General Information of Target

Target ID LDTP04489
Target Name Serine/threonine-protein kinase Nek2 (NEK2)
Gene Name NEK2
Gene ID 4751
Synonyms
NEK2A; NLK1; Serine/threonine-protein kinase Nek2; EC 2.7.11.1; HSPK 21; Never in mitosis A-related kinase 2; NimA-related protein kinase 2; NimA-like protein kinase 1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPSRAEDYEVLYTIGTGSYGRCQKIRRKSDGKILVWKELDYGSMTEAEKQMLVSEVNLLR
ELKHPNIVRYYDRIIDRTNTTLYIVMEYCEGGDLASVITKGTKERQYLDEEFVLRVMTQL
TLALKECHRRSDGGHTVLHRDLKPANVFLDGKQNVKLGDFGLARILNHDTSFAKTFVGTP
YYMSPEQMNRMSYNEKSDIWSLGCLLYELCALMPPFTAFSQKELAGKIREGKFRRIPYRY
SDELNEIITRMLNLKDYHRPSVEEILENPLIADLVADEQRRNLERRGRQLGEPEKSQDSS
PVLSELKLKEIQLQERERALKAREERLEQKEQELCVRERLAEDKLARAENLLKNYSLLKE
RKFLSLASNPELLNLPSSVIKKKVHFSGESKENIMRSENSESQLTSKSKCKDLKKRLHAA
QLRAQALSDIEKNYQLKSRQILGMR
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, NEK Ser/Thr protein kinase family, NIMA subfamily
Subcellular location
Cytoplasm; Nucleus
Function
Protein kinase which is involved in the control of centrosome separation and bipolar spindle formation in mitotic cells and chromatin condensation in meiotic cells. Regulates centrosome separation (essential for the formation of bipolar spindles and high-fidelity chromosome separation) by phosphorylating centrosomal proteins such as CROCC, CEP250 and NINL, resulting in their displacement from the centrosomes. Regulates kinetochore microtubule attachment stability in mitosis via phosphorylation of NDC80. Involved in regulation of mitotic checkpoint protein complex via phosphorylation of CDC20 and MAD2L1. Plays an active role in chromatin condensation during the first meiotic division through phosphorylation of HMGA2. Phosphorylates: PPP1CC; SGO1; NECAB3 and NPM1. Essential for localization of MAD2L1 to kinetochore and MAPK1 and NPM1 to the centrosome. Phosphorylates CEP68 and CNTLN directly or indirectly. NEK2-mediated phosphorylation of CEP68 promotes CEP68 dissociation from the centrosome and its degradation at the onset of mitosis. Involved in the regulation of centrosome disjunction. Phosphorylates CCDC102B either directly or indirectly which causes CCDC102B to dissociate from the centrosome and allows for centrosome separation.; [Isoform 1]: Phosphorylates and activates NEK11 in G1/S-arrested cells.; [Isoform 2]: Not present in the nucleolus and, in contrast to isoform 1, does not phosphorylate and activate NEK11 in G1/S-arrested cells.
TTD ID
T49102
Uniprot ID
P51955
DrugMap ID
TT3VZ24
Ensemble ID
ENST00000366998.4
HGNC ID
HGNC:7745
ChEMBL ID
CHEMBL3835

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.V262I; p.L340I .
NALM6 SNV: p.R259Q DBIA    Probe Info 
NCIH716 SNV: p.M44L .
SISO SNV: p.L166Ter .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C335(1.19)  LDD3333  [1]
ATP probe
 Probe Info 
N.A.  LDD0199  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C335(1.03)  LDD1507  [3]
 LDCM0215  AC10 HEK-293T C335(1.02)  LDD1508  [3]
 LDCM0226  AC11 HEK-293T C335(1.02)  LDD1509  [3]
 LDCM0237  AC12 HEK-293T C335(0.93)  LDD1510  [3]
 LDCM0259  AC14 HEK-293T C335(0.87)  LDD1512  [3]
 LDCM0270  AC15 HEK-293T C335(1.08)  LDD1513  [3]
 LDCM0276  AC17 HEK-293T C335(1.05)  LDD1515  [3]
 LDCM0277  AC18 HEK-293T C335(1.04)  LDD1516  [3]
 LDCM0278  AC19 HEK-293T C335(1.04)  LDD1517  [3]
 LDCM0279  AC2 HEK-293T C335(1.02)  LDD1518  [3]
 LDCM0280  AC20 HEK-293T C335(1.11)  LDD1519  [3]
 LDCM0281  AC21 HEK-293T C335(0.97)  LDD1520  [3]
 LDCM0282  AC22 HEK-293T C335(0.95)  LDD1521  [3]
 LDCM0283  AC23 HEK-293T C335(0.97)  LDD1522  [3]
 LDCM0284  AC24 HEK-293T C335(1.10)  LDD1523  [3]
 LDCM0285  AC25 HEK-293T C335(0.97)  LDD1524  [3]
 LDCM0286  AC26 HEK-293T C335(0.97)  LDD1525  [3]
 LDCM0287  AC27 HEK-293T C335(1.04)  LDD1526  [3]
 LDCM0288  AC28 HEK-293T C335(0.98)  LDD1527  [3]
 LDCM0289  AC29 HEK-293T C335(0.96)  LDD1528  [3]
 LDCM0290  AC3 HEK-293T C335(1.04)  LDD1529  [3]
 LDCM0291  AC30 HEK-293T C335(0.90)  LDD1530  [3]
 LDCM0292  AC31 HEK-293T C335(0.98)  LDD1531  [3]
 LDCM0293  AC32 HEK-293T C335(1.00)  LDD1532  [3]
 LDCM0294  AC33 HEK-293T C335(0.96)  LDD1533  [3]
 LDCM0295  AC34 HEK-293T C335(0.91)  LDD1534  [3]
 LDCM0296  AC35 HEK-293T C335(1.03)  LDD1535  [3]
 LDCM0297  AC36 HEK-293T C335(1.04)  LDD1536  [3]
 LDCM0298  AC37 HEK-293T C335(1.01)  LDD1537  [3]
 LDCM0299  AC38 HEK-293T C335(0.84)  LDD1538  [3]
 LDCM0300  AC39 HEK-293T C335(1.08)  LDD1539  [3]
 LDCM0301  AC4 HEK-293T C335(1.00)  LDD1540  [3]
 LDCM0302  AC40 HEK-293T C335(1.08)  LDD1541  [3]
 LDCM0303  AC41 HEK-293T C335(1.08)  LDD1542  [3]
 LDCM0304  AC42 HEK-293T C335(1.10)  LDD1543  [3]
 LDCM0305  AC43 HEK-293T C335(1.03)  LDD1544  [3]
 LDCM0306  AC44 HEK-293T C335(1.04)  LDD1545  [3]
 LDCM0307  AC45 HEK-293T C335(1.00)  LDD1546  [3]
 LDCM0308  AC46 HEK-293T C335(0.95)  LDD1547  [3]
 LDCM0309  AC47 HEK-293T C335(1.06)  LDD1548  [3]
 LDCM0310  AC48 HEK-293T C335(1.12)  LDD1549  [3]
 LDCM0311  AC49 HEK-293T C335(0.95)  LDD1550  [3]
 LDCM0312  AC5 HEK-293T C335(1.01)  LDD1551  [3]
 LDCM0313  AC50 HEK-293T C335(1.00)  LDD1552  [3]
 LDCM0314  AC51 HEK-293T C335(1.04)  LDD1553  [3]
 LDCM0315  AC52 HEK-293T C335(0.91)  LDD1554  [3]
 LDCM0316  AC53 HEK-293T C335(1.02)  LDD1555  [3]
 LDCM0317  AC54 HEK-293T C335(0.86)  LDD1556  [3]
 LDCM0318  AC55 HEK-293T C335(1.02)  LDD1557  [3]
 LDCM0319  AC56 HEK-293T C335(1.10)  LDD1558  [3]
 LDCM0320  AC57 HEK-293T C335(0.99)  LDD1559  [3]
 LDCM0321  AC58 HEK-293T C335(0.95)  LDD1560  [3]
 LDCM0322  AC59 HEK-293T C335(1.06)  LDD1561  [3]
 LDCM0323  AC6 HEK-293T C335(0.98)  LDD1562  [3]
 LDCM0324  AC60 HEK-293T C335(1.04)  LDD1563  [3]
 LDCM0325  AC61 HEK-293T C335(1.11)  LDD1564  [3]
 LDCM0326  AC62 HEK-293T C335(0.92)  LDD1565  [3]
 LDCM0327  AC63 HEK-293T C335(1.07)  LDD1566  [3]
 LDCM0328  AC64 HEK-293T C335(1.09)  LDD1567  [3]
 LDCM0334  AC7 HEK-293T C335(1.09)  LDD1568  [3]
 LDCM0345  AC8 HEK-293T C335(1.18)  LDD1569  [3]
 LDCM0248  AKOS034007472 HEK-293T C335(1.03)  LDD1511  [3]
 LDCM0356  AKOS034007680 HEK-293T C335(1.02)  LDD1570  [3]
 LDCM0275  AKOS034007705 HEK-293T C335(1.07)  LDD1514  [3]
 LDCM0367  CL1 HEK-293T C335(0.98)  LDD1571  [3]
 LDCM0368  CL10 HEK-293T C335(0.83)  LDD1572  [3]
 LDCM0369  CL100 HEK-293T C335(1.06)  LDD1573  [3]
 LDCM0370  CL101 HEK-293T C335(1.00)  LDD1574  [3]
 LDCM0371  CL102 HEK-293T C335(1.01)  LDD1575  [3]
 LDCM0372  CL103 HEK-293T C335(1.04)  LDD1576  [3]
 LDCM0373  CL104 HEK-293T C335(1.06)  LDD1577  [3]
 LDCM0374  CL105 HEK-293T C335(1.10)  LDD1578  [3]
 LDCM0375  CL106 HEK-293T C335(0.98)  LDD1579  [3]
 LDCM0376  CL107 HEK-293T C335(0.97)  LDD1580  [3]
 LDCM0377  CL108 HEK-293T C335(1.03)  LDD1581  [3]
 LDCM0378  CL109 HEK-293T C335(0.94)  LDD1582  [3]
 LDCM0379  CL11 HEK-293T C335(0.96)  LDD1583  [3]
 LDCM0380  CL110 HEK-293T C335(0.94)  LDD1584  [3]
 LDCM0381  CL111 HEK-293T C335(0.99)  LDD1585  [3]
 LDCM0382  CL112 HEK-293T C335(0.99)  LDD1586  [3]
 LDCM0383  CL113 HEK-293T C335(1.07)  LDD1587  [3]
 LDCM0384  CL114 HEK-293T C335(0.98)  LDD1588  [3]
 LDCM0385  CL115 HEK-293T C335(1.04)  LDD1589  [3]
 LDCM0386  CL116 HEK-293T C335(1.02)  LDD1590  [3]
 LDCM0387  CL117 HEK-293T C335(1.01)  LDD1591  [3]
 LDCM0388  CL118 HEK-293T C335(1.10)  LDD1592  [3]
 LDCM0389  CL119 HEK-293T C335(1.04)  LDD1593  [3]
 LDCM0390  CL12 HEK-293T C335(1.22)  LDD1594  [3]
 LDCM0391  CL120 HEK-293T C335(1.00)  LDD1595  [3]
 LDCM0392  CL121 HEK-293T C335(1.20)  LDD1596  [3]
 LDCM0393  CL122 HEK-293T C335(0.97)  LDD1597  [3]
 LDCM0394  CL123 HEK-293T C335(0.95)  LDD1598  [3]
 LDCM0395  CL124 HEK-293T C335(0.93)  LDD1599  [3]
 LDCM0396  CL125 HEK-293T C335(1.13)  LDD1600  [3]
 LDCM0397  CL126 HEK-293T C335(1.00)  LDD1601  [3]
 LDCM0398  CL127 HEK-293T C335(1.06)  LDD1602  [3]
 LDCM0399  CL128 HEK-293T C335(1.04)  LDD1603  [3]
 LDCM0400  CL13 HEK-293T C335(1.12)  LDD1604  [3]
 LDCM0401  CL14 HEK-293T C335(0.96)  LDD1605  [3]
 LDCM0402  CL15 HEK-293T C335(0.87)  LDD1606  [3]
 LDCM0403  CL16 HEK-293T C335(1.05)  LDD1607  [3]
 LDCM0404  CL17 HEK-293T C335(0.95)  LDD1608  [3]
 LDCM0405  CL18 HEK-293T C335(1.09)  LDD1609  [3]
 LDCM0406  CL19 HEK-293T C335(1.00)  LDD1610  [3]
 LDCM0407  CL2 HEK-293T C335(0.96)  LDD1611  [3]
 LDCM0408  CL20 HEK-293T C335(1.11)  LDD1612  [3]
 LDCM0409  CL21 HEK-293T C335(0.92)  LDD1613  [3]
 LDCM0410  CL22 HEK-293T C335(0.91)  LDD1614  [3]
 LDCM0411  CL23 HEK-293T C335(1.02)  LDD1615  [3]
 LDCM0412  CL24 HEK-293T C335(1.35)  LDD1616  [3]
 LDCM0413  CL25 HEK-293T C335(1.04)  LDD1617  [3]
 LDCM0414  CL26 HEK-293T C335(1.03)  LDD1618  [3]
 LDCM0415  CL27 HEK-293T C335(1.04)  LDD1619  [3]
 LDCM0416  CL28 HEK-293T C335(1.00)  LDD1620  [3]
 LDCM0417  CL29 HEK-293T C335(0.94)  LDD1621  [3]
 LDCM0418  CL3 HEK-293T C335(0.95)  LDD1622  [3]
 LDCM0419  CL30 HEK-293T C335(1.08)  LDD1623  [3]
 LDCM0420  CL31 HEK-293T C335(1.00)  LDD1624  [3]
 LDCM0421  CL32 HEK-293T C335(1.06)  LDD1625  [3]
 LDCM0422  CL33 HEK-293T C335(0.85)  LDD1626  [3]
 LDCM0423  CL34 HEK-293T C335(0.88)  LDD1627  [3]
 LDCM0424  CL35 HEK-293T C335(1.04)  LDD1628  [3]
 LDCM0425  CL36 HEK-293T C335(1.10)  LDD1629  [3]
 LDCM0426  CL37 HEK-293T C335(1.04)  LDD1630  [3]
 LDCM0428  CL39 HEK-293T C335(0.98)  LDD1632  [3]
 LDCM0429  CL4 HEK-293T C335(0.95)  LDD1633  [3]
 LDCM0430  CL40 HEK-293T C335(0.98)  LDD1634  [3]
 LDCM0431  CL41 HEK-293T C335(0.98)  LDD1635  [3]
 LDCM0432  CL42 HEK-293T C335(0.93)  LDD1636  [3]
 LDCM0433  CL43 HEK-293T C335(0.95)  LDD1637  [3]
 LDCM0434  CL44 HEK-293T C335(1.04)  LDD1638  [3]
 LDCM0435  CL45 HEK-293T C335(1.07)  LDD1639  [3]
 LDCM0436  CL46 HEK-293T C335(0.97)  LDD1640  [3]
 LDCM0437  CL47 HEK-293T C335(1.04)  LDD1641  [3]
 LDCM0438  CL48 HEK-293T C335(1.35)  LDD1642  [3]
 LDCM0439  CL49 HEK-293T C335(1.13)  LDD1643  [3]
 LDCM0440  CL5 HEK-293T C335(1.02)  LDD1644  [3]
 LDCM0441  CL50 HEK-293T C335(0.95)  LDD1645  [3]
 LDCM0443  CL52 HEK-293T C335(1.00)  LDD1646  [3]
 LDCM0444  CL53 HEK-293T C335(0.95)  LDD1647  [3]
 LDCM0445  CL54 HEK-293T C335(0.92)  LDD1648  [3]
 LDCM0446  CL55 HEK-293T C335(1.10)  LDD1649  [3]
 LDCM0447  CL56 HEK-293T C335(1.13)  LDD1650  [3]
 LDCM0448  CL57 HEK-293T C335(0.92)  LDD1651  [3]
 LDCM0449  CL58 HEK-293T C335(0.86)  LDD1652  [3]
 LDCM0450  CL59 HEK-293T C335(1.08)  LDD1653  [3]
 LDCM0451  CL6 HEK-293T C335(1.06)  LDD1654  [3]
 LDCM0452  CL60 HEK-293T C335(1.31)  LDD1655  [3]
 LDCM0453  CL61 HEK-293T C335(1.08)  LDD1656  [3]
 LDCM0454  CL62 HEK-293T C335(1.01)  LDD1657  [3]
 LDCM0455  CL63 HEK-293T C335(0.99)  LDD1658  [3]
 LDCM0456  CL64 HEK-293T C335(0.97)  LDD1659  [3]
 LDCM0457  CL65 HEK-293T C335(1.01)  LDD1660  [3]
 LDCM0458  CL66 HEK-293T C335(0.89)  LDD1661  [3]
 LDCM0459  CL67 HEK-293T C335(1.04)  LDD1662  [3]
 LDCM0460  CL68 HEK-293T C335(1.06)  LDD1663  [3]
 LDCM0461  CL69 HEK-293T C335(1.03)  LDD1664  [3]
 LDCM0462  CL7 HEK-293T C335(1.02)  LDD1665  [3]
 LDCM0463  CL70 HEK-293T C335(0.91)  LDD1666  [3]
 LDCM0464  CL71 HEK-293T C335(1.01)  LDD1667  [3]
 LDCM0465  CL72 HEK-293T C335(1.28)  LDD1668  [3]
 LDCM0466  CL73 HEK-293T C335(1.03)  LDD1669  [3]
 LDCM0467  CL74 HEK-293T C335(1.02)  LDD1670  [3]
 LDCM0469  CL76 HEK-293T C335(1.04)  LDD1672  [3]
 LDCM0470  CL77 HEK-293T C335(1.01)  LDD1673  [3]
 LDCM0471  CL78 HEK-293T C335(1.06)  LDD1674  [3]
 LDCM0472  CL79 HEK-293T C335(1.02)  LDD1675  [3]
 LDCM0473  CL8 HEK-293T C335(0.90)  LDD1676  [3]
 LDCM0474  CL80 HEK-293T C335(1.06)  LDD1677  [3]
 LDCM0475  CL81 HEK-293T C335(1.04)  LDD1678  [3]
 LDCM0476  CL82 HEK-293T C335(0.85)  LDD1679  [3]
 LDCM0477  CL83 HEK-293T C335(1.01)  LDD1680  [3]
 LDCM0478  CL84 HEK-293T C335(1.12)  LDD1681  [3]
 LDCM0479  CL85 HEK-293T C335(1.02)  LDD1682  [3]
 LDCM0480  CL86 HEK-293T C335(1.04)  LDD1683  [3]
 LDCM0481  CL87 HEK-293T C335(1.06)  LDD1684  [3]
 LDCM0482  CL88 HEK-293T C335(1.01)  LDD1685  [3]
 LDCM0483  CL89 HEK-293T C335(0.93)  LDD1686  [3]
 LDCM0484  CL9 HEK-293T C335(1.09)  LDD1687  [3]
 LDCM0485  CL90 HEK-293T C335(1.01)  LDD1688  [3]
 LDCM0486  CL91 HEK-293T C335(1.05)  LDD1689  [3]
 LDCM0487  CL92 HEK-293T C335(1.08)  LDD1690  [3]
 LDCM0488  CL93 HEK-293T C335(1.07)  LDD1691  [3]
 LDCM0489  CL94 HEK-293T C335(1.04)  LDD1692  [3]
 LDCM0490  CL95 HEK-293T C335(1.00)  LDD1693  [3]
 LDCM0491  CL96 HEK-293T C335(1.21)  LDD1694  [3]
 LDCM0492  CL97 HEK-293T C335(0.98)  LDD1695  [3]
 LDCM0493  CL98 HEK-293T C335(1.03)  LDD1696  [3]
 LDCM0494  CL99 HEK-293T C335(1.10)  LDD1697  [3]
 LDCM0495  E2913 HEK-293T C335(1.13)  LDD1698  [3]
 LDCM0468  Fragment33 HEK-293T C335(1.02)  LDD1671  [3]
 LDCM0427  Fragment51 HEK-293T C335(1.05)  LDD1631  [3]
 LDCM0022  KB02 HEK-293T C335(1.06)  LDD1492  [3]
 LDCM0023  KB03 HEK-293T C335(1.05)  LDD1497  [3]
 LDCM0024  KB05 MOLM-13 C335(1.19)  LDD3333  [1]

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
Cell division cycle protein 27 homolog (CDC27) APC3/CDC27 family P30260
Serine/threonine-protein kinase Nek11 (NEK11) NEK Ser/Thr protein kinase family Q8NG66
Kinesin-like protein KIF24 (KIF24) Kinesin family Q5T7B8
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Anaphase-promoting complex subunit 4 (ANAPC4) APC4 family Q9UJX5

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
Investigative
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gsk579289a Small molecular drug D0X1RH
Pmid20936789c31 Small molecular drug D0K0UJ
Pmid21627121c2 Small molecular drug D0C3KE
5-[(Z)-(5-chloro-2-oxo-12-dihydro-3h-indol-3-ylidene)Methyl]-n24-trimethyl-1h-pyrrole-3-carboxamide . DB07180

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 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.
3 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