receptor interacting serine/threonine kinase 2 | Receptor interacting protein kinase (RIPK) family | IUPHAR Guide to IMMUNOPHARMACOLOGY

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receptor interacting serine/threonine kinase 2

Target id: 2190

Nomenclature: receptor interacting serine/threonine kinase 2

Abbreviated Name: RIPK2

Family: Receptor interacting protein kinase (RIPK) family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

   GtoImmuPdb view: ON :     receptor interacting serine/threonine kinase 2 has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 540 8q21 RIPK2 receptor interacting serine/threonine kinase 2
Mouse - 539 4 A2 Ripk2 receptor (TNFRSF)-interacting serine-threonine kinase 2
Rat - 539 5 q13 Ripk2 receptor-interacting serine-threonine kinase 2
Previous and Unofficial Names
CARD3 | CARDIAK | CCK | RICK | RIP2
Database Links
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 2.7.11.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
GSK583 Rn Inhibition 8.7 pIC50 5
pIC50 8.7 (IC50 2x10-9 M) [5]
RIPK2 inhibitor 8 Hs Inhibition 8.5 pIC50 6
pIC50 8.5 (IC50 3x10-9 M) [6]
GSK583 Hs Inhibition 8.3 pIC50 5
pIC50 8.3 (IC50 5x10-9 M) [5]
Src kinase inhibitor I Hs Inhibition 7.6 pIC50 2
pIC50 7.6 (IC50 2.6x10-8 M) [2]
View species-specific inhibitor tables
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 3,10

Key to terms and symbols Click column headers to sort
Target used in screen: RIPK2
Ligand Sp. Type Action Affinity Units
vandetanib Hs Inhibitor Inhibition 8.3 pKd
PD-173955 Hs Inhibitor Inhibition 7.8 pKd
foretinib Hs Inhibitor Inhibition 7.7 pKd
SB203580 Hs Inhibitor Inhibition 7.6 pKd
dasatinib Hs Inhibitor Inhibition 7.5 pKd
PP-242 Hs Inhibitor Inhibition 7.1 pKd
cediranib Hs Inhibitor Inhibition 7.0 pKd
Ki-20227 Hs Inhibitor Inhibition 6.5 pKd
canertinib Hs Inhibitor Inhibition 6.5 pKd
PLX-4720 Hs Inhibitor Inhibition 6.4 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 1,4

Key to terms and symbols Click column headers to sort
Target used in screen: RIPK2/RIPK2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
K-252a Hs Inhibitor Inhibition 11.4 5.0 3.0
dorsomorphin Hs Inhibitor Inhibition 15.9 14.0 7.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 19.7 16.0 29.0
alsterpaullone 2-cyanoethyl Hs Inhibitor Inhibition 21.5 18.0 10.0
vandetanib Hs Inhibitor Inhibition 23.4
dasatinib Hs Inhibitor Inhibition 25.2
Lck inhibitor Hs Inhibitor Inhibition 28.6 21.0 15.0
TWS119 Hs Inhibitor Inhibition 30.5 18.0 11.0
PD 169316 Hs Inhibitor Inhibition 32.8 19.0 25.0
AG 1024 Hs Inhibitor Inhibition 32.8 26.0 16.0
Displaying the top 10 most potent ligands  View all ligands in screen »

References

Show »

1. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1039-45. [PMID:22037377]

2. Bain J, Plater L, Elliott M, Shpiro N, Hastie CJ, McLauchlan H, Klevernic I, Arthur JS, Alessi DR, Cohen P. (2007) The selectivity of protein kinase inhibitors: a further update. Biochem. J., 408 (3): 297-315. [PMID:17850214]

3. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol., 29 (11): 1046-51. [PMID:22037378]

4. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem. J., 451 (2): 313-28. [PMID:23398362]

5. Haile PA, Votta BJ, Marquis RW, Bury MJ, Mehlmann JF, Singhaus Jr R, Charnley AK, Lakdawala AS, Convery MA, Lipshutz DB et al.. (2016) The Identification and Pharmacological Characterization of 6-(tert-Butylsulfonyl)-N-(5-fluoro-1H-indazol-3-yl)quinolin-4-amine (GSK583), a Highly Potent and Selective Inhibitor of RIP2 Kinase. J. Med. Chem., 59 (10): 4867-80. [PMID:27109867]

6. He X, Da Ros S, Nelson J, Zhu X, Jiang T, Okram B, Jiang S, Michellys PY, Iskandar M, Espinola S et al.. (2017) Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases. ACS Med Chem Lett, 8 (10): 1048-1053. [PMID:29057049]

7. Jun JC, Cominelli F, Abbott DW. (2013) RIP2 activity in inflammatory disease and implications for novel therapeutics. J. Leukoc. Biol., 94 (5): 927-32. [PMID:23794710]

8. Oberst A. (2016) Death in the fast lane: what's next for necroptosis?. FEBS J., 283 (14): 2616-25. [PMID:26395133]

9. Silke J, Rickard JA, Gerlic M. (2015) The diverse role of RIP kinases in necroptosis and inflammation. Nat. Immunol., 16 (7): 689-97. [PMID:26086143]

10. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem. Biol., 17 (11): 1241-9. [PMID:21095574]

How to cite this page

Receptor interacting protein kinase (RIPK) family: receptor interacting serine/threonine kinase 2. Last modified on 26/10/2017. Accessed on 20/01/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=2190.