Details of the Target

General Information of Target

Target ID LDTP02199
Target Name Annexin A2 (ANXA2)
Gene Name ANXA2
Gene ID 302
Synonyms
ANX2; ANX2L4; CAL1H; LPC2D; Annexin A2; Annexin II; Annexin-2; Calpactin I heavy chain; Calpactin-1 heavy chain; Chromobindin-8; Lipocortin II; Placental anticoagulant protein IV; PAP-IV; Protein I; p36
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSTVHEILCKLSLEGDHSTPPSAYGSVKAYTNFDAERDALNIETAIKTKGVDEVTIVNIL
TNRSNAQRQDIAFAYQRRTKKELASALKSALSGHLETVILGLLKTPAQYDASELKASMKG
LGTDEDSLIEIICSRTNQELQEINRVYKEMYKTDLEKDIISDTSGDFRKLMVALAKGRRA
EDGSVIDYELIDQDARDLYDAGVKRKGTDVPKWISIMTERSVPHLQKVFDRYKSYSPYDM
LESIRKEVKGDLENAFLNLVQCIQNKPLYFADRLYDSMKGKGTRDKVLIRIMVSRSEVDM
LKIRSEFKRKYGKSLYYYIQQDTKGDYQKALLYLCGGDD
Target Type
Literature-reported
Target Bioclass
Transporter and channel
Family
Annexin family
Subcellular location
Secreted, extracellular space, extracellular matrix, basement membrane
Function
Calcium-regulated membrane-binding protein whose affinity for calcium is greatly enhanced by anionic phospholipids. It binds two calcium ions with high affinity. May be involved in heat-stress response. Inhibits PCSK9-enhanced LDLR degradation, probably reduces PCSK9 protein levels via a translational mechanism but also competes with LDLR for binding with PCSK9.; (Microbial infection) Binds M.pneumoniae CARDS toxin, probably serves as one receptor for this pathogen. When ANXA2 is down-regulated by siRNA, less toxin binds to human cells and less vacuolization (a symptom of M.pneumoniae infection) is seen.
TTD ID
T04386
Uniprot ID
P07355
DrugMap ID
TT4YANI
Ensemble ID
ENST00000332680.8
HGNC ID
HGNC:537
ChEMBL ID
CHEMBL1764938

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CHL1 SNV: p.S2F .
CORL23 SNV: p.A45V .
LNCaP clone FGC SNV: p.G325D .
MFE319 SNV: p.S234R .
NOMO1 SNV: p.L128F .
SNU869 SNV: p.Y147F DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 46 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
A-EBA
 Probe Info  		50.00  LDD0214  [1]
m-APA
 Probe Info  		15.00  LDD0402  [2]
P1
 Probe Info  		1.53  LDD0452  [3]
P2
 Probe Info  		3.26  LDD0449  [3]
P3
 Probe Info  		4.35  LDD0450  [3]
P8
 Probe Info  		3.25  LDD0451  [3]
N1
 Probe Info  		2.11  LDD0242  [4]
TH211
 Probe Info  		Y24(7.98)  LDD0257  [5]
STPyne
 Probe Info  		K115(6.19); K119(4.98); K148(5.30); K152(7.11)  LDD0277  [6]
ONAyne
 Probe Info  		K227(0.00); K148(0.00); K206(0.00); K204(0.00)  LDD0273  [6]
OPA-S-S-alkyne
 Probe Info  		K49(3.95); K281(5.78); K279(5.78); K204(7.37)  LDD3494  [7]
Probe 1
 Probe Info  		Y188(10.54); Y199(25.69); Y275(24.95)  LDD3495  [8]
DBIA
 Probe Info  		C280(7.93)  LDD3312  [9]
JZ128-DTB
 Probe Info  		C133(0.00); C335(0.00)  LDD0462  [10]
BTD
 Probe Info  		C133(0.62)  LDD2126  [11]
AZ-9
 Probe Info  		9.62  LDD2154  [12]
AHL-Pu-1
 Probe Info  		C262(3.34)  LDD0170  [13]
EA-probe
 Probe Info  		N.A.  LDD0440  [14]
HHS-482
 Probe Info  		Y109(0.98); Y188(1.13); Y235(0.64); Y238(0.91)  LDD0285  [15]
HHS-475
 Probe Info  		Y316(0.74); Y317(0.81); Y24(0.86); Y275(0.94)  LDD0264  [16]
HHS-465
 Probe Info  		Y238(10.00); Y24(1.56); Y30(10.00); Y317(5.56)  LDD2237  [17]
ATP probe
 Probe Info  		K227(0.00); K49(0.00); K233(0.00); K279(0.00)  LDD0199  [18]
4-Iodoacetamidophenylacetylene
 Probe Info  		C335(0.00); C262(0.00)  LDD0038  [19]
IA-alkyne
 Probe Info  		C133(0.00); C9(0.00); C335(0.00)  LDD0032  [20]
IPIAA_H
 Probe Info  		N.A.  LDD0030  [21]
IPIAA_L
 Probe Info  		C133(0.00); C262(0.00)  LDD0031  [21]
Lodoacetamide azide
 Probe Info  		C262(0.00); C133(0.00); C335(0.00)  LDD0037  [19]
ATP probe
 Probe Info  		K49(0.00); K227(0.00); K47(0.00); K249(0.00)  LDD0035  [22]
NAIA_4
 Probe Info  		C133(0.00); C262(0.00)  LDD2226  [23]
TFBX
 Probe Info  		C335(0.00); C9(0.00)  LDD0027  [24]
WYneC
 Probe Info  		N.A.  LDD0014  [25]
WYneN
 Probe Info  		C133(0.00); C9(0.00)  LDD0021  [25]
WYneO
 Probe Info  		N.A.  LDD0022  [25]
IPM
 Probe Info  		C9(0.00); C133(0.00)  LDD2156  [26]
NHS
 Probe Info  		K47(0.00); K49(0.00); K302(0.00); K227(0.00)  LDD0010  [25]
PF-06672131
 Probe Info  		C9(0.00); C133(0.00); C335(0.00)  LDD0017  [27]
SF
 Probe Info  		Y30(0.00); Y24(0.00); Y317(0.00); Y238(0.00)  LDD0028  [28]
VSF
 Probe Info  		N.A.  LDD0007  [25]
1c-yne
 Probe Info  		K233(0.00); K49(0.00); K212(0.00); K104(0.00)  LDD0228  [29]
Acrolein
 Probe Info  		C133(0.00); H17(0.00); H94(0.00); C335(0.00)  LDD0217  [30]
Crotonaldehyde
 Probe Info  		H17(0.00); C133(0.00); C335(0.00)  LDD0219  [30]
Methacrolein
 Probe Info  		H17(0.00); C133(0.00); C335(0.00)  LDD0218  [30]
AOyne
 Probe Info  		15.00  LDD0443  [31]
NAIA_5
 Probe Info  		N.A.  LDD2223  [23]
TPP-AC
 Probe Info  		N.A.  LDD0427  [32]
THL-R
 Probe Info  		N.A.  LDD0077  [33]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe13
 Probe Info  		10.56  LDD0475  [34]
FFF probe2
 Probe Info  		8.85  LDD0463  [34]
FFF probe3
 Probe Info  		6.23  LDD0464  [34]
FFF probe6
 Probe Info  		7.49  LDD0482  [34]
STS-1
 Probe Info  		N.A.  LDD0069  [35]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C262(3.34)  LDD0170  [13]
 LDCM0214  AC1 HEK-293T C262(0.95)  LDD1507  [36]
 LDCM0215  AC10 HEK-293T C262(0.91)  LDD1508  [36]
 LDCM0226  AC11 HEK-293T C262(1.04)  LDD1509  [36]
 LDCM0237  AC12 HEK-293T C262(0.93)  LDD1510  [36]
 LDCM0259  AC14 HEK-293T C262(1.21)  LDD1512  [36]
 LDCM0270  AC15 HEK-293T C262(1.01)  LDD1513  [36]
 LDCM0276  AC17 HEK-293T C262(1.04)  LDD1515  [36]
 LDCM0277  AC18 HEK-293T C262(0.91)  LDD1516  [36]
 LDCM0278  AC19 HEK-293T C262(0.82)  LDD1517  [36]
 LDCM0279  AC2 HEK-293T C262(0.95)  LDD1518  [36]
 LDCM0280  AC20 HEK-293T C262(0.96)  LDD1519  [36]
 LDCM0281  AC21 HEK-293T C262(0.96)  LDD1520  [36]
 LDCM0282  AC22 HEK-293T C262(1.16)  LDD1521  [36]
 LDCM0283  AC23 HEK-293T C262(0.99)  LDD1522  [36]
 LDCM0284  AC24 HEK-293T C262(1.02)  LDD1523  [36]
 LDCM0285  AC25 HEK-293T C262(0.87)  LDD1524  [36]
 LDCM0286  AC26 HEK-293T C262(1.01)  LDD1525  [36]
 LDCM0287  AC27 HEK-293T C262(1.03)  LDD1526  [36]
 LDCM0288  AC28 HEK-293T C262(1.00)  LDD1527  [36]
 LDCM0289  AC29 HEK-293T C262(1.07)  LDD1528  [36]
 LDCM0290  AC3 HEK-293T C262(0.94)  LDD1529  [36]
 LDCM0291  AC30 HEK-293T C262(1.18)  LDD1530  [36]
 LDCM0292  AC31 HEK-293T C262(0.95)  LDD1531  [36]
 LDCM0293  AC32 HEK-293T C262(1.03)  LDD1532  [36]
 LDCM0294  AC33 HEK-293T C262(0.92)  LDD1533  [36]
 LDCM0295  AC34 HEK-293T C262(1.01)  LDD1534  [36]
 LDCM0296  AC35 HEK-293T C262(0.89)  LDD1535  [36]
 LDCM0297  AC36 HEK-293T C262(0.95)  LDD1536  [36]
 LDCM0298  AC37 HEK-293T C262(1.01)  LDD1537  [36]
 LDCM0299  AC38 HEK-293T C262(1.10)  LDD1538  [36]
 LDCM0300  AC39 HEK-293T C262(0.91)  LDD1539  [36]
 LDCM0301  AC4 HEK-293T C262(0.93)  LDD1540  [36]
 LDCM0302  AC40 HEK-293T C262(0.97)  LDD1541  [36]
 LDCM0303  AC41 HEK-293T C262(1.03)  LDD1542  [36]
 LDCM0304  AC42 HEK-293T C262(1.07)  LDD1543  [36]
 LDCM0305  AC43 HEK-293T C262(0.97)  LDD1544  [36]
 LDCM0306  AC44 HEK-293T C262(1.03)  LDD1545  [36]
 LDCM0307  AC45 HEK-293T C262(0.97)  LDD1546  [36]
 LDCM0308  AC46 HEK-293T C262(1.08)  LDD1547  [36]
 LDCM0309  AC47 HEK-293T C262(0.98)  LDD1548  [36]
 LDCM0310  AC48 HEK-293T C262(1.15)  LDD1549  [36]
 LDCM0311  AC49 HEK-293T C262(0.87)  LDD1550  [36]
 LDCM0312  AC5 HEK-293T C262(0.95)  LDD1551  [36]
 LDCM0313  AC50 HEK-293T C262(1.09)  LDD1552  [36]
 LDCM0314  AC51 HEK-293T C262(1.04)  LDD1553  [36]
 LDCM0315  AC52 HEK-293T C262(0.97)  LDD1554  [36]
 LDCM0316  AC53 HEK-293T C262(0.96)  LDD1555  [36]
 LDCM0317  AC54 HEK-293T C262(1.15)  LDD1556  [36]
 LDCM0318  AC55 HEK-293T C262(0.94)  LDD1557  [36]
 LDCM0319  AC56 HEK-293T C262(0.99)  LDD1558  [36]
 LDCM0320  AC57 HEK-293T C262(0.97)  LDD1559  [36]
 LDCM0321  AC58 HEK-293T C262(1.13)  LDD1560  [36]
 LDCM0322  AC59 HEK-293T C262(1.20)  LDD1561  [36]
 LDCM0323  AC6 HEK-293T C262(1.06)  LDD1562  [36]
 LDCM0324  AC60 HEK-293T C262(0.98)  LDD1563  [36]
 LDCM0325  AC61 HEK-293T C262(1.01)  LDD1564  [36]
 LDCM0326  AC62 HEK-293T C262(1.10)  LDD1565  [36]
 LDCM0327  AC63 HEK-293T C262(1.02)  LDD1566  [36]
 LDCM0328  AC64 HEK-293T C262(1.05)  LDD1567  [36]
 LDCM0334  AC7 HEK-293T C262(1.00)  LDD1568  [36]
 LDCM0345  AC8 HEK-293T C262(0.98)  LDD1569  [36]
 LDCM0248  AKOS034007472 HEK-293T C262(1.19)  LDD1511  [36]
 LDCM0356  AKOS034007680 HEK-293T C262(0.87)  LDD1570  [36]
 LDCM0275  AKOS034007705 HEK-293T C262(0.94)  LDD1514  [36]
 LDCM0156  Aniline NCI-H1299 12.96  LDD0403  [2]
 LDCM0151  AZ-11 HeLa 9.62  LDD2154  [12]
 LDCM0630  CCW28-3 231MFP C133(1.12); C262(1.04)  LDD2214  [37]
 LDCM0108  Chloroacetamide HeLa H17(0.00); C335(0.00)  LDD0222  [30]
 LDCM0632  CL-Sc Hep-G2 C9(0.79)  LDD2227  [23]
 LDCM0367  CL1 HEK-293T C262(1.13)  LDD1571  [36]
 LDCM0368  CL10 HEK-293T C262(0.66)  LDD1572  [36]
 LDCM0369  CL100 HEK-293T C262(0.82)  LDD1573  [36]
 LDCM0370  CL101 HEK-293T C262(1.06)  LDD1574  [36]
 LDCM0371  CL102 HEK-293T C262(0.96)  LDD1575  [36]
 LDCM0372  CL103 HEK-293T C262(0.85)  LDD1576  [36]
 LDCM0373  CL104 HEK-293T C262(1.03)  LDD1577  [36]
 LDCM0374  CL105 HEK-293T C262(0.98)  LDD1578  [36]
 LDCM0375  CL106 HEK-293T C262(0.99)  LDD1579  [36]
 LDCM0376  CL107 HEK-293T C262(1.01)  LDD1580  [36]
 LDCM0377  CL108 HEK-293T C262(0.99)  LDD1581  [36]
 LDCM0378  CL109 HEK-293T C262(1.17)  LDD1582  [36]
 LDCM0379  CL11 HEK-293T C262(0.95)  LDD1583  [36]
 LDCM0380  CL110 HEK-293T C262(0.86)  LDD1584  [36]
 LDCM0381  CL111 HEK-293T C262(0.85)  LDD1585  [36]
 LDCM0382  CL112 HEK-293T C262(0.80)  LDD1586  [36]
 LDCM0383  CL113 HEK-293T C262(1.03)  LDD1587  [36]
 LDCM0384  CL114 HEK-293T C262(0.91)  LDD1588  [36]
 LDCM0385  CL115 HEK-293T C262(0.92)  LDD1589  [36]
 LDCM0386  CL116 HEK-293T C262(0.90)  LDD1590  [36]
 LDCM0387  CL117 HEK-293T C262(0.97)  LDD1591  [36]
 LDCM0388  CL118 HEK-293T C262(0.95)  LDD1592  [36]
 LDCM0389  CL119 HEK-293T C262(1.01)  LDD1593  [36]
 LDCM0390  CL12 HEK-293T C262(1.01)  LDD1594  [36]
 LDCM0391  CL120 HEK-293T C262(1.09)  LDD1595  [36]
 LDCM0392  CL121 HEK-293T C262(0.95)  LDD1596  [36]
 LDCM0393  CL122 HEK-293T C262(1.15)  LDD1597  [36]
 LDCM0394  CL123 HEK-293T C262(0.86)  LDD1598  [36]
 LDCM0395  CL124 HEK-293T C262(0.87)  LDD1599  [36]
 LDCM0396  CL125 HEK-293T C262(1.10)  LDD1600  [36]
 LDCM0397  CL126 HEK-293T C262(1.15)  LDD1601  [36]
 LDCM0398  CL127 HEK-293T C262(1.10)  LDD1602  [36]
 LDCM0399  CL128 HEK-293T C262(1.02)  LDD1603  [36]
 LDCM0400  CL13 HEK-293T C262(0.87)  LDD1604  [36]
 LDCM0401  CL14 HEK-293T C262(1.05)  LDD1605  [36]
 LDCM0402  CL15 HEK-293T C262(0.77)  LDD1606  [36]
 LDCM0403  CL16 HEK-293T C262(1.08)  LDD1607  [36]
 LDCM0404  CL17 HEK-293T C262(0.18)  LDD1608  [36]
 LDCM0405  CL18 HEK-293T C262(1.03)  LDD1609  [36]
 LDCM0406  CL19 HEK-293T C262(0.89)  LDD1610  [36]
 LDCM0407  CL2 HEK-293T C262(0.82)  LDD1611  [36]
 LDCM0408  CL20 HEK-293T C262(0.92)  LDD1612  [36]
 LDCM0409  CL21 HEK-293T C262(1.05)  LDD1613  [36]
 LDCM0410  CL22 HEK-293T C262(0.76)  LDD1614  [36]
 LDCM0411  CL23 HEK-293T C262(0.94)  LDD1615  [36]
 LDCM0412  CL24 HEK-293T C262(0.97)  LDD1616  [36]
 LDCM0413  CL25 HEK-293T C262(0.96)  LDD1617  [36]
 LDCM0414  CL26 HEK-293T C262(0.88)  LDD1618  [36]
 LDCM0415  CL27 HEK-293T C262(0.96)  LDD1619  [36]
 LDCM0416  CL28 HEK-293T C262(0.95)  LDD1620  [36]
 LDCM0417  CL29 HEK-293T C262(0.69)  LDD1621  [36]
 LDCM0418  CL3 HEK-293T C262(0.98)  LDD1622  [36]
 LDCM0419  CL30 HEK-293T C262(1.10)  LDD1623  [36]
 LDCM0420  CL31 HEK-293T C262(0.87)  LDD1624  [36]
 LDCM0421  CL32 HEK-293T C262(1.09)  LDD1625  [36]
 LDCM0422  CL33 HEK-293T C262(0.91)  LDD1626  [36]
 LDCM0423  CL34 HEK-293T C262(0.74)  LDD1627  [36]
 LDCM0424  CL35 HEK-293T C262(1.01)  LDD1628  [36]
 LDCM0425  CL36 HEK-293T C262(1.03)  LDD1629  [36]
 LDCM0426  CL37 HEK-293T C262(1.06)  LDD1630  [36]
 LDCM0428  CL39 HEK-293T C262(0.88)  LDD1632  [36]
 LDCM0429  CL4 HEK-293T C262(0.82)  LDD1633  [36]
 LDCM0430  CL40 HEK-293T C262(1.06)  LDD1634  [36]
 LDCM0431  CL41 HEK-293T C262(1.12)  LDD1635  [36]
 LDCM0432  CL42 HEK-293T C262(1.14)  LDD1636  [36]
 LDCM0433  CL43 HEK-293T C262(1.10)  LDD1637  [36]
 LDCM0434  CL44 HEK-293T C262(1.10)  LDD1638  [36]
 LDCM0435  CL45 HEK-293T C262(0.80)  LDD1639  [36]
 LDCM0436  CL46 HEK-293T C262(0.87)  LDD1640  [36]
 LDCM0437  CL47 HEK-293T C262(1.12)  LDD1641  [36]
 LDCM0438  CL48 HEK-293T C262(1.11)  LDD1642  [36]
 LDCM0439  CL49 HEK-293T C262(1.07)  LDD1643  [36]
 LDCM0440  CL5 HEK-293T C262(0.80)  LDD1644  [36]
 LDCM0441  CL50 HEK-293T C262(0.79)  LDD1645  [36]
 LDCM0443  CL52 HEK-293T C262(0.85)  LDD1646  [36]
 LDCM0444  CL53 HEK-293T C262(0.87)  LDD1647  [36]
 LDCM0445  CL54 HEK-293T C262(0.90)  LDD1648  [36]
 LDCM0446  CL55 HEK-293T C262(0.95)  LDD1649  [36]
 LDCM0447  CL56 HEK-293T C262(1.18)  LDD1650  [36]
 LDCM0448  CL57 HEK-293T C262(0.94)  LDD1651  [36]
 LDCM0449  CL58 HEK-293T C262(0.74)  LDD1652  [36]
 LDCM0450  CL59 HEK-293T C262(1.07)  LDD1653  [36]
 LDCM0451  CL6 HEK-293T C262(0.78)  LDD1654  [36]
 LDCM0452  CL60 HEK-293T C262(0.69)  LDD1655  [36]
 LDCM0453  CL61 HEK-293T C262(1.25)  LDD1656  [36]
 LDCM0454  CL62 HEK-293T C262(1.13)  LDD1657  [36]
 LDCM0455  CL63 HEK-293T C262(0.90)  LDD1658  [36]
 LDCM0456  CL64 HEK-293T C262(0.89)  LDD1659  [36]
 LDCM0457  CL65 HEK-293T C262(0.97)  LDD1660  [36]
 LDCM0458  CL66 HEK-293T C262(0.93)  LDD1661  [36]
 LDCM0459  CL67 HEK-293T C262(1.01)  LDD1662  [36]
 LDCM0460  CL68 HEK-293T C262(1.06)  LDD1663  [36]
 LDCM0461  CL69 HEK-293T C262(1.21)  LDD1664  [36]
 LDCM0462  CL7 HEK-293T C262(0.78)  LDD1665  [36]
 LDCM0463  CL70 HEK-293T C262(0.83)  LDD1666  [36]
 LDCM0464  CL71 HEK-293T C262(1.04)  LDD1667  [36]
 LDCM0465  CL72 HEK-293T C262(1.03)  LDD1668  [36]
 LDCM0466  CL73 HEK-293T C262(1.05)  LDD1669  [36]
 LDCM0467  CL74 HEK-293T C262(1.02)  LDD1670  [36]
 LDCM0469  CL76 HEK-293T C262(0.92)  LDD1672  [36]
 LDCM0470  CL77 HEK-293T C262(0.89)  LDD1673  [36]
 LDCM0471  CL78 HEK-293T C262(0.97)  LDD1674  [36]
 LDCM0472  CL79 HEK-293T C262(1.23)  LDD1675  [36]
 LDCM0473  CL8 HEK-293T C262(0.92)  LDD1676  [36]
 LDCM0474  CL80 HEK-293T C262(1.20)  LDD1677  [36]
 LDCM0475  CL81 HEK-293T C262(1.13)  LDD1678  [36]
 LDCM0476  CL82 HEK-293T C262(0.91)  LDD1679  [36]
 LDCM0477  CL83 HEK-293T C262(1.15)  LDD1680  [36]
 LDCM0478  CL84 HEK-293T C262(0.99)  LDD1681  [36]
 LDCM0479  CL85 HEK-293T C262(1.17)  LDD1682  [36]
 LDCM0480  CL86 HEK-293T C262(0.99)  LDD1683  [36]
 LDCM0481  CL87 HEK-293T C262(1.02)  LDD1684  [36]
 LDCM0482  CL88 HEK-293T C262(1.03)  LDD1685  [36]
 LDCM0483  CL89 HEK-293T C262(0.94)  LDD1686  [36]
 LDCM0484  CL9 HEK-293T C262(0.98)  LDD1687  [36]
 LDCM0485  CL90 HEK-293T C262(0.68)  LDD1688  [36]
 LDCM0486  CL91 HEK-293T C262(1.05)  LDD1689  [36]
 LDCM0487  CL92 HEK-293T C262(0.96)  LDD1690  [36]
 LDCM0488  CL93 HEK-293T C262(0.91)  LDD1691  [36]
 LDCM0489  CL94 HEK-293T C262(0.91)  LDD1692  [36]
 LDCM0490  CL95 HEK-293T C262(0.85)  LDD1693  [36]
 LDCM0491  CL96 HEK-293T C262(0.99)  LDD1694  [36]
 LDCM0492  CL97 HEK-293T C262(0.89)  LDD1695  [36]
 LDCM0493  CL98 HEK-293T C262(0.90)  LDD1696  [36]
 LDCM0494  CL99 HEK-293T C262(0.93)  LDD1697  [36]
 LDCM0181  Compound 41 HEK-293T 3.17  LDD0502  [34]
 LDCM0634  CY-0357 Hep-G2 C9(0.71)  LDD2228  [23]
 LDCM0495  E2913 HEK-293T C262(0.94)  LDD1698  [36]
 LDCM0175  Ethacrynic acid HeLa N.A.  LDD0440  [14]
 LDCM0625  F8 Ramos C335(0.11)  LDD2187  [38]
 LDCM0572  Fragment10 Ramos C335(0.64)  LDD2189  [38]
 LDCM0573  Fragment11 Ramos C335(20.00)  LDD2190  [38]
 LDCM0574  Fragment12 Ramos C335(0.54)  LDD2191  [38]
 LDCM0575  Fragment13 Ramos C335(0.89)  LDD2192  [38]
 LDCM0576  Fragment14 Ramos C335(0.70)  LDD2193  [38]
 LDCM0579  Fragment20 Ramos C335(0.51)  LDD2194  [38]
 LDCM0580  Fragment21 Ramos C335(0.79)  LDD2195  [38]
 LDCM0582  Fragment23 Ramos C335(1.11)  LDD2196  [38]
 LDCM0578  Fragment27 Ramos C335(0.94)  LDD2197  [38]
 LDCM0588  Fragment30 Ramos C335(0.90)  LDD2199  [38]
 LDCM0589  Fragment31 Ramos C335(1.04)  LDD2200  [38]
 LDCM0590  Fragment32 Ramos C335(0.49)  LDD2201  [38]
 LDCM0468  Fragment33 HEK-293T C262(1.07)  LDD1671  [36]
 LDCM0596  Fragment38 Ramos C335(0.61)  LDD2203  [38]
 LDCM0566  Fragment4 Ramos C335(0.70)  LDD2184  [38]
 LDCM0427  Fragment51 HEK-293T C262(0.95)  LDD1631  [36]
 LDCM0610  Fragment52 Ramos C335(0.94)  LDD2204  [38]
 LDCM0614  Fragment56 Ramos C335(1.08)  LDD2205  [38]
 LDCM0569  Fragment7 Ramos C335(0.58)  LDD2186  [38]
 LDCM0571  Fragment9 Ramos C335(0.60)  LDD2188  [38]
 LDCM0116  HHS-0101 DM93 Y316(0.74); Y317(0.81); Y24(0.86); Y275(0.94)  LDD0264  [16]
 LDCM0117  HHS-0201 DM93 Y316(0.58); Y317(0.68); Y24(0.73); Y275(0.74)  LDD0265  [16]
 LDCM0118  HHS-0301 DM93 Y317(0.70); Y316(0.70); Y235(0.76); Y24(0.80)  LDD0266  [16]
 LDCM0119  HHS-0401 DM93 Y316(0.68); Y317(0.69); Y24(0.73); Y275(0.80)  LDD0267  [16]
 LDCM0120  HHS-0701 DM93 Y316(0.45); Y317(0.60); Y275(0.62); Y24(0.64)  LDD0268  [16]
 LDCM0107  IAA HeLa H17(0.00); C335(0.00); H224(0.00)  LDD0221  [30]
 LDCM0123  JWB131 DM93 Y109(0.98); Y188(1.13); Y235(0.64); Y238(0.91)  LDD0285  [15]
 LDCM0124  JWB142 DM93 Y109(1.31); Y188(1.02); Y235(1.10); Y238(0.91)  LDD0286  [15]
 LDCM0125  JWB146 DM93 Y109(0.90); Y188(1.01); Y235(0.25); Y238(0.88)  LDD0287  [15]
 LDCM0126  JWB150 DM93 Y188(2.38); Y235(0.73); Y238(4.52); Y24(2.83)  LDD0288  [15]
 LDCM0127  JWB152 DM93 Y109(1.37); Y188(2.39); Y235(0.34); Y238(2.46)  LDD0289  [15]
 LDCM0128  JWB198 DM93 Y109(0.17); Y188(1.45); Y235(0.13); Y238(2.14)  LDD0290  [15]
 LDCM0129  JWB202 DM93 Y109(0.72); Y188(1.10); Y235(0.44); Y238(0.91)  LDD0291  [15]
 LDCM0130  JWB211 DM93 Y109(0.44); Y188(0.98); Y235(0.32); Y238(0.98)  LDD0292  [15]
 LDCM0179  JZ128 PC-3 C133(0.00); C335(0.00)  LDD0462  [10]
 LDCM0022  KB02 HEK-293T C335(0.97); C262(1.13)  LDD1492  [36]
 LDCM0023  KB03 HEK-293T C335(0.96); C262(1.02)  LDD1497  [36]
 LDCM0024  KB05 HMCB C280(7.93)  LDD3312  [9]
 LDCM0109  NEM HeLa H17(0.00); C133(0.00); C335(0.00); H94(0.00)  LDD0223  [30]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C133(0.62)  LDD2126  [11]
 LDCM0018  Orlistat Hep-G2 N.A.  LDD0077  [33]
 LDCM0131  RA190 MM1.R C133(1.27); C335(1.24)  LDD0304  [39]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Proprotein convertase subtilisin/kexin type 9 (PCSK9) Peptidase S8 family Q8NBP7
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Annexin A2 (ANXA2) Annexin family P07355
Protein S100-A10 (S100A10) S-100 family P60903
Na(+)/H(+) exchange regulatory cofactor NHE-RF2 (NHERF2) . Q15599
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
DNA mismatch repair protein Mlh1 (MLH1) DNA mismatch repair MutL/HexB family P40692
Proliferating cell nuclear antigen (PCNA) PCNA family P12004
Protection of telomeres protein 1 (POT1) Telombin family Q9NUX5
WAP four-disulfide core domain protein 2 (WFDC2) . Q14508

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tenecteplase BiotechDrug DB00031
Fluocinolone Acetonide Small molecular drug DB00591
Artenimol . DB11638
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Lanoteplase . DB06245

References

1 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
2 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
3 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
4 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
5 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.
6 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
7 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
8 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
9 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
10 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
11 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
12 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
13 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
14 Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function. Mol Pharm. 2018 Jun 4;15(6):2413-2422. doi: 10.1021/acs.molpharmaceut.8b00250. Epub 2018 May 15.
15 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.
16 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
17 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
18 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.
19 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
20 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
21 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
22 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
23 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
24 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
25 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
26 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
27 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
28 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
29 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
30 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.
31 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
32 Differently Tagged Probes for Protein Profiling of Mitochondria. Chembiochem. 2019 May 2;20(9):1155-1160. doi: 10.1002/cbic.201800735. Epub 2019 Mar 26.
33 Activity-based proteome profiling of potential cellular targets of Orlistat--an FDA-approved drug with anti-tumor activities. J Am Chem Soc. 2010 Jan 20;132(2):656-66. doi: 10.1021/ja907716f.
34 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.
35 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
36 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
37 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
38 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
39 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.