EPH receptor B1 | Type XIII RTKs: Ephrin receptor family | IUPHAR/BPS Guide to PHARMACOLOGY

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EPH receptor B1

Target not currently curated in GtoImmuPdb

Target id: 1830

Nomenclature: EPH receptor B1

Abbreviated Name: EphB1

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 1 984 3q21-q23 EPHB1 EPH receptor B1
Mouse 1 984 9 Ephb1 Eph receptor B1
Rat 1 984 8q32 Ephb1 Eph receptor B1
Previous and Unofficial Names
EPHT2 | Eph receptor B2 (ELK-related protein tyrosine kinase) | Ephb2 | ephrin type-B receptor 1 | tyrosine-protein kinase receptor EPH-2
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
RefSeq Nucleotide
RefSeq Protein
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Solution structures of the fn3 domain of human ephrin type-B receptor 1
Resolution:  0.0Å
Species:  Human
Enzyme Reaction
EC Number:

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

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 66 [PMID: 19788238] Hs Inhibition 9.0 pIC50 5
pIC50 9.0 (IC50 1.1x10-9 M) [5]
compound 20 [PMID: 23489211] Rn Inhibition 5.4 pIC50 4
pIC50 5.4 (IC50 3.8x10-6 M) [4]
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.
Reference: 2,6

Key to terms and symbols Click column headers to sort
Target used in screen: EPHB1
Ligand Sp. Type Action Value Parameter
dasatinib Hs Inhibitor Inhibition 9.4 pKd
PD-173955 Hs Inhibitor Inhibition 8.4 pKd
foretinib Hs Inhibitor Inhibition 7.9 pKd
bosutinib Hs Inhibitor Inhibition 7.5 pKd
crizotinib Hs Inhibitor Inhibition 6.9 pKd
AST-487 Hs Inhibitor Inhibition 6.7 pKd
staurosporine Hs Inhibitor Inhibition 6.6 pKd
vandetanib Hs Inhibitor Inhibition 6.5 pKd
MLN-8054 Hs Inhibitor Inhibition 6.5 pKd
NVP-TAE684 Hs Inhibitor Inhibition 6.5 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.


Reference: 1,3

Key to terms and symbols Click column headers to sort
Target used in screen: EphB1/EPHB1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition 4.8
nilotinib Hs Inhibitor Inhibition 10.6
bosutinib Hs Inhibitor Inhibition 11.8
staurosporine Hs Inhibitor Inhibition 12.0 18.5 -0.5
dorsomorphin Hs Inhibitor Inhibition 17.0 37.0 0.0
Cdk1/2 inhibitor III Hs Inhibitor Inhibition 19.4 1.0 -1.0
vandetanib Hs Inhibitor Inhibition 27.8
IKK-2 inhibitor IV Hs Inhibitor Inhibition 28.9 11.0 0.0
TWS119 Hs Inhibitor Inhibition 40.0 7.0 -1.0
PP1 analog II Hs Inhibitor Inhibition 47.7 13.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »


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. 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]

3. 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]

4. 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]

5. 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]

6. 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 B1. Last modified on 11/02/2015. Accessed on 20/02/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1830.