Details of the Target

General Information of Target

Target ID LDTP04077
Target Name Dual specificity mitogen-activated protein kinase kinase 4 (MAP2K4)
Gene Name MAP2K4
Gene ID 6416
Synonyms
JNKK1; MEK4; MKK4; PRKMK4; SEK1; SERK1; SKK1; Dual specificity mitogen-activated protein kinase kinase 4; MAP kinase kinase 4; MAPKK 4; EC 2.7.12.2; JNK-activating kinase 1; MAPK/ERK kinase 4; MEK 4; SAPK/ERK kinase 1; SEK1; Stress-activated protein kinase kinase 1; SAPK kinase 1; SAPKK-1; SAPKK1; c-Jun N-terminal kinase kinase 1; JNKK
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAAPSPSGGGGSGGGSGSGTPGPVGSPAPGHPAVSSMQGKRKALKLNFANPPFKSTARFT
LNPNPTGVQNPHIERLRTHSIESSGKLKISPEQHWDFTAEDLKDLGEIGRGAYGSVNKMV
HKPSGQIMAVKRIRSTVDEKEQKQLLMDLDVVMRSSDCPYIVQFYGALFREGDCWICMEL
MSTSFDKFYKYVYSVLDDVIPEEILGKITLATVKALNHLKENLKIIHRDIKPSNILLDRS
GNIKLCDFGISGQLVDSIAKTRDAGCRPYMAPERIDPSASRQGYDVRSDVWSLGITLYEL
ATGRFPYPKWNSVFDQLTQVVKGDPPQLSNSEEREFSPSFINFVNLCLTKDESKRPKYKE
LLKHPFILMYEERAVEVACYVCKILDQMPATPSSPMYVD
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase subfamily
Subcellular location
Cytoplasm
Function
Dual specificity protein kinase which acts as an essential component of the MAP kinase signal transduction pathway. Essential component of the stress-activated protein kinase/c-Jun N-terminal kinase (SAP/JNK) signaling pathway. With MAP2K7/MKK7, is the one of the only known kinase to directly activate the stress-activated protein kinase/c-Jun N-terminal kinases MAPK8/JNK1, MAPK9/JNK2 and MAPK10/JNK3. MAP2K4/MKK4 and MAP2K7/MKK7 both activate the JNKs by phosphorylation, but they differ in their preference for the phosphorylation site in the Thr-Pro-Tyr motif. MAP2K4 shows preference for phosphorylation of the Tyr residue and MAP2K7/MKK7 for the Thr residue. The phosphorylation of the Thr residue by MAP2K7/MKK7 seems to be the prerequisite for JNK activation at least in response to pro-inflammatory cytokines, while other stimuli activate both MAP2K4/MKK4 and MAP2K7/MKK7 which synergistically phosphorylate JNKs. MAP2K4 is required for maintaining peripheral lymphoid homeostasis. The MKK/JNK signaling pathway is also involved in mitochondrial death signaling pathway, including the release cytochrome c, leading to apoptosis. Whereas MAP2K7/MKK7 exclusively activates JNKs, MAP2K4/MKK4 additionally activates the p38 MAPKs MAPK11, MAPK12, MAPK13 and MAPK14.
Uniprot ID
P45985
Ensemble ID
ENST00000353533.10
HGNC ID
HGNC:6844
ChEMBL ID
CHEMBL2897

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL51 SNV: p.G265D DBIA    Probe Info 
ECC2 Deletion: p.N222TfsTer2 .
HCT15 SNV: p.L385M .
HLF SNV: p.G14S DBIA    Probe Info 
IGR1 SNV: p.S80I DBIA    Probe Info 
Ishikawa (Heraklio) 02 ER Deletion: p.N70TfsTer4
SNV: p.R134Q		 DBIA    Probe Info 
JVM3 SNV: p.I384T DBIA    Probe Info 
MELHO SNV: p.I384S DBIA    Probe Info 
MFE319 SNV: p.L216P; p.P325H .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 20 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
STPyne
 Probe Info  		K220(4.13); K45(1.84)  LDD0277  [2]
AHL-Pu-1
 Probe Info  		C379(6.61)  LDD0170  [3]
EA-probe
 Probe Info  		C246(0.90)  LDD2210  [4]
DBIA
 Probe Info  		C266(15.37); C246(4.34)  LDD0209  [5]
AMP probe
 Probe Info  		N.A.  LDD0200  [6]
ATP probe
 Probe Info  		K231(0.00); K88(0.00)  LDD0199  [6]
4-Iodoacetamidophenylacetylene
 Probe Info  		C347(0.00); C246(0.00); C158(0.00)  LDD0038  [7]
IA-alkyne
 Probe Info  		C266(0.00); C246(0.00); C158(0.00); C347(0.00)  LDD0036  [7]
Lodoacetamide azide
 Probe Info  		C347(0.00); C246(0.00); C158(0.00); C266(0.00)  LDD0037  [7]
ATP probe
 Probe Info  		N.A.  LDD0035  [8]
JW-RF-010
 Probe Info  		C246(0.00); C266(0.00)  LDD0026  [9]
NAIA_4
 Probe Info  		C246(0.00); C266(0.00)  LDD2226  [10]
WYneN
 Probe Info  		N.A.  LDD0021  [11]
IPM
 Probe Info  		N.A.  LDD0005  [11]
TFBX
 Probe Info  		C246(0.00); C266(0.00)  LDD0148  [9]
Phosphinate-6
 Probe Info  		C266(0.00); C246(0.00)  LDD0018  [12]
1c-yne
 Probe Info  		N.A.  LDD0228  [13]
AOyne
 Probe Info  		15.00  LDD0443  [14]
NAIA_5
 Probe Info  		C266(0.00); C347(0.00); C246(0.00)  LDD2223  [10]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C379(6.61)  LDD0170  [3]
 LDCM0026  4SU-RNA+native RNA DM93 C379(7.01)  LDD0171  [3]
 LDCM0214  AC1 HEK-293T C266(1.19); C246(1.25); C158(1.07); C347(0.82)  LDD1507  [15]
 LDCM0215  AC10 HEK-293T C266(0.96); C246(0.99); C158(1.02); C347(0.94)  LDD1508  [15]
 LDCM0226  AC11 HEK-293T C266(0.78); C246(1.01); C158(1.00); C347(1.02)  LDD1509  [15]
 LDCM0237  AC12 HEK-293T C266(0.95); C246(0.97); C158(1.14); C347(1.03)  LDD1510  [15]
 LDCM0259  AC14 HEK-293T C266(0.96); C246(0.97); C158(0.99); C347(1.03)  LDD1512  [15]
 LDCM0270  AC15 HEK-293T C266(0.86); C246(1.04); C158(1.00); C347(0.98)  LDD1513  [15]
 LDCM0276  AC17 HEK-293T C266(0.93); C246(1.09); C158(1.05); C347(0.99)  LDD1515  [15]
 LDCM0277  AC18 HEK-293T C266(1.10); C246(1.19); C158(1.13); C347(0.83)  LDD1516  [15]
 LDCM0278  AC19 HEK-293T C266(0.83); C246(0.97); C158(1.04); C347(0.93)  LDD1517  [15]
 LDCM0279  AC2 HEK-293T C266(1.26); C246(0.97); C158(0.90); C347(0.93)  LDD1518  [15]
 LDCM0280  AC20 HEK-293T C266(0.91); C246(0.96); C158(0.98); C347(0.97)  LDD1519  [15]
 LDCM0281  AC21 HEK-293T C266(0.91); C246(1.01); C158(1.02); C347(0.91)  LDD1520  [15]
 LDCM0282  AC22 HEK-293T C266(0.88); C246(0.97); C158(1.07); C347(1.00)  LDD1521  [15]
 LDCM0283  AC23 HEK-293T C266(0.83); C246(0.98); C158(0.95); C347(1.00)  LDD1522  [15]
 LDCM0284  AC24 HEK-293T C266(0.97); C246(0.94); C158(0.92); C347(1.19)  LDD1523  [15]
 LDCM0285  AC25 HEK-293T C266(0.98); C246(1.05); C158(1.12); C347(0.92)  LDD1524  [15]
 LDCM0286  AC26 HEK-293T C266(1.03); C246(0.98); C158(0.91); C347(0.92)  LDD1525  [15]
 LDCM0287  AC27 HEK-293T C266(0.85); C246(1.02); C158(0.93); C347(1.03)  LDD1526  [15]
 LDCM0288  AC28 HEK-293T C266(1.08); C246(4.84); C158(0.89); C347(1.20)  LDD1527  [15]
 LDCM0289  AC29 HEK-293T C266(0.96); C246(1.01); C158(0.96); C347(0.92)  LDD1528  [15]
 LDCM0290  AC3 HEK-293T C266(1.20); C246(0.98); C158(1.02); C347(1.03)  LDD1529  [15]
 LDCM0291  AC30 HEK-293T C266(0.87); C246(0.89); C158(1.06); C347(1.04)  LDD1530  [15]
 LDCM0292  AC31 HEK-293T C266(0.96); C246(0.98); C158(0.95); C347(0.99)  LDD1531  [15]
 LDCM0293  AC32 HEK-293T C266(0.89); C246(0.95); C158(0.98); C347(1.04)  LDD1532  [15]
 LDCM0294  AC33 HEK-293T C266(0.97); C246(1.04); C158(1.18); C347(0.91)  LDD1533  [15]
 LDCM0295  AC34 HEK-293T C266(0.88); C246(0.98); C158(1.10); C347(0.92)  LDD1534  [15]
 LDCM0296  AC35 HEK-293T C266(0.86); C246(0.93); C158(1.00); C347(1.00)  LDD1535  [15]
 LDCM0297  AC36 HEK-293T C266(1.05); C246(0.99); C158(1.12); C347(0.95)  LDD1536  [15]
 LDCM0298  AC37 HEK-293T C266(0.89); C246(0.96); C158(1.15); C347(1.10)  LDD1537  [15]
 LDCM0299  AC38 HEK-293T C266(0.88); C246(0.92); C158(0.96); C347(1.06)  LDD1538  [15]
 LDCM0300  AC39 HEK-293T C266(0.82); C246(0.96); C158(1.01); C347(1.00)  LDD1539  [15]
 LDCM0301  AC4 HEK-293T C266(1.10); C246(1.01); C158(1.01); C347(1.00)  LDD1540  [15]
 LDCM0302  AC40 HEK-293T C266(0.87); C246(1.36); C158(1.12); C347(0.91)  LDD1541  [15]
 LDCM0303  AC41 HEK-293T C266(0.98); C246(1.07); C158(1.14); C347(0.97)  LDD1542  [15]
 LDCM0304  AC42 HEK-293T C266(1.27); C246(1.17); C158(0.87); C347(0.92)  LDD1543  [15]
 LDCM0305  AC43 HEK-293T C266(0.80); C246(0.94); C158(1.12); C347(0.97)  LDD1544  [15]
 LDCM0306  AC44 HEK-293T C266(1.04); C246(0.99); C158(0.96); C347(1.05)  LDD1545  [15]
 LDCM0307  AC45 HEK-293T C266(0.92); C246(1.04); C158(1.02); C347(0.99)  LDD1546  [15]
 LDCM0308  AC46 HEK-293T C266(0.91); C246(0.95); C158(1.02); C347(1.00)  LDD1547  [15]
 LDCM0309  AC47 HEK-293T C266(0.88); C246(0.99); C158(0.97); C347(1.03)  LDD1548  [15]
 LDCM0310  AC48 HEK-293T C266(0.83); C246(0.99); C158(0.95); C347(1.08)  LDD1549  [15]
 LDCM0311  AC49 HEK-293T C266(1.00); C246(0.97); C158(1.16); C347(1.00)  LDD1550  [15]
 LDCM0312  AC5 HEK-293T C266(1.02); C246(1.01); C158(1.04); C347(1.00)  LDD1551  [15]
 LDCM0313  AC50 HEK-293T C266(1.30); C246(0.97); C158(0.89); C347(0.94)  LDD1552  [15]
 LDCM0314  AC51 HEK-293T C266(0.95); C246(0.93); C158(1.03); C347(1.10)  LDD1553  [15]
 LDCM0315  AC52 HEK-293T C266(0.80); C246(1.31); C158(0.99); C347(0.97)  LDD1554  [15]
 LDCM0316  AC53 HEK-293T C266(1.04); C246(0.91); C158(1.10); C347(1.03)  LDD1555  [15]
 LDCM0317  AC54 HEK-293T C266(0.90); C246(0.92); C158(0.94); C347(1.04)  LDD1556  [15]
 LDCM0318  AC55 HEK-293T C266(0.95); C246(0.94); C158(1.04); C347(0.96)  LDD1557  [15]
 LDCM0319  AC56 HEK-293T C266(1.03); C246(0.96); C158(1.06); C347(1.03)  LDD1558  [15]
 LDCM0320  AC57 HEK-293T C266(1.05); C246(1.06); C158(1.22); C347(1.00)  LDD1559  [15]
 LDCM0321  AC58 HEK-293T C266(1.03); C246(0.97); C158(1.14); C347(0.92)  LDD1560  [15]
 LDCM0322  AC59 HEK-293T C266(1.07); C246(0.98); C158(1.06); C347(1.00)  LDD1561  [15]
 LDCM0323  AC6 HEK-293T C266(0.80); C246(1.00); C158(1.04); C347(0.96)  LDD1562  [15]
 LDCM0324  AC60 HEK-293T C266(0.92); C246(2.03); C158(1.00); C347(0.71)  LDD1563  [15]
 LDCM0325  AC61 HEK-293T C266(1.08); C246(1.01); C158(1.03); C347(0.99)  LDD1564  [15]
 LDCM0326  AC62 HEK-293T C266(0.99); C246(0.94); C158(1.04); C347(0.95)  LDD1565  [15]
 LDCM0327  AC63 HEK-293T C266(0.95); C246(1.14); C158(1.08); C347(0.98)  LDD1566  [15]
 LDCM0328  AC64 HEK-293T C266(1.25); C246(0.99); C158(1.15); C347(1.07)  LDD1567  [15]
 LDCM0334  AC7 HEK-293T C266(0.98); C246(1.04); C158(1.10); C347(1.12)  LDD1568  [15]
 LDCM0345  AC8 HEK-293T C266(0.92); C246(1.02); C158(1.14); C347(0.97)  LDD1569  [15]
 LDCM0248  AKOS034007472 HEK-293T C266(0.89); C246(1.02); C158(1.00); C347(1.02)  LDD1511  [15]
 LDCM0356  AKOS034007680 HEK-293T C266(1.03); C246(1.02); C158(0.98); C347(1.00)  LDD1570  [15]
 LDCM0275  AKOS034007705 HEK-293T C266(0.78); C246(1.19); C158(1.01); C347(0.94)  LDD1514  [15]
 LDCM0156  Aniline NCI-H1299 11.67  LDD0403  [1]
 LDCM0630  CCW28-3 231MFP C246(0.82)  LDD2214  [16]
 LDCM0632  CL-Sc Hep-G2 C246(1.39); C266(1.12); C379(0.35)  LDD2227  [10]
 LDCM0367  CL1 HEK-293T C246(4.26); C158(1.20); C347(0.79); C379(0.97)  LDD1571  [15]
 LDCM0368  CL10 HEK-293T C266(0.38); C246(4.86); C158(1.15); C347(0.63)  LDD1572  [15]
 LDCM0369  CL100 HEK-293T C246(0.93); C158(0.97); C347(1.00); C379(0.97)  LDD1573  [15]
 LDCM0370  CL101 HEK-293T C246(0.89); C158(1.10); C347(1.03); C379(0.96)  LDD1574  [15]
 LDCM0371  CL102 HEK-293T C266(1.07); C246(2.49); C158(1.09); C347(1.00)  LDD1575  [15]
 LDCM0372  CL103 HEK-293T C266(0.76); C246(1.02); C158(1.00); C347(0.93)  LDD1576  [15]
 LDCM0373  CL104 HEK-293T C246(0.95); C158(1.03); C347(0.97); C379(0.89)  LDD1577  [15]
 LDCM0374  CL105 HEK-293T C246(0.96); C158(1.05); C347(0.78); C379(0.97)  LDD1578  [15]
 LDCM0375  CL106 HEK-293T C266(0.98); C246(0.94); C158(1.15); C347(0.94)  LDD1579  [15]
 LDCM0376  CL107 HEK-293T C266(0.84); C246(0.96); C158(0.99); C347(0.99)  LDD1580  [15]
 LDCM0377  CL108 HEK-293T C246(1.13); C158(0.98); C347(0.86); C379(0.92)  LDD1581  [15]
 LDCM0378  CL109 HEK-293T C246(0.87); C158(1.03); C347(1.04); C379(0.89)  LDD1582  [15]
 LDCM0379  CL11 HEK-293T C266(0.18); C246(1.31); C158(1.03); C347(0.91)  LDD1583  [15]
 LDCM0380  CL110 HEK-293T C266(0.97); C246(1.18); C158(1.15); C347(0.85)  LDD1584  [15]
 LDCM0381  CL111 HEK-293T C266(0.84); C246(4.09); C158(1.18); C347(0.70)  LDD1585  [15]
 LDCM0382  CL112 HEK-293T C246(1.18); C158(1.14); C347(0.89); C379(0.94)  LDD1586  [15]
 LDCM0383  CL113 HEK-293T C246(0.87); C158(1.00); C347(0.96); C379(0.89)  LDD1587  [15]
 LDCM0384  CL114 HEK-293T C266(1.05); C246(1.06); C158(1.09); C347(0.83)  LDD1588  [15]
 LDCM0385  CL115 HEK-293T C266(0.94); C246(1.23); C158(1.06); C347(0.88)  LDD1589  [15]
 LDCM0386  CL116 HEK-293T C246(0.94); C158(0.87); C347(1.02); C379(0.90)  LDD1590  [15]
 LDCM0387  CL117 HEK-293T C246(0.96); C158(1.40); C347(0.87); C379(0.99)  LDD1591  [15]
 LDCM0388  CL118 HEK-293T C266(1.03); C246(1.07); C158(0.95); C347(0.92)  LDD1592  [15]
 LDCM0389  CL119 HEK-293T C266(0.82); C246(0.97); C158(0.96); C347(0.96)  LDD1593  [15]
 LDCM0390  CL12 HEK-293T C266(0.37); C246(1.02); C158(1.08); C347(0.89)  LDD1594  [15]
 LDCM0391  CL120 HEK-293T C246(1.04); C158(1.00); C347(1.00); C379(0.91)  LDD1595  [15]
 LDCM0392  CL121 HEK-293T C246(0.88); C158(1.06); C347(1.02); C379(0.93)  LDD1596  [15]
 LDCM0393  CL122 HEK-293T C266(1.02); C246(1.83); C158(1.12); C347(0.86)  LDD1597  [15]
 LDCM0394  CL123 HEK-293T C266(0.97); C246(2.21); C158(0.98); C347(0.80)  LDD1598  [15]
 LDCM0395  CL124 HEK-293T C246(0.94); C158(1.16); C347(0.86); C379(0.78)  LDD1599  [15]
 LDCM0396  CL125 HEK-293T C246(0.92); C158(1.09); C347(1.00); C379(0.96)  LDD1600  [15]
 LDCM0397  CL126 HEK-293T C266(1.17); C246(3.61); C158(1.13); C347(0.60)  LDD1601  [15]
 LDCM0398  CL127 HEK-293T C266(1.07); C246(1.46); C158(1.03); C347(0.94)  LDD1602  [15]
 LDCM0399  CL128 HEK-293T C246(0.93); C158(0.98); C347(1.05); C379(0.98)  LDD1603  [15]
 LDCM0400  CL13 HEK-293T C246(2.80); C158(1.05); C347(0.82); C379(1.07)  LDD1604  [15]
 LDCM0401  CL14 HEK-293T C266(0.84); C246(1.37); C158(1.03); C347(0.90)  LDD1605  [15]
 LDCM0402  CL15 HEK-293T C266(0.60); C246(1.50); C158(1.08); C347(0.84)  LDD1606  [15]
 LDCM0403  CL16 HEK-293T C246(0.98); C158(1.02); C347(1.09); C379(0.89)  LDD1607  [15]
 LDCM0404  CL17 HEK-293T C266(0.66); C246(2.08); C158(1.23); C347(1.00)  LDD1608  [15]
 LDCM0405  CL18 HEK-293T C266(0.49); C246(1.04); C158(1.03); C347(0.87)  LDD1609  [15]
 LDCM0406  CL19 HEK-293T C266(0.29); C246(1.02); C158(1.09); C347(0.97)  LDD1610  [15]
 LDCM0407  CL2 HEK-293T C266(0.71); C246(1.01); C158(0.95); C347(0.97)  LDD1611  [15]
 LDCM0408  CL20 HEK-293T C266(0.25); C246(1.03); C158(1.14); C347(0.97)  LDD1612  [15]
 LDCM0409  CL21 HEK-293T C266(0.29); C246(2.26); C158(0.94); C347(0.74)  LDD1613  [15]
 LDCM0410  CL22 HEK-293T C266(0.33); C246(1.81); C158(1.03); C347(0.72)  LDD1614  [15]
 LDCM0411  CL23 HEK-293T C266(0.19); C246(0.98); C158(1.00); C347(0.99)  LDD1615  [15]
 LDCM0412  CL24 HEK-293T C266(0.37); C246(1.02); C158(0.97); C347(0.89)  LDD1616  [15]
 LDCM0413  CL25 HEK-293T C246(0.90); C158(1.07); C347(0.64); C379(0.77)  LDD1617  [15]
 LDCM0414  CL26 HEK-293T C266(0.93); C246(1.17); C158(1.00); C347(0.93)  LDD1618  [15]
 LDCM0415  CL27 HEK-293T C266(0.75); C246(1.08); C158(1.07); C347(0.98)  LDD1619  [15]
 LDCM0416  CL28 HEK-293T C246(1.18); C158(1.20); C347(0.93); C379(0.85)  LDD1620  [15]
 LDCM0417  CL29 HEK-293T C266(0.68); C246(0.97); C158(1.09); C347(1.17)  LDD1621  [15]
 LDCM0418  CL3 HEK-293T C266(0.66); C246(1.11); C158(1.11); C347(0.97)  LDD1622  [15]
 LDCM0419  CL30 HEK-293T C266(0.46); C246(0.95); C158(0.84); C347(0.88)  LDD1623  [15]
 LDCM0420  CL31 HEK-293T C266(0.29); C246(3.47); C158(0.92); C347(0.67)  LDD1624  [15]
 LDCM0421  CL32 HEK-293T C266(0.28); C246(1.09); C158(1.14); C347(0.85)  LDD1625  [15]
 LDCM0422  CL33 HEK-293T C266(0.34); C246(6.83); C158(1.09); C347(0.58)  LDD1626  [15]
 LDCM0423  CL34 HEK-293T C266(0.30); C246(1.06); C158(1.09); C347(0.90)  LDD1627  [15]
 LDCM0424  CL35 HEK-293T C266(0.19); C246(1.00); C158(0.93); C347(0.89)  LDD1628  [15]
 LDCM0425  CL36 HEK-293T C266(0.38); C246(1.52); C158(1.06); C347(0.80)  LDD1629  [15]
 LDCM0426  CL37 HEK-293T C246(1.10); C158(1.19); C347(1.15); C379(0.83)  LDD1630  [15]
 LDCM0428  CL39 HEK-293T C266(0.80); C246(7.72); C158(1.08); C347(0.71)  LDD1632  [15]
 LDCM0429  CL4 HEK-293T C246(1.13); C158(0.92); C347(1.01); C379(1.03)  LDD1633  [15]
 LDCM0430  CL40 HEK-293T C246(1.00); C158(0.93); C347(0.99); C379(0.91)  LDD1634  [15]
 LDCM0431  CL41 HEK-293T C266(0.73); C246(1.03); C158(1.19); C347(0.89)  LDD1635  [15]
 LDCM0432  CL42 HEK-293T C266(0.54); C246(0.97); C158(1.06); C347(0.95)  LDD1636  [15]
 LDCM0433  CL43 HEK-293T C266(0.27); C246(1.00); C158(0.95); C347(1.03)  LDD1637  [15]
 LDCM0434  CL44 HEK-293T C266(0.33); C246(1.00); C158(0.96); C347(0.89)  LDD1638  [15]
 LDCM0435  CL45 HEK-293T C266(0.39); C246(1.57); C158(0.95); C347(0.77)  LDD1639  [15]
 LDCM0436  CL46 HEK-293T C266(0.29); C246(1.21); C158(0.96); C347(0.84)  LDD1640  [15]
 LDCM0437  CL47 HEK-293T C266(0.20); C246(1.10); C158(0.92); C347(0.93)  LDD1641  [15]
 LDCM0438  CL48 HEK-293T C266(0.45); C246(1.10); C158(1.03); C347(0.97)  LDD1642  [15]
 LDCM0439  CL49 HEK-293T C246(0.92); C158(1.29); C347(1.22); C379(0.90)  LDD1643  [15]
 LDCM0440  CL5 HEK-293T C266(0.74); C246(1.14); C158(1.11); C347(0.98)  LDD1644  [15]
 LDCM0441  CL50 HEK-293T C266(0.96); C246(1.00); C158(1.20); C347(0.96)  LDD1645  [15]
 LDCM0443  CL52 HEK-293T C246(0.90); C158(0.89); C347(1.00); C379(0.89)  LDD1646  [15]
 LDCM0444  CL53 HEK-293T C266(0.72); C246(1.00); C158(1.30); C347(0.79)  LDD1647  [15]
 LDCM0445  CL54 HEK-293T C266(0.45); C246(3.69); C158(1.25); C347(0.66)  LDD1648  [15]
 LDCM0446  CL55 HEK-293T C266(0.30); C246(0.98); C158(1.02); C347(0.96)  LDD1649  [15]
 LDCM0447  CL56 HEK-293T C266(0.30); C246(1.19); C158(1.12); C347(0.89)  LDD1650  [15]
 LDCM0448  CL57 HEK-293T C266(0.43); C246(1.10); C158(1.03); C347(0.73)  LDD1651  [15]
 LDCM0449  CL58 HEK-293T C266(0.31); C246(0.93); C158(1.07); C347(0.87)  LDD1652  [15]
 LDCM0450  CL59 HEK-293T C266(0.21); C246(1.07); C158(0.95); C347(0.89)  LDD1653  [15]
 LDCM0451  CL6 HEK-293T C266(0.54); C246(0.99); C158(1.15); C347(0.83)  LDD1654  [15]
 LDCM0452  CL60 HEK-293T C266(0.35); C246(1.65); C158(1.06); C347(0.82)  LDD1655  [15]
 LDCM0453  CL61 HEK-293T C246(0.95); C158(1.03); C347(1.29); C379(0.87)  LDD1656  [15]
 LDCM0454  CL62 HEK-293T C266(1.14); C246(0.97); C158(1.07); C347(1.03)  LDD1657  [15]
 LDCM0455  CL63 HEK-293T C266(0.83); C246(0.94); C158(0.96); C347(0.99)  LDD1658  [15]
 LDCM0456  CL64 HEK-293T C246(0.91); C158(1.42); C347(0.92); C379(0.89)  LDD1659  [15]
 LDCM0457  CL65 HEK-293T C266(0.81); C246(1.03); C158(1.15); C347(1.00)  LDD1660  [15]
 LDCM0458  CL66 HEK-293T C266(0.60); C246(1.24); C158(1.11); C347(0.91)  LDD1661  [15]
 LDCM0459  CL67 HEK-293T C266(0.37); C246(0.96); C158(1.09); C347(1.03)  LDD1662  [15]
 LDCM0460  CL68 HEK-293T C266(0.33); C246(1.27); C158(1.11); C347(0.91)  LDD1663  [15]
 LDCM0461  CL69 HEK-293T C266(0.41); C246(1.43); C158(0.87); C347(0.79)  LDD1664  [15]
 LDCM0462  CL7 HEK-293T C266(0.33); C246(1.17); C158(1.00); C347(1.01)  LDD1665  [15]
 LDCM0463  CL70 HEK-293T C266(0.41); C246(0.95); C158(1.14); C347(0.82)  LDD1666  [15]
 LDCM0464  CL71 HEK-293T C266(0.23); C246(0.96); C158(0.95); C347(0.92)  LDD1667  [15]
 LDCM0465  CL72 HEK-293T C266(0.43); C246(0.95); C158(1.20); C347(0.90)  LDD1668  [15]
 LDCM0466  CL73 HEK-293T C246(1.16); C158(1.23); C347(0.87); C379(0.85)  LDD1669  [15]
 LDCM0467  CL74 HEK-293T C266(1.06); C246(0.93); C158(1.11); C347(1.02)  LDD1670  [15]
 LDCM0469  CL76 HEK-293T C246(0.96); C158(1.04); C347(1.06); C379(0.95)  LDD1672  [15]
 LDCM0470  CL77 HEK-293T C266(0.80); C246(1.19); C158(1.17); C347(0.79)  LDD1673  [15]
 LDCM0471  CL78 HEK-293T C266(0.59); C246(0.97); C158(1.16); C347(0.99)  LDD1674  [15]
 LDCM0472  CL79 HEK-293T C266(0.41); C246(0.95); C158(1.04); C347(1.02)  LDD1675  [15]
 LDCM0473  CL8 HEK-293T C266(0.31); C246(5.50); C158(1.78); C347(0.66)  LDD1676  [15]
 LDCM0474  CL80 HEK-293T C266(0.37); C246(1.04); C158(1.09); C347(1.07)  LDD1677  [15]
 LDCM0475  CL81 HEK-293T C266(0.40); C246(0.96); C158(0.98); C347(0.97)  LDD1678  [15]
 LDCM0476  CL82 HEK-293T C266(0.38); C246(1.09); C158(1.05); C347(1.03)  LDD1679  [15]
 LDCM0477  CL83 HEK-293T C266(0.27); C246(1.46); C158(0.97); C347(0.92)  LDD1680  [15]
 LDCM0478  CL84 HEK-293T C266(0.46); C246(1.16); C158(1.02); C347(0.83)  LDD1681  [15]
 LDCM0479  CL85 HEK-293T C246(0.96); C158(1.28); C347(1.09); C379(0.90)  LDD1682  [15]
 LDCM0480  CL86 HEK-293T C266(1.30); C246(1.01); C158(1.17); C347(0.97)  LDD1683  [15]
 LDCM0481  CL87 HEK-293T C266(1.11); C246(1.55); C158(1.11); C347(0.92)  LDD1684  [15]
 LDCM0482  CL88 HEK-293T C246(1.00); C158(1.03); C347(1.10); C379(0.90)  LDD1685  [15]
 LDCM0483  CL89 HEK-293T C266(0.90); C246(1.04); C158(1.18); C347(1.01)  LDD1686  [15]
 LDCM0484  CL9 HEK-293T C266(0.32); C246(1.10); C158(1.09); C347(0.97)  LDD1687  [15]
 LDCM0485  CL90 HEK-293T C266(0.69); C246(6.56); C158(1.06); C347(0.62)  LDD1688  [15]
 LDCM0486  CL91 HEK-293T C266(0.54); C246(1.04); C158(1.05); C347(1.08)  LDD1689  [15]
 LDCM0487  CL92 HEK-293T C266(0.49); C246(1.55); C158(1.20); C347(0.85)  LDD1690  [15]
 LDCM0488  CL93 HEK-293T C266(0.45); C246(2.20); C158(1.02); C347(0.85)  LDD1691  [15]
 LDCM0489  CL94 HEK-293T C266(0.46); C246(1.01); C158(1.14); C347(0.91)  LDD1692  [15]
 LDCM0490  CL95 HEK-293T C266(0.36); C246(1.02); C158(0.95); C347(0.70)  LDD1693  [15]
 LDCM0491  CL96 HEK-293T C266(0.57); C246(1.09); C158(1.12); C347(0.87)  LDD1694  [15]
 LDCM0492  CL97 HEK-293T C246(0.97); C158(1.13); C347(0.81); C379(0.99)  LDD1695  [15]
 LDCM0493  CL98 HEK-293T C266(1.14); C246(1.26); C158(1.06); C347(0.80)  LDD1696  [15]
 LDCM0494  CL99 HEK-293T C266(1.21); C246(1.13); C158(1.16); C347(0.86)  LDD1697  [15]
 LDCM0495  E2913 HEK-293T C266(0.76); C246(0.93); C158(1.14); C347(0.86)  LDD1698  [15]
 LDCM0175  Ethacrynic acid HeLa C246(0.90)  LDD2210  [4]
 LDCM0625  F8 Ramos C266(0.94); C246(0.93)  LDD2187  [17]
 LDCM0572  Fragment10 MDA-MB-231 C246(20.00)  LDD1389  [18]
 LDCM0573  Fragment11 MDA-MB-231 C246(2.38)  LDD1391  [18]
 LDCM0574  Fragment12 MDA-MB-231 C246(20.00)  LDD1393  [18]
 LDCM0575  Fragment13 MDA-MB-231 C246(2.63)  LDD1395  [18]
 LDCM0576  Fragment14 MDA-MB-231 C246(20.00)  LDD1397  [18]
 LDCM0579  Fragment20 MDA-MB-231 C246(2.04)  LDD1402  [18]
 LDCM0580  Fragment21 MDA-MB-231 C246(1.51)  LDD1404  [18]
 LDCM0581  Fragment22 MDA-MB-231 C246(1.03)  LDD1406  [18]
 LDCM0582  Fragment23 MDA-MB-231 C246(1.09)  LDD1408  [18]
 LDCM0584  Fragment25 MDA-MB-231 C246(0.54)  LDD1411  [18]
 LDCM0578  Fragment27 MDA-MB-231 C246(0.69)  LDD1401  [18]
 LDCM0586  Fragment28 MDA-MB-231 C246(1.04)  LDD1415  [18]
 LDCM0587  Fragment29 MDA-MB-231 C246(1.04)  LDD1417  [18]
 LDCM0588  Fragment30 MDA-MB-231 C246(1.10)  LDD1419  [18]
 LDCM0589  Fragment31 MDA-MB-231 C246(1.58)  LDD1421  [18]
 LDCM0590  Fragment32 MDA-MB-231 C246(20.00)  LDD1423  [18]
 LDCM0468  Fragment33 MDA-MB-231 C246(17.82)  LDD1425  [18]
 LDCM0592  Fragment34 MDA-MB-231 C246(0.80)  LDD1427  [18]
 LDCM0594  Fragment36 MDA-MB-231 C246(2.54)  LDD1431  [18]
 LDCM0596  Fragment38 MDA-MB-231 C246(1.71)  LDD1433  [18]
 LDCM0597  Fragment39 MDA-MB-231 C246(20.00)  LDD1435  [18]
 LDCM0566  Fragment4 MDA-MB-231 C246(3.88)  LDD1378  [18]
 LDCM0599  Fragment41 MDA-MB-231 C246(1.52)  LDD1438  [18]
 LDCM0601  Fragment43 MDA-MB-231 C246(20.00)  LDD1441  [18]
 LDCM0602  Fragment44 MDA-MB-231 C246(0.82)  LDD1443  [18]
 LDCM0603  Fragment45 MDA-MB-231 C246(3.41)  LDD1444  [18]
 LDCM0604  Fragment46 MDA-MB-231 C246(1.02)  LDD1445  [18]
 LDCM0605  Fragment47 MDA-MB-231 C246(1.11)  LDD1446  [18]
 LDCM0606  Fragment48 MDA-MB-231 C246(0.86)  LDD1447  [18]
 LDCM0608  Fragment50 MDA-MB-231 C246(20.00)  LDD1449  [18]
 LDCM0427  Fragment51 HEK-293T C266(0.84); C246(1.28); C158(0.98); C347(0.93)  LDD1631  [15]
 LDCM0610  Fragment52 Ramos C266(1.05); C246(0.51)  LDD2204  [17]
 LDCM0611  Fragment53 MDA-MB-231 C246(1.13)  LDD1454  [18]
 LDCM0612  Fragment54 MDA-MB-231 C246(1.13)  LDD1456  [18]
 LDCM0613  Fragment55 MDA-MB-231 C246(1.52)  LDD1457  [18]
 LDCM0614  Fragment56 MDA-MB-231 C246(1.36)  LDD1458  [18]
 LDCM0568  Fragment6 MDA-MB-231 C246(1.04)  LDD1382  [18]
 LDCM0569  Fragment7 MDA-MB-231 C246(3.31)  LDD1383  [18]
 LDCM0570  Fragment8 MDA-MB-231 C246(20.00)  LDD1385  [18]
 LDCM0571  Fragment9 MDA-MB-231 C246(20.00)  LDD1387  [18]
 LDCM0022  KB02 MDA-MB-231 C246(13.07)  LDD1374  [18]
 LDCM0023  KB03 Jurkat C266(15.37); C246(4.34)  LDD0209  [5]
 LDCM0024  KB05 MKN-1 C358(1.96); C257(5.99); C169(2.03)  LDD3331  [19]
 LDCM0627  NUDT7-COV-1 HEK-293T C266(1.10); C246(1.01); C246(0.98)  LDD2206  [20]
 LDCM0628  OTUB2-COV-1 HEK-293T C379(0.93); C246(0.43); C246(0.13)  LDD2207  [20]
 LDCM0131  RA190 MM1.R C158(1.16); C379(0.90); C246(0.75)  LDD0304  [21]

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 8 (MAPK8) CMGC Ser/Thr protein kinase family P45983
Mitogen-activated protein kinase kinase kinase 1 (MAP3K1) STE Ser/Thr protein kinase family Q13233

References

1 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.
2 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
3 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
4 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.
5 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
6 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.
7 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
8 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
9 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
10 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
11 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
12 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
13 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.
14 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.
15 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
16 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.
17 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
18 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
19 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
20 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.
21 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.