Details of the Target

General Information of Target

Target ID LDTP03475
Target Name Ephrin type-A receptor 3 (EPHA3)
Gene Name EPHA3
Gene ID 2042
Synonyms
ETK; ETK1; HEK; TYRO4; Ephrin type-A receptor 3; EC 2.7.10.1; EPH-like kinase 4; EK4; hEK4; HEK; Human embryo kinase; Tyrosine-protein kinase TYRO4; Tyrosine-protein kinase receptor ETK1; Eph-like tyrosine kinase 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDCQLSILLLLSCSVLDSFGELIPQPSNEVNLLDSKTIQGELGWISYPSHGWEEISGVDE
HYTPIRTYQVCNVMDHSQNNWLRTNWVPRNSAQKIYVELKFTLRDCNSIPLVLGTCKETF
NLYYMESDDDHGVKFREHQFTKIDTIAADESFTQMDLGDRILKLNTEIREVGPVNKKGFY
LAFQDVGACVALVSVRVYFKKCPFTVKNLAMFPDTVPMDSQSLVEVRGSCVNNSKEEDPP
RMYCSTEGEWLVPIGKCSCNAGYEERGFMCQACRPGFYKALDGNMKCAKCPPHSSTQEDG
SMNCRCENNYFRADKDPPSMACTRPPSSPRNVISNINETSVILDWSWPLDTGGRKDVTFN
IICKKCGWNIKQCEPCSPNVRFLPRQFGLTNTTVTVTDLLAHTNYTFEIDAVNGVSELSS
PPRQFAAVSITTNQAAPSPVLTIKKDRTSRNSISLSWQEPEHPNGIILDYEVKYYEKQEQ
ETSYTILRARGTNVTISSLKPDTIYVFQIRARTAAGYGTNSRKFEFETSPDSFSISGESS
QVVMIAISAAVAIILLTVVIYVLIGRFCGYKSKHGADEKRLHFGNGHLKLPGLRTYVDPH
TYEDPTQAVHEFAKELDATNISIDKVVGAGEFGEVCSGRLKLPSKKEISVAIKTLKVGYT
EKQRRDFLGEASIMGQFDHPNIIRLEGVVTKSKPVMIVTEYMENGSLDSFLRKHDAQFTV
IQLVGMLRGIASGMKYLSDMGYVHRDLAARNILINSNLVCKVSDFGLSRVLEDDPEAAYT
TRGGKIPIRWTSPEAIAYRKFTSASDVWSYGIVLWEVMSYGERPYWEMSNQDVIKAVDEG
YRLPPPMDCPAALYQLMLDCWQKDRNNRPKFEQIVSILDKLIRNPGSLKIITSAAARPSN
LLLDQSNVDITTFRTTGDWLNGVWTAHCKEIFTGVEYSSCDTIAKISTDDMKKVGVTVVG
PQKKIISSIKALETQSKNGPVPV
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, Ephrin receptor subfamily
Subcellular location
Secreted; Cell membrane
Function
Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin 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. Highly promiscuous for ephrin-A ligands it binds preferentially EFNA5. Upon activation by EFNA5 regulates cell-cell adhesion, cytoskeletal organization and cell migration. Plays a role in cardiac cells migration and differentiation and regulates the formation of the atrioventricular canal and septum during development probably through activation by EFNA1. Involved in the retinotectal mapping of neurons. May also control the segregation but not the guidance of motor and sensory axons during neuromuscular circuit development.
TTD ID
T28413
Uniprot ID
P29320
DrugMap ID
TTHS2LR
Ensemble ID
ENST00000336596.7
HGNC ID
HGNC:3387
ChEMBL ID
CHEMBL4954

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.Q508K .
CMK SNV: p.V762L .
COLO678 SNV: p.P217T .
COLO792 SNV: p.R324Q
Substitution: p.S706F		 DBIA    Probe Info 
HEC1B SNV: p.E816G .
JHH4 SNV: p.R305K .
KMS12BM SNV: p.F533L .
LOXIMVI SNV: p.W808Ter .
MCC26 SNV: p.M951I .
MDAMB231 SNV: p.E839Ter .
MDAMB436 SNV: p.L747V .
MEWO SNV: p.S46F; p.E53K .
NCIH1666 SNV: p.F135S .
NCIH2172 SNV: p.S258P .
NUGC3 SNV: p.N755I .
PC9 SNV: p.H76N .
SBC5 Substitution: p.I453T .
SG231 SNV: p.C202Ter .
SW756 SNV: p.K945E .
SW948 SNV: p.R83G .
TF1 SNV: p.T102I .
TYKNU SNV: p.P384A .
U87MG SNV: p.K500N .

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
Probe 1
 Probe Info  		Y779(9.37)  LDD3495  [1]
DBIA
 Probe Info  		C636(2.77)  LDD3423  [2]
IA-alkyne
 Probe Info  		C71(0.00); C760(0.00); C322(0.00); C363(0.00)  LDD0167  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C940(1.21)  LDD1507  [4]
 LDCM0215  AC10 HEK-293T C940(0.95)  LDD1508  [4]
 LDCM0226  AC11 HEK-293T C940(1.24)  LDD1509  [4]
 LDCM0237  AC12 HEK-293T C940(0.93); C849(1.13)  LDD1510  [4]
 LDCM0259  AC14 HEK-293T C940(1.10)  LDD1512  [4]
 LDCM0270  AC15 HEK-293T C940(1.25); C849(1.11)  LDD1513  [4]
 LDCM0276  AC17 HEK-293T C940(1.12)  LDD1515  [4]
 LDCM0277  AC18 HEK-293T C940(1.19)  LDD1516  [4]
 LDCM0278  AC19 HEK-293T C940(0.99)  LDD1517  [4]
 LDCM0279  AC2 HEK-293T C940(0.85)  LDD1518  [4]
 LDCM0280  AC20 HEK-293T C940(0.91); C849(1.05)  LDD1519  [4]
 LDCM0281  AC21 HEK-293T C940(0.82); C636(0.89)  LDD1520  [4]
 LDCM0282  AC22 HEK-293T C940(1.01)  LDD1521  [4]
 LDCM0283  AC23 HEK-293T C940(0.88); C849(0.98)  LDD1522  [4]
 LDCM0284  AC24 HEK-293T C940(1.07); C760(0.85)  LDD1523  [4]
 LDCM0285  AC25 HEK-293T C940(1.28)  LDD1524  [4]
 LDCM0286  AC26 HEK-293T C940(1.06)  LDD1525  [4]
 LDCM0287  AC27 HEK-293T C940(1.30)  LDD1526  [4]
 LDCM0288  AC28 HEK-293T C940(1.06); C849(1.04)  LDD1527  [4]
 LDCM0289  AC29 HEK-293T C940(1.00); C636(1.01)  LDD1528  [4]
 LDCM0290  AC3 HEK-293T C940(1.36)  LDD1529  [4]
 LDCM0291  AC30 HEK-293T C940(1.07)  LDD1530  [4]
 LDCM0292  AC31 HEK-293T C940(1.21); C849(0.97)  LDD1531  [4]
 LDCM0293  AC32 HEK-293T C940(1.00); C760(0.95)  LDD1532  [4]
 LDCM0294  AC33 HEK-293T C940(1.11)  LDD1533  [4]
 LDCM0295  AC34 HEK-293T C940(1.08)  LDD1534  [4]
 LDCM0296  AC35 HEK-293T C940(1.49)  LDD1535  [4]
 LDCM0297  AC36 HEK-293T C940(1.08); C849(1.29)  LDD1536  [4]
 LDCM0298  AC37 HEK-293T C940(0.90); C636(1.04)  LDD1537  [4]
 LDCM0299  AC38 HEK-293T C940(0.96)  LDD1538  [4]
 LDCM0300  AC39 HEK-293T C940(1.03); C849(1.24)  LDD1539  [4]
 LDCM0301  AC4 HEK-293T C940(1.09); C849(1.13)  LDD1540  [4]
 LDCM0302  AC40 HEK-293T C940(1.08); C760(1.16)  LDD1541  [4]
 LDCM0303  AC41 HEK-293T C940(1.23)  LDD1542  [4]
 LDCM0304  AC42 HEK-293T C940(1.53)  LDD1543  [4]
 LDCM0305  AC43 HEK-293T C940(1.01)  LDD1544  [4]
 LDCM0306  AC44 HEK-293T C940(1.06); C849(1.13)  LDD1545  [4]
 LDCM0307  AC45 HEK-293T C940(0.90); C636(1.12)  LDD1546  [4]
 LDCM0308  AC46 HEK-293T C940(1.10)  LDD1547  [4]
 LDCM0309  AC47 HEK-293T C940(0.96); C849(1.27)  LDD1548  [4]
 LDCM0310  AC48 HEK-293T C940(1.02); C760(1.07)  LDD1549  [4]
 LDCM0311  AC49 HEK-293T C940(1.25)  LDD1550  [4]
 LDCM0312  AC5 HEK-293T C940(0.99); C636(0.98)  LDD1551  [4]
 LDCM0313  AC50 HEK-293T C940(1.14)  LDD1552  [4]
 LDCM0314  AC51 HEK-293T C940(1.08)  LDD1553  [4]
 LDCM0315  AC52 HEK-293T C940(1.13); C849(1.03)  LDD1554  [4]
 LDCM0316  AC53 HEK-293T C940(0.82); C636(0.95)  LDD1555  [4]
 LDCM0317  AC54 HEK-293T C940(1.08)  LDD1556  [4]
 LDCM0318  AC55 HEK-293T C940(1.40); C849(1.09)  LDD1557  [4]
 LDCM0319  AC56 HEK-293T C940(1.08); C760(1.09)  LDD1558  [4]
 LDCM0320  AC57 HEK-293T C940(0.93)  LDD1559  [4]
 LDCM0321  AC58 HEK-293T C940(1.12)  LDD1560  [4]
 LDCM0322  AC59 HEK-293T C940(1.52)  LDD1561  [4]
 LDCM0323  AC6 HEK-293T C940(1.27)  LDD1562  [4]
 LDCM0324  AC60 HEK-293T C940(0.90); C849(0.99)  LDD1563  [4]
 LDCM0325  AC61 HEK-293T C940(1.05); C636(0.96)  LDD1564  [4]
 LDCM0326  AC62 HEK-293T C940(1.03)  LDD1565  [4]
 LDCM0327  AC63 HEK-293T C940(1.12); C849(1.31)  LDD1566  [4]
 LDCM0328  AC64 HEK-293T C940(1.13); C760(0.94)  LDD1567  [4]
 LDCM0334  AC7 HEK-293T C940(1.19); C849(0.99)  LDD1568  [4]
 LDCM0345  AC8 HEK-293T C940(1.13); C760(0.89)  LDD1569  [4]
 LDCM0248  AKOS034007472 HEK-293T C940(1.01); C636(1.01)  LDD1511  [4]
 LDCM0356  AKOS034007680 HEK-293T C940(1.16)  LDD1570  [4]
 LDCM0275  AKOS034007705 HEK-293T C940(1.06); C760(1.04)  LDD1514  [4]
 LDCM0367  CL1 HEK-293T C940(1.13)  LDD1571  [4]
 LDCM0368  CL10 HEK-293T C940(1.57)  LDD1572  [4]
 LDCM0370  CL101 HEK-293T C940(1.27)  LDD1574  [4]
 LDCM0371  CL102 HEK-293T C940(0.92)  LDD1575  [4]
 LDCM0372  CL103 HEK-293T C940(1.20)  LDD1576  [4]
 LDCM0374  CL105 HEK-293T C940(1.22)  LDD1578  [4]
 LDCM0375  CL106 HEK-293T C940(0.98)  LDD1579  [4]
 LDCM0376  CL107 HEK-293T C940(0.88)  LDD1580  [4]
 LDCM0378  CL109 HEK-293T C940(1.12)  LDD1582  [4]
 LDCM0379  CL11 HEK-293T C940(1.54); C849(0.99)  LDD1583  [4]
 LDCM0380  CL110 HEK-293T C940(1.03)  LDD1584  [4]
 LDCM0381  CL111 HEK-293T C940(0.95)  LDD1585  [4]
 LDCM0383  CL113 HEK-293T C940(1.41)  LDD1587  [4]
 LDCM0384  CL114 HEK-293T C940(1.12)  LDD1588  [4]
 LDCM0385  CL115 HEK-293T C940(1.11)  LDD1589  [4]
 LDCM0387  CL117 HEK-293T C940(1.08)  LDD1591  [4]
 LDCM0388  CL118 HEK-293T C940(0.88)  LDD1592  [4]
 LDCM0389  CL119 HEK-293T C940(1.18)  LDD1593  [4]
 LDCM0390  CL12 HEK-293T C940(1.38); C760(1.10)  LDD1594  [4]
 LDCM0392  CL121 HEK-293T C940(1.54)  LDD1596  [4]
 LDCM0393  CL122 HEK-293T C940(1.01)  LDD1597  [4]
 LDCM0394  CL123 HEK-293T C940(1.13)  LDD1598  [4]
 LDCM0396  CL125 HEK-293T C940(1.11)  LDD1600  [4]
 LDCM0397  CL126 HEK-293T C940(1.08)  LDD1601  [4]
 LDCM0398  CL127 HEK-293T C940(0.99)  LDD1602  [4]
 LDCM0400  CL13 HEK-293T C940(1.11)  LDD1604  [4]
 LDCM0401  CL14 HEK-293T C940(1.21)  LDD1605  [4]
 LDCM0402  CL15 HEK-293T C940(1.06)  LDD1606  [4]
 LDCM0404  CL17 HEK-293T C940(0.98)  LDD1608  [4]
 LDCM0405  CL18 HEK-293T C940(1.19)  LDD1609  [4]
 LDCM0406  CL19 HEK-293T C940(1.14)  LDD1610  [4]
 LDCM0407  CL2 HEK-293T C940(1.15)  LDD1611  [4]
 LDCM0408  CL20 HEK-293T C940(1.26); C849(0.79)  LDD1612  [4]
 LDCM0409  CL21 HEK-293T C940(1.55); C636(1.08)  LDD1613  [4]
 LDCM0410  CL22 HEK-293T C940(1.26)  LDD1614  [4]
 LDCM0411  CL23 HEK-293T C940(1.32); C849(1.38)  LDD1615  [4]
 LDCM0412  CL24 HEK-293T C940(1.31); C760(1.17)  LDD1616  [4]
 LDCM0413  CL25 HEK-293T C940(1.08)  LDD1617  [4]
 LDCM0414  CL26 HEK-293T C940(0.95)  LDD1618  [4]
 LDCM0415  CL27 HEK-293T C940(1.22)  LDD1619  [4]
 LDCM0417  CL29 HEK-293T C940(1.13)  LDD1621  [4]
 LDCM0418  CL3 HEK-293T C940(1.10)  LDD1622  [4]
 LDCM0419  CL30 HEK-293T C940(1.26)  LDD1623  [4]
 LDCM0420  CL31 HEK-293T C940(1.28)  LDD1624  [4]
 LDCM0421  CL32 HEK-293T C940(1.13); C849(0.99)  LDD1625  [4]
 LDCM0422  CL33 HEK-293T C940(1.30); C636(0.64)  LDD1626  [4]
 LDCM0423  CL34 HEK-293T C940(1.25)  LDD1627  [4]
 LDCM0424  CL35 HEK-293T C940(1.14); C849(1.24)  LDD1628  [4]
 LDCM0425  CL36 HEK-293T C940(1.26); C760(1.17)  LDD1629  [4]
 LDCM0426  CL37 HEK-293T C940(1.09)  LDD1630  [4]
 LDCM0428  CL39 HEK-293T C940(0.98)  LDD1632  [4]
 LDCM0431  CL41 HEK-293T C940(1.26)  LDD1635  [4]
 LDCM0432  CL42 HEK-293T C940(1.08)  LDD1636  [4]
 LDCM0433  CL43 HEK-293T C940(1.07)  LDD1637  [4]
 LDCM0434  CL44 HEK-293T C940(0.99); C849(0.88)  LDD1638  [4]
 LDCM0435  CL45 HEK-293T C940(0.94); C636(1.00)  LDD1639  [4]
 LDCM0436  CL46 HEK-293T C940(1.35)  LDD1640  [4]
 LDCM0437  CL47 HEK-293T C940(1.34); C849(1.23)  LDD1641  [4]
 LDCM0438  CL48 HEK-293T C940(1.09); C760(0.96)  LDD1642  [4]
 LDCM0439  CL49 HEK-293T C940(1.02)  LDD1643  [4]
 LDCM0440  CL5 HEK-293T C940(1.26)  LDD1644  [4]
 LDCM0441  CL50 HEK-293T C940(1.08)  LDD1645  [4]
 LDCM0444  CL53 HEK-293T C940(1.24)  LDD1647  [4]
 LDCM0445  CL54 HEK-293T C940(1.55)  LDD1648  [4]
 LDCM0446  CL55 HEK-293T C940(1.22)  LDD1649  [4]
 LDCM0447  CL56 HEK-293T C940(1.01); C849(0.89)  LDD1650  [4]
 LDCM0448  CL57 HEK-293T C940(1.09); C636(0.62)  LDD1651  [4]
 LDCM0449  CL58 HEK-293T C940(1.40)  LDD1652  [4]
 LDCM0450  CL59 HEK-293T C940(1.25); C849(1.13)  LDD1653  [4]
 LDCM0451  CL6 HEK-293T C940(1.29)  LDD1654  [4]
 LDCM0452  CL60 HEK-293T C940(1.28); C760(1.05)  LDD1655  [4]
 LDCM0453  CL61 HEK-293T C940(1.15)  LDD1656  [4]
 LDCM0454  CL62 HEK-293T C940(0.96)  LDD1657  [4]
 LDCM0455  CL63 HEK-293T C940(0.94)  LDD1658  [4]
 LDCM0457  CL65 HEK-293T C940(0.98)  LDD1660  [4]
 LDCM0458  CL66 HEK-293T C940(1.21)  LDD1661  [4]
 LDCM0459  CL67 HEK-293T C940(1.28)  LDD1662  [4]
 LDCM0460  CL68 HEK-293T C940(1.08); C849(0.92)  LDD1663  [4]
 LDCM0461  CL69 HEK-293T C940(1.38); C636(0.80)  LDD1664  [4]
 LDCM0462  CL7 HEK-293T C940(1.21)  LDD1665  [4]
 LDCM0463  CL70 HEK-293T C940(1.38)  LDD1666  [4]
 LDCM0464  CL71 HEK-293T C940(0.98); C849(1.02)  LDD1667  [4]
 LDCM0465  CL72 HEK-293T C940(1.20); C760(1.11)  LDD1668  [4]
 LDCM0466  CL73 HEK-293T C940(1.42)  LDD1669  [4]
 LDCM0467  CL74 HEK-293T C940(1.01)  LDD1670  [4]
 LDCM0470  CL77 HEK-293T C940(1.30)  LDD1673  [4]
 LDCM0471  CL78 HEK-293T C940(1.25)  LDD1674  [4]
 LDCM0472  CL79 HEK-293T C940(1.50)  LDD1675  [4]
 LDCM0473  CL8 HEK-293T C940(1.39); C849(0.74)  LDD1676  [4]
 LDCM0474  CL80 HEK-293T C940(1.13); C849(0.96)  LDD1677  [4]
 LDCM0475  CL81 HEK-293T C940(1.02); C636(0.70)  LDD1678  [4]
 LDCM0476  CL82 HEK-293T C940(1.15)  LDD1679  [4]
 LDCM0477  CL83 HEK-293T C940(1.28); C849(1.19)  LDD1680  [4]
 LDCM0478  CL84 HEK-293T C940(1.17); C760(1.28)  LDD1681  [4]
 LDCM0479  CL85 HEK-293T C940(1.18)  LDD1682  [4]
 LDCM0480  CL86 HEK-293T C940(1.04)  LDD1683  [4]
 LDCM0481  CL87 HEK-293T C940(0.85)  LDD1684  [4]
 LDCM0483  CL89 HEK-293T C940(1.02)  LDD1686  [4]
 LDCM0484  CL9 HEK-293T C940(1.01); C636(0.95)  LDD1687  [4]
 LDCM0485  CL90 HEK-293T C940(1.28)  LDD1688  [4]
 LDCM0486  CL91 HEK-293T C940(1.13)  LDD1689  [4]
 LDCM0487  CL92 HEK-293T C940(1.07); C849(0.80)  LDD1690  [4]
 LDCM0488  CL93 HEK-293T C940(0.89); C636(0.91)  LDD1691  [4]
 LDCM0489  CL94 HEK-293T C940(1.12)  LDD1692  [4]
 LDCM0490  CL95 HEK-293T C940(1.00); C849(1.14)  LDD1693  [4]
 LDCM0491  CL96 HEK-293T C940(1.29); C760(0.94)  LDD1694  [4]
 LDCM0492  CL97 HEK-293T C940(1.15)  LDD1695  [4]
 LDCM0493  CL98 HEK-293T C940(1.12)  LDD1696  [4]
 LDCM0494  CL99 HEK-293T C940(0.93)  LDD1697  [4]
 LDCM0495  E2913 HEK-293T C940(1.03)  LDD1698  [4]
 LDCM0468  Fragment33 HEK-293T C940(0.98)  LDD1671  [4]
 LDCM0427  Fragment51 HEK-293T C940(1.07)  LDD1631  [4]
 LDCM0022  KB02 HEK-293T C636(0.79)  LDD1492  [4]
 LDCM0023  KB03 HEK-293T C636(0.88)  LDD1497  [4]
 LDCM0024  KB05 SK-ES1 C636(2.77)  LDD3423  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ephrin type-A receptor 2 (EPHA2) Tyr protein kinase family P29317
Ephrin type-A receptor 7 (EPHA7) Tyr protein kinase family Q15375

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Kb-004 Antibody D0FJ9W
Ifabotuzumab . D08NZG
Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid19788238c66 Small molecular drug D05FXD
Pmid21561767c8h Small molecular drug D02BXJ
Pmid23489211c20 Small molecular drug D0X8BU

References

1 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
4 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402