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EPH receptor B6

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Target id: 1834

Nomenclature: EPH receptor B6

Abbreviated Name: EphB6

Family: Type XIII RTKs: Ephrin receptor family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1021 7q34 EPHB6 EPH receptor B6
Mouse 1 1014 6 B2.1 Ephb6 Eph receptor B6
Rat 1 1013 4q23 Ephb6 Eph receptor B6
Previous and Unofficial Names Click here for help
ephrin type-B receptor 6 | tyrosine-protein kinase-defective receptor EPH-6 | MEP | Cekl
Database Links Click here for help
Alphafold O15197 (Hs), O08644 (Mm), P0C0K7 (Rn)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.120.260, 2.60.40.10
ChEMBL Target CHEMBL5836 (Hs), CHEMBL4739668 (Mm)
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)
Pharos O15197 (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 Click here for help
EC Number: 2.7.10.1

Download all structure-activity data for this target as a CSV file go icon to follow link

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] Small molecule or natural product Click here for species-specific activity table Mm Inhibition 5.2 pIC50 2
⤷ pIC50 5.2 (IC50 5.8x10-6 M) [2]
DiscoveRx KINOMEscan® screen Click here for help
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 Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.4 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
Ki-20227 Small molecule or natural product Hs Inhibitor Inhibition 8.3 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.2 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 7.5 pKd
CHIR-265 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
barasertib-hQPA Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure 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]

Contributors

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