General Information of Target

Target ID LDTP05674
Target Name Tyrosine-protein kinase Mer (MERTK)
Gene Name MERTK
Gene ID 10461
Synonyms
MER; Tyrosine-protein kinase Mer; EC 2.7.10.1; Proto-oncogene c-Mer; Receptor tyrosine kinase MerTK
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGPAPLPLLLGLFLPALWRRAITEAREEAKPYPLFPGPFPGSLQTDHTPLLSLPHASGYQ
PALMFSPTQPGRPHTGNVAIPQVTSVESKPLPPLAFKHTVGHIILSEHKGVKFNCSISVP
NIYQDTTISWWKDGKELLGAHHAITQFYPDDEVTAIIASFSITSVQRSDNGSYICKMKIN
NEEIVSDPIYIEVQGLPHFTKQPESMNVTRNTAFNLTCQAVGPPEPVNIFWVQNSSRVNE
QPEKSPSVLTVPGLTEMAVFSCEAHNDKGLTVSKGVQINIKAIPSPPTEVSIRNSTAHSI
LISWVPGFDGYSPFRNCSIQVKEADPLSNGSVMIFNTSALPHLYQIKQLQALANYSIGVS
CMNEIGWSAVSPWILASTTEGAPSVAPLNVTVFLNESSDNVDIRWMKPPTKQQDGELVGY
RISHVWQSAGISKELLEEVGQNGSRARISVQVHNATCTVRIAAVTRGGVGPFSDPVKIFI
PAHGWVDYAPSSTPAPGNADPVLIIFGCFCGFILIGLILYISLAIRKRVQETKFGNAFTE
EDSELVVNYIAKKSFCRRAIELTLHSLGVSEELQNKLEDVVIDRNLLILGKILGEGEFGS
VMEGNLKQEDGTSLKVAVKTMKLDNSSQREIEEFLSEAACMKDFSHPNVIRLLGVCIEMS
SQGIPKPMVILPFMKYGDLHTYLLYSRLETGPKHIPLQTLLKFMVDIALGMEYLSNRNFL
HRDLAARNCMLRDDMTVCVADFGLSKKIYSGDYYRQGRIAKMPVKWIAIESLADRVYTSK
SDVWAFGVTMWEIATRGMTPYPGVQNHEMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTD
PLDRPTFSVLRLQLEKLLESLPDVRNQADVIYVNTQLLESSEGLAQGSTLAPLDLNIDPD
SIIASCTPRAAISVVTAEVHDSKPHEGRYILNGGSEEWEDLTSAPSAAVTAEKNSVLPGE
RLVRNGVSWSHSSMLPLGSSLPDELLFADDSSEGSEVLM
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, AXL/UFO subfamily
Subcellular location
Cell membrane
Function
Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to several ligands including LGALS3, TUB, TULP1 or GAS6. Regulates many physiological processes including cell survival, migration, differentiation, and phagocytosis of apoptotic cells (efferocytosis). Ligand binding at the cell surface induces autophosphorylation of MERTK on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with GRB2 or PLCG2 and induces phosphorylation of MAPK1, MAPK2, FAK/PTK2 or RAC1. MERTK signaling plays a role in various processes such as macrophage clearance of apoptotic cells, platelet aggregation, cytoskeleton reorganization and engulfment. Functions in the retinal pigment epithelium (RPE) as a regulator of rod outer segments fragments phagocytosis. Also plays an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.
TTD ID
T55781
Uniprot ID
Q12866
DrugMap ID
TTO7LKR
Ensemble ID
ENST00000295408.9
HGNC ID
HGNC:7027
ChEMBL ID
CHEMBL5331

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info 
C825(4.39)  LDD2157  [1]
DBIA
 Probe Info 
C640(0.95)  LDD1507  [2]
ATP probe
 Probe Info 
K746(0.00); K747(0.00)  LDD0199  [3]
IPM
 Probe Info 
N.A.  LDD2156  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C640(0.95)  LDD1507  [2]
 LDCM0215  AC10 HEK-293T C640(1.05)  LDD1508  [2]
 LDCM0226  AC11 HEK-293T C640(0.98)  LDD1509  [2]
 LDCM0237  AC12 HEK-293T C640(1.15)  LDD1510  [2]
 LDCM0259  AC14 HEK-293T C640(0.94)  LDD1512  [2]
 LDCM0270  AC15 HEK-293T C640(0.96)  LDD1513  [2]
 LDCM0276  AC17 HEK-293T C640(1.01)  LDD1515  [2]
 LDCM0277  AC18 HEK-293T C640(0.99)  LDD1516  [2]
 LDCM0278  AC19 HEK-293T C640(0.98)  LDD1517  [2]
 LDCM0279  AC2 HEK-293T C640(1.05)  LDD1518  [2]
 LDCM0280  AC20 HEK-293T C640(0.88)  LDD1519  [2]
 LDCM0281  AC21 HEK-293T C640(0.79)  LDD1520  [2]
 LDCM0282  AC22 HEK-293T C640(1.17)  LDD1521  [2]
 LDCM0283  AC23 HEK-293T C640(0.93)  LDD1522  [2]
 LDCM0284  AC24 HEK-293T C640(0.95)  LDD1523  [2]
 LDCM0285  AC25 HEK-293T C640(0.89)  LDD1524  [2]
 LDCM0286  AC26 HEK-293T C640(0.99)  LDD1525  [2]
 LDCM0287  AC27 HEK-293T C640(1.24)  LDD1526  [2]
 LDCM0288  AC28 HEK-293T C640(1.14)  LDD1527  [2]
 LDCM0289  AC29 HEK-293T C640(0.82)  LDD1528  [2]
 LDCM0290  AC3 HEK-293T C640(1.04)  LDD1529  [2]
 LDCM0291  AC30 HEK-293T C640(0.91)  LDD1530  [2]
 LDCM0292  AC31 HEK-293T C640(1.01)  LDD1531  [2]
 LDCM0293  AC32 HEK-293T C640(1.07)  LDD1532  [2]
 LDCM0294  AC33 HEK-293T C640(0.94)  LDD1533  [2]
 LDCM0295  AC34 HEK-293T C640(1.25)  LDD1534  [2]
 LDCM0296  AC35 HEK-293T C640(1.03)  LDD1535  [2]
 LDCM0297  AC36 HEK-293T C640(1.01)  LDD1536  [2]
 LDCM0298  AC37 HEK-293T C640(1.00)  LDD1537  [2]
 LDCM0299  AC38 HEK-293T C640(0.89)  LDD1538  [2]
 LDCM0300  AC39 HEK-293T C640(0.95)  LDD1539  [2]
 LDCM0301  AC4 HEK-293T C640(0.97)  LDD1540  [2]
 LDCM0302  AC40 HEK-293T C640(1.06)  LDD1541  [2]
 LDCM0303  AC41 HEK-293T C640(0.92)  LDD1542  [2]
 LDCM0304  AC42 HEK-293T C640(1.26)  LDD1543  [2]
 LDCM0305  AC43 HEK-293T C640(0.95)  LDD1544  [2]
 LDCM0306  AC44 HEK-293T C640(1.00)  LDD1545  [2]
 LDCM0307  AC45 HEK-293T C640(0.97)  LDD1546  [2]
 LDCM0308  AC46 HEK-293T C640(0.93)  LDD1547  [2]
 LDCM0309  AC47 HEK-293T C640(1.02)  LDD1548  [2]
 LDCM0310  AC48 HEK-293T C640(0.98)  LDD1549  [2]
 LDCM0311  AC49 HEK-293T C640(0.92)  LDD1550  [2]
 LDCM0312  AC5 HEK-293T C640(1.06)  LDD1551  [2]
 LDCM0313  AC50 HEK-293T C640(1.23)  LDD1552  [2]
 LDCM0314  AC51 HEK-293T C640(0.99)  LDD1553  [2]
 LDCM0315  AC52 HEK-293T C640(1.04)  LDD1554  [2]
 LDCM0316  AC53 HEK-293T C640(0.92)  LDD1555  [2]
 LDCM0317  AC54 HEK-293T C640(1.19)  LDD1556  [2]
 LDCM0318  AC55 HEK-293T C640(0.95)  LDD1557  [2]
 LDCM0319  AC56 HEK-293T C640(0.96)  LDD1558  [2]
 LDCM0320  AC57 HEK-293T C640(0.99)  LDD1559  [2]
 LDCM0321  AC58 HEK-293T C640(1.08)  LDD1560  [2]
 LDCM0322  AC59 HEK-293T C640(0.92)  LDD1561  [2]
 LDCM0323  AC6 HEK-293T C640(1.09)  LDD1562  [2]
 LDCM0324  AC60 HEK-293T C640(0.98)  LDD1563  [2]
 LDCM0325  AC61 HEK-293T C640(0.99)  LDD1564  [2]
 LDCM0326  AC62 HEK-293T C640(0.99)  LDD1565  [2]
 LDCM0327  AC63 HEK-293T C640(0.84)  LDD1566  [2]
 LDCM0328  AC64 HEK-293T C640(1.11)  LDD1567  [2]
 LDCM0334  AC7 HEK-293T C640(1.11)  LDD1568  [2]
 LDCM0345  AC8 HEK-293T C640(0.91)  LDD1569  [2]
 LDCM0248  AKOS034007472 HEK-293T C640(0.86)  LDD1511  [2]
 LDCM0356  AKOS034007680 HEK-293T C640(0.95)  LDD1570  [2]
 LDCM0275  AKOS034007705 HEK-293T C640(1.05)  LDD1514  [2]
 LDCM0367  CL1 HEK-293T C640(0.87)  LDD1571  [2]
 LDCM0368  CL10 HEK-293T C640(1.05)  LDD1572  [2]
 LDCM0369  CL100 HEK-293T C640(0.96)  LDD1573  [2]
 LDCM0370  CL101 HEK-293T C640(0.89)  LDD1574  [2]
 LDCM0371  CL102 HEK-293T C640(0.98)  LDD1575  [2]
 LDCM0372  CL103 HEK-293T C640(1.00)  LDD1576  [2]
 LDCM0373  CL104 HEK-293T C640(0.89)  LDD1577  [2]
 LDCM0374  CL105 HEK-293T C640(0.72)  LDD1578  [2]
 LDCM0375  CL106 HEK-293T C640(0.94)  LDD1579  [2]
 LDCM0376  CL107 HEK-293T C640(1.00)  LDD1580  [2]
 LDCM0377  CL108 HEK-293T C640(1.01)  LDD1581  [2]
 LDCM0378  CL109 HEK-293T C640(0.98)  LDD1582  [2]
 LDCM0379  CL11 HEK-293T C640(0.95)  LDD1583  [2]
 LDCM0380  CL110 HEK-293T C640(1.09)  LDD1584  [2]
 LDCM0381  CL111 HEK-293T C640(1.16)  LDD1585  [2]
 LDCM0382  CL112 HEK-293T C640(0.92)  LDD1586  [2]
 LDCM0383  CL113 HEK-293T C640(0.90)  LDD1587  [2]
 LDCM0384  CL114 HEK-293T C640(1.01)  LDD1588  [2]
 LDCM0385  CL115 HEK-293T C640(1.02)  LDD1589  [2]
 LDCM0386  CL116 HEK-293T C640(0.91)  LDD1590  [2]
 LDCM0387  CL117 HEK-293T C640(0.95)  LDD1591  [2]
 LDCM0388  CL118 HEK-293T C640(1.01)  LDD1592  [2]
 LDCM0389  CL119 HEK-293T C640(0.99)  LDD1593  [2]
 LDCM0390  CL12 HEK-293T C640(1.12)  LDD1594  [2]
 LDCM0391  CL120 HEK-293T C640(1.08)  LDD1595  [2]
 LDCM0392  CL121 HEK-293T C640(0.91)  LDD1596  [2]
 LDCM0393  CL122 HEK-293T C640(1.00)  LDD1597  [2]
 LDCM0394  CL123 HEK-293T C640(0.96)  LDD1598  [2]
 LDCM0395  CL124 HEK-293T C640(0.94)  LDD1599  [2]
 LDCM0396  CL125 HEK-293T C640(0.87)  LDD1600  [2]
 LDCM0397  CL126 HEK-293T C640(1.11)  LDD1601  [2]
 LDCM0398  CL127 HEK-293T C640(0.97)  LDD1602  [2]
 LDCM0399  CL128 HEK-293T C640(0.95)  LDD1603  [2]
 LDCM0400  CL13 HEK-293T C640(0.89)  LDD1604  [2]
 LDCM0401  CL14 HEK-293T C640(1.12)  LDD1605  [2]
 LDCM0402  CL15 HEK-293T C640(1.09)  LDD1606  [2]
 LDCM0403  CL16 HEK-293T C640(0.94)  LDD1607  [2]
 LDCM0404  CL17 HEK-293T C640(1.02)  LDD1608  [2]
 LDCM0405  CL18 HEK-293T C640(0.95)  LDD1609  [2]
 LDCM0406  CL19 HEK-293T C640(1.16)  LDD1610  [2]
 LDCM0407  CL2 HEK-293T C640(1.00)  LDD1611  [2]
 LDCM0408  CL20 HEK-293T C640(1.03)  LDD1612  [2]
 LDCM0409  CL21 HEK-293T C640(0.86)  LDD1613  [2]
 LDCM0410  CL22 HEK-293T C640(1.01)  LDD1614  [2]
 LDCM0411  CL23 HEK-293T C640(0.98)  LDD1615  [2]
 LDCM0412  CL24 HEK-293T C640(1.24)  LDD1616  [2]
 LDCM0413  CL25 HEK-293T C640(1.22)  LDD1617  [2]
 LDCM0414  CL26 HEK-293T C640(1.07)  LDD1618  [2]
 LDCM0415  CL27 HEK-293T C640(1.19)  LDD1619  [2]
 LDCM0416  CL28 HEK-293T C640(1.11)  LDD1620  [2]
 LDCM0417  CL29 HEK-293T C640(1.00)  LDD1621  [2]
 LDCM0418  CL3 HEK-293T C640(0.88)  LDD1622  [2]
 LDCM0419  CL30 HEK-293T C640(1.17)  LDD1623  [2]
 LDCM0420  CL31 HEK-293T C640(1.04)  LDD1624  [2]
 LDCM0421  CL32 HEK-293T C640(0.92)  LDD1625  [2]
 LDCM0422  CL33 HEK-293T C640(1.14)  LDD1626  [2]
 LDCM0423  CL34 HEK-293T C640(1.02)  LDD1627  [2]
 LDCM0424  CL35 HEK-293T C640(1.08)  LDD1628  [2]
 LDCM0425  CL36 HEK-293T C640(1.20)  LDD1629  [2]
 LDCM0426  CL37 HEK-293T C640(0.95)  LDD1630  [2]
 LDCM0428  CL39 HEK-293T C640(1.07)  LDD1632  [2]
 LDCM0429  CL4 HEK-293T C640(1.00)  LDD1633  [2]
 LDCM0430  CL40 HEK-293T C640(0.93)  LDD1634  [2]
 LDCM0431  CL41 HEK-293T C640(0.86)  LDD1635  [2]
 LDCM0432  CL42 HEK-293T C640(1.13)  LDD1636  [2]
 LDCM0433  CL43 HEK-293T C640(0.99)  LDD1637  [2]
 LDCM0434  CL44 HEK-293T C640(0.95)  LDD1638  [2]
 LDCM0435  CL45 HEK-293T C640(0.96)  LDD1639  [2]
 LDCM0436  CL46 HEK-293T C640(1.00)  LDD1640  [2]
 LDCM0437  CL47 HEK-293T C640(0.90)  LDD1641  [2]
 LDCM0438  CL48 HEK-293T C640(1.12)  LDD1642  [2]
 LDCM0439  CL49 HEK-293T C640(0.87)  LDD1643  [2]
 LDCM0440  CL5 HEK-293T C640(1.03)  LDD1644  [2]
 LDCM0441  CL50 HEK-293T C640(1.19)  LDD1645  [2]
 LDCM0443  CL52 HEK-293T C640(0.85)  LDD1646  [2]
 LDCM0444  CL53 HEK-293T C640(0.87)  LDD1647  [2]
 LDCM0445  CL54 HEK-293T C640(1.11)  LDD1648  [2]
 LDCM0446  CL55 HEK-293T C640(1.00)  LDD1649  [2]
 LDCM0447  CL56 HEK-293T C640(1.07)  LDD1650  [2]
 LDCM0448  CL57 HEK-293T C640(0.99)  LDD1651  [2]
 LDCM0449  CL58 HEK-293T C640(0.97)  LDD1652  [2]
 LDCM0450  CL59 HEK-293T C640(1.00)  LDD1653  [2]
 LDCM0451  CL6 HEK-293T C640(1.08)  LDD1654  [2]
 LDCM0452  CL60 HEK-293T C640(1.06)  LDD1655  [2]
 LDCM0453  CL61 HEK-293T C640(1.10)  LDD1656  [2]
 LDCM0454  CL62 HEK-293T C640(0.93)  LDD1657  [2]
 LDCM0455  CL63 HEK-293T C640(1.13)  LDD1658  [2]
 LDCM0456  CL64 HEK-293T C640(0.95)  LDD1659  [2]
 LDCM0457  CL65 HEK-293T C640(1.02)  LDD1660  [2]
 LDCM0458  CL66 HEK-293T C640(1.17)  LDD1661  [2]
 LDCM0459  CL67 HEK-293T C640(1.33)  LDD1662  [2]
 LDCM0460  CL68 HEK-293T C640(1.14)  LDD1663  [2]
 LDCM0461  CL69 HEK-293T C640(0.96)  LDD1664  [2]
 LDCM0462  CL7 HEK-293T C640(1.22)  LDD1665  [2]
 LDCM0463  CL70 HEK-293T C640(1.07)  LDD1666  [2]
 LDCM0464  CL71 HEK-293T C640(0.86)  LDD1667  [2]
 LDCM0465  CL72 HEK-293T C640(1.17)  LDD1668  [2]
 LDCM0466  CL73 HEK-293T C640(0.99)  LDD1669  [2]
 LDCM0467  CL74 HEK-293T C640(1.13)  LDD1670  [2]
 LDCM0469  CL76 HEK-293T C640(0.90)  LDD1672  [2]
 LDCM0470  CL77 HEK-293T C640(0.84)  LDD1673  [2]
 LDCM0471  CL78 HEK-293T C640(1.23)  LDD1674  [2]
 LDCM0472  CL79 HEK-293T C640(1.02)  LDD1675  [2]
 LDCM0473  CL8 HEK-293T C640(1.02)  LDD1676  [2]
 LDCM0474  CL80 HEK-293T C640(1.00)  LDD1677  [2]
 LDCM0475  CL81 HEK-293T C640(0.88)  LDD1678  [2]
 LDCM0476  CL82 HEK-293T C640(0.87)  LDD1679  [2]
 LDCM0477  CL83 HEK-293T C640(0.97)  LDD1680  [2]
 LDCM0478  CL84 HEK-293T C640(1.14)  LDD1681  [2]
 LDCM0479  CL85 HEK-293T C640(1.04)  LDD1682  [2]
 LDCM0480  CL86 HEK-293T C640(1.09)  LDD1683  [2]
 LDCM0481  CL87 HEK-293T C640(1.03)  LDD1684  [2]
 LDCM0482  CL88 HEK-293T C640(0.89)  LDD1685  [2]
 LDCM0483  CL89 HEK-293T C640(1.27)  LDD1686  [2]
 LDCM0484  CL9 HEK-293T C640(0.88)  LDD1687  [2]
 LDCM0485  CL90 HEK-293T C640(1.03)  LDD1688  [2]
 LDCM0486  CL91 HEK-293T C640(1.07)  LDD1689  [2]
 LDCM0487  CL92 HEK-293T C640(1.16)  LDD1690  [2]
 LDCM0488  CL93 HEK-293T C640(0.86)  LDD1691  [2]
 LDCM0489  CL94 HEK-293T C640(0.96)  LDD1692  [2]
 LDCM0490  CL95 HEK-293T C640(1.11)  LDD1693  [2]
 LDCM0491  CL96 HEK-293T C640(1.09)  LDD1694  [2]
 LDCM0492  CL97 HEK-293T C640(1.05)  LDD1695  [2]
 LDCM0493  CL98 HEK-293T C640(1.09)  LDD1696  [2]
 LDCM0494  CL99 HEK-293T C640(1.08)  LDD1697  [2]
 LDCM0495  E2913 HEK-293T C640(1.12)  LDD1698  [2]
 LDCM0468  Fragment33 HEK-293T C640(1.03)  LDD1671  [2]
 LDCM0427  Fragment51 HEK-293T C640(1.03)  LDD1631  [2]

The Interaction Atlas With This Target

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
Mk-2461 Small molecular drug D00DRL
Ono-7475 Small molecular drug DA1MG8
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Incb81776 Small molecular drug DQX83Z
Mrx-2843 Small molecular drug D10LNV
Pf-07265807 Small molecular drug DP4KH3
Rxdx-106 Small molecular drug D7HZ3T
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
G749 Small molecular drug D0N3XP
Ldc1267 Small molecular drug D09TFN
Unc2025 Small molecular drug DCJX65
Unc569 Small molecular drug DI81LW
2-({6-[(3-chlorophenyl)Amino]-9-isopropyl-9h-purin-2-yl}Amino)Ethanol . DB08325

References

1 From chemoproteomic-detected amino acids to genomic coordinates: insights into precise multi-omic data integration. Mol Syst Biol. 2021 Feb;17(2):e9840. doi: 10.15252/msb.20209840.
Mass spectrometry data entry: PXD022151
2 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
3 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.
4 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019