Details of the Target

General Information of Target

Target ID LDTP04549
Target Name Homeobox protein Nkx-2.5 (NKX2-5)
Gene Name NKX2-5
Gene ID 1482
Synonyms
CSX; NKX2.5; NKX2E; Homeobox protein Nkx-2.5; Cardiac-specific homeobox; Homeobox protein CSX; Homeobox protein NK-2 homolog E
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MFPSPALTPTPFSVKDILNLEQQQRSLAAAGELSARLEATLAPSSCMLAAFKPEAYAGPE
AAAPGLPELRAELGRAPSPAKCASAFPAAPAFYPRAYSDPDPAKDPRAEKKELCALQKAV
ELEKTEADNAERPRARRRRKPRVLFSQAQVYELERRFKQQRYLSAPERDQLASVLKLTST
QVKIWFQNRRYKCKRQRQDQTLELVGLPPPPPPPARRIAVPVLVRDGKPCLGDSAPYAPA
YGVGLNPYGYNAYPAYPGYGGAACSPGYSCTAAYPAGPSPAQPATAAANNNFVNFGVGDL
NAVQSPGIPQSNSGVSTLHGIRAW
Target Bioclass
Transcription factor
Family
NK-2 homeobox family
Subcellular location
Nucleus
Function
Transcription factor required for the development of the heart and the spleen. During heart development, acts as a transcriptional activator of NPPA/ANF in cooperation with GATA4. May cooperate with TBX2 to negatively modulate expression of NPPA/ANF in the atrioventricular canal. Binds to the core DNA motif of NPPA promoter. Together with PBX1, required for spleen development through a mechanism that involves CDKN2B repression. Positively regulates transcription of genes such as COL3A1 and MMP2, resulting in increased pulmonary endothelial fibrosis in response to hypoxia.
Uniprot ID
P52952
Ensemble ID
ENST00000329198.5
HGNC ID
HGNC:2488

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A375 SNV: p.Y241N .
CALU6 SNV: p.P257L .
ETK1 SNV: p.Y274S .
LS180 SNV: p.P239S .
NCIH1793 SNV: p.Y248N .
TOV21G SNV: p.P280Q .

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
TH211
 Probe Info  		Y93(5.23)  LDD0257  [1]
DBIA
 Probe Info  		C114(0.95); C46(1.02)  LDD1492  [2]
IPM
 Probe Info  		N.A.  LDD0005  [3]
Phosphinate-6
 Probe Info  		C82(0.00); C114(0.00)  LDD0018  [4]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C46(1.02)  LDD1507  [2]
 LDCM0215  AC10 HEK-293T C114(1.21)  LDD1508  [2]
 LDCM0226  AC11 HEK-293T C46(1.00); C82(1.10)  LDD1509  [2]
 LDCM0237  AC12 HEK-293T C114(1.03)  LDD1510  [2]
 LDCM0259  AC14 HEK-293T C46(1.17); C114(1.06)  LDD1512  [2]
 LDCM0270  AC15 HEK-293T C46(0.83)  LDD1513  [2]
 LDCM0276  AC17 HEK-293T C46(1.03)  LDD1515  [2]
 LDCM0277  AC18 HEK-293T C114(1.02)  LDD1516  [2]
 LDCM0278  AC19 HEK-293T C46(1.07); C82(1.12)  LDD1517  [2]
 LDCM0279  AC2 HEK-293T C114(0.98)  LDD1518  [2]
 LDCM0280  AC20 HEK-293T C114(0.95)  LDD1519  [2]
 LDCM0281  AC21 HEK-293T C46(1.25); C82(0.98)  LDD1520  [2]
 LDCM0282  AC22 HEK-293T C46(0.92); C114(0.98)  LDD1521  [2]
 LDCM0283  AC23 HEK-293T C46(0.95)  LDD1522  [2]
 LDCM0284  AC24 HEK-293T C114(1.01)  LDD1523  [2]
 LDCM0285  AC25 HEK-293T C46(1.07)  LDD1524  [2]
 LDCM0286  AC26 HEK-293T C114(0.99)  LDD1525  [2]
 LDCM0287  AC27 HEK-293T C46(1.05); C82(0.94)  LDD1526  [2]
 LDCM0288  AC28 HEK-293T C114(1.00)  LDD1527  [2]
 LDCM0289  AC29 HEK-293T C46(1.31); C82(1.00)  LDD1528  [2]
 LDCM0290  AC3 HEK-293T C46(1.04); C82(1.02)  LDD1529  [2]
 LDCM0291  AC30 HEK-293T C46(1.14); C114(1.03)  LDD1530  [2]
 LDCM0292  AC31 HEK-293T C46(0.92)  LDD1531  [2]
 LDCM0293  AC32 HEK-293T C114(0.96)  LDD1532  [2]
 LDCM0294  AC33 HEK-293T C46(1.10)  LDD1533  [2]
 LDCM0295  AC34 HEK-293T C114(1.12)  LDD1534  [2]
 LDCM0296  AC35 HEK-293T C46(1.05); C82(1.11)  LDD1535  [2]
 LDCM0297  AC36 HEK-293T C114(1.11)  LDD1536  [2]
 LDCM0298  AC37 HEK-293T C46(1.50); C82(0.97)  LDD1537  [2]
 LDCM0299  AC38 HEK-293T C46(1.18); C114(1.00)  LDD1538  [2]
 LDCM0300  AC39 HEK-293T C46(1.14)  LDD1539  [2]
 LDCM0301  AC4 HEK-293T C114(1.05)  LDD1540  [2]
 LDCM0302  AC40 HEK-293T C114(1.07)  LDD1541  [2]
 LDCM0303  AC41 HEK-293T C46(1.06)  LDD1542  [2]
 LDCM0304  AC42 HEK-293T C114(1.13)  LDD1543  [2]
 LDCM0305  AC43 HEK-293T C46(1.16); C82(1.03)  LDD1544  [2]
 LDCM0306  AC44 HEK-293T C114(1.13)  LDD1545  [2]
 LDCM0307  AC45 HEK-293T C46(1.24); C82(1.08)  LDD1546  [2]
 LDCM0308  AC46 HEK-293T C46(1.11); C114(0.99)  LDD1547  [2]
 LDCM0309  AC47 HEK-293T C46(1.16)  LDD1548  [2]
 LDCM0310  AC48 HEK-293T C114(1.12)  LDD1549  [2]
 LDCM0311  AC49 HEK-293T C46(0.94)  LDD1550  [2]
 LDCM0312  AC5 HEK-293T C46(1.06); C82(0.91)  LDD1551  [2]
 LDCM0313  AC50 HEK-293T C114(1.13)  LDD1552  [2]
 LDCM0314  AC51 HEK-293T C46(0.92); C82(0.88)  LDD1553  [2]
 LDCM0315  AC52 HEK-293T C114(1.10)  LDD1554  [2]
 LDCM0316  AC53 HEK-293T C46(1.07); C82(1.03)  LDD1555  [2]
 LDCM0317  AC54 HEK-293T C46(1.19); C114(1.06)  LDD1556  [2]
 LDCM0318  AC55 HEK-293T C46(0.89)  LDD1557  [2]
 LDCM0319  AC56 HEK-293T C114(1.04)  LDD1558  [2]
 LDCM0320  AC57 HEK-293T C46(1.14)  LDD1559  [2]
 LDCM0321  AC58 HEK-293T C114(1.13)  LDD1560  [2]
 LDCM0322  AC59 HEK-293T C46(1.10); C82(1.07)  LDD1561  [2]
 LDCM0323  AC6 HEK-293T C46(1.00); C114(1.10)  LDD1562  [2]
 LDCM0324  AC60 HEK-293T C114(1.07)  LDD1563  [2]
 LDCM0325  AC61 HEK-293T C46(1.40); C82(1.07)  LDD1564  [2]
 LDCM0326  AC62 HEK-293T C46(1.19); C114(0.98)  LDD1565  [2]
 LDCM0327  AC63 HEK-293T C46(0.91)  LDD1566  [2]
 LDCM0328  AC64 HEK-293T C114(1.05)  LDD1567  [2]
 LDCM0334  AC7 HEK-293T C46(0.93)  LDD1568  [2]
 LDCM0345  AC8 HEK-293T C114(1.00)  LDD1569  [2]
 LDCM0248  AKOS034007472 HEK-293T C46(1.16); C82(1.00)  LDD1511  [2]
 LDCM0356  AKOS034007680 HEK-293T C46(0.97)  LDD1570  [2]
 LDCM0275  AKOS034007705 HEK-293T C114(1.00)  LDD1514  [2]
 LDCM0367  CL1 HEK-293T C46(0.94)  LDD1571  [2]
 LDCM0368  CL10 HEK-293T C46(1.10); C114(1.11)  LDD1572  [2]
 LDCM0369  CL100 HEK-293T C46(1.13)  LDD1573  [2]
 LDCM0370  CL101 HEK-293T C46(1.00)  LDD1574  [2]
 LDCM0371  CL102 HEK-293T C46(0.73)  LDD1575  [2]
 LDCM0372  CL103 HEK-293T C46(0.94)  LDD1576  [2]
 LDCM0373  CL104 HEK-293T C46(0.92)  LDD1577  [2]
 LDCM0374  CL105 HEK-293T C46(1.01)  LDD1578  [2]
 LDCM0375  CL106 HEK-293T C46(0.84)  LDD1579  [2]
 LDCM0376  CL107 HEK-293T C46(0.80)  LDD1580  [2]
 LDCM0377  CL108 HEK-293T C46(0.98)  LDD1581  [2]
 LDCM0378  CL109 HEK-293T C46(0.95)  LDD1582  [2]
 LDCM0379  CL11 HEK-293T C46(0.82)  LDD1583  [2]
 LDCM0380  CL110 HEK-293T C46(1.10)  LDD1584  [2]
 LDCM0381  CL111 HEK-293T C46(0.81)  LDD1585  [2]
 LDCM0382  CL112 HEK-293T C46(1.11)  LDD1586  [2]
 LDCM0383  CL113 HEK-293T C46(0.95)  LDD1587  [2]
 LDCM0384  CL114 HEK-293T C46(1.13)  LDD1588  [2]
 LDCM0385  CL115 HEK-293T C46(1.01)  LDD1589  [2]
 LDCM0386  CL116 HEK-293T C46(1.11)  LDD1590  [2]
 LDCM0387  CL117 HEK-293T C46(0.92)  LDD1591  [2]
 LDCM0388  CL118 HEK-293T C46(0.95)  LDD1592  [2]
 LDCM0389  CL119 HEK-293T C46(0.91)  LDD1593  [2]
 LDCM0390  CL12 HEK-293T C114(1.24)  LDD1594  [2]
 LDCM0391  CL120 HEK-293T C46(0.96)  LDD1595  [2]
 LDCM0392  CL121 HEK-293T C46(1.20)  LDD1596  [2]
 LDCM0393  CL122 HEK-293T C46(0.92)  LDD1597  [2]
 LDCM0394  CL123 HEK-293T C46(0.94)  LDD1598  [2]
 LDCM0395  CL124 HEK-293T C46(0.95)  LDD1599  [2]
 LDCM0396  CL125 HEK-293T C46(0.94)  LDD1600  [2]
 LDCM0397  CL126 HEK-293T C46(1.27)  LDD1601  [2]
 LDCM0398  CL127 HEK-293T C46(0.87)  LDD1602  [2]
 LDCM0399  CL128 HEK-293T C46(1.25)  LDD1603  [2]
 LDCM0400  CL13 HEK-293T C46(0.90)  LDD1604  [2]
 LDCM0401  CL14 HEK-293T C46(1.04)  LDD1605  [2]
 LDCM0402  CL15 HEK-293T C46(0.88)  LDD1606  [2]
 LDCM0403  CL16 HEK-293T C46(0.90)  LDD1607  [2]
 LDCM0404  CL17 HEK-293T C46(1.06)  LDD1608  [2]
 LDCM0405  CL18 HEK-293T C114(1.14)  LDD1609  [2]
 LDCM0406  CL19 HEK-293T C46(1.01); C82(1.17)  LDD1610  [2]
 LDCM0407  CL2 HEK-293T C46(1.22)  LDD1611  [2]
 LDCM0408  CL20 HEK-293T C114(1.10)  LDD1612  [2]
 LDCM0409  CL21 HEK-293T C46(1.01); C82(1.46)  LDD1613  [2]
 LDCM0410  CL22 HEK-293T C46(0.95); C114(1.13)  LDD1614  [2]
 LDCM0411  CL23 HEK-293T C46(0.81)  LDD1615  [2]
 LDCM0412  CL24 HEK-293T C114(1.11)  LDD1616  [2]
 LDCM0413  CL25 HEK-293T C46(0.90)  LDD1617  [2]
 LDCM0414  CL26 HEK-293T C46(0.99)  LDD1618  [2]
 LDCM0415  CL27 HEK-293T C46(0.90)  LDD1619  [2]
 LDCM0416  CL28 HEK-293T C46(0.95)  LDD1620  [2]
 LDCM0417  CL29 HEK-293T C46(0.95)  LDD1621  [2]
 LDCM0418  CL3 HEK-293T C46(0.88)  LDD1622  [2]
 LDCM0419  CL30 HEK-293T C114(1.06)  LDD1623  [2]
 LDCM0420  CL31 HEK-293T C46(0.77); C82(1.05)  LDD1624  [2]
 LDCM0421  CL32 HEK-293T C114(0.99)  LDD1625  [2]
 LDCM0422  CL33 HEK-293T C46(0.92); C82(1.19)  LDD1626  [2]
 LDCM0423  CL34 HEK-293T C46(0.79); C114(1.07)  LDD1627  [2]
 LDCM0424  CL35 HEK-293T C46(0.75)  LDD1628  [2]
 LDCM0425  CL36 HEK-293T C114(1.10)  LDD1629  [2]
 LDCM0426  CL37 HEK-293T C46(0.84)  LDD1630  [2]
 LDCM0428  CL39 HEK-293T C46(1.09)  LDD1632  [2]
 LDCM0429  CL4 HEK-293T C46(1.18)  LDD1633  [2]
 LDCM0430  CL40 HEK-293T C46(0.96)  LDD1634  [2]
 LDCM0431  CL41 HEK-293T C46(0.97)  LDD1635  [2]
 LDCM0432  CL42 HEK-293T C114(1.11)  LDD1636  [2]
 LDCM0433  CL43 HEK-293T C46(0.91); C82(0.93)  LDD1637  [2]
 LDCM0434  CL44 HEK-293T C114(1.03)  LDD1638  [2]
 LDCM0435  CL45 HEK-293T C46(1.28); C82(1.12)  LDD1639  [2]
 LDCM0436  CL46 HEK-293T C46(0.85); C114(1.06)  LDD1640  [2]
 LDCM0437  CL47 HEK-293T C46(0.83)  LDD1641  [2]
 LDCM0438  CL48 HEK-293T C114(1.07)  LDD1642  [2]
 LDCM0439  CL49 HEK-293T C46(0.92)  LDD1643  [2]
 LDCM0440  CL5 HEK-293T C46(1.14)  LDD1644  [2]
 LDCM0441  CL50 HEK-293T C46(0.92)  LDD1645  [2]
 LDCM0443  CL52 HEK-293T C46(1.01)  LDD1646  [2]
 LDCM0444  CL53 HEK-293T C46(1.01)  LDD1647  [2]
 LDCM0445  CL54 HEK-293T C114(1.32)  LDD1648  [2]
 LDCM0446  CL55 HEK-293T C46(0.96); C82(1.02)  LDD1649  [2]
 LDCM0447  CL56 HEK-293T C114(1.16)  LDD1650  [2]
 LDCM0448  CL57 HEK-293T C46(1.12); C82(1.24)  LDD1651  [2]
 LDCM0449  CL58 HEK-293T C46(0.98); C114(1.05)  LDD1652  [2]
 LDCM0450  CL59 HEK-293T C46(0.81)  LDD1653  [2]
 LDCM0451  CL6 HEK-293T C114(1.23)  LDD1654  [2]
 LDCM0452  CL60 HEK-293T C114(1.16)  LDD1655  [2]
 LDCM0453  CL61 HEK-293T C46(1.01)  LDD1656  [2]
 LDCM0454  CL62 HEK-293T C46(1.04)  LDD1657  [2]
 LDCM0455  CL63 HEK-293T C46(1.01)  LDD1658  [2]
 LDCM0456  CL64 HEK-293T C46(0.90)  LDD1659  [2]
 LDCM0457  CL65 HEK-293T C46(0.99)  LDD1660  [2]
 LDCM0458  CL66 HEK-293T C114(1.19)  LDD1661  [2]
 LDCM0459  CL67 HEK-293T C46(1.04); C82(0.95)  LDD1662  [2]
 LDCM0460  CL68 HEK-293T C114(1.15)  LDD1663  [2]
 LDCM0461  CL69 HEK-293T C46(1.14); C82(1.25)  LDD1664  [2]
 LDCM0462  CL7 HEK-293T C46(1.04); C82(1.47)  LDD1665  [2]
 LDCM0463  CL70 HEK-293T C46(0.86); C114(1.03)  LDD1666  [2]
 LDCM0464  CL71 HEK-293T C46(0.87)  LDD1667  [2]
 LDCM0465  CL72 HEK-293T C114(1.24)  LDD1668  [2]
 LDCM0466  CL73 HEK-293T C46(0.92)  LDD1669  [2]
 LDCM0467  CL74 HEK-293T C46(1.05)  LDD1670  [2]
 LDCM0469  CL76 HEK-293T C46(1.00)  LDD1672  [2]
 LDCM0470  CL77 HEK-293T C46(1.02)  LDD1673  [2]
 LDCM0471  CL78 HEK-293T C114(1.08)  LDD1674  [2]
 LDCM0472  CL79 HEK-293T C46(1.11); C82(1.06)  LDD1675  [2]
 LDCM0473  CL8 HEK-293T C114(1.18)  LDD1676  [2]
 LDCM0474  CL80 HEK-293T C114(1.01)  LDD1677  [2]
 LDCM0475  CL81 HEK-293T C46(0.99); C82(1.03)  LDD1678  [2]
 LDCM0476  CL82 HEK-293T C46(1.02); C114(1.05)  LDD1679  [2]
 LDCM0477  CL83 HEK-293T C46(0.78)  LDD1680  [2]
 LDCM0478  CL84 HEK-293T C114(1.15)  LDD1681  [2]
 LDCM0479  CL85 HEK-293T C46(0.77)  LDD1682  [2]
 LDCM0480  CL86 HEK-293T C46(1.09)  LDD1683  [2]
 LDCM0481  CL87 HEK-293T C46(1.09)  LDD1684  [2]
 LDCM0482  CL88 HEK-293T C46(1.01)  LDD1685  [2]
 LDCM0483  CL89 HEK-293T C46(1.00)  LDD1686  [2]
 LDCM0484  CL9 HEK-293T C46(1.00); C82(1.23)  LDD1687  [2]
 LDCM0485  CL90 HEK-293T C114(1.61)  LDD1688  [2]
 LDCM0486  CL91 HEK-293T C46(0.82); C82(1.00)  LDD1689  [2]
 LDCM0487  CL92 HEK-293T C114(1.14)  LDD1690  [2]
 LDCM0488  CL93 HEK-293T C46(0.85); C82(1.08)  LDD1691  [2]
 LDCM0489  CL94 HEK-293T C46(0.98); C114(1.13)  LDD1692  [2]
 LDCM0490  CL95 HEK-293T C46(0.92)  LDD1693  [2]
 LDCM0491  CL96 HEK-293T C114(1.10)  LDD1694  [2]
 LDCM0492  CL97 HEK-293T C46(0.94)  LDD1695  [2]
 LDCM0493  CL98 HEK-293T C46(1.16)  LDD1696  [2]
 LDCM0494  CL99 HEK-293T C46(0.84)  LDD1697  [2]
 LDCM0495  E2913 HEK-293T C46(0.81)  LDD1698  [2]
 LDCM0468  Fragment33 HEK-293T C46(1.01)  LDD1671  [2]
 LDCM0427  Fragment51 HEK-293T C46(0.93)  LDD1631  [2]
 LDCM0022  KB02 HEK-293T C114(0.95); C46(1.02)  LDD1492  [2]
 LDCM0023  KB03 HEK-293T C114(0.97); C46(1.07)  LDD1497  [2]
 LDCM0024  KB05 HEK-293T C114(0.95); C46(1.15)  LDD1502  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Importin subunit alpha-3 (KPNA4) Importin alpha family O00629
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Transcription factor GATA-4 (GATA4) . P43694
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Keratin-associated protein 8-1 (KRTAP8-1) KRTAP type 8 family Q8IUC2

References

1 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
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 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
4 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004