EPH receptor B2 | Type XIII RTKs: Ephrin receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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EPH receptor B2

Target not currently curated in GtoImmuPdb

Target id: 1831

Nomenclature: EPH receptor B2

Abbreviated Name: EphB2

Family: Type XIII RTKs: Ephrin receptor 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 1 987 1p36.1-p35 EPHB2 EPH receptor B2
Mouse 1 986 4 D-E Ephb2 Eph receptor B2
Rat - 986 5q36 Ephb2 Eph receptor B2
Previous and Unofficial Names
EPHT3 | DRT | Tyro5 | ephrin type-B receptor 2 | Neural kinase | Nuk receptor tyrosine kinase | tyrosine-protein kinase receptor EPH-3 | eteck | Nuk | Prkm5 | Sek3 | tyrosine-protein kinase receptor SEK-3
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  EphB2/SNEW Antagonistic Peptide Complex
PDB Id:  2QBX
Resolution:  2.3Å
Species:  Human
References:  2
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of Eph A4 receptor
PDB Id:  3CKH
Resolution:  2.8Å
Species:  Human
References:  7
Enzyme Reaction
EC Number: 2.7.10.1

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 Parameter Reference
DDR1/2 inhibitor 5n Hs Inhibition 6.6 pKd 8
pKd 6.6 (Kd 2.6x10-7 M) [8]
compound 66 [PMID: 19788238] Hs Inhibition 8.9 pIC50 6
pIC50 8.9 (IC50 1.2x10-9 M) [6]
compound 20 [PMID: 23489211] Mm Inhibition 5.4 pIC50 5
pIC50 5.4 (IC50 3.8x10-6 M) [5]
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: 3,9

Key to terms and symbols Click column headers to sort
Target used in screen: EPHB2
Ligand Sp. Type Action Affinity Parameter
dasatinib Hs Inhibitor Inhibition 9.4 pKd
foretinib Hs Inhibitor Inhibition 8.4 pKd
bosutinib Hs Inhibitor Inhibition 8.1 pKd
PD-173955 Hs Inhibitor Inhibition 7.7 pKd
AST-487 Hs Inhibitor Inhibition 6.9 pKd
vandetanib Hs Inhibitor Inhibition 6.4 pKd
doramapimod Hs Inhibitor Inhibition 6.4 pKd
PP-242 Hs Inhibitor Inhibition 6.3 pKd
nilotinib Hs Inhibitor Inhibition 6.2 pKd
tamatinib Hs Inhibitor Inhibition 6.1 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: EphB2/EPHB2
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition -0.2
nilotinib Hs Inhibitor Inhibition 1.5
bosutinib Hs Inhibitor Inhibition 17.4
vandetanib Hs Inhibitor Inhibition 24.4
staurosporine Hs Inhibitor Inhibition 27.6 21.5 0.0
dorsomorphin Hs Inhibitor Inhibition 33.6 25.0 0.0
TWS119 Hs Inhibitor Inhibition 40.7 4.0 -1.0
PP1 analog II Hs Inhibitor Inhibition 44.6 3.0 -1.0
JAK3 inhibitor II Hs Inhibitor Inhibition 66.1 65.0 1.0
sunitinib Hs Inhibitor Inhibition 72.1
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Prostate cancer/brain cancer susceptibility
OMIM: 603688
Orphanet: ORPHA1331

References

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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. Chrencik JE, Brooun A, Recht MI, Nicola G, Davis LK, Abagyan R, Widmer H, Pasquale EB, Kuhn P. (2007) Three-dimensional structure of the EphB2 receptor in complex with an antagonistic peptide reveals a novel mode of inhibition. J. Biol. Chem., 282 (50): 36505-13. [PMID:17897949]

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. Incerti M, Tognolini M, Russo S, Pala D, Giorgio C, Hassan-Mohamed I, Noberini R, Pasquale EB, Vicini P, Piersanti S et al.. (2013) Amino acid conjugates of lithocholic acid as antagonists of the EphA2 receptor. J. Med. Chem., 56 (7): 2936-47. [PMID:23489211]

6. Lafleur K, Huang D, Zhou T, Caflisch A, Nevado C. (2009) Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4). J. Med. Chem., 52 (20): 6433-46. [PMID:19788238]

7. Qin H, Shi J, Noberini R, Pasquale EB, Song J. (2008) Crystal structure and NMR binding reveal that two small molecule antagonists target the high affinity ephrin-binding channel of the EphA4 receptor. J. Biol. Chem., 283 (43): 29473-84. [PMID:18708347]

8. Wang Z, Zhang Y, Pinkas DM, Fox AE, Luo J, Huang H, Cui S, Xiang Q, Xu T, Xun Q et al.. (2018) Design, Synthesis, and Biological Evaluation of 3-(Imidazo[1,2- a]pyrazin-3-ylethynyl)-4-isopropyl- N-(3-((4-methylpiperazin-1-yl)methyl)-5-(trifluoromethyl)phenyl)benzamide as a Dual Inhibitor of Discoidin Domain Receptors 1 and 2. J. Med. Chem., 61 (17): 7977-7990. [PMID:30075624]

9. 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

Type XIII RTKs: Ephrin receptor family: EPH receptor B2. Last modified on 16/10/2018. Accessed on 24/04/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1831.