General Information of Target

Target ID LDTP04632
Target Name Ephrin type-B receptor 1 (EPHB1)
Gene Name EPHB1
Gene ID 2047
Synonyms
ELK; EPHT2; HEK6; NET; Ephrin type-B receptor 1; EC 2.7.10.1; ELK; EPH tyrosine kinase 2; EPH-like kinase 6; EK6; hEK6; Neuronally-expressed EPH-related tyrosine kinase; NET; Tyrosine-protein kinase receptor EPH-2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MALDYLLLLLLASAVAAMEETLMDTRTATAELGWTANPASGWEEVSGYDENLNTIRTYQV
CNVFEPNQNNWLLTTFINRRGAHRIYTEMRFTVRDCSSLPNVPGSCKETFNLYYYETDSV
IATKKSAFWSEAPYLKVDTIAADESFSQVDFGGRLMKVNTEVRSFGPLTRNGFYLAFQDY
GACMSLLSVRVFFKKCPSIVQNFAVFPETMTGAESTSLVIARGTCIPNAEEVDVPIKLYC
NGDGEWMVPIGRCTCKPGYEPENSVACKACPAGTFKASQEAEGCSHCPSNSRSPAEASPI
CTCRTGYYRADFDPPEVACTSVPSGPRNVISIVNETSIILEWHPPRETGGRDDVTYNIIC
KKCRADRRSCSRCDDNVEFVPRQLGLTECRVSISSLWAHTPYTFDIQAINGVSSKSPFPP
QHVSVNITTNQAAPSTVPIMHQVSATMRSITLSWPQPEQPNGIILDYEIRYYEKEHNEFN
SSMARSQTNTARIDGLRPGMVYVVQVRARTVAGYGKFSGKMCFQTLTDDDYKSELREQLP
LIAGSAAAGVVFVVSLVAISIVCSRKRAYSKEAVYSDKLQHYSTGRGSPGMKIYIDPFTY
EDPNEAVREFAKEIDVSFVKIEEVIGAGEFGEVYKGRLKLPGKREIYVAIKTLKAGYSEK
QRRDFLSEASIMGQFDHPNIIRLEGVVTKSRPVMIITEFMENGALDSFLRQNDGQFTVIQ
LVGMLRGIAAGMKYLAEMNYVHRDLAARNILVNSNLVCKVSDFGLSRYLQDDTSDPTYTS
SLGGKIPVRWTAPEAIAYRKFTSASDVWSYGIVMWEVMSFGERPYWDMSNQDVINAIEQD
YRLPPPMDCPAALHQLMLDCWQKDRNSRPRFAEIVNTLDKMIRNPASLKTVATITAVPSQ
PLLDRSIPDFTAFTTVDDWLSAIKMVQYRDSFLTAGFTSLQLVTQMTSEDLLRIGITLAG
HQKKILNSIHSMRVQISQSPTAMA
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, Ephrin receptor subfamily
Subcellular location
Cell membrane
Function
Receptor tyrosine kinase which binds promiscuously transmembrane ephrin-B family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Cognate/functional ephrin ligands for this receptor include EFNB1, EFNB2 and EFNB3. During nervous system development, regulates retinal axon guidance redirecting ipsilaterally ventrotemporal retinal ganglion cells axons at the optic chiasm midline. This probably requires repulsive interaction with EFNB2. In the adult nervous system together with EFNB3, regulates chemotaxis, proliferation and polarity of the hippocampus neural progenitors. In addition to its role in axon guidance also plays an important redundant role with other ephrin-B receptors in development and maturation of dendritic spines and synapse formation. May also regulate angiogenesis. More generally, may play a role in targeted cell migration and adhesion. Upon activation by EFNB1 and probably other ephrin-B ligands activates the MAPK/ERK and the JNK signaling cascades to regulate cell migration and adhesion respectively. Involved in the maintenance of the pool of satellite cells (muscle stem cells) by promoting their self-renewal and reducing their activation and differentiation.
TTD ID
T02446
Uniprot ID
P54762
DrugMap ID
TT8MDAC
Ensemble ID
ENST00000398015.8
HGNC ID
HGNC:3392
ChEMBL ID
CHEMBL5072

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
DU145 SNV: p.A445S .
HT115 SNV: p.E161Ter .
Ishikawa (Heraklio) 02 ER SNV: p.I439S .
NCIH1666 SNV: p.R390L .
NCIH1793 SNV: p.P103A; p.E794Ter .
NCIH2286 SNV: p.P850Q .
OAW42 SNV: p.R567W .
PF382 SNV: p.W919R .
RKO SNV: p.D375G .
SNU1 Insertion: p.Q421TfsTer48 .
SNU1079 SNV: p.T957N .
SUIT2 SNV: p.I695F .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C849(0.75); C860(0.75)  LDD1094  [1]
Acrolein
 Probe Info 
N.A.  LDD0217  [2]
Methacrolein
 Probe Info 
N.A.  LDD0218  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 PaTu 8988t C849(0.75); C860(0.75)  LDD1094  [1]
 LDCM0226  AC11 PaTu 8988t C849(0.93); C860(0.93)  LDD1105  [1]
 LDCM0237  AC12 PaTu 8988t C849(0.97); C860(0.97)  LDD1116  [1]
 LDCM0259  AC14 PaTu 8988t C849(0.80); C860(0.80)  LDD1138  [1]
 LDCM0263  AC143 PaTu 8988t C849(0.84); C860(0.84)  LDD1142  [1]
 LDCM0264  AC144 PaTu 8988t C849(0.90); C860(0.90)  LDD1143  [1]
 LDCM0265  AC145 PaTu 8988t C849(0.74); C860(0.74)  LDD1144  [1]
 LDCM0266  AC146 PaTu 8988t C849(0.93); C860(0.93)  LDD1145  [1]
 LDCM0267  AC147 PaTu 8988t C849(0.92); C860(0.92)  LDD1146  [1]
 LDCM0268  AC148 PaTu 8988t C849(0.77); C860(0.77)  LDD1147  [1]
 LDCM0269  AC149 PaTu 8988t C849(0.92); C860(0.92)  LDD1148  [1]
 LDCM0270  AC15 PaTu 8988t C849(1.00); C860(1.00)  LDD1149  [1]
 LDCM0271  AC150 PaTu 8988t C849(0.83); C860(0.83)  LDD1150  [1]
 LDCM0272  AC151 PaTu 8988t C849(0.87); C860(0.87)  LDD1151  [1]
 LDCM0273  AC152 PaTu 8988t C849(0.81); C860(0.81)  LDD1152  [1]
 LDCM0274  AC153 PaTu 8988t C849(0.81); C860(0.81)  LDD1153  [1]
 LDCM0621  AC154 PaTu 8988t C849(0.96); C860(0.96)  LDD2166  [1]
 LDCM0622  AC155 PaTu 8988t C849(0.90); C860(0.90)  LDD2167  [1]
 LDCM0623  AC156 PaTu 8988t C849(0.83); C860(0.83)  LDD2168  [1]
 LDCM0624  AC157 PaTu 8988t C849(1.31); C860(1.31)  LDD2169  [1]
 LDCM0276  AC17 PaTu 8988t C849(0.94); C860(0.94)  LDD1155  [1]
 LDCM0277  AC18 PaTu 8988t C849(0.82); C860(0.82)  LDD1156  [1]
 LDCM0278  AC19 PaTu 8988t C849(1.01); C860(1.01)  LDD1157  [1]
 LDCM0280  AC20 PaTu 8988t C849(0.97); C860(0.97)  LDD1159  [1]
 LDCM0281  AC21 PaTu 8988t C849(0.85); C860(0.85)  LDD1160  [1]
 LDCM0282  AC22 PaTu 8988t C849(0.87); C860(0.87)  LDD1161  [1]
 LDCM0283  AC23 PaTu 8988t C849(0.69); C860(0.69)  LDD1162  [1]
 LDCM0284  AC24 PaTu 8988t C849(0.80); C860(0.80)  LDD1163  [1]
 LDCM0308  AC46 PaTu 8988t C849(0.90); C860(0.90)  LDD1187  [1]
 LDCM0309  AC47 PaTu 8988t C849(0.77); C860(0.77)  LDD1188  [1]
 LDCM0310  AC48 PaTu 8988t C849(0.67); C860(0.67)  LDD1189  [1]
 LDCM0311  AC49 PaTu 8988t C849(0.70); C860(0.70)  LDD1190  [1]
 LDCM0313  AC50 PaTu 8988t C849(0.63); C860(0.63)  LDD1192  [1]
 LDCM0314  AC51 PaTu 8988t C849(0.91); C860(0.91)  LDD1193  [1]
 LDCM0315  AC52 PaTu 8988t C849(0.68); C860(0.68)  LDD1194  [1]
 LDCM0316  AC53 PaTu 8988t C849(0.66); C860(0.66)  LDD1195  [1]
 LDCM0317  AC54 PaTu 8988t C849(0.62); C860(0.62)  LDD1196  [1]
 LDCM0318  AC55 PaTu 8988t C849(0.76); C860(0.76)  LDD1197  [1]
 LDCM0319  AC56 PaTu 8988t C849(0.93); C860(0.93)  LDD1198  [1]
 LDCM0320  AC57 PaTu 8988t C849(0.63); C860(0.63)  LDD1199  [1]
 LDCM0321  AC58 PaTu 8988t C849(0.61); C860(0.61)  LDD1200  [1]
 LDCM0322  AC59 PaTu 8988t C849(0.65); C860(0.65)  LDD1201  [1]
 LDCM0323  AC6 PaTu 8988t C849(0.94); C860(0.94)  LDD1202  [1]
 LDCM0324  AC60 PaTu 8988t C849(0.53); C860(0.53)  LDD1203  [1]
 LDCM0325  AC61 PaTu 8988t C849(0.79); C860(0.79)  LDD1204  [1]
 LDCM0326  AC62 PaTu 8988t C849(0.64); C860(0.64)  LDD1205  [1]
 LDCM0327  AC63 PaTu 8988t C849(0.71); C860(0.71)  LDD1206  [1]
 LDCM0328  AC64 PaTu 8988t C849(0.82); C860(0.82)  LDD1207  [1]
 LDCM0329  AC65 PaTu 8988t C849(0.72); C860(0.72)  LDD1208  [1]
 LDCM0330  AC66 PaTu 8988t C849(0.72); C860(0.72)  LDD1209  [1]
 LDCM0331  AC67 PaTu 8988t C849(0.76); C860(0.76)  LDD1210  [1]
 LDCM0334  AC7 PaTu 8988t C849(1.43); C860(1.43)  LDD1213  [1]
 LDCM0345  AC8 PaTu 8988t C849(1.06); C860(1.06)  LDD1224  [1]
 LDCM0248  AKOS034007472 PaTu 8988t C849(0.73); C860(0.73)  LDD1127  [1]
 LDCM0356  AKOS034007680 PaTu 8988t C849(0.88); C860(0.88)  LDD1235  [1]
 LDCM0275  AKOS034007705 PaTu 8988t C849(0.99); C860(0.99)  LDD1154  [1]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [2]
 LDCM0370  CL101 PaTu 8988t C849(0.94); C860(0.94)  LDD1249  [1]
 LDCM0371  CL102 PaTu 8988t C849(1.07); C860(1.07)  LDD1250  [1]
 LDCM0372  CL103 PaTu 8988t C849(0.66); C860(0.66)  LDD1251  [1]
 LDCM0373  CL104 PaTu 8988t C849(1.04); C860(1.04)  LDD1252  [1]
 LDCM0374  CL105 PaTu 8988t C849(0.85); C860(0.85)  LDD1253  [1]
 LDCM0375  CL106 PaTu 8988t C849(1.05); C860(1.05)  LDD1254  [1]
 LDCM0376  CL107 PaTu 8988t C849(1.04); C860(1.04)  LDD1255  [1]
 LDCM0377  CL108 PaTu 8988t C849(0.84); C860(0.84)  LDD1256  [1]
 LDCM0378  CL109 PaTu 8988t C849(0.85); C860(0.85)  LDD1257  [1]
 LDCM0380  CL110 PaTu 8988t C849(0.80); C860(0.80)  LDD1259  [1]
 LDCM0381  CL111 PaTu 8988t C849(0.76); C860(0.76)  LDD1260  [1]
 LDCM0392  CL121 PaTu 8988t C849(0.77); C860(0.77)  LDD1271  [1]
 LDCM0393  CL122 PaTu 8988t C849(0.87); C860(0.87)  LDD1272  [1]
 LDCM0394  CL123 PaTu 8988t C849(0.62); C860(0.62)  LDD1273  [1]
 LDCM0395  CL124 PaTu 8988t C849(0.75); C860(0.75)  LDD1274  [1]
 LDCM0396  CL125 PaTu 8988t C849(0.82); C860(0.82)  LDD1275  [1]
 LDCM0397  CL126 PaTu 8988t C849(0.78); C860(0.78)  LDD1276  [1]
 LDCM0398  CL127 PaTu 8988t C849(0.67); C860(0.67)  LDD1277  [1]
 LDCM0399  CL128 PaTu 8988t C849(0.74); C860(0.74)  LDD1278  [1]
 LDCM0420  CL31 PaTu 8988t C849(0.88); C860(0.88)  LDD1299  [1]
 LDCM0421  CL32 PaTu 8988t C849(0.64); C860(0.64)  LDD1300  [1]
 LDCM0422  CL33 PaTu 8988t C849(0.75); C860(0.75)  LDD1301  [1]
 LDCM0423  CL34 PaTu 8988t C849(0.72); C860(0.72)  LDD1302  [1]
 LDCM0424  CL35 PaTu 8988t C849(0.66); C860(0.66)  LDD1303  [1]
 LDCM0425  CL36 PaTu 8988t C849(0.45); C860(0.45)  LDD1304  [1]
 LDCM0426  CL37 PaTu 8988t C849(0.62); C860(0.62)  LDD1305  [1]
 LDCM0428  CL39 PaTu 8988t C849(0.72); C860(0.72)  LDD1307  [1]
 LDCM0430  CL40 PaTu 8988t C849(0.72); C860(0.72)  LDD1309  [1]
 LDCM0431  CL41 PaTu 8988t C849(0.69); C860(0.69)  LDD1310  [1]
 LDCM0432  CL42 PaTu 8988t C849(0.63); C860(0.63)  LDD1311  [1]
 LDCM0433  CL43 PaTu 8988t C849(0.47); C860(0.47)  LDD1312  [1]
 LDCM0434  CL44 PaTu 8988t C849(0.60); C860(0.60)  LDD1313  [1]
 LDCM0435  CL45 PaTu 8988t C849(0.72); C860(0.72)  LDD1314  [1]
 LDCM0453  CL61 PaTu 8988t C849(0.74); C860(0.74)  LDD1332  [1]
 LDCM0454  CL62 PaTu 8988t C849(1.15); C860(1.15)  LDD1333  [1]
 LDCM0455  CL63 PaTu 8988t C849(1.15); C860(1.15)  LDD1334  [1]
 LDCM0456  CL64 PaTu 8988t C849(1.02); C860(1.02)  LDD1335  [1]
 LDCM0457  CL65 PaTu 8988t C849(0.85); C860(0.85)  LDD1336  [1]
 LDCM0458  CL66 PaTu 8988t C849(0.99); C860(0.99)  LDD1337  [1]
 LDCM0459  CL67 PaTu 8988t C849(0.79); C860(0.79)  LDD1338  [1]
 LDCM0460  CL68 PaTu 8988t C849(0.69); C860(0.69)  LDD1339  [1]
 LDCM0461  CL69 PaTu 8988t C849(0.73); C860(0.73)  LDD1340  [1]
 LDCM0463  CL70 PaTu 8988t C849(0.79); C860(0.79)  LDD1342  [1]
 LDCM0464  CL71 PaTu 8988t C849(1.13); C860(1.13)  LDD1343  [1]
 LDCM0465  CL72 PaTu 8988t C849(1.64); C860(1.64)  LDD1344  [1]
 LDCM0466  CL73 PaTu 8988t C849(0.86); C860(0.86)  LDD1345  [1]
 LDCM0467  CL74 PaTu 8988t C849(1.08); C860(1.08)  LDD1346  [1]
 LDCM0468  Fragment33 PaTu 8988t C849(0.89); C860(0.89)  LDD1347  [1]
 LDCM0427  Fragment51 PaTu 8988t C849(0.56); C860(0.56)  LDD1306  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
Growth factor receptor-bound protein 10 (GRB10) GRB7/10/14 family Q13322
Growth factor receptor-bound protein 7 (GRB7) GRB7/10/14 family Q14451

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Chlortetracycline . DB09093
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid19788238c66 Small molecular drug D05FXD
Pmid23489211c20 Small molecular drug D0X8BU

References

1 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
2 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.