EPH receptor B6 | Type XIII RTKs: Ephrin receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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EPH receptor B6

Target not currently curated in GtoImmuPdb

Target id: 1834

Nomenclature: EPH receptor B6

Abbreviated Name: EphB6

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

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1021 7q33-q35 EPHB6 EPH receptor B6
Mouse 1 1014 6 Ephb6 Eph receptor B6
Rat 1 1013 4q22 Ephb6 Eph receptor B6
Previous and Unofficial Names
ephrin type-B receptor 6 | tyrosine-protein kinase-defective receptor EPH-6 | MEP | Cekl
Database Links
BRENDA 2.7.10.1
CATH/Gene3D 2.60.120.260, 2.60.40.10
ChEMBL Target CHEMBL5836 (Hs)
Ensembl Gene ENSG00000106123 (Hs), ENSMUSG00000029869 (Mm), ENSRNOG00000014367 (Rn)
Entrez Gene 2051 (Hs), 13848 (Mm), 312275 (Rn)
Human Protein Atlas ENSG00000106123 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:2051 (Hs), mmu:13848 (Mm), rno:312275 (Rn)
OMIM 602757 (Hs)
RefSeq Nucleotide NM_004445 (Hs), NM_001146351 (Mm), NM_001107857 (Rn)
RefSeq Protein NP_004436 (Hs), NP_031706 (Mm), NP_001139823 (Mm), NP_001101327 (Rn)
UniProtKB O15197 (Hs), O08644 (Mm), P0C0K7 (Rn)
Wikipedia EPHB6 (Hs)
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 Value Parameter Reference
compound 20 [PMID: 23489211] Mm Inhibition 5.2 pIC50 2
⤷ pIC50 5.2 (IC50 5.8x10-6 M) [2]
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: 1,3
Key to terms and symbols Click column headers to sort
Target used in screen: EPHB6
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 10.4 pKd
foretinib Hs Inhibitor Inhibition 8.9 pKd
PD-173955 Hs Inhibitor Inhibition 8.7 pKd
Ki-20227 Hs Inhibitor Inhibition 8.3 pKd
crizotinib Hs Inhibitor Inhibition 8.2 pKd
tozasertib Hs Inhibitor Inhibition 7.6 pKd
linifanib Hs Inhibitor Inhibition 7.5 pKd
CHIR-265 Hs Inhibitor Inhibition 7.4 pKd
barasertib-hQPA Hs Inhibitor Inhibition 7.3 pKd
vandetanib Hs Inhibitor Inhibition 7.1 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. 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]

3. 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 B6. Last modified on 09/02/2015. Accessed on 21/11/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1834.