 2

Inhibition of 6x-histidine-tagged human recombinant ATX expressed in HEK293 cells using bisP-nitrophenyl phosphate as a substrate

8005-8111

P08575

Leukocyte common antigen

IC50

=

700

nM

11356112

10.1021/jm000447i

Receptor-type tyrosine-protein phosphatase C

In vitro inhibitory activity against the cytosolic portion of CD45 protein-tyrosine phosphatase using pNPP as the substrate

R092-0051

Q13332

Receptor-type tyrosine-protein phosphatase S

IC50

=

4300

nM

26602279

10.1016/j.bmcl.2015.11.026

Receptor-type tyrosine-protein phosphatase S

Inhibition of recombinant human PTP-sigma (residues 1367 to 1948) using para-nitrophenylphosphate as substrate for 60 mins by fluorescence analysis

4489-1466

O75365

Protein-tyrosine phosphatase 4A3

IC50

=

1100

nM

23726031

10.1016/j.bmcl.2013.04.092

Protein tyrosine phosphatase type IVA 3

Inhibition of human His6-tagged full length PRL3 assessed as inhibition of DiFMUP dephosphorylation

0111-0158

P34913

Epoxide hydratase

IC50

=

1.6

nM

22079754

10.1016/j.bmcl.2011.10.074

Bifunctional epoxide hydrolase 2

Inhibition of human soluble epoxide hydrolase using CMNPC as substrate after 5 mins by fluorescent assay

2817-4329

P18031

Protein-tyrosine phosphatase 1B

Ki

=

3000

nM

21420867

10.1016/j.bmc.2011.02.047

Tyrosine-protein phosphatase non-receptor type 1

Inhibition of PTP1B

Publications

1.J. Med. Chem. 2009 52(21):6716-6723. Multidentate small-molecule inhibitors of vaccinia H1-related (VHR) phosphatase decrease proliferation of cervix cancer cells. Wu S Vossius S Rahmouni S Miletic AV Vang T Vazquez-Rodriguez J Cerignoli F Arimura Y Williams S Hayes T Moutschen M Vasile S Pellecchia M Mustelin T Tautz L.

2.J. Med. Chem. 2001 44(24):4042-4049. Discovery and biological evaluation of a new family of potent inhibitors of the dual specificity protein phosphatase Cdc25. Lazo JS Aslan DC Southwick EC Cooley KA Ducruet AP Joo B Vogt A Wipf P.

3.J. Med. Chem. 2017 60(18):7703-7724. A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase To Counter Nonalcoholic Steatohepatitis. Schmidt J Rotter M Weiser T Wittmann S Weizel L Kaiser A Heering J Goebel T Angioni C Wurglics M Paulke A Geisslinger G Kahnt A Steinhilber D Proschak E Merk D.

4.Bioorg. Med. Chem. Lett. 2009 19(1):222-225. Design and synthesis of pyrazole derivatives as potent and selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). Sidique S Ardecky R Su Y Narisawa S Brown B Millán JL Sergienko E Cosford ND.

5.J. Med. Chem. 2009 52(21):6919-6925. Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP). Dahl R Sergienko EA Su Y Mostofi YS Yang L Simao AM Narisawa S Brown B Mangravita-Novo A Vicchiarelli M Smith LH O'Neill WC Millán JL Cosford ND.

6.Bioorg. Med. Chem. Lett. 2006 16(19):5212-5216. Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase. Jones PD Tsai HJ Do ZN Morisseau C Hammock BD.

7.Bioorg. Med. Chem. Lett. 2009 19(8):2240-2243. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 138-triazaspiro[45]decan-4-one privileged structure that engenders PLD2 selectivity. Lavieri R Scott SA Lewis JA Selvy PE Armstrong MD Alex Brown H Lindsley CW.
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