receptor (TNFRSF)-interacting serine-threonine kinase 1

Target id: 2189

Nomenclature: receptor (TNFRSF)-interacting serine-threonine kinase 1

Abbreviated Name: RIPK1

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

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 671 6p25.2 RIPK1 receptor (TNFRSF)-interacting serine-threonine kinase 1
Mouse - 656 13 A3.3 Ripk1 receptor (TNFRSF)-interacting serine-threonine kinase 1
Rat - 658 17 p12 Ripk1 receptor (TNFRSF)-interacting serine-threonine kinase 1
Previous and Unofficial Names
RIP
Rip1
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG BRITE Hierarchy
KEGG Gene
OMIM
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of RIP1 kinase in complex with necrostatin-4
PDB Id:  4ITJ
Resolution:  1.8Å
Species:  Human
References:  3
Enzyme Reaction
EC Number: 2.7.11.1
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: 1-2

Key to terms and symbols Click column headers to sort
Target used in screen: RIPK1
Ligand Sp. Type Action Affinity Units
tozasertib Hs Inhibitor Inhibition 7.7 pKd
KW-2449 Hs Inhibitor Inhibition 7.19 pKd
AST-487 Hs Inhibitor Inhibition 6.68 pKd
JNJ-28312141 Hs Inhibitor Inhibition 6.62 pKd
pazopanib Hs Inhibitor Inhibition 6.59 pKd
dovitinib Hs Inhibitor Inhibition 6.49 pKd
sunitinib Hs Inhibitor Inhibition 6.43 pKd
foretinib Hs Inhibitor Inhibition 6.07 pKd
quizartinib Hs Inhibitor Inhibition 6.05 pKd
SU-14813 Hs Inhibitor Inhibition 5.92 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »

References

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1. 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]

2. 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]

3. Xie T, Peng W, Liu Y, Yan C, Maki J, Degterev A, Yuan J, Shi Y. (2013) Structural Basis of RIP1 Inhibition by Necrostatins. Structure21 (3): 493-9. [PMID:23473668]

How to cite this page

Receptor interacting protein kinase (RIPK) family: receptor (TNFRSF)-interacting serine-threonine kinase 1. Last modified on 18/08/2014. Accessed on 28/11/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2189.