General Information of Target

Target ID LDTP04509
Target Name Dual specificity mitogen-activated protein kinase kinase 6 (MAP2K6)
Gene Name MAP2K6
Gene ID 5608
Synonyms
MEK6; MKK6; PRKMK6; SKK3; Dual specificity mitogen-activated protein kinase kinase 6; MAP kinase kinase 6; MAPKK 6; EC 2.7.12.2; MAPK/ERK kinase 6; MEK 6; Stress-activated protein kinase kinase 3; SAPK kinase 3; SAPKK-3; SAPKK3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSQSKGKKRNPGLKIPKEAFEQPQTSSTPPRDLDSKACISIGNQNFEVKADDLEPIMELG
RGAYGVVEKMRHVPSGQIMAVKRIRATVNSQEQKRLLMDLDISMRTVDCPFTVTFYGALF
REGDVWICMELMDTSLDKFYKQVIDKGQTIPEDILGKIAVSIVKALEHLHSKLSVIHRDV
KPSNVLINALGQVKMCDFGISGYLVDSVAKTIDAGCKPYMAPERINPELNQKGYSVKSDI
WSLGITMIELAILRFPYDSWGTPFQQLKQVVEEPSPQLPADKFSAEFVDFTSQCLKKNSK
ERPTYPELMQHPFFTLHESKGTDVASFVKLILGD
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase subfamily
Subcellular location
Nucleus
Function
Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. With MAP3K3/MKK3, catalyzes the concomitant phosphorylation of a threonine and a tyrosine residue in the MAP kinases p38 MAPK11, MAPK12, MAPK13 and MAPK14 and plays an important role in the regulation of cellular responses to cytokines and all kinds of stresses. Especially, MAP2K3/MKK3 and MAP2K6/MKK6 are both essential for the activation of MAPK11 and MAPK13 induced by environmental stress, whereas MAP2K6/MKK6 is the major MAPK11 activator in response to TNF. MAP2K6/MKK6 also phosphorylates and activates PAK6. The p38 MAP kinase signal transduction pathway leads to direct activation of transcription factors. Nuclear targets of p38 MAP kinase include the transcription factors ATF2 and ELK1. Within the p38 MAPK signal transduction pathway, MAP3K6/MKK6 mediates phosphorylation of STAT4 through MAPK14 activation, and is therefore required for STAT4 activation and STAT4-regulated gene expression in response to IL-12 stimulation. The pathway is also crucial for IL-6-induced SOCS3 expression and down-regulation of IL-6-mediated gene induction; and for IFNG-dependent gene transcription. Has a role in osteoclast differentiation through NF-kappa-B transactivation by TNFSF11, and in endochondral ossification and since SOX9 is another likely downstream target of the p38 MAPK pathway. MAP2K6/MKK6 mediates apoptotic cell death in thymocytes. Acts also as a regulator for melanocytes dendricity, through the modulation of Rho family GTPases.
Uniprot ID
P52564
Ensemble ID
ENST00000589647.5
HGNC ID
HGNC:6846
ChEMBL ID
CHEMBL2171

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
SKMEL5 SNV: p.P110L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 17 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info 
C38(5.97); C212(7.03)  LDD3331  [1]
AHL-Pu-1
 Probe Info 
C38(2.13)  LDD0169  [2]
Acrolein
 Probe Info 
N.A.  LDD0221  [3]
AMP probe
 Probe Info 
N.A.  LDD0200  [4]
ATP probe
 Probe Info 
K82(0.00); K181(0.00); K296(0.00)  LDD0199  [4]
IA-alkyne
 Probe Info 
N.A.  LDD0032  [5]
ATP probe
 Probe Info 
K181(0.00); K82(0.00)  LDD0035  [6]
JW-RF-010
 Probe Info 
N.A.  LDD0026  [7]
NAIA_5
 Probe Info 
C38(0.00); C216(0.00)  LDD2225  [8]
TFBX
 Probe Info 
C196(0.00); C216(0.00)  LDD0027  [7]
WYneN
 Probe Info 
N.A.  LDD0021  [9]
IPM
 Probe Info 
C196(0.00); C38(0.00)  LDD0005  [9]
STPyne
 Probe Info 
N.A.  LDD0009  [9]
Phosphinate-6
 Probe Info 
N.A.  LDD0018  [10]
1c-yne
 Probe Info 
N.A.  LDD0228  [11]
AOyne
 Probe Info 
15.00  LDD0443  [12]
HHS-482
 Probe Info 
Y203(1.07)  LDD2239  [13]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA HEK-293T C38(2.13)  LDD0169  [2]
 LDCM0214  AC1 HEK-293T C38(1.02); C109(1.05); C294(0.99)  LDD1507  [14]
 LDCM0215  AC10 HEK-293T C38(0.97); C109(1.04); C216(0.85); C294(1.03)  LDD1508  [14]
 LDCM0226  AC11 HEK-293T C38(0.90); C109(1.10); C294(0.94)  LDD1509  [14]
 LDCM0237  AC12 HEK-293T C38(0.98); C109(1.05); C216(1.03); C294(1.03)  LDD1510  [14]
 LDCM0259  AC14 HEK-293T C38(0.97); C109(1.00); C216(0.86); C294(0.97)  LDD1512  [14]
 LDCM0270  AC15 HEK-293T C38(1.09); C109(1.10); C216(0.96); C294(1.06)  LDD1513  [14]
 LDCM0276  AC17 HEK-293T C38(1.09); C109(0.97); C294(1.10)  LDD1515  [14]
 LDCM0277  AC18 HEK-293T C38(1.07); C109(1.34); C216(0.82); C294(1.28)  LDD1516  [14]
 LDCM0278  AC19 HEK-293T C38(0.91); C109(0.94); C294(0.98)  LDD1517  [14]
 LDCM0279  AC2 HEK-293T C38(1.01); C109(1.02); C216(0.75); C294(1.07)  LDD1518  [14]
 LDCM0280  AC20 HEK-293T C38(1.01); C109(1.02); C216(0.92); C294(1.05)  LDD1519  [14]
 LDCM0281  AC21 HEK-293T C38(0.96); C109(0.96); C216(0.96); C294(0.87)  LDD1520  [14]
 LDCM0282  AC22 HEK-293T C38(1.07); C109(1.02); C216(0.94); C294(1.15)  LDD1521  [14]
 LDCM0283  AC23 HEK-293T C38(1.00); C109(0.91); C216(1.08); C294(0.91)  LDD1522  [14]
 LDCM0284  AC24 HEK-293T C38(1.02); C109(0.88); C216(0.99); C294(0.98)  LDD1523  [14]
 LDCM0285  AC25 HEK-293T C38(0.94); C109(1.04); C294(1.05)  LDD1524  [14]
 LDCM0286  AC26 HEK-293T C38(1.00); C109(1.01); C216(0.82); C294(1.04)  LDD1525  [14]
 LDCM0287  AC27 HEK-293T C38(0.90); C109(1.05); C294(0.96)  LDD1526  [14]
 LDCM0288  AC28 HEK-293T C38(1.02); C109(0.97); C216(0.89); C294(1.64)  LDD1527  [14]
 LDCM0289  AC29 HEK-293T C38(0.96); C109(1.08); C216(0.98); C294(1.04)  LDD1528  [14]
 LDCM0290  AC3 HEK-293T C38(0.94); C109(1.20); C294(1.05)  LDD1529  [14]
 LDCM0291  AC30 HEK-293T C38(1.01); C109(1.08); C216(0.90); C294(1.00)  LDD1530  [14]
 LDCM0292  AC31 HEK-293T C38(0.96); C109(1.20); C216(0.82); C294(1.03)  LDD1531  [14]
 LDCM0293  AC32 HEK-293T C38(0.99); C109(0.98); C216(0.85); C294(0.97)  LDD1532  [14]
 LDCM0294  AC33 HEK-293T C38(0.94); C109(0.91); C294(0.94)  LDD1533  [14]
 LDCM0295  AC34 HEK-293T C38(1.06); C109(0.87); C216(0.69); C294(1.08)  LDD1534  [14]
 LDCM0296  AC35 HEK-293T C38(0.96); C109(1.07); C294(0.93)  LDD1535  [14]
 LDCM0297  AC36 HEK-293T C38(0.93); C109(1.11); C216(1.01); C294(1.02)  LDD1536  [14]
 LDCM0298  AC37 HEK-293T C38(0.98); C109(0.96); C216(0.91); C294(0.91)  LDD1537  [14]
 LDCM0299  AC38 HEK-293T C38(1.00); C109(1.07); C216(0.89); C294(0.94)  LDD1538  [14]
 LDCM0300  AC39 HEK-293T C38(1.01); C109(1.01); C216(1.18); C294(0.97)  LDD1539  [14]
 LDCM0301  AC4 HEK-293T C38(1.03); C109(1.16); C216(1.00); C294(1.06)  LDD1540  [14]
 LDCM0302  AC40 HEK-293T C38(0.92); C109(1.11); C216(1.00); C294(1.32)  LDD1541  [14]
 LDCM0303  AC41 HEK-293T C38(1.04); C109(0.80); C294(0.99)  LDD1542  [14]
 LDCM0304  AC42 HEK-293T C38(1.04); C109(1.35); C216(0.78); C294(1.10)  LDD1543  [14]
 LDCM0305  AC43 HEK-293T C38(0.90); C109(1.09); C294(0.90)  LDD1544  [14]
 LDCM0306  AC44 HEK-293T C38(0.97); C109(1.03); C216(1.07); C294(1.03)  LDD1545  [14]
 LDCM0307  AC45 HEK-293T C38(0.94); C109(0.97); C216(0.99); C294(0.91)  LDD1546  [14]
 LDCM0308  AC46 HEK-293T C38(1.06); C109(1.04); C216(0.97); C294(0.93)  LDD1547  [14]
 LDCM0309  AC47 HEK-293T C38(1.10); C109(0.89); C216(1.18); C294(1.06)  LDD1548  [14]
 LDCM0310  AC48 HEK-293T C38(0.93); C109(1.01); C216(0.94); C294(0.98)  LDD1549  [14]
 LDCM0311  AC49 HEK-293T C38(0.97); C109(0.78); C294(0.96)  LDD1550  [14]
 LDCM0312  AC5 HEK-293T C38(1.05); C109(1.04); C216(0.97); C294(0.98)  LDD1551  [14]
 LDCM0313  AC50 HEK-293T C38(1.01); C109(1.01); C216(0.81); C294(1.11)  LDD1552  [14]
 LDCM0314  AC51 HEK-293T C38(0.91); C109(1.06); C294(1.04)  LDD1553  [14]
 LDCM0315  AC52 HEK-293T C38(0.98); C109(1.17); C216(1.04); C294(1.09)  LDD1554  [14]
 LDCM0316  AC53 HEK-293T C38(0.97); C109(1.04); C216(0.97); C294(0.89)  LDD1555  [14]
 LDCM0317  AC54 HEK-293T C38(0.97); C109(1.06); C216(0.94); C294(0.99)  LDD1556  [14]
 LDCM0318  AC55 HEK-293T C38(0.95); C109(1.13); C216(1.09); C294(1.03)  LDD1557  [14]
 LDCM0319  AC56 HEK-293T C38(1.03); C109(0.95); C216(1.10); C294(0.99)  LDD1558  [14]
 LDCM0320  AC57 HEK-293T C38(1.04); C109(0.91); C294(1.07)  LDD1559  [14]
 LDCM0321  AC58 HEK-293T C38(0.94); C109(1.10); C216(0.80); C294(1.05)  LDD1560  [14]
 LDCM0322  AC59 HEK-293T C38(1.01); C109(1.11); C294(0.96)  LDD1561  [14]
 LDCM0323  AC6 HEK-293T C38(1.05); C109(1.23); C216(1.00); C294(0.91)  LDD1562  [14]
 LDCM0324  AC60 HEK-293T C38(1.05); C109(1.33); C216(1.00); C294(1.03)  LDD1563  [14]
 LDCM0325  AC61 HEK-293T C38(0.99); C109(0.98); C216(0.93); C294(1.19)  LDD1564  [14]
 LDCM0326  AC62 HEK-293T C38(1.03); C109(1.02); C216(0.93); C294(1.05)  LDD1565  [14]
 LDCM0327  AC63 HEK-293T C38(1.03); C109(1.30); C216(0.91); C294(1.04)  LDD1566  [14]
 LDCM0328  AC64 HEK-293T C38(0.96); C109(1.11); C216(0.96); C294(1.00)  LDD1567  [14]
 LDCM0334  AC7 HEK-293T C38(1.05); C109(0.87); C216(0.91); C294(1.04)  LDD1568  [14]
 LDCM0345  AC8 HEK-293T C38(1.00); C109(0.97); C216(0.92); C294(1.02)  LDD1569  [14]
 LDCM0248  AKOS034007472 HEK-293T C38(0.92); C109(0.97); C216(0.98); C294(0.92)  LDD1511  [14]
 LDCM0356  AKOS034007680 HEK-293T C38(1.03); C109(0.89); C294(0.95)  LDD1570  [14]
 LDCM0275  AKOS034007705 HEK-293T C38(1.02); C109(1.05); C216(1.02); C294(1.10)  LDD1514  [14]
 LDCM0632  CL-Sc Hep-G2 C216(1.42)  LDD2227  [8]
 LDCM0367  CL1 HEK-293T C38(0.95); C109(1.10)  LDD1571  [14]
 LDCM0368  CL10 HEK-293T C38(0.94); C109(1.13); C216(0.79); C294(0.96)  LDD1572  [14]
 LDCM0369  CL100 HEK-293T C38(0.97); C109(1.06); C216(0.90); C294(1.03)  LDD1573  [14]
 LDCM0370  CL101 HEK-293T C38(0.97); C109(0.90)  LDD1574  [14]
 LDCM0371  CL102 HEK-293T C38(0.93); C109(1.15); C216(1.07); C294(1.00)  LDD1575  [14]
 LDCM0372  CL103 HEK-293T C38(0.89); C109(1.08); C216(0.91); C294(0.94)  LDD1576  [14]
 LDCM0373  CL104 HEK-293T C38(0.84); C109(1.05); C216(0.81); C294(1.05)  LDD1577  [14]
 LDCM0374  CL105 HEK-293T C38(0.95); C109(0.67)  LDD1578  [14]
 LDCM0375  CL106 HEK-293T C38(0.93); C109(0.92); C216(0.91); C294(0.98)  LDD1579  [14]
 LDCM0376  CL107 HEK-293T C38(0.96); C109(0.92); C216(0.92); C294(1.00)  LDD1580  [14]
 LDCM0377  CL108 HEK-293T C38(0.94); C109(1.03); C216(0.95); C294(1.08)  LDD1581  [14]
 LDCM0378  CL109 HEK-293T C38(0.92); C109(0.97)  LDD1582  [14]
 LDCM0379  CL11 HEK-293T C38(0.93); C109(1.12); C216(1.26); C294(1.01)  LDD1583  [14]
 LDCM0380  CL110 HEK-293T C38(0.85); C109(0.95); C216(0.91); C294(0.98)  LDD1584  [14]
 LDCM0381  CL111 HEK-293T C38(0.87); C109(0.95); C216(0.91); C294(1.00)  LDD1585  [14]
 LDCM0382  CL112 HEK-293T C38(0.92); C109(1.00); C216(0.90); C294(1.06)  LDD1586  [14]
 LDCM0383  CL113 HEK-293T C38(0.99); C109(1.03)  LDD1587  [14]
 LDCM0384  CL114 HEK-293T C38(0.91); C109(1.00); C216(1.07); C294(0.98)  LDD1588  [14]
 LDCM0385  CL115 HEK-293T C38(0.89); C109(0.99); C216(1.05); C294(1.06)  LDD1589  [14]
 LDCM0386  CL116 HEK-293T C38(0.92); C109(1.00); C216(0.90); C294(1.03)  LDD1590  [14]
 LDCM0387  CL117 HEK-293T C38(0.94); C109(0.97)  LDD1591  [14]
 LDCM0388  CL118 HEK-293T C38(0.87); C109(1.02); C216(1.11); C294(0.88)  LDD1592  [14]
 LDCM0389  CL119 HEK-293T C38(0.91); C109(0.90); C216(1.08); C294(1.07)  LDD1593  [14]
 LDCM0390  CL12 HEK-293T C38(1.10); C109(1.01); C216(0.31); C294(1.04)  LDD1594  [14]
 LDCM0391  CL120 HEK-293T C38(1.00); C109(0.96); C216(0.92); C294(1.05)  LDD1595  [14]
 LDCM0392  CL121 HEK-293T C38(0.97); C109(1.01)  LDD1596  [14]
 LDCM0393  CL122 HEK-293T C38(0.88); C109(1.41); C216(1.04); C294(1.16)  LDD1597  [14]
 LDCM0394  CL123 HEK-293T C38(0.90); C109(0.94); C216(0.96); C294(0.96)  LDD1598  [14]
 LDCM0395  CL124 HEK-293T C38(0.89); C109(0.98); C216(0.92); C294(1.06)  LDD1599  [14]
 LDCM0396  CL125 HEK-293T C38(0.98); C109(0.98)  LDD1600  [14]
 LDCM0397  CL126 HEK-293T C38(1.00); C109(0.98); C216(1.11); C294(0.90)  LDD1601  [14]
 LDCM0398  CL127 HEK-293T C38(0.94); C109(0.90); C216(0.98); C294(0.98)  LDD1602  [14]
 LDCM0399  CL128 HEK-293T C38(0.86); C109(0.96); C216(0.92); C294(1.14)  LDD1603  [14]
 LDCM0400  CL13 HEK-293T C38(1.02); C109(1.20)  LDD1604  [14]
 LDCM0401  CL14 HEK-293T C38(0.93); C109(0.99); C216(0.91); C294(0.91)  LDD1605  [14]
 LDCM0402  CL15 HEK-293T C38(0.82); C109(1.19); C216(0.86); C294(1.21)  LDD1606  [14]
 LDCM0403  CL16 HEK-293T C38(1.04); C109(0.99); C216(0.82); C294(1.01)  LDD1607  [14]
 LDCM0404  CL17 HEK-293T C38(0.94); C109(1.20); C294(0.93)  LDD1608  [14]
 LDCM0405  CL18 HEK-293T C38(1.07); C109(1.10); C216(0.84); C294(1.13)  LDD1609  [14]
 LDCM0406  CL19 HEK-293T C38(1.07); C109(1.24); C294(1.04)  LDD1610  [14]
 LDCM0407  CL2 HEK-293T C38(0.88); C109(1.06); C216(0.99); C294(0.95)  LDD1611  [14]
 LDCM0408  CL20 HEK-293T C38(1.02); C109(1.05); C216(1.08); C294(1.05)  LDD1612  [14]
 LDCM0409  CL21 HEK-293T C38(0.90); C109(1.11); C216(0.63); C294(0.83)  LDD1613  [14]
 LDCM0410  CL22 HEK-293T C38(1.09); C109(0.99); C216(0.64); C294(0.93)  LDD1614  [14]
 LDCM0411  CL23 HEK-293T C38(0.98); C109(1.02); C216(1.44); C294(0.94)  LDD1615  [14]
 LDCM0412  CL24 HEK-293T C38(1.09); C109(1.03); C216(0.26); C294(1.01)  LDD1616  [14]
 LDCM0413  CL25 HEK-293T C38(0.92); C109(1.42)  LDD1617  [14]
 LDCM0414  CL26 HEK-293T C38(0.89); C109(1.16); C216(0.95); C294(1.12)  LDD1618  [14]
 LDCM0415  CL27 HEK-293T C38(0.94); C109(1.01); C216(0.95); C294(0.96)  LDD1619  [14]
 LDCM0416  CL28 HEK-293T C38(0.96); C109(1.12); C216(0.82); C294(1.02)  LDD1620  [14]
 LDCM0417  CL29 HEK-293T C38(0.95); C109(0.75); C294(1.03)  LDD1621  [14]
 LDCM0418  CL3 HEK-293T C38(0.92); C109(1.26); C216(0.91); C294(1.05)  LDD1622  [14]
 LDCM0419  CL30 HEK-293T C38(1.01); C109(1.05); C216(0.85); C294(1.16)  LDD1623  [14]
 LDCM0420  CL31 HEK-293T C38(0.93); C109(1.06); C294(0.99)  LDD1624  [14]
 LDCM0421  CL32 HEK-293T C38(0.95); C109(1.18); C216(1.05); C294(1.01)  LDD1625  [14]
 LDCM0422  CL33 HEK-293T C38(0.90); C109(0.96); C216(0.59); C294(0.92)  LDD1626  [14]
 LDCM0423  CL34 HEK-293T C38(0.98); C109(0.93); C216(0.61); C294(1.03)  LDD1627  [14]
 LDCM0424  CL35 HEK-293T C38(1.08); C109(0.82); C216(1.22); C294(1.16)  LDD1628  [14]
 LDCM0425  CL36 HEK-293T C38(1.00); C109(1.01); C216(0.23); C294(1.04)  LDD1629  [14]
 LDCM0426  CL37 HEK-293T C38(0.95); C109(1.07)  LDD1630  [14]
 LDCM0428  CL39 HEK-293T C38(0.89); C109(1.40); C216(0.87); C294(1.04)  LDD1632  [14]
 LDCM0429  CL4 HEK-293T C38(0.93); C109(1.08); C216(0.82); C294(1.06)  LDD1633  [14]
 LDCM0430  CL40 HEK-293T C38(1.02); C109(0.94); C216(0.87); C294(1.03)  LDD1634  [14]
 LDCM0431  CL41 HEK-293T C38(0.99); C109(1.21); C294(1.09)  LDD1635  [14]
 LDCM0432  CL42 HEK-293T C38(1.06); C109(1.06); C216(0.88); C294(1.05)  LDD1636  [14]
 LDCM0433  CL43 HEK-293T C38(0.94); C109(1.07); C294(0.91)  LDD1637  [14]
 LDCM0434  CL44 HEK-293T C38(1.02); C109(0.96); C216(1.05); C294(1.09)  LDD1638  [14]
 LDCM0435  CL45 HEK-293T C38(0.97); C109(1.05); C216(0.76); C294(0.94)  LDD1639  [14]
 LDCM0436  CL46 HEK-293T C38(1.02); C109(0.96); C216(0.65); C294(0.82)  LDD1640  [14]
 LDCM0437  CL47 HEK-293T C38(1.03); C109(0.93); C216(1.22); C294(1.25)  LDD1641  [14]
 LDCM0438  CL48 HEK-293T C38(0.97); C109(1.07); C216(0.21); C294(1.04)  LDD1642  [14]
 LDCM0439  CL49 HEK-293T C38(0.87); C109(1.30)  LDD1643  [14]
 LDCM0440  CL5 HEK-293T C38(1.07); C109(1.02); C294(1.04)  LDD1644  [14]
 LDCM0441  CL50 HEK-293T C38(0.88); C109(0.95); C216(1.01); C294(0.87)  LDD1645  [14]
 LDCM0443  CL52 HEK-293T C38(0.94); C109(1.03); C216(0.85); C294(1.03)  LDD1646  [14]
 LDCM0444  CL53 HEK-293T C38(1.02); C109(1.17); C294(0.97)  LDD1647  [14]
 LDCM0445  CL54 HEK-293T C38(1.01); C109(1.45); C216(0.69); C294(0.96)  LDD1648  [14]
 LDCM0446  CL55 HEK-293T C38(0.95); C109(1.04); C294(0.91)  LDD1649  [14]
 LDCM0447  CL56 HEK-293T C38(1.00); C109(1.07); C216(1.21); C294(0.99)  LDD1650  [14]
 LDCM0448  CL57 HEK-293T C38(0.93); C109(1.07); C216(0.70); C294(0.98)  LDD1651  [14]
 LDCM0449  CL58 HEK-293T C38(1.01); C109(0.96); C216(0.64); C294(0.94)  LDD1652  [14]
 LDCM0450  CL59 HEK-293T C38(0.97); C109(1.01); C216(1.42); C294(1.02)  LDD1653  [14]
 LDCM0451  CL6 HEK-293T C38(1.02); C109(0.99); C216(0.81); C294(1.07)  LDD1654  [14]
 LDCM0452  CL60 HEK-293T C38(0.99); C109(1.06); C216(0.24); C294(1.02)  LDD1655  [14]
 LDCM0453  CL61 HEK-293T C38(0.92); C109(0.91)  LDD1656  [14]
 LDCM0454  CL62 HEK-293T C38(1.00); C109(1.04); C216(1.11); C294(0.98)  LDD1657  [14]
 LDCM0455  CL63 HEK-293T C38(0.90); C109(0.84); C216(0.97); C294(1.07)  LDD1658  [14]
 LDCM0456  CL64 HEK-293T C38(0.90); C109(1.09); C216(0.80); C294(1.03)  LDD1659  [14]
 LDCM0457  CL65 HEK-293T C38(0.98); C109(1.14); C294(0.97)  LDD1660  [14]
 LDCM0458  CL66 HEK-293T C38(1.05); C109(1.08); C216(0.80); C294(1.11)  LDD1661  [14]
 LDCM0459  CL67 HEK-293T C38(0.92); C109(1.17); C294(0.90)  LDD1662  [14]
 LDCM0460  CL68 HEK-293T C38(0.97); C109(1.14); C216(1.15); C294(1.05)  LDD1663  [14]
 LDCM0461  CL69 HEK-293T C38(0.92); C109(1.17); C216(0.69); C294(0.86)  LDD1664  [14]
 LDCM0462  CL7 HEK-293T C38(0.95); C109(1.22); C294(1.10)  LDD1665  [14]
 LDCM0463  CL70 HEK-293T C38(1.03); C109(1.06); C216(0.70); C294(1.17)  LDD1666  [14]
 LDCM0464  CL71 HEK-293T C38(1.01); C109(1.13); C216(1.22); C294(1.06)  LDD1667  [14]
 LDCM0465  CL72 HEK-293T C38(1.00); C109(1.05); C216(0.31); C294(0.97)  LDD1668  [14]
 LDCM0466  CL73 HEK-293T C38(0.91); C109(1.00)  LDD1669  [14]
 LDCM0467  CL74 HEK-293T C38(0.90); C109(1.02); C216(1.02); C294(0.95)  LDD1670  [14]
 LDCM0469  CL76 HEK-293T C38(1.04); C109(0.99); C216(0.90); C294(1.03)  LDD1672  [14]
 LDCM0470  CL77 HEK-293T C38(0.93); C109(1.13); C294(1.01)  LDD1673  [14]
 LDCM0471  CL78 HEK-293T C38(1.05); C109(1.01); C216(0.73); C294(1.08)  LDD1674  [14]
 LDCM0472  CL79 HEK-293T C38(0.98); C109(1.20); C294(0.95)  LDD1675  [14]
 LDCM0473  CL8 HEK-293T C38(0.79); C109(1.22); C216(1.04); C294(1.35)  LDD1676  [14]
 LDCM0474  CL80 HEK-293T C38(0.90); C109(1.12); C216(1.15); C294(1.03)  LDD1677  [14]
 LDCM0475  CL81 HEK-293T C38(1.00); C109(0.99); C216(0.75); C294(0.82)  LDD1678  [14]
 LDCM0476  CL82 HEK-293T C38(1.06); C109(1.17); C216(0.76); C294(1.05)  LDD1679  [14]
 LDCM0477  CL83 HEK-293T C38(0.97); C109(0.90); C216(1.22); C294(1.07)  LDD1680  [14]
 LDCM0478  CL84 HEK-293T C38(1.00); C109(1.05); C216(0.40); C294(1.04)  LDD1681  [14]
 LDCM0479  CL85 HEK-293T C38(0.90); C109(1.23)  LDD1682  [14]
 LDCM0480  CL86 HEK-293T C38(0.90); C109(1.03); C216(1.14); C294(0.99)  LDD1683  [14]
 LDCM0481  CL87 HEK-293T C38(0.89); C109(1.38); C216(1.05); C294(1.01)  LDD1684  [14]
 LDCM0482  CL88 HEK-293T C38(1.00); C109(1.16); C216(0.90); C294(1.07)  LDD1685  [14]
 LDCM0483  CL89 HEK-293T C38(1.01); C109(0.85); C294(1.01)  LDD1686  [14]
 LDCM0484  CL9 HEK-293T C38(1.01); C109(1.25); C216(0.68); C294(0.91)  LDD1687  [14]
 LDCM0485  CL90 HEK-293T C38(0.86); C109(1.30); C216(0.75); C294(1.21)  LDD1688  [14]
 LDCM0486  CL91 HEK-293T C38(0.89); C109(1.11); C294(0.94)  LDD1689  [14]
 LDCM0487  CL92 HEK-293T C38(0.97); C109(1.24); C216(1.08); C294(1.11)  LDD1690  [14]
 LDCM0488  CL93 HEK-293T C38(0.98); C109(1.00); C216(0.78); C294(0.82)  LDD1691  [14]
 LDCM0489  CL94 HEK-293T C38(1.05); C109(1.04); C216(0.83); C294(0.93)  LDD1692  [14]
 LDCM0490  CL95 HEK-293T C38(0.89); C109(0.69); C216(1.29); C294(0.92)  LDD1693  [14]
 LDCM0491  CL96 HEK-293T C38(0.96); C109(1.37); C216(0.62); C294(0.91)  LDD1694  [14]
 LDCM0492  CL97 HEK-293T C38(0.95); C109(1.49)  LDD1695  [14]
 LDCM0493  CL98 HEK-293T C38(0.90); C109(1.12); C216(1.10); C294(0.86)  LDD1696  [14]
 LDCM0494  CL99 HEK-293T C38(0.92); C109(0.98); C216(1.09); C294(0.94)  LDD1697  [14]
 LDCM0495  E2913 HEK-293T C38(0.86); C109(1.22); C216(1.07); C294(1.03)  LDD1698  [14]
 LDCM0625  F8 Ramos C38(1.17); C216(1.87); C196(0.74)  LDD2187  [15]
 LDCM0572  Fragment10 Ramos C38(1.14); C216(2.44); C196(0.70)  LDD2189  [15]
 LDCM0573  Fragment11 Ramos C38(18.22); C216(0.20); C196(6.10)  LDD2190  [15]
 LDCM0574  Fragment12 Ramos C38(1.13); C216(1.13); C196(1.11)  LDD2191  [15]
 LDCM0575  Fragment13 Ramos C38(1.15); C216(1.05); C196(0.63)  LDD2192  [15]
 LDCM0576  Fragment14 Ramos C38(1.37); C216(1.15); C196(1.25)  LDD2193  [15]
 LDCM0579  Fragment20 Ramos C38(1.24); C216(1.20)  LDD2194  [15]
 LDCM0580  Fragment21 Ramos C38(0.96); C216(0.96); C196(0.64)  LDD2195  [15]
 LDCM0582  Fragment23 Ramos C38(1.40); C216(1.65); C196(0.96)  LDD2196  [15]
 LDCM0578  Fragment27 Ramos C38(1.05); C216(0.93); C196(0.75)  LDD2197  [15]
 LDCM0586  Fragment28 Ramos C38(0.83); C216(0.87); C196(0.90)  LDD2198  [15]
 LDCM0588  Fragment30 Ramos C38(0.97); C216(1.31); C196(0.66)  LDD2199  [15]
 LDCM0589  Fragment31 Ramos C38(0.91); C216(0.99); C196(0.70)  LDD2200  [15]
 LDCM0590  Fragment32 Ramos C38(1.16); C216(2.46); C196(1.08)  LDD2201  [15]
 LDCM0468  Fragment33 HEK-293T C38(0.93); C109(0.89); C216(0.95); C294(1.03)  LDD1671  [14]
 LDCM0596  Fragment38 Ramos C38(0.74); C216(0.90); C196(0.50)  LDD2203  [15]
 LDCM0566  Fragment4 Ramos C38(0.79); C216(1.09); C196(0.89)  LDD2184  [15]
 LDCM0427  Fragment51 HEK-293T C38(0.87); C109(0.96); C216(0.95); C294(0.96)  LDD1631  [14]
 LDCM0610  Fragment52 Ramos C38(0.89); C216(1.19); C196(0.48)  LDD2204  [15]
 LDCM0614  Fragment56 Ramos C38(0.95); C216(1.15); C196(0.46)  LDD2205  [15]
 LDCM0569  Fragment7 Ramos C38(1.34); C216(1.89)  LDD2186  [15]
 LDCM0571  Fragment9 Ramos C38(1.27); C216(1.38); C196(0.45)  LDD2188  [15]
 LDCM0107  IAA HeLa N.A.  LDD0221  [3]
 LDCM0022  KB02 HEK-293T C216(1.00); C38(1.00); C294(0.94); C109(0.89)  LDD1492  [14]
 LDCM0023  KB03 HEK-293T C216(1.02); C38(0.92); C294(0.95); C109(1.02)  LDD1497  [14]
 LDCM0024  KB05 MKN-1 C38(5.97); C212(7.03)  LDD3331  [1]
 LDCM0109  NEM HeLa N.A.  LDD0233  [3]
 LDCM0627  NUDT7-COV-1 HEK-293T C216(1.66); C196(0.91)  LDD2206  [16]
 LDCM0628  OTUB2-COV-1 HEK-293T C216(1.12); C196(0.82)  LDD2207  [16]

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
Mitogen-activated protein kinase 14 (MAPK14) CMGC Ser/Thr protein kinase family Q16539
Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) TKL Ser/Thr protein kinase family Q5S007
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Wolframin (WFS1) . O76024
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nuclear factor erythroid 2-related factor 2 (NFE2L2) BZIP family Q16236
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
PRKCA-binding protein (PICK1) . Q9NRD5

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

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 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
3 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.
4 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.
5 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
6 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
7 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
8 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
9 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
10 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
11 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.
12 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.
13 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.
14 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
15 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
16 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.