General Information of Target

Target ID LDTP04631
Target Name Ephrin type-B receptor 4 (EPHB4)
Gene Name EPHB4
Gene ID 2050
Synonyms
HTK; MYK1; TYRO11; Ephrin type-B receptor 4; EC 2.7.10.1; Hepatoma transmembrane kinase; Tyrosine-protein kinase TYRO11
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MELRVLLCWASLAAALEETLLNTKLETADLKWVTFPQVDGQWEELSGLDEEQHSVRTYEV
CDVQRAPGQAHWLRTGWVPRRGAVHVYATLRFTMLECLSLPRAGRSCKETFTVFYYESDA
DTATALTPAWMENPYIKVDTVAAEHLTRKRPGAEATGKVNVKTLRLGPLSKAGFYLAFQD
QGACMALLSLHLFYKKCAQLTVNLTRFPETVPRELVVPVAGSCVVDAVPAPGPSPSLYCR
EDGQWAEQPVTGCSCAPGFEAAEGNTKCRACAQGTFKPLSGEGSCQPCPANSHSNTIGSA
VCQCRVGYFRARTDPRGAPCTTPPSAPRSVVSRLNGSSLHLEWSAPLESGGREDLTYALR
CRECRPGGSCAPCGGDLTFDPGPRDLVEPWVVVRGLRPDFTYTFEVTALNGVSSLATGPV
PFEPVNVTTDREVPPAVSDIRVTRSSPSSLSLAWAVPRAPSGAVLDYEVKYHEKGAEGPS
SVRFLKTSENRAELRGLKRGASYLVQVRARSEAGYGPFGQEHHSQTQLDESEGWREQLAL
IAGTAVVGVVLVLVVIVVAVLCLRKQSNGREAEYSDKHGQYLIGHGTKVYIDPFTYEDPN
EAVREFAKEIDVSYVKIEEVIGAGEFGEVCRGRLKAPGKKESCVAIKTLKGGYTERQRRE
FLSEASIMGQFEHPNIIRLEGVVTNSMPVMILTEFMENGALDSFLRLNDGQFTVIQLVGM
LRGIASGMRYLAEMSYVHRDLAARNILVNSNLVCKVSDFGLSRFLEENSSDPTYTSSLGG
KIPIRWTAPEAIAFRKFTSASDAWSYGIVMWEVMSFGERPYWDMSNQDVINAIEQDYRLP
PPPDCPTSLHQLMLDCWQKDRNARPRFPQVVSALDKMIRNPASLKIVARENGGASHPLLD
QRQPHYSAFGSVGEWLRAIKMGRYEESFAAAGFGSFELVSQISAEDLLRIGVTLAGHQKK
ILASVQHMKSQAKPGTPGGTGGPAPQY
Target Type
Clinical trial
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. Together with its cognate ligand/functional ligand EFNB2 it is involved in the regulation of cell adhesion and migration, and plays a central role in heart morphogenesis, angiogenesis and blood vessel remodeling and permeability. EPHB4-mediated forward signaling controls cellular repulsion and segregation from EFNB2-expressing cells.
TTD ID
T49507
Uniprot ID
P54760
DrugMap ID
TTI4ZX2
Ensemble ID
ENST00000358173.8
HGNC ID
HGNC:3395
ChEMBL ID
CHEMBL5147

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.T587A DBIA    Probe Info 
A431 SNV: p.T847P .
CCK81 SNV: p.W9Ter .
COLO829 SNV: p.P346L .
Ishikawa (Heraklio) 02 ER Deletion: p.R384GfsTer26 DBIA    Probe Info 
JURKAT SNV: p.G375R .
KYSE30 SNV: p.I646M .
LNCaP clone FGC SNV: p.D576G .
MCC13 Substitution: p.A70V .
MCC26 SNV: p.T147I .
MFE319 Deletion: .
SNV: p.M185V
.
OVCAR4 SNV: p.E43V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info 
K470(0.45)  LDD0277  [1]
OPA-S-S-alkyne
 Probe Info 
K474(0.75); K267(3.27); K486(4.21)  LDD3494  [2]
DBIA
 Probe Info 
C320(1.91)  LDD3318  [3]
BTD
 Probe Info 
C643(0.49)  LDD2100  [4]
ATP probe
 Probe Info 
N.A.  LDD0199  [5]
IA-alkyne
 Probe Info 
C754(0.00); C223(0.00); C320(0.00)  LDD0162  [6]
IPM
 Probe Info 
C754(0.00); C643(0.00)  LDD0147  [7]
Acrolein
 Probe Info 
N.A.  LDD0217  [8]
NAIA_5
 Probe Info 
C97(0.00); C320(0.00); C239(0.00); C223(0.00)  LDD2223  [9]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Dasatinib-CA-3PAP
 Probe Info 
N.A.  LDD0365  [10]
Dasatinib-CA-8PAP
 Probe Info 
N.A.  LDD0364  [10]
DFG-out-3
 Probe Info 
35.00  LDD0074  [11]
DFG-out-4
 Probe Info 
71.00  LDD0075  [11]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C643(0.58)  LDD2142  [4]
 LDCM0214  AC1 HEK-293T C643(1.06); C630(1.12)  LDD1507  [12]
 LDCM0215  AC10 HEK-293T C643(0.96); C630(1.02)  LDD1508  [12]
 LDCM0226  AC11 HEK-293T C643(0.98); C630(1.02)  LDD1509  [12]
 LDCM0237  AC12 HEK-293T C643(0.98); C630(0.97); C320(0.85)  LDD1510  [12]
 LDCM0259  AC14 HEK-293T C643(1.03); C630(1.05)  LDD1512  [12]
 LDCM0270  AC15 HEK-293T C643(0.97); C630(1.10)  LDD1513  [12]
 LDCM0276  AC17 HEK-293T C643(0.99); C630(1.12)  LDD1515  [12]
 LDCM0277  AC18 HEK-293T C643(0.93); C630(0.91)  LDD1516  [12]
 LDCM0278  AC19 HEK-293T C643(0.96); C630(1.15)  LDD1517  [12]
 LDCM0279  AC2 HEK-293T C643(0.90); C630(0.98)  LDD1518  [12]
 LDCM0280  AC20 HEK-293T C643(0.98); C630(1.06); C320(0.98)  LDD1519  [12]
 LDCM0281  AC21 HEK-293T C643(0.99); C320(0.90)  LDD1520  [12]
 LDCM0282  AC22 HEK-293T C643(0.94); C630(1.20)  LDD1521  [12]
 LDCM0283  AC23 HEK-293T C643(0.98); C630(1.08)  LDD1522  [12]
 LDCM0284  AC24 HEK-293T C643(0.95); C630(0.99); C320(1.01)  LDD1523  [12]
 LDCM0285  AC25 HEK-293T C643(1.04); C630(1.05)  LDD1524  [12]
 LDCM0286  AC26 HEK-293T C643(0.96); C630(0.99)  LDD1525  [12]
 LDCM0287  AC27 HEK-293T C643(1.02); C630(1.14)  LDD1526  [12]
 LDCM0288  AC28 HEK-293T C643(1.00); C630(1.16); C320(0.78)  LDD1527  [12]
 LDCM0289  AC29 HEK-293T C643(1.00); C320(0.85)  LDD1528  [12]
 LDCM0290  AC3 HEK-293T C643(0.96); C630(1.06)  LDD1529  [12]
 LDCM0291  AC30 HEK-293T C643(1.03); C630(1.13)  LDD1530  [12]
 LDCM0292  AC31 HEK-293T C643(0.95); C630(1.06)  LDD1531  [12]
 LDCM0293  AC32 HEK-293T C643(0.94); C630(1.11); C320(0.90)  LDD1532  [12]
 LDCM0294  AC33 HEK-293T C643(1.04); C630(1.23)  LDD1533  [12]
 LDCM0295  AC34 HEK-293T C643(0.88); C630(1.06)  LDD1534  [12]
 LDCM0296  AC35 HEK-293T C643(0.94); C630(1.06)  LDD1535  [12]
 LDCM0297  AC36 HEK-293T C643(0.93); C630(0.97); C320(0.75)  LDD1536  [12]
 LDCM0298  AC37 HEK-293T C643(0.95); C320(1.13)  LDD1537  [12]
 LDCM0299  AC38 HEK-293T C643(0.93); C630(1.23)  LDD1538  [12]
 LDCM0300  AC39 HEK-293T C643(0.98); C630(1.05)  LDD1539  [12]
 LDCM0301  AC4 HEK-293T C643(1.00); C630(1.18); C320(0.84)  LDD1540  [12]
 LDCM0302  AC40 HEK-293T C643(0.96); C630(1.04); C320(0.98)  LDD1541  [12]
 LDCM0303  AC41 HEK-293T C643(1.08); C630(1.12)  LDD1542  [12]
 LDCM0304  AC42 HEK-293T C643(0.92); C630(1.10)  LDD1543  [12]
 LDCM0305  AC43 HEK-293T C643(0.95); C630(0.99)  LDD1544  [12]
 LDCM0306  AC44 HEK-293T C643(0.98); C630(0.98); C320(0.90)  LDD1545  [12]
 LDCM0307  AC45 HEK-293T C643(1.02); C320(0.96)  LDD1546  [12]
 LDCM0308  AC46 HEK-293T C643(0.91); C630(1.21)  LDD1547  [12]
 LDCM0309  AC47 HEK-293T C643(1.00); C630(1.19)  LDD1548  [12]
 LDCM0310  AC48 HEK-293T C643(0.98); C630(1.09); C320(1.14)  LDD1549  [12]
 LDCM0311  AC49 HEK-293T C643(1.02); C630(1.09)  LDD1550  [12]
 LDCM0312  AC5 HEK-293T C643(1.02); C320(0.98)  LDD1551  [12]
 LDCM0313  AC50 HEK-293T C643(0.94); C630(1.03)  LDD1552  [12]
 LDCM0314  AC51 HEK-293T C643(0.90); C630(1.12)  LDD1553  [12]
 LDCM0315  AC52 HEK-293T C643(0.97); C630(1.06); C320(0.85)  LDD1554  [12]
 LDCM0316  AC53 HEK-293T C643(0.98); C320(0.96)  LDD1555  [12]
 LDCM0317  AC54 HEK-293T C643(0.95); C630(1.10)  LDD1556  [12]
 LDCM0318  AC55 HEK-293T C643(0.94); C630(1.12)  LDD1557  [12]
 LDCM0319  AC56 HEK-293T C643(0.97); C630(0.99); C320(0.97)  LDD1558  [12]
 LDCM0320  AC57 HEK-293T C643(1.03); C630(1.25)  LDD1559  [12]
 LDCM0321  AC58 HEK-293T C643(0.90); C630(1.00)  LDD1560  [12]
 LDCM0322  AC59 HEK-293T C643(0.94); C630(1.14)  LDD1561  [12]
 LDCM0323  AC6 HEK-293T C643(0.94); C630(1.17)  LDD1562  [12]
 LDCM0324  AC60 HEK-293T C643(0.97); C630(1.12); C320(0.85)  LDD1563  [12]
 LDCM0325  AC61 HEK-293T C643(1.01); C320(0.91)  LDD1564  [12]
 LDCM0326  AC62 HEK-293T C643(0.97); C630(1.08)  LDD1565  [12]
 LDCM0327  AC63 HEK-293T C643(1.00); C630(1.07)  LDD1566  [12]
 LDCM0328  AC64 HEK-293T C643(1.00); C630(1.21); C320(0.98)  LDD1567  [12]
 LDCM0334  AC7 HEK-293T C643(0.96); C630(1.01)  LDD1568  [12]
 LDCM0345  AC8 HEK-293T C643(0.95); C630(1.09); C320(0.89)  LDD1569  [12]
 LDCM0248  AKOS034007472 HEK-293T C643(1.00); C320(0.88)  LDD1511  [12]
 LDCM0356  AKOS034007680 HEK-293T C643(1.06); C630(1.15)  LDD1570  [12]
 LDCM0275  AKOS034007705 HEK-293T C643(0.95); C630(1.00); C320(0.97)  LDD1514  [12]
 LDCM0367  CL1 HEK-293T C643(0.93); C630(0.87)  LDD1571  [12]
 LDCM0368  CL10 HEK-293T C643(1.07); C630(1.22)  LDD1572  [12]
 LDCM0369  CL100 HEK-293T C643(0.95); C630(0.97)  LDD1573  [12]
 LDCM0370  CL101 HEK-293T C643(1.04); C630(1.07)  LDD1574  [12]
 LDCM0371  CL102 HEK-293T C643(1.15); C630(1.03)  LDD1575  [12]
 LDCM0372  CL103 HEK-293T C643(0.99)  LDD1576  [12]
 LDCM0373  CL104 HEK-293T C643(0.97); C630(0.92)  LDD1577  [12]
 LDCM0374  CL105 HEK-293T C643(0.98); C630(0.96)  LDD1578  [12]
 LDCM0375  CL106 HEK-293T C643(0.99); C630(0.94)  LDD1579  [12]
 LDCM0376  CL107 HEK-293T C643(0.92)  LDD1580  [12]
 LDCM0377  CL108 HEK-293T C643(0.97); C630(1.00)  LDD1581  [12]
 LDCM0378  CL109 HEK-293T C643(1.02); C630(0.87)  LDD1582  [12]
 LDCM0379  CL11 HEK-293T C643(1.13); C630(1.12)  LDD1583  [12]
 LDCM0380  CL110 HEK-293T C643(1.26); C630(1.07)  LDD1584  [12]
 LDCM0381  CL111 HEK-293T C643(1.06)  LDD1585  [12]
 LDCM0382  CL112 HEK-293T C643(1.11); C630(0.99)  LDD1586  [12]
 LDCM0383  CL113 HEK-293T C643(0.95); C630(1.04)  LDD1587  [12]
 LDCM0384  CL114 HEK-293T C643(1.06); C630(1.12)  LDD1588  [12]
 LDCM0385  CL115 HEK-293T C643(0.95)  LDD1589  [12]
 LDCM0386  CL116 HEK-293T C643(0.90); C630(1.05)  LDD1590  [12]
 LDCM0387  CL117 HEK-293T C643(0.95); C630(0.96)  LDD1591  [12]
 LDCM0388  CL118 HEK-293T C643(0.99); C630(0.98)  LDD1592  [12]
 LDCM0389  CL119 HEK-293T C643(0.96)  LDD1593  [12]
 LDCM0390  CL12 HEK-293T C643(1.16); C630(1.06); C320(1.17)  LDD1594  [12]
 LDCM0391  CL120 HEK-293T C643(0.92); C630(1.06)  LDD1595  [12]
 LDCM0392  CL121 HEK-293T C643(0.93); C630(1.19)  LDD1596  [12]
 LDCM0393  CL122 HEK-293T C643(0.94); C630(1.00)  LDD1597  [12]
 LDCM0394  CL123 HEK-293T C643(0.90)  LDD1598  [12]
 LDCM0395  CL124 HEK-293T C643(0.93); C630(1.00)  LDD1599  [12]
 LDCM0396  CL125 HEK-293T C643(0.90); C630(1.07)  LDD1600  [12]
 LDCM0397  CL126 HEK-293T C643(0.97); C630(1.10)  LDD1601  [12]
 LDCM0398  CL127 HEK-293T C643(0.97)  LDD1602  [12]
 LDCM0399  CL128 HEK-293T C643(0.97); C630(1.07)  LDD1603  [12]
 LDCM0400  CL13 HEK-293T C643(1.03); C630(1.12)  LDD1604  [12]
 LDCM0401  CL14 HEK-293T C643(1.04); C630(1.01)  LDD1605  [12]
 LDCM0402  CL15 HEK-293T C643(0.97)  LDD1606  [12]
 LDCM0403  CL16 HEK-293T C643(0.93); C630(1.07)  LDD1607  [12]
 LDCM0404  CL17 HEK-293T C643(1.25); C630(1.05)  LDD1608  [12]
 LDCM0405  CL18 HEK-293T C643(0.92); C630(1.17)  LDD1609  [12]
 LDCM0406  CL19 HEK-293T C643(0.97); C630(1.16)  LDD1610  [12]
 LDCM0407  CL2 HEK-293T C643(1.06); C630(1.01)  LDD1611  [12]
 LDCM0408  CL20 HEK-293T C643(1.02); C630(1.17); C320(0.85)  LDD1612  [12]
 LDCM0409  CL21 HEK-293T C643(1.10); C320(0.95)  LDD1613  [12]
 LDCM0410  CL22 HEK-293T C643(1.05); C630(1.06)  LDD1614  [12]
 LDCM0411  CL23 HEK-293T C643(1.08); C630(1.10)  LDD1615  [12]
 LDCM0412  CL24 HEK-293T C643(1.10); C630(1.13); C320(1.23)  LDD1616  [12]
 LDCM0413  CL25 HEK-293T C643(0.86); C630(1.05)  LDD1617  [12]
 LDCM0414  CL26 HEK-293T C643(1.00); C630(0.96)  LDD1618  [12]
 LDCM0415  CL27 HEK-293T C643(0.96)  LDD1619  [12]
 LDCM0416  CL28 HEK-293T C643(0.98); C630(1.00)  LDD1620  [12]
 LDCM0417  CL29 HEK-293T C643(1.03); C630(1.30)  LDD1621  [12]
 LDCM0418  CL3 HEK-293T C643(0.92)  LDD1622  [12]
 LDCM0419  CL30 HEK-293T C643(0.99); C630(1.15)  LDD1623  [12]
 LDCM0420  CL31 HEK-293T C643(1.06); C630(1.11)  LDD1624  [12]
 LDCM0421  CL32 HEK-293T C643(1.06); C630(1.13); C320(0.95)  LDD1625  [12]
 LDCM0422  CL33 HEK-293T C643(1.04); C320(0.99)  LDD1626  [12]
 LDCM0423  CL34 HEK-293T C643(1.14); C630(1.05)  LDD1627  [12]
 LDCM0424  CL35 HEK-293T C643(1.16); C630(1.18)  LDD1628  [12]
 LDCM0425  CL36 HEK-293T C643(1.16); C630(1.03); C320(1.21)  LDD1629  [12]
 LDCM0426  CL37 HEK-293T C643(0.97); C630(0.98)  LDD1630  [12]
 LDCM0428  CL39 HEK-293T C643(0.91)  LDD1632  [12]
 LDCM0429  CL4 HEK-293T C643(0.91); C630(0.95)  LDD1633  [12]
 LDCM0430  CL40 HEK-293T C643(0.93); C630(0.96)  LDD1634  [12]
 LDCM0431  CL41 HEK-293T C643(1.24); C630(1.07)  LDD1635  [12]
 LDCM0432  CL42 HEK-293T C643(1.02); C630(1.16)  LDD1636  [12]
 LDCM0433  CL43 HEK-293T C643(1.02); C630(1.19)  LDD1637  [12]
 LDCM0434  CL44 HEK-293T C643(1.12); C630(0.98); C320(0.95)  LDD1638  [12]
 LDCM0435  CL45 HEK-293T C643(1.21); C320(0.94)  LDD1639  [12]
 LDCM0436  CL46 HEK-293T C643(1.13); C630(0.97)  LDD1640  [12]
 LDCM0437  CL47 HEK-293T C643(1.24); C630(1.17)  LDD1641  [12]
 LDCM0438  CL48 HEK-293T C643(1.17); C630(1.08); C320(1.17)  LDD1642  [12]
 LDCM0439  CL49 HEK-293T C643(0.94); C630(1.06)  LDD1643  [12]
 LDCM0440  CL5 HEK-293T C643(1.03); C630(1.08)  LDD1644  [12]
 LDCM0441  CL50 HEK-293T C643(1.05); C630(1.04)  LDD1645  [12]
 LDCM0443  CL52 HEK-293T C643(0.92); C630(0.96)  LDD1646  [12]
 LDCM0444  CL53 HEK-293T C643(1.21); C630(1.26)  LDD1647  [12]
 LDCM0445  CL54 HEK-293T C643(0.85); C630(1.17)  LDD1648  [12]
 LDCM0446  CL55 HEK-293T C643(0.99); C630(1.09)  LDD1649  [12]
 LDCM0447  CL56 HEK-293T C643(1.09); C630(1.05); C320(0.94)  LDD1650  [12]
 LDCM0448  CL57 HEK-293T C643(1.03); C320(0.95)  LDD1651  [12]
 LDCM0449  CL58 HEK-293T C643(1.09); C630(1.03)  LDD1652  [12]
 LDCM0450  CL59 HEK-293T C643(1.12); C630(1.17)  LDD1653  [12]
 LDCM0451  CL6 HEK-293T C643(0.98); C630(1.06)  LDD1654  [12]
 LDCM0452  CL60 HEK-293T C643(1.12); C630(1.11); C320(1.28)  LDD1655  [12]
 LDCM0453  CL61 HEK-293T C643(0.94); C630(0.98)  LDD1656  [12]
 LDCM0454  CL62 HEK-293T C643(1.03); C630(1.02)  LDD1657  [12]
 LDCM0455  CL63 HEK-293T C643(0.97)  LDD1658  [12]
 LDCM0456  CL64 HEK-293T C643(1.00); C630(1.05)  LDD1659  [12]
 LDCM0457  CL65 HEK-293T C643(1.02); C630(1.11)  LDD1660  [12]
 LDCM0458  CL66 HEK-293T C643(0.97); C630(1.13)  LDD1661  [12]
 LDCM0459  CL67 HEK-293T C643(1.00); C630(1.16)  LDD1662  [12]
 LDCM0460  CL68 HEK-293T C643(1.00); C630(1.13); C320(0.87)  LDD1663  [12]
 LDCM0461  CL69 HEK-293T C643(1.04); C320(0.98)  LDD1664  [12]
 LDCM0462  CL7 HEK-293T C643(0.92); C630(1.24)  LDD1665  [12]
 LDCM0463  CL70 HEK-293T C643(1.13); C630(1.06)  LDD1666  [12]
 LDCM0464  CL71 HEK-293T C643(1.17); C630(1.01)  LDD1667  [12]
 LDCM0465  CL72 HEK-293T C643(1.09); C630(1.17); C320(1.02)  LDD1668  [12]
 LDCM0466  CL73 HEK-293T C643(0.98); C630(1.08)  LDD1669  [12]
 LDCM0467  CL74 HEK-293T C643(1.03); C630(1.06)  LDD1670  [12]
 LDCM0469  CL76 HEK-293T C643(0.94); C630(1.03)  LDD1672  [12]
 LDCM0470  CL77 HEK-293T C643(1.16); C630(1.13)  LDD1673  [12]
 LDCM0471  CL78 HEK-293T C643(1.00); C630(0.97)  LDD1674  [12]
 LDCM0472  CL79 HEK-293T C643(0.95); C630(1.30)  LDD1675  [12]
 LDCM0473  CL8 HEK-293T C643(1.03); C630(1.10); C320(0.66)  LDD1676  [12]
 LDCM0474  CL80 HEK-293T C643(0.97); C630(1.16); C320(0.90)  LDD1677  [12]
 LDCM0475  CL81 HEK-293T C643(1.03); C320(1.08)  LDD1678  [12]
 LDCM0476  CL82 HEK-293T C643(1.06); C630(1.04)  LDD1679  [12]
 LDCM0477  CL83 HEK-293T C643(1.12); C630(1.21)  LDD1680  [12]
 LDCM0478  CL84 HEK-293T C643(1.10); C630(0.99); C320(1.01)  LDD1681  [12]
 LDCM0479  CL85 HEK-293T C643(0.94); C630(0.93)  LDD1682  [12]
 LDCM0480  CL86 HEK-293T C643(0.95); C630(1.00)  LDD1683  [12]
 LDCM0481  CL87 HEK-293T C643(1.00)  LDD1684  [12]
 LDCM0482  CL88 HEK-293T C643(0.97); C630(1.12)  LDD1685  [12]
 LDCM0483  CL89 HEK-293T C643(1.07); C630(1.08)  LDD1686  [12]
 LDCM0484  CL9 HEK-293T C643(1.04); C320(1.00)  LDD1687  [12]
 LDCM0485  CL90 HEK-293T C643(0.85); C630(1.15)  LDD1688  [12]
 LDCM0486  CL91 HEK-293T C643(0.95); C630(1.21)  LDD1689  [12]
 LDCM0487  CL92 HEK-293T C643(0.96); C630(1.08); C320(0.80)  LDD1690  [12]
 LDCM0488  CL93 HEK-293T C643(1.07); C320(1.02)  LDD1691  [12]
 LDCM0489  CL94 HEK-293T C643(1.13); C630(1.12)  LDD1692  [12]
 LDCM0490  CL95 HEK-293T C643(1.37); C630(1.43)  LDD1693  [12]
 LDCM0491  CL96 HEK-293T C643(1.06); C630(1.14); C320(0.92)  LDD1694  [12]
 LDCM0492  CL97 HEK-293T C643(0.95); C630(0.93)  LDD1695  [12]
 LDCM0493  CL98 HEK-293T C643(1.02); C630(1.04)  LDD1696  [12]
 LDCM0494  CL99 HEK-293T C643(1.03)  LDD1697  [12]
 LDCM0097  Dasatinib K562 N.A.  LDD0364  [10]
 LDCM0017  DFG-out-2 A431 71.00  LDD0075  [11]
 LDCM0495  E2913 HEK-293T C643(0.98)  LDD1698  [12]
 LDCM0468  Fragment33 HEK-293T C643(0.91)  LDD1671  [12]
 LDCM0427  Fragment51 HEK-293T C643(0.99); C630(0.89)  LDD1631  [12]
 LDCM0022  KB02 HEK-293T C643(0.89)  LDD1492  [12]
 LDCM0023  KB03 HEK-293T C643(0.97)  LDD1497  [12]
 LDCM0024  KB05 MELHO C320(1.91)  LDD3318  [3]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C643(0.49)  LDD2100  [4]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C643(0.81)  LDD2108  [4]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C643(0.83)  LDD2114  [4]
 LDCM0016  Ranjitkar_cp1 A431 35.00  LDD0074  [11]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ephrin type-A receptor 5 (EPHA5) Tyr protein kinase family P54756
Ephrin type-A receptor 6 (EPHA6) Tyr protein kinase family Q9UF33
Ephrin type-A receptor 7 (EPHA7) Tyr protein kinase family Q15375
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ephrin-B2 (EFNB2) Ephrin family P52799
Erythropoietin (EPO) EPO/TPO family P01588

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
Dasatinib Small molecular drug DB01254
Fostamatinib Small molecular drug DB12010
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Kd019 Small molecular drug D06WRF
Investigative
Click To Hide/Show 13 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ephb4-131 Antibody D0Q6GK
Pmid19788238c66 Small molecular drug D05FXD
Pmid23489211c20 Small molecular drug D0X8BU
Tesevatinib Small molecular drug DB11973
Tg-100435 Small molecular drug D0H1OK
3-({4-[(5-chloro-13-benzodioxol-4-yl)Amino]Pyrimidin-2-yl}Amino)Benzamide . DB07256
3-({4-[(5-chloro-13-benzodioxol-4-yl)Amino]Pyrimidin-2-yl}Amino)Benzenesulfonamide . DB07252
N'-(3-chloro-4-methoxy-phenyl)-n-(345-trimethoxyphenyl)-135-triazine-24-diamine . DB07251
N'-(5-chloro-13-benzodioxol-4-yl)-n-(3-methylsulfonylphenyl)Pyrimidine-24-diamine . DB07253
N'-(5-chloro-13-benzodioxol-4-yl)-n-(3-morpholin-4-ylphenyl)Pyrimidine-24-diamine . DB07255
N'-(5-chloro-13-benzodioxol-4-yl)-n-(345- Trimethoxyphenyl)Pyrimidine-24-diamine . DB07250
N-(5-chloro-13-benzodioxol-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)Quinazolin-4-amine . DB07249
N-[3-[[4-[(5-chloro-13-benzodioxol-4-yl)Amino]Pyrimidin-2-yl]Amino]Phenyl]Methanesulfonamide . DB07254

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
3 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
4 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
5 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
6 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
7 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
8 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.
9 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264
10 Streamlined Target Deconvolution Approach Utilizing a Single Photoreactive Chloroalkane Capture Tag. ACS Chem Biol. 2021 Feb 19;16(2):404-413. doi: 10.1021/acschembio.0c00987. Epub 2021 Feb 5.
11 Affinity-based probes based on type II kinase inhibitors. J Am Chem Soc. 2012 Nov 21;134(46):19017-25. doi: 10.1021/ja306035v. Epub 2012 Nov 6.
12 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