Details of the Target

General Information of Target

Target ID LDTP03692
Target Name Bifunctional epoxide hydrolase 2 (EPHX2)
Gene Name EPHX2
Gene ID 2053
Synonyms
Bifunctional epoxide hydrolase 2 [Includes: Cytosolic epoxide hydrolase 2; CEH; EC 3.3.2.10; Epoxide hydratase; Soluble epoxide hydrolase; SEH; Lipid-phosphate phosphatase; EC 3.1.3.76)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTLRAAVFDLDGVLALPAVFGVLGRTEEALALPRGLLNDAFQKGGPEGATTRLMKGEITL
SQWIPLMEENCRKCSETAKVCLPKNFSIKEIFDKAISARKINRPMLQAALMLRKKGFTTA
ILTNTWLDDRAERDGLAQLMCELKMHFDFLIESCQVGMVKPEPQIYKFLLDTLKASPSEV
VFLDDIGANLKPARDLGMVTILVQDTDTALKELEKVTGIQLLNTPAPLPTSCNPSDMSHG
YVTVKPRVRLHFVELGSGPAVCLCHGFPESWYSWRYQIPALAQAGYRVLAMDMKGYGESS
APPEIEEYCMEVLCKEMVTFLDKLGLSQAVFIGHDWGGMLVWYMALFYPERVRAVASLNT
PFIPANPNMSPLESIKANPVFDYQLYFQEPGVAEAELEQNLSRTFKSLFRASDESVLSMH
KVCEAGGLFVNSPEEPSLSRMVTEEEIQFYVQQFKKSGFRGPLNWYRNMERNWKWACKSL
GRKILIPALMVTAEKDFVLVPQMSQHMEDWIPHLKRGHIEDCGHWTQMDKPTEVNQILIK
WLDSDARNPPVVSKM
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
AB hydrolase superfamily, Epoxide hydrolase family
Subcellular location
Cytoplasm
Function
Bifunctional enzyme. The C-terminal domain has epoxide hydrolase activity and acts on epoxides (alkene oxides, oxiranes) and arene oxides. Plays a role in xenobiotic metabolism by degrading potentially toxic epoxides. Also determines steady-state levels of physiological mediators.; Bifunctional enzyme. The N-terminal domain has lipid phosphatase activity, with the highest activity towards threo-9,10-phosphonooxy-hydroxy-octadecanoic acid, followed by erythro-9,10-phosphonooxy-hydroxy-octadecanoic acid, 12-phosphonooxy-octadec-9Z-enoic acid and 12-phosphonooxy-octadec-9E-enoic acid. Has phosphatase activity toward lyso-glycerophospholipids with also some lower activity toward lysolipids of sphingolipid and isoprenoid phosphates.
TTD ID
T35734
Uniprot ID
P34913
DrugMap ID
TT7WVHI
Ensemble ID
ENST00000380476.7
HGNC ID
HGNC:3402
ChEMBL ID
CHEMBL2409

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
COLO678 SNV: p.P65T DBIA    Probe Info 
IGROV1 SNV: p.M339V .
JURKAT SNV: p.V416A .
LS123 SNV: p.P229L DBIA    Probe Info 
MEWO SNV: p.V500A .
MOLT4 SNV: p.C309S IA-alkyne    Probe Info 
NCIH2286 Deletion: p.D134WfsTer8 .
NCIH23 SNV: p.K245N .
SW403 SNV: p.E47Ter .
U87MG SNV: p.S544Y .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 6 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C88(1.78); C423(1.80)  LDD3335  [1]
4-Iodoacetamidophenylacetylene
 Probe Info  		C141(0.00); C71(0.00); C522(0.00); C74(0.00)  LDD0038  [2]
IA-alkyne
 Probe Info  		C141(0.00); C71(0.00); C232(0.00); C74(0.00)  LDD0036  [2]
IPIAA_L
 Probe Info  		C232(0.00); C423(0.00)  LDD0031  [3]
Lodoacetamide azide
 Probe Info  		C141(0.00); C71(0.00); C423(0.00); C522(0.00)  LDD0037  [2]
NAIA_5
 Probe Info  		N.A.  LDD2224  [4]
PAL-AfBPP Probe
Click To Hide/Show 17 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C027
 Probe Info  		21.86  LDD1733  [5]
C149
 Probe Info  		6.19  LDD1830  [5]
C158
 Probe Info  		8.88  LDD1838  [5]
C164
 Probe Info  		5.90  LDD1844  [5]
C205
 Probe Info  		7.41  LDD1880  [5]
C222
 Probe Info  		12.91  LDD1896  [5]
C232
 Probe Info  		45.57  LDD1905  [5]
C234
 Probe Info  		16.22  LDD1907  [5]
C237
 Probe Info  		11.00  LDD1910  [5]
C331
 Probe Info  		6.59  LDD1994  [5]
C361
 Probe Info  		33.59  LDD2022  [5]
C387
 Probe Info  		12.21  LDD2046  [5]
FFF probe13
 Probe Info  		20.00  LDD0476  [6]
FFF probe3
 Probe Info  		9.43  LDD0465  [6]
DFG-out-3
 Probe Info  		2.00  LDD0074  [7]
AEA-DA
 Probe Info  		20.00  LDD0146  [8]
OEA-DA
 Probe Info  		20.00  LDD0046  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C423(1.07); C141(0.96)  LDD1507  [10]
 LDCM0215  AC10 HEK-293T C423(1.14); C141(0.91)  LDD1508  [10]
 LDCM0226  AC11 HEK-293T C423(0.89); C141(1.11); C71(0.98)  LDD1509  [10]
 LDCM0237  AC12 HEK-293T C423(1.09); C141(1.00); C71(0.84)  LDD1510  [10]
 LDCM0259  AC14 HEK-293T C423(0.98); C141(0.89); C71(0.91)  LDD1512  [10]
 LDCM0270  AC15 HEK-293T C423(1.04); C141(0.98)  LDD1513  [10]
 LDCM0276  AC17 HEK-293T C423(1.03); C141(0.94)  LDD1515  [10]
 LDCM0277  AC18 HEK-293T C423(0.92); C141(1.02)  LDD1516  [10]
 LDCM0278  AC19 HEK-293T C423(0.89); C141(0.99); C71(0.62)  LDD1517  [10]
 LDCM0279  AC2 HEK-293T C423(0.91); C141(1.03)  LDD1518  [10]
 LDCM0280  AC20 HEK-293T C423(1.07); C141(1.03); C71(1.03)  LDD1519  [10]
 LDCM0281  AC21 HEK-293T C423(0.88); C141(1.00); C71(0.62)  LDD1520  [10]
 LDCM0282  AC22 HEK-293T C423(0.86); C141(1.01); C71(0.92)  LDD1521  [10]
 LDCM0283  AC23 HEK-293T C423(1.02); C141(0.95)  LDD1522  [10]
 LDCM0284  AC24 HEK-293T C423(0.82); C141(1.00); C71(1.15)  LDD1523  [10]
 LDCM0285  AC25 HEK-293T C423(1.02); C141(0.95)  LDD1524  [10]
 LDCM0286  AC26 HEK-293T C423(1.01); C141(0.98)  LDD1525  [10]
 LDCM0287  AC27 HEK-293T C423(0.98); C141(1.04); C71(0.89)  LDD1526  [10]
 LDCM0288  AC28 HEK-293T C423(0.99); C141(0.98); C71(0.96)  LDD1527  [10]
 LDCM0289  AC29 HEK-293T C423(1.04); C141(1.00); C71(0.88)  LDD1528  [10]
 LDCM0290  AC3 HEK-293T C423(1.10); C141(1.02); C71(1.06)  LDD1529  [10]
 LDCM0291  AC30 HEK-293T C423(0.90); C141(0.92); C71(0.89)  LDD1530  [10]
 LDCM0292  AC31 HEK-293T C423(1.19); C141(1.01)  LDD1531  [10]
 LDCM0293  AC32 HEK-293T C423(0.85); C141(1.05); C71(1.05)  LDD1532  [10]
 LDCM0294  AC33 HEK-293T C423(1.04); C141(1.00)  LDD1533  [10]
 LDCM0295  AC34 HEK-293T C423(0.90); C141(1.00)  LDD1534  [10]
 LDCM0296  AC35 HEK-293T C423(0.94); C141(1.05); C71(1.14)  LDD1535  [10]
 LDCM0297  AC36 HEK-293T C423(1.17); C141(1.01); C71(1.26)  LDD1536  [10]
 LDCM0298  AC37 HEK-293T C423(0.98); C141(1.03); C71(0.88)  LDD1537  [10]
 LDCM0299  AC38 HEK-293T C423(0.90); C141(0.94); C71(0.88)  LDD1538  [10]
 LDCM0300  AC39 HEK-293T C423(1.09); C141(0.93)  LDD1539  [10]
 LDCM0301  AC4 HEK-293T C423(1.17); C141(1.02); C71(1.25)  LDD1540  [10]
 LDCM0302  AC40 HEK-293T C423(1.09); C141(1.04); C71(1.01)  LDD1541  [10]
 LDCM0303  AC41 HEK-293T C423(1.22); C141(0.97)  LDD1542  [10]
 LDCM0304  AC42 HEK-293T C423(0.85); C141(0.97)  LDD1543  [10]
 LDCM0305  AC43 HEK-293T C423(1.04); C141(1.16); C71(0.99)  LDD1544  [10]
 LDCM0306  AC44 HEK-293T C423(1.09); C141(1.03); C71(0.91)  LDD1545  [10]
 LDCM0307  AC45 HEK-293T C423(0.93); C141(0.98); C71(0.63)  LDD1546  [10]
 LDCM0308  AC46 HEK-293T C423(0.84); C141(0.94); C71(1.00)  LDD1547  [10]
 LDCM0309  AC47 HEK-293T C423(1.13); C141(0.97)  LDD1548  [10]
 LDCM0310  AC48 HEK-293T C423(0.93); C141(0.97); C71(1.16)  LDD1549  [10]
 LDCM0311  AC49 HEK-293T C423(1.05); C141(1.03)  LDD1550  [10]
 LDCM0312  AC5 HEK-293T C423(0.96); C141(1.03); C71(0.77)  LDD1551  [10]
 LDCM0313  AC50 HEK-293T C423(0.92); C141(0.97)  LDD1552  [10]
 LDCM0314  AC51 HEK-293T C423(1.01); C141(1.18); C71(1.02)  LDD1553  [10]
 LDCM0315  AC52 HEK-293T C423(1.21); C141(1.03); C71(1.12)  LDD1554  [10]
 LDCM0316  AC53 HEK-293T C423(1.27); C141(0.93); C71(0.65)  LDD1555  [10]
 LDCM0317  AC54 HEK-293T C423(0.91); C141(1.00); C71(0.89)  LDD1556  [10]
 LDCM0318  AC55 HEK-293T C423(1.13); C141(1.05)  LDD1557  [10]
 LDCM0319  AC56 HEK-293T C423(0.89); C141(0.99); C71(0.97)  LDD1558  [10]
 LDCM0320  AC57 HEK-293T C423(1.07); C141(1.07)  LDD1559  [10]
 LDCM0321  AC58 HEK-293T C423(0.98); C141(1.00)  LDD1560  [10]
 LDCM0322  AC59 HEK-293T C423(1.13); C141(1.11); C71(0.88)  LDD1561  [10]
 LDCM0323  AC6 HEK-293T C423(0.87); C141(0.90); C71(1.07)  LDD1562  [10]
 LDCM0324  AC60 HEK-293T C423(1.12); C141(1.02); C71(1.50)  LDD1563  [10]
 LDCM0325  AC61 HEK-293T C423(0.94); C141(0.97); C71(0.61)  LDD1564  [10]
 LDCM0326  AC62 HEK-293T C423(0.86); C141(1.04); C71(1.06)  LDD1565  [10]
 LDCM0327  AC63 HEK-293T C423(1.21); C141(0.96)  LDD1566  [10]
 LDCM0328  AC64 HEK-293T C423(1.13); C141(1.11); C71(1.16)  LDD1567  [10]
 LDCM0334  AC7 HEK-293T C423(1.28); C141(0.96)  LDD1568  [10]
 LDCM0345  AC8 HEK-293T C423(0.95); C141(1.05); C71(1.05)  LDD1569  [10]
 LDCM0248  AKOS034007472 HEK-293T C423(1.10); C141(1.09); C71(0.55)  LDD1511  [10]
 LDCM0356  AKOS034007680 HEK-293T C423(1.03); C141(0.97)  LDD1570  [10]
 LDCM0275  AKOS034007705 HEK-293T C423(0.89); C141(0.97); C71(1.16)  LDD1514  [10]
 LDCM0367  CL1 HEK-293T C423(1.08); C141(1.02); C71(1.22)  LDD1571  [10]
 LDCM0368  CL10 HEK-293T C423(0.80); C141(0.79); C71(0.80)  LDD1572  [10]
 LDCM0369  CL100 HEK-293T C423(0.98); C141(0.99)  LDD1573  [10]
 LDCM0370  CL101 HEK-293T C423(1.03); C141(1.02); C71(0.97)  LDD1574  [10]
 LDCM0371  CL102 HEK-293T C423(0.98); C141(0.97); C71(1.13)  LDD1575  [10]
 LDCM0372  CL103 HEK-293T C423(1.03); C141(1.04)  LDD1576  [10]
 LDCM0373  CL104 HEK-293T C423(0.98); C141(0.93)  LDD1577  [10]
 LDCM0374  CL105 HEK-293T C423(0.98); C141(1.01); C71(0.97)  LDD1578  [10]
 LDCM0375  CL106 HEK-293T C423(0.91); C141(0.91); C71(0.70)  LDD1579  [10]
 LDCM0376  CL107 HEK-293T C423(0.96); C141(1.02)  LDD1580  [10]
 LDCM0377  CL108 HEK-293T C423(1.07); C141(0.98)  LDD1581  [10]
 LDCM0378  CL109 HEK-293T C423(1.02); C141(1.03); C71(1.19)  LDD1582  [10]
 LDCM0379  CL11 HEK-293T C423(1.06); C141(0.91)  LDD1583  [10]
 LDCM0380  CL110 HEK-293T C423(1.00); C141(0.89); C71(0.77)  LDD1584  [10]
 LDCM0381  CL111 HEK-293T C423(1.16); C141(0.94)  LDD1585  [10]
 LDCM0382  CL112 HEK-293T C423(1.05); C141(0.87)  LDD1586  [10]
 LDCM0383  CL113 HEK-293T C423(1.17); C141(1.06); C71(0.95)  LDD1587  [10]
 LDCM0384  CL114 HEK-293T C423(0.81); C141(0.88); C71(0.77)  LDD1588  [10]
 LDCM0385  CL115 HEK-293T C423(1.04); C141(1.08)  LDD1589  [10]
 LDCM0386  CL116 HEK-293T C423(1.04); C141(0.92)  LDD1590  [10]
 LDCM0387  CL117 HEK-293T C423(1.06); C141(1.01); C71(1.33)  LDD1591  [10]
 LDCM0388  CL118 HEK-293T C423(0.95); C141(1.07); C71(0.68)  LDD1592  [10]
 LDCM0389  CL119 HEK-293T C423(0.99); C141(1.06)  LDD1593  [10]
 LDCM0390  CL12 HEK-293T C423(1.07); C141(1.14); C71(1.38)  LDD1594  [10]
 LDCM0391  CL120 HEK-293T C423(1.14); C141(1.03)  LDD1595  [10]
 LDCM0392  CL121 HEK-293T C423(0.91); C141(1.01); C71(1.25)  LDD1596  [10]
 LDCM0393  CL122 HEK-293T C423(0.98); C141(1.10); C71(0.87)  LDD1597  [10]
 LDCM0394  CL123 HEK-293T C423(1.05); C141(0.99)  LDD1598  [10]
 LDCM0395  CL124 HEK-293T C423(0.97); C141(0.98)  LDD1599  [10]
 LDCM0396  CL125 HEK-293T C423(0.96); C141(1.03); C71(1.14)  LDD1600  [10]
 LDCM0397  CL126 HEK-293T C423(0.99); C141(0.98); C71(0.93)  LDD1601  [10]
 LDCM0398  CL127 HEK-293T C423(0.96); C141(1.03)  LDD1602  [10]
 LDCM0399  CL128 HEK-293T C423(1.12); C141(0.93)  LDD1603  [10]
 LDCM0400  CL13 HEK-293T C423(1.04); C141(0.95); C71(1.50)  LDD1604  [10]
 LDCM0401  CL14 HEK-293T C423(1.03); C141(0.98); C71(0.94)  LDD1605  [10]
 LDCM0402  CL15 HEK-293T C423(0.95); C141(0.96)  LDD1606  [10]
 LDCM0403  CL16 HEK-293T C423(1.20); C141(1.03)  LDD1607  [10]
 LDCM0404  CL17 HEK-293T C423(0.91); C141(0.93)  LDD1608  [10]
 LDCM0405  CL18 HEK-293T C423(0.96); C141(0.94)  LDD1609  [10]
 LDCM0406  CL19 HEK-293T C423(1.05); C141(1.19); C71(1.24)  LDD1610  [10]
 LDCM0407  CL2 HEK-293T C423(0.87); C141(1.10); C71(0.98)  LDD1611  [10]
 LDCM0408  CL20 HEK-293T C423(1.14); C141(1.15); C71(0.89)  LDD1612  [10]
 LDCM0409  CL21 HEK-293T C423(1.24); C141(1.03); C71(0.62)  LDD1613  [10]
 LDCM0410  CL22 HEK-293T C423(1.17); C141(0.99); C71(0.79)  LDD1614  [10]
 LDCM0411  CL23 HEK-293T C423(1.19); C141(0.96)  LDD1615  [10]
 LDCM0412  CL24 HEK-293T C423(0.99); C141(1.20); C71(0.98)  LDD1616  [10]
 LDCM0413  CL25 HEK-293T C423(1.09); C141(0.96); C71(1.19)  LDD1617  [10]
 LDCM0414  CL26 HEK-293T C423(0.98); C141(0.94); C71(1.01)  LDD1618  [10]
 LDCM0415  CL27 HEK-293T C423(1.07); C141(1.09)  LDD1619  [10]
 LDCM0416  CL28 HEK-293T C423(1.16); C141(0.87)  LDD1620  [10]
 LDCM0417  CL29 HEK-293T C423(1.20); C141(0.98)  LDD1621  [10]
 LDCM0418  CL3 HEK-293T C423(1.12); C141(1.20)  LDD1622  [10]
 LDCM0419  CL30 HEK-293T C423(0.97); C141(1.08)  LDD1623  [10]
 LDCM0420  CL31 HEK-293T C423(1.18); C141(1.11); C71(1.09)  LDD1624  [10]
 LDCM0421  CL32 HEK-293T C423(1.09); C141(1.06); C71(1.15)  LDD1625  [10]
 LDCM0422  CL33 HEK-293T C423(1.11); C141(0.89); C71(0.39)  LDD1626  [10]
 LDCM0423  CL34 HEK-293T C423(1.09); C141(0.90); C71(0.66)  LDD1627  [10]
 LDCM0424  CL35 HEK-293T C423(1.18); C141(1.02)  LDD1628  [10]
 LDCM0425  CL36 HEK-293T C423(0.89); C141(1.17); C71(0.81)  LDD1629  [10]
 LDCM0426  CL37 HEK-293T C423(0.99); C141(0.99); C71(1.12)  LDD1630  [10]
 LDCM0428  CL39 HEK-293T C423(1.08); C141(1.03)  LDD1632  [10]
 LDCM0429  CL4 HEK-293T C423(1.33); C141(0.96)  LDD1633  [10]
 LDCM0430  CL40 HEK-293T C423(1.06); C141(0.96)  LDD1634  [10]
 LDCM0431  CL41 HEK-293T C423(1.05); C141(0.91)  LDD1635  [10]
 LDCM0432  CL42 HEK-293T C423(1.08); C141(1.00)  LDD1636  [10]
 LDCM0433  CL43 HEK-293T C423(1.35); C141(1.08); C71(1.01)  LDD1637  [10]
 LDCM0434  CL44 HEK-293T C423(1.16); C141(1.02); C71(0.84)  LDD1638  [10]
 LDCM0435  CL45 HEK-293T C423(1.14); C141(0.47); C71(0.66)  LDD1639  [10]
 LDCM0436  CL46 HEK-293T C423(1.01); C141(0.93); C71(0.63)  LDD1640  [10]
 LDCM0437  CL47 HEK-293T C423(1.08); C141(1.03)  LDD1641  [10]
 LDCM0438  CL48 HEK-293T C423(0.91); C141(1.09); C71(1.16)  LDD1642  [10]
 LDCM0439  CL49 HEK-293T C423(1.02); C141(1.10); C71(1.08)  LDD1643  [10]
 LDCM0440  CL5 HEK-293T C423(1.11); C141(1.09)  LDD1644  [10]
 LDCM0441  CL50 HEK-293T C423(1.18); C141(1.09); C71(0.88)  LDD1645  [10]
 LDCM0443  CL52 HEK-293T C423(1.03); C141(0.99)  LDD1646  [10]
 LDCM0444  CL53 HEK-293T C423(0.88); C141(0.94)  LDD1647  [10]
 LDCM0445  CL54 HEK-293T C423(0.98); C141(0.84)  LDD1648  [10]
 LDCM0446  CL55 HEK-293T C423(1.06); C141(1.23); C71(1.07)  LDD1649  [10]
 LDCM0447  CL56 HEK-293T C423(1.08); C141(1.10); C71(1.07)  LDD1650  [10]
 LDCM0448  CL57 HEK-293T C423(1.16); C141(0.95); C71(0.79)  LDD1651  [10]
 LDCM0449  CL58 HEK-293T C423(0.93); C141(0.84); C71(1.08)  LDD1652  [10]
 LDCM0450  CL59 HEK-293T C423(1.06); C141(0.94)  LDD1653  [10]
 LDCM0451  CL6 HEK-293T C423(1.11); C141(0.88)  LDD1654  [10]
 LDCM0452  CL60 HEK-293T C423(1.08); C141(1.12); C71(0.99)  LDD1655  [10]
 LDCM0453  CL61 HEK-293T C423(1.08); C141(1.09); C71(1.20)  LDD1656  [10]
 LDCM0454  CL62 HEK-293T C423(0.97); C141(1.00); C71(1.15)  LDD1657  [10]
 LDCM0455  CL63 HEK-293T C423(0.99); C141(1.09)  LDD1658  [10]
 LDCM0456  CL64 HEK-293T C423(1.13); C141(0.86)  LDD1659  [10]
 LDCM0457  CL65 HEK-293T C423(1.09); C141(1.01)  LDD1660  [10]
 LDCM0458  CL66 HEK-293T C423(1.15); C141(0.91)  LDD1661  [10]
 LDCM0459  CL67 HEK-293T C423(1.12); C141(1.20); C71(1.04)  LDD1662  [10]
 LDCM0460  CL68 HEK-293T C423(1.14); C141(1.11); C71(1.13)  LDD1663  [10]
 LDCM0461  CL69 HEK-293T C423(1.10); C141(1.13); C71(0.59)  LDD1664  [10]
 LDCM0462  CL7 HEK-293T C423(1.08); C141(1.22); C71(1.08)  LDD1665  [10]
 LDCM0463  CL70 HEK-293T C423(1.21); C141(1.11); C71(1.04)  LDD1666  [10]
 LDCM0464  CL71 HEK-293T C423(1.11); C141(1.02)  LDD1667  [10]
 LDCM0465  CL72 HEK-293T C423(0.97); C141(1.06); C71(1.03)  LDD1668  [10]
 LDCM0466  CL73 HEK-293T C423(0.88); C141(1.03); C71(1.48)  LDD1669  [10]
 LDCM0467  CL74 HEK-293T C423(0.94); C141(1.04); C71(0.94)  LDD1670  [10]
 LDCM0469  CL76 HEK-293T C423(1.08); C141(0.96)  LDD1672  [10]
 LDCM0470  CL77 HEK-293T C423(1.03); C141(0.95)  LDD1673  [10]
 LDCM0471  CL78 HEK-293T C423(0.94); C141(1.03)  LDD1674  [10]
 LDCM0472  CL79 HEK-293T C423(1.06); C141(1.16); C71(0.90)  LDD1675  [10]
 LDCM0473  CL8 HEK-293T C423(0.99); C141(1.04); C71(1.50)  LDD1676  [10]
 LDCM0474  CL80 HEK-293T C423(1.14); C141(1.12); C71(1.20)  LDD1677  [10]
 LDCM0475  CL81 HEK-293T C423(1.14); C141(1.17); C71(0.55)  LDD1678  [10]
 LDCM0476  CL82 HEK-293T C423(1.07); C141(1.09); C71(0.86)  LDD1679  [10]
 LDCM0477  CL83 HEK-293T C423(0.93); C141(1.11)  LDD1680  [10]
 LDCM0478  CL84 HEK-293T C423(0.96); C141(1.00); C71(1.36)  LDD1681  [10]
 LDCM0479  CL85 HEK-293T C423(0.99); C141(1.04); C71(1.16)  LDD1682  [10]
 LDCM0480  CL86 HEK-293T C423(1.08); C141(1.09); C71(0.76)  LDD1683  [10]
 LDCM0481  CL87 HEK-293T C423(1.24); C141(1.02)  LDD1684  [10]
 LDCM0482  CL88 HEK-293T C423(1.09); C141(0.91)  LDD1685  [10]
 LDCM0483  CL89 HEK-293T C423(1.12); C141(0.97)  LDD1686  [10]
 LDCM0484  CL9 HEK-293T C423(1.11); C141(1.13); C71(0.64)  LDD1687  [10]
 LDCM0485  CL90 HEK-293T C423(0.86); C141(0.82)  LDD1688  [10]
 LDCM0486  CL91 HEK-293T C423(1.07); C141(1.17); C71(1.00)  LDD1689  [10]
 LDCM0487  CL92 HEK-293T C423(1.16); C141(1.04); C71(0.86)  LDD1690  [10]
 LDCM0488  CL93 HEK-293T C423(0.93); C141(1.02); C71(0.28)  LDD1691  [10]
 LDCM0489  CL94 HEK-293T C423(0.86); C141(0.90); C71(1.19)  LDD1692  [10]
 LDCM0490  CL95 HEK-293T C423(0.92); C141(0.85)  LDD1693  [10]
 LDCM0491  CL96 HEK-293T C423(0.89); C141(1.00); C71(0.72)  LDD1694  [10]
 LDCM0492  CL97 HEK-293T C423(1.08); C141(0.96); C71(0.94)  LDD1695  [10]
 LDCM0493  CL98 HEK-293T C423(0.97); C141(1.00); C71(0.84)  LDD1696  [10]
 LDCM0494  CL99 HEK-293T C423(1.06); C141(0.95)  LDD1697  [10]
 LDCM0495  E2913 HEK-293T C423(1.19); C141(1.10)  LDD1698  [10]
 LDCM0082  FK866 A-549 20.00  LDD0146  [8]
 LDCM0573  Fragment11 Ramos C141(1.02)  LDD2190  [11]
 LDCM0576  Fragment14 Ramos C141(0.46)  LDD2193  [11]
 LDCM0468  Fragment33 HEK-293T C423(1.08); C141(1.01)  LDD1671  [10]
 LDCM0566  Fragment4 Ramos C141(0.93)  LDD2184  [11]
 LDCM0427  Fragment51 HEK-293T C423(1.13); C141(1.06); C71(1.03)  LDD1631  [10]
 LDCM0569  Fragment7 Ramos C141(1.18)  LDD2186  [11]
 LDCM0022  KB02 HEK-293T C423(1.01); C71(1.10)  LDD1492  [10]
 LDCM0023  KB03 HEK-293T C423(1.03); C71(0.92)  LDD1497  [10]
 LDCM0024  KB05 MONO-MAC-6 C88(1.78); C423(1.80)  LDD3335  [1]
 LDCM0016  Ranjitkar_cp1 A431 2.00  LDD0074  [7]
 LDCM0137  SR-4995 HEK-293T 20.00  LDD0334  [9]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ar9281 Small molecular drug D0KL3U
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gsk2256294 . D0A8KQ
Investigative
Click To Hide/Show 108 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,3-diphenylurea Small molecular drug D0X7IM
1-(1-adamantyl)-3-(1-propionylpiperidin-4-yl)Urea Small molecular drug D0U4KM
1-(1-propionylpiperidin-4-yl)-3-m-tolylurea Small molecular drug D0N1SE
1-(1-propionylpiperidin-4-yl)-3-o-tolylurea Small molecular drug D0P8MM
1-(1-propionylpiperidin-4-yl)-3-p-tolylurea Small molecular drug D0I4KB
1-(3-(3-morpholinopropoxy)Phenyl)-3-phenylurea Small molecular drug D02UJV
1-(3-chloro-phenyl)-3-(4-hydroxy-decyl)-urea Small molecular drug D06RJQ
1-(3-chloro-phenyl)-3-cyclohexyl-urea Small molecular drug D0B0ES
1-(4-(3-morpholinopropoxy)Phenyl)-3-phenylurea Small molecular drug D01OZF
1-adamantan-1-yl-3-((R)-1-phenyl-ethyl)-urea Small molecular drug D07HSQ
1-adamantan-1-yl-3-(1-benzyl-piperidin-4-yl)-urea Small molecular drug D0F3PF
1-adamantan-1-yl-3-(1-butyl-piperidin-4-yl)-urea Small molecular drug D0D3GF
1-adamantan-1-yl-3-(1-ethyl-piperidin-4-yl)-urea Small molecular drug D0XS3W
1-adamantan-1-yl-3-(1-propyl-piperidin-4-yl)-urea Small molecular drug D0IC8U
1-adamantan-1-yl-3-(2-heptyloxyethyl)Urea Small molecular drug D0YS1G
1-adamantan-1-yl-3-(2-hydroxy-phenyl)-urea Small molecular drug D08AZT
1-adamantan-1-yl-3-(2-hydroxyethyl)Urea Small molecular drug D0J0YB
1-adamantan-1-yl-3-(2-methoxy-phenyl)-urea Small molecular drug D09DPC
1-adamantan-1-yl-3-(3-hexyloxypropyl)Urea Small molecular drug D0VW6Y
1-adamantan-1-yl-3-(3-hydroxy-phenyl)-urea Small molecular drug D01JJV
1-adamantan-1-yl-3-(3-hydroxypropyl)Urea Small molecular drug D05MAT
1-adamantan-1-yl-3-(3-methoxy-phenyl)-urea Small molecular drug D0V8EQ
1-adamantan-1-yl-3-(4-hydroxy-decyl)-urea Small molecular drug D0T9ZN
1-adamantan-1-yl-3-(4-hydroxy-phenyl)-urea Small molecular drug D0Q8NE
1-adamantan-1-yl-3-(4-hydroxybutyl)Urea Small molecular drug D0F5XQ
1-adamantan-1-yl-3-(4-methoxy-phenyl)-urea Small molecular drug D04NJC
1-adamantan-1-yl-3-(4-pentyloxybutyl)Urea Small molecular drug D07TOI
1-adamantan-1-yl-3-(4-pentyloxycylclohexyl)Urea Small molecular drug D05MTA
1-adamantan-1-yl-3-(5-butoxypentyl)Urea Small molecular drug D0M0KA
1-adamantan-1-yl-3-(5-hydroxypentyl)Urea Small molecular drug D0UJ9V
1-adamantan-1-yl-3-(6-hydroxyhexyl)Urea Small molecular drug D0Z8RL
1-adamantan-1-yl-3-(6-propyloxyhexyl)Urea Small molecular drug D00RST
1-adamantan-1-yl-3-decyl-urea Small molecular drug D0XG0G
1-adamantan-1-yl-3-phenyl-urea Small molecular drug D0Z6SS
1-adamantan-1-yl-3-piperidin-4-yl-urea Small molecular drug D0J5KK
1-adamantan-1-yl-3-piperidin-4-ylmethyl-urea Small molecular drug D09VSL
1-adamantan-1-yl-3-[4-(4-fluorophenoxy)Butyl]Urea Small molecular drug D0A4VS
1-cycloheptyl-3-(1-propionylpiperidin-4-yl)Urea Small molecular drug D0F3VZ
1-cyclohexyl-3-(1-propionylpiperidin-4-yl)Urea Small molecular drug D01NFH
1-cyclohexyl-3-(4-methoxy-phenyl)-urea Small molecular drug D09FEC
1-cyclohexyl-3-phenethyl-urea Small molecular drug D08RPW
1-cyclohexyl-3-phenyl-urea Small molecular drug D0C5GW
1-octyl-3-(1-propionylpiperidin-4-yl)Urea Small molecular drug D04ARH
1-phenyl-3-(1-propionylpiperidin-4-yl)Urea Small molecular drug D0R6CW
12-(3-adamantan-1-yl-ureido)-dodeca Noic Acid Small molecular drug D0S0SH
12-(3-n-hexylureido)Dodec-8(Z)-enoic Acid Small molecular drug D08TWI
12-(3-n-pentylureidooxy)Dodec-8(Z)-enoic Acid Small molecular drug D0B0MU
13-(3-n-pentylthioureido)Tridec-8(Z)-enoic Acid Small molecular drug D0C8HN
13-(3-n-pentylureido)Tridec-5(Z)-enoic Acid Small molecular drug D0X1EG
13-(3-n-pentylureido)Tridec-8(E)-enoic Acid Small molecular drug D07UIO
13-(3-n-pentylureido)Tridec-8-ynoic Acid Small molecular drug D02CKF
13-(3-pentyluredo)Tridec-8(Z)-enoic Acid Small molecular drug D0U0WU
13-(5-n-pentylfuran-2-yl)Tridec-8(Z)-enoic Acid Small molecular drug D07HWV
13-(N-isopropylheptanamido)Tridec-8(Z)-enoic Acid Small molecular drug D08AKP
13-(N-methyl-n-heptnamido)Tridec-8(Z)-enoic Acid Small molecular drug D01CGC
13-(N-pentylcarbamoyloxy)Tridec-8(Z)-enoic Acid Small molecular drug D03CSL
13-n-heptanamidotridec-5-ynoic Acid Small molecular drug D07BJC
13-n-heptanamidotridec-8(Z)-enoic Acid Small molecular drug D00CHD
14-(N-hexylamino)-14-oxotetradec-8(Z)-enoic Acid Small molecular drug D05IKY
16-(3-ethylureido)Hexadec-11(Z)-enoic Acid Small molecular drug D0AT6Z
2-adamantan-1-yl-n-decyl-acetamide Small molecular drug D0U6TM
2-cyclohexyl-n-(4-methoxy-phenyl)-acetamide Small molecular drug D0K6OL
2-cyclohexyl-n-phenethyl-acetamide Small molecular drug D04PNC
2-cyclohexyl-n-phenyl-acetamide Small molecular drug D08YJF
3-(3-adamantan-1-yl-ureido)-benzoic Acid Small molecular drug D0RK4K
4,4-diphenyl-n-(Pyridin-3-yl)-butyramide Small molecular drug D0BI0Z
4-(3-adamantan-1-yl-ureido)-benzoic Acid Small molecular drug D08WHU
4-(3-cyclohexylureido)Butanoic Acid Small molecular drug D0TS7G
4-{[(Cyclohexylamino)Carbonyl]Amino}Butanoic Acid Small molecular drug DB08257
6-amino-n-(2,4-dichlorobenzyl)Nicotinamide Small molecular drug D0B3GP
6-amino-n-(3,3-diphenylpropyl)Nicotinamide Small molecular drug D0P3WB
6-{[(Cyclohexylamino)Carbonyl]Amino}Hexanoic Acid Small molecular drug D09WQW
9-(3-n-pentylureido)Non-4(Z)-enoic Acid Small molecular drug D08XYV
9-(3-n-pentylureido)Non-4-ynoic Acid Small molecular drug D02ATA
Cis-1-adamantan-1-yl-3-(4-hydroxycyclohexyl)Urea Small molecular drug D0X6ZY
Cis-1-adamantan-1-yl-3-(4-methoxycyclohexyl)Urea Small molecular drug D08RFH
Dodecanoic Acid Adamantan-1-ylamide Small molecular drug D06DZO
Ebselen Small molecular drug DB12610
Methyl 14-(3-n-butylureido)Tetradec-8(Z)-enoate Small molecular drug D03IVU
Methyl 4-(3-cyclohexylureido)Butanoate Small molecular drug D05NZH
Methyl 6-(3-cyclohexylureido)Hexanoate Small molecular drug D0J7FK
N,N'-dicyclohexyl-urea Small molecular drug D0RX9W
N-(3,3-diphenyl-propyl)-2-pyridine-3-ylacetamide Small molecular drug D07BQN
N-(3,3-diphenyl-propyl)-isonicotinamide Small molecular drug D01DZF
N-(3,3-diphenyl-propyl)-nicotinamide Small molecular drug D08HUX
N-(3-chloro-phenyl)-2-cyclohexyl-acetamide Small molecular drug D08IBD
N-(3-phenyl-propyl)-nicotinamide Small molecular drug D0D0KT
N-(4,4-diphenyl-butyl)-nicotinamide Small molecular drug D08USX
N-(Biphenyl-3-yl)Benzo[D]Isoxazol-3-amine Small molecular drug D0C1EP
N-(Biphenyl-4-yl)Benzo[D]Isoxazol-3-amine Small molecular drug D0IM1Q
N-(Naphthalen-1-yl)Benzo[D]Isoxazol-3-amine Small molecular drug D00HAZ
N-(Naphthalen-2-yl)Benzo[D]Isoxazol-3-amine Small molecular drug D0Z0XL
N-adamantyl-n'-cyclohexylurea Small molecular drug D00VZE
N-benzyl-6-(3,3,3-trifluoropropoxy)Nicotinamide Small molecular drug D02YEE
N-cyclohexyl-2-(4-methoxy-phenyl)-acetamide Small molecular drug D0S3KS
N-cyclohexyl-2-phenyl-acetamide Small molecular drug D07QNN
N-cyclohexyl-4-phenyl-butyramide Small molecular drug D0K6GX
N-cyclohexyl-n'-(4-iodophenyl)Urea Small molecular drug D0G8HM
N-cyclohexyl-n'-(Propyl)Phenyl Urea Small molecular drug D07MHZ
N-cyclohexyl-n'-decylurea Small molecular drug D0D7ID
N-[(Cyclohexylamino)Carbonyl]Glycine Small molecular drug D0B4CV
N-[3,3-bis-(4-fluorophenyl)-propyl]-benzamide Small molecular drug D0I0YE
N-[3,3-bis-(4-fluorophenyl)-propyl]-nicotinamide Small molecular drug D0K6IW
Trans,Trans-1,3-bis-(4-hydroxycyclohexyl)Urea Small molecular drug D0R1YP
[4-(3-adamantan-1-yl-ureido)-phenyl]-acetic Acid Small molecular drug D06OFY
7-{[(Cyclohexylamino)Carbonyl]Amino}Heptanoic Acid . DB08259
Ar-9281 . DB06345
Exrd-4605 . D0X0ZD

References

1 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
2 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
3 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
4 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
5 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
6 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
7 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.
8 A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045.
9 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570
10 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
11 Site-specific quantitative cysteine profiling with data-independent acquisition-based mass spectrometry. Methods Enzymol. 2023;679:295-322. doi: 10.1016/bs.mie.2022.07.037. Epub 2022 Sep 7.
Mass spectrometry data entry: PXD027578