Details of the Target

General Information of Target

Target ID LDTP05774
Target Name Dual specificity mitogen-activated protein kinase kinase 5 (MAP2K5)
Gene Name MAP2K5
Gene ID 5607
Synonyms
MEK5; MKK5; PRKMK5; Dual specificity mitogen-activated protein kinase kinase 5; MAP kinase kinase 5; MAPKK 5; EC 2.7.12.2; MAPK/ERK kinase 5; MEK 5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLWLALGPFPAMENQVLVIRIKIPNSGAVDWTVHSGPQLLFRDVLDVIGQVLPEATTTAF
EYEDEDGDRITVRSDEEMKAMLSYYYSTVMEQQVNGQLIEPLQIFPRACKPPGERNIHGL
KVNTRAGPSQHSSPAVSDSLPSNSLKKSSAELKKILANGQMNEQDIRYRDTLGHGNGGTV
YKAYHVPSGKILAVKVILLDITLELQKQIMSELEILYKCDSSYIIGFYGAFFVENRISIC
TEFMDGGSLDVYRKMPEHVLGRIAVAVVKGLTYLWSLKILHRDVKPSNMLVNTRGQVKLC
DFGVSTQLVNSIAKTYVGTNAYMAPERISGEQYGIHSDVWSLGISFMELALGRFPYPQIQ
KNQGSLMPLQLLQCIVDEDSPVLPVGEFSEPFVHFITQCMRKQPKERPAPEELMGHPFIV
QFNDGNAAVVSMWVCRALEERRSQQGPP
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, MAP kinase kinase subfamily
Function
Acts as a scaffold for the formation of a ternary MAP3K2/MAP3K3-MAP3K5-MAPK7 signaling complex. Activation of this pathway appears to play a critical role in protecting cells from stress-induced apoptosis, neuronal survival and cardiac development and angiogenesis. As part of the MAPK/ERK signaling pathway, acts as a negative regulator of apoptosis in cardiomyocytes via promotion of STUB1/CHIP-mediated ubiquitination and degradation of ICER-type isoforms of CREM.
TTD ID
T17143
Uniprot ID
Q13163
DrugMap ID
TTV3O87
Ensemble ID
ENST00000178640.10
HGNC ID
HGNC:6845
ChEMBL ID
CHEMBL4948

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CORL23 SNV: p.C109S .
HUH28 SNV: p.N362T .
KYSE510 SNV: p.S149Y .
L428 SNV: p.L39Ter .
MELJUSO SNV: p.L383F .
MOLT4 SNV: p.G119D .
NCIH2286 SNV: p.W433C .
OE33 SNV: p.A427V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
NAIA_5
 Probe Info  		C300(0.57)  LDD2227  [1]
DBIA
 Probe Info  		C109(14.31)  LDD0209  [2]
ATP probe
 Probe Info  		N.A.  LDD0199  [3]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [4]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [4]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [5]
IPM
 Probe Info  		N.A.  LDD0005  [6]
TFBX
 Probe Info  		N.A.  LDD0148  [5]
AOyne
 Probe Info  		15.00  LDD0443  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C300(0.91)  LDD0531  [8]
 LDCM0215  AC10 HCT 116 C300(1.15)  LDD0532  [8]
 LDCM0226  AC11 HCT 116 C300(1.19)  LDD0543  [8]
 LDCM0237  AC12 HCT 116 C300(1.03)  LDD0554  [8]
 LDCM0246  AC128 HCT 116 C300(1.22)  LDD0563  [8]
 LDCM0247  AC129 HCT 116 C300(1.18)  LDD0564  [8]
 LDCM0249  AC130 HCT 116 C300(1.06)  LDD0566  [8]
 LDCM0250  AC131 HCT 116 C300(1.04)  LDD0567  [8]
 LDCM0251  AC132 HCT 116 C300(1.04)  LDD0568  [8]
 LDCM0252  AC133 HCT 116 C300(0.99)  LDD0569  [8]
 LDCM0253  AC134 HCT 116 C300(1.20)  LDD0570  [8]
 LDCM0254  AC135 HCT 116 C300(1.11)  LDD0571  [8]
 LDCM0255  AC136 HCT 116 C300(1.14)  LDD0572  [8]
 LDCM0256  AC137 HCT 116 C300(1.01)  LDD0573  [8]
 LDCM0257  AC138 HCT 116 C300(1.02)  LDD0574  [8]
 LDCM0258  AC139 HCT 116 C300(0.95)  LDD0575  [8]
 LDCM0259  AC14 HCT 116 C300(1.17)  LDD0576  [8]
 LDCM0260  AC140 HCT 116 C300(1.13)  LDD0577  [8]
 LDCM0261  AC141 HCT 116 C300(1.11)  LDD0578  [8]
 LDCM0262  AC142 HCT 116 C300(1.04)  LDD0579  [8]
 LDCM0270  AC15 HCT 116 C300(1.21)  LDD0587  [8]
 LDCM0276  AC17 HEK-293T C109(1.05); C300(0.99)  LDD1515  [9]
 LDCM0277  AC18 HEK-293T C109(0.98); C300(1.01)  LDD1516  [9]
 LDCM0278  AC19 HEK-293T C109(1.08); C300(0.96); C435(0.88)  LDD1517  [9]
 LDCM0279  AC2 HCT 116 C300(0.90)  LDD0596  [8]
 LDCM0280  AC20 HEK-293T C109(1.06); C300(0.96)  LDD1519  [9]
 LDCM0281  AC21 HEK-293T C109(1.01); C300(1.00)  LDD1520  [9]
 LDCM0282  AC22 HEK-293T C109(0.95); C300(0.88)  LDD1521  [9]
 LDCM0283  AC23 HEK-293T C109(1.01); C300(1.01)  LDD1522  [9]
 LDCM0284  AC24 HEK-293T C109(1.03); C300(0.91)  LDD1523  [9]
 LDCM0285  AC25 HCT 116 C300(0.90)  LDD0602  [8]
 LDCM0286  AC26 HCT 116 C300(1.29)  LDD0603  [8]
 LDCM0287  AC27 HCT 116 C300(1.14)  LDD0604  [8]
 LDCM0288  AC28 HCT 116 C300(1.07)  LDD0605  [8]
 LDCM0289  AC29 HCT 116 C300(1.15)  LDD0606  [8]
 LDCM0290  AC3 HCT 116 C300(0.89)  LDD0607  [8]
 LDCM0291  AC30 HCT 116 C300(1.22)  LDD0608  [8]
 LDCM0292  AC31 HCT 116 C300(0.97)  LDD0609  [8]
 LDCM0293  AC32 HCT 116 C300(1.28)  LDD0610  [8]
 LDCM0294  AC33 HCT 116 C300(1.33)  LDD0611  [8]
 LDCM0295  AC34 HCT 116 C300(1.17)  LDD0612  [8]
 LDCM0296  AC35 HEK-293T C109(1.02); C300(1.12); C435(1.12)  LDD1535  [9]
 LDCM0297  AC36 HEK-293T C109(1.16); C300(1.00)  LDD1536  [9]
 LDCM0298  AC37 HEK-293T C109(1.02); C300(0.97)  LDD1537  [9]
 LDCM0299  AC38 HEK-293T C109(0.96); C300(0.95)  LDD1538  [9]
 LDCM0300  AC39 HEK-293T C109(1.05); C300(0.93)  LDD1539  [9]
 LDCM0301  AC4 HCT 116 C300(0.92)  LDD0618  [8]
 LDCM0302  AC40 HEK-293T C109(0.97); C300(1.03)  LDD1541  [9]
 LDCM0303  AC41 HEK-293T C109(1.08); C300(1.07)  LDD1542  [9]
 LDCM0304  AC42 HEK-293T C109(1.17); C300(0.99)  LDD1543  [9]
 LDCM0305  AC43 HEK-293T C109(1.03); C300(1.04); C435(0.98)  LDD1544  [9]
 LDCM0306  AC44 HEK-293T C109(1.12); C300(1.01)  LDD1545  [9]
 LDCM0307  AC45 HEK-293T C109(1.07); C300(0.96)  LDD1546  [9]
 LDCM0308  AC46 HEK-293T C109(1.03); C300(0.91)  LDD1547  [9]
 LDCM0309  AC47 HEK-293T C109(0.99); C300(0.96)  LDD1548  [9]
 LDCM0310  AC48 HEK-293T C109(0.94); C300(1.02)  LDD1549  [9]
 LDCM0311  AC49 HEK-293T C109(1.17); C300(0.98)  LDD1550  [9]
 LDCM0312  AC5 HCT 116 C300(0.96)  LDD0629  [8]
 LDCM0313  AC50 HEK-293T C109(0.96); C300(0.99)  LDD1552  [9]
 LDCM0314  AC51 HEK-293T C109(1.03); C300(1.04); C435(1.20)  LDD1553  [9]
 LDCM0315  AC52 HEK-293T C109(1.14); C300(0.98)  LDD1554  [9]
 LDCM0316  AC53 HEK-293T C109(1.00); C300(0.96)  LDD1555  [9]
 LDCM0317  AC54 HEK-293T C109(0.98); C300(0.96)  LDD1556  [9]
 LDCM0318  AC55 HEK-293T C109(1.09); C300(0.98)  LDD1557  [9]
 LDCM0319  AC56 HEK-293T C109(1.14); C300(0.93)  LDD1558  [9]
 LDCM0320  AC57 HEK-293T C109(1.02); C300(1.07)  LDD1559  [9]
 LDCM0321  AC58 HEK-293T C109(0.87); C300(1.04)  LDD1560  [9]
 LDCM0322  AC59 HEK-293T C109(0.99); C300(1.10); C435(0.92)  LDD1561  [9]
 LDCM0323  AC6 HCT 116 C300(1.05)  LDD0640  [8]
 LDCM0324  AC60 HEK-293T C109(1.07); C300(0.99)  LDD1563  [9]
 LDCM0325  AC61 HEK-293T C109(1.07); C300(1.10)  LDD1564  [9]
 LDCM0326  AC62 HEK-293T C109(0.95); C300(0.96)  LDD1565  [9]
 LDCM0327  AC63 HEK-293T C109(1.01); C300(1.03)  LDD1566  [9]
 LDCM0328  AC64 HEK-293T C109(0.96); C300(1.01)  LDD1567  [9]
 LDCM0334  AC7 HCT 116 C300(1.13)  LDD0651  [8]
 LDCM0345  AC8 HCT 116 C300(1.08)  LDD0662  [8]
 LDCM0248  AKOS034007472 HCT 116 C300(1.19)  LDD0565  [8]
 LDCM0356  AKOS034007680 HCT 116 C300(1.16)  LDD0673  [8]
 LDCM0275  AKOS034007705 HCT 116 C300(1.51)  LDD0592  [8]
 LDCM0632  CL-Sc Hep-G2 C300(0.57)  LDD2227  [1]
 LDCM0367  CL1 HEK-293T C109(1.06); C300(1.23)  LDD1571  [9]
 LDCM0368  CL10 HEK-293T C109(0.99); C300(1.35)  LDD1572  [9]
 LDCM0369  CL100 HCT 116 C300(0.98)  LDD0686  [8]
 LDCM0370  CL101 HCT 116 C300(1.10)  LDD0687  [8]
 LDCM0371  CL102 HCT 116 C300(1.05)  LDD0688  [8]
 LDCM0372  CL103 HCT 116 C300(1.11)  LDD0689  [8]
 LDCM0373  CL104 HCT 116 C300(1.22)  LDD0690  [8]
 LDCM0374  CL105 HEK-293T C109(1.15); C300(1.07)  LDD1578  [9]
 LDCM0375  CL106 HEK-293T C109(0.96); C300(1.04)  LDD1579  [9]
 LDCM0376  CL107 HEK-293T C109(1.00); C300(0.93)  LDD1580  [9]
 LDCM0377  CL108 HEK-293T C109(1.04); C300(0.88)  LDD1581  [9]
 LDCM0378  CL109 HEK-293T C109(1.07); C300(1.04)  LDD1582  [9]
 LDCM0379  CL11 HEK-293T C109(0.97); C300(1.21)  LDD1583  [9]
 LDCM0380  CL110 HEK-293T C109(1.02); C300(0.94)  LDD1584  [9]
 LDCM0381  CL111 HEK-293T C109(0.97); C300(0.98)  LDD1585  [9]
 LDCM0382  CL112 HCT 116 C300(1.03)  LDD0699  [8]
 LDCM0383  CL113 HCT 116 C300(1.01)  LDD0700  [8]
 LDCM0384  CL114 HCT 116 C300(0.91)  LDD0701  [8]
 LDCM0385  CL115 HCT 116 C300(1.10)  LDD0702  [8]
 LDCM0386  CL116 HCT 116 C300(1.05)  LDD0703  [8]
 LDCM0387  CL117 HEK-293T C109(1.13); C300(1.06)  LDD1591  [9]
 LDCM0388  CL118 HEK-293T C109(1.03); C300(1.01)  LDD1592  [9]
 LDCM0389  CL119 HEK-293T C109(1.01); C300(0.96)  LDD1593  [9]
 LDCM0390  CL12 HEK-293T C109(0.89); C300(1.20)  LDD1594  [9]
 LDCM0391  CL120 HEK-293T C109(1.32); C300(0.86)  LDD1595  [9]
 LDCM0392  CL121 HEK-293T C109(0.99); C300(1.06)  LDD1596  [9]
 LDCM0393  CL122 HEK-293T C109(0.98); C300(1.27)  LDD1597  [9]
 LDCM0394  CL123 HEK-293T C109(0.96); C300(1.24)  LDD1598  [9]
 LDCM0395  CL124 HEK-293T C109(1.01); C300(1.15)  LDD1599  [9]
 LDCM0396  CL125 HEK-293T C109(1.04); C300(1.11)  LDD1600  [9]
 LDCM0397  CL126 HEK-293T C109(0.95); C300(1.07)  LDD1601  [9]
 LDCM0398  CL127 HEK-293T C109(0.98); C300(0.97)  LDD1602  [9]
 LDCM0399  CL128 HEK-293T C109(1.11); C300(1.08)  LDD1603  [9]
 LDCM0400  CL13 HEK-293T C109(1.12); C300(1.77)  LDD1604  [9]
 LDCM0401  CL14 HEK-293T C109(0.86); C300(1.04)  LDD1605  [9]
 LDCM0402  CL15 HEK-293T C109(0.96); C300(1.19)  LDD1606  [9]
 LDCM0403  CL16 HCT 116 C300(0.85)  LDD0720  [8]
 LDCM0404  CL17 HCT 116 C300(0.89)  LDD0721  [8]
 LDCM0405  CL18 HCT 116 C300(1.07)  LDD0722  [8]
 LDCM0406  CL19 HCT 116 C300(1.01)  LDD0723  [8]
 LDCM0407  CL2 HEK-293T C109(1.01); C300(1.16)  LDD1611  [9]
 LDCM0408  CL20 HCT 116 C300(1.22)  LDD0725  [8]
 LDCM0409  CL21 HCT 116 C300(1.19)  LDD0726  [8]
 LDCM0410  CL22 HCT 116 C300(1.58)  LDD0727  [8]
 LDCM0411  CL23 HCT 116 C300(1.02)  LDD0728  [8]
 LDCM0412  CL24 HCT 116 C300(1.11)  LDD0729  [8]
 LDCM0413  CL25 HCT 116 C300(1.07)  LDD0730  [8]
 LDCM0414  CL26 HCT 116 C300(1.00)  LDD0731  [8]
 LDCM0415  CL27 HCT 116 C300(0.99)  LDD0732  [8]
 LDCM0416  CL28 HCT 116 C300(1.11)  LDD0733  [8]
 LDCM0417  CL29 HCT 116 C300(1.20)  LDD0734  [8]
 LDCM0418  CL3 HEK-293T C109(0.90); C300(1.08)  LDD1622  [9]
 LDCM0419  CL30 HCT 116 C300(0.91)  LDD0736  [8]
 LDCM0420  CL31 HCT 116 C300(0.98)  LDD0737  [8]
 LDCM0421  CL32 HCT 116 C300(0.84)  LDD0738  [8]
 LDCM0422  CL33 HCT 116 C300(0.83)  LDD0739  [8]
 LDCM0423  CL34 HCT 116 C300(0.91)  LDD0740  [8]
 LDCM0424  CL35 HCT 116 C300(1.17)  LDD0741  [8]
 LDCM0425  CL36 HCT 116 C300(1.06)  LDD0742  [8]
 LDCM0426  CL37 HCT 116 C300(1.13)  LDD0743  [8]
 LDCM0428  CL39 HCT 116 C300(0.97)  LDD0745  [8]
 LDCM0429  CL4 HEK-293T C109(1.03); C300(1.13)  LDD1633  [9]
 LDCM0430  CL40 HCT 116 C300(0.97)  LDD0747  [8]
 LDCM0431  CL41 HCT 116 C300(1.15)  LDD0748  [8]
 LDCM0432  CL42 HCT 116 C300(1.13)  LDD0749  [8]
 LDCM0433  CL43 HCT 116 C300(1.26)  LDD0750  [8]
 LDCM0434  CL44 HCT 116 C300(1.06)  LDD0751  [8]
 LDCM0435  CL45 HCT 116 C300(1.07)  LDD0752  [8]
 LDCM0436  CL46 HCT 116 C300(0.83)  LDD0753  [8]
 LDCM0437  CL47 HCT 116 C300(0.95)  LDD0754  [8]
 LDCM0438  CL48 HCT 116 C300(0.93)  LDD0755  [8]
 LDCM0439  CL49 HCT 116 C300(0.90)  LDD0756  [8]
 LDCM0440  CL5 HEK-293T C109(1.06); C300(1.10)  LDD1644  [9]
 LDCM0441  CL50 HCT 116 C300(0.96)  LDD0758  [8]
 LDCM0442  CL51 HCT 116 C300(0.77)  LDD0759  [8]
 LDCM0443  CL52 HCT 116 C300(0.87)  LDD0760  [8]
 LDCM0444  CL53 HCT 116 C300(0.86)  LDD0761  [8]
 LDCM0445  CL54 HCT 116 C300(0.86)  LDD0762  [8]
 LDCM0446  CL55 HCT 116 C300(0.85)  LDD0763  [8]
 LDCM0447  CL56 HCT 116 C300(0.82)  LDD0764  [8]
 LDCM0448  CL57 HCT 116 C300(0.71)  LDD0765  [8]
 LDCM0449  CL58 HCT 116 C300(1.01)  LDD0766  [8]
 LDCM0450  CL59 HCT 116 C300(1.00)  LDD0767  [8]
 LDCM0451  CL6 HEK-293T C109(1.09); C300(1.03)  LDD1654  [9]
 LDCM0452  CL60 HCT 116 C300(1.02)  LDD0769  [8]
 LDCM0453  CL61 HCT 116 C300(1.17)  LDD0770  [8]
 LDCM0454  CL62 HCT 116 C300(1.10)  LDD0771  [8]
 LDCM0455  CL63 HCT 116 C300(1.00)  LDD0772  [8]
 LDCM0456  CL64 HCT 116 C300(0.96)  LDD0773  [8]
 LDCM0457  CL65 HCT 116 C300(1.11)  LDD0774  [8]
 LDCM0458  CL66 HCT 116 C300(1.14)  LDD0775  [8]
 LDCM0459  CL67 HCT 116 C300(1.23)  LDD0776  [8]
 LDCM0460  CL68 HCT 116 C300(0.97)  LDD0777  [8]
 LDCM0461  CL69 HCT 116 C300(0.94)  LDD0778  [8]
 LDCM0462  CL7 HEK-293T C109(0.99); C300(1.28); C435(0.95)  LDD1665  [9]
 LDCM0463  CL70 HCT 116 C300(1.04)  LDD0780  [8]
 LDCM0464  CL71 HCT 116 C300(0.99)  LDD0781  [8]
 LDCM0465  CL72 HCT 116 C300(1.14)  LDD0782  [8]
 LDCM0466  CL73 HCT 116 C300(1.03)  LDD0783  [8]
 LDCM0467  CL74 HCT 116 C300(1.01)  LDD0784  [8]
 LDCM0469  CL76 HCT 116 C300(1.01)  LDD0786  [8]
 LDCM0470  CL77 HCT 116 C300(0.91)  LDD0787  [8]
 LDCM0471  CL78 HCT 116 C300(0.99)  LDD0788  [8]
 LDCM0472  CL79 HCT 116 C300(1.09)  LDD0789  [8]
 LDCM0473  CL8 HEK-293T C109(0.93); C300(1.87)  LDD1676  [9]
 LDCM0474  CL80 HCT 116 C300(0.86)  LDD0791  [8]
 LDCM0475  CL81 HCT 116 C300(0.99)  LDD0792  [8]
 LDCM0476  CL82 HCT 116 C300(1.33)  LDD0793  [8]
 LDCM0477  CL83 HCT 116 C300(0.98)  LDD0794  [8]
 LDCM0478  CL84 HCT 116 C300(1.18)  LDD0795  [8]
 LDCM0479  CL85 HCT 116 C300(0.98)  LDD0796  [8]
 LDCM0480  CL86 HCT 116 C300(0.91)  LDD0797  [8]
 LDCM0481  CL87 HCT 116 C300(1.04)  LDD0798  [8]
 LDCM0482  CL88 HCT 116 C300(0.90)  LDD0799  [8]
 LDCM0483  CL89 HCT 116 C300(1.20)  LDD0800  [8]
 LDCM0484  CL9 HEK-293T C109(0.90); C300(1.21)  LDD1687  [9]
 LDCM0485  CL90 HCT 116 C300(0.90)  LDD0802  [8]
 LDCM0486  CL91 HCT 116 C300(0.86)  LDD0803  [8]
 LDCM0487  CL92 HCT 116 C300(0.87)  LDD0804  [8]
 LDCM0488  CL93 HCT 116 C300(0.87)  LDD0805  [8]
 LDCM0489  CL94 HCT 116 C300(0.91)  LDD0806  [8]
 LDCM0490  CL95 HCT 116 C300(0.83)  LDD0807  [8]
 LDCM0491  CL96 HCT 116 C300(0.83)  LDD0808  [8]
 LDCM0492  CL97 HCT 116 C300(0.84)  LDD0809  [8]
 LDCM0493  CL98 HCT 116 C300(0.94)  LDD0810  [8]
 LDCM0494  CL99 HCT 116 C300(0.94)  LDD0811  [8]
 LDCM0495  E2913 HEK-293T C109(1.08); C300(0.97)  LDD1698  [9]
 LDCM0625  F8 Ramos C109(0.97)  LDD2187  [10]
 LDCM0573  Fragment11 Ramos C109(0.37)  LDD2190  [10]
 LDCM0574  Fragment12 Ramos C109(1.04)  LDD2191  [10]
 LDCM0575  Fragment13 Ramos C109(0.72)  LDD2192  [10]
 LDCM0576  Fragment14 Ramos C109(1.11)  LDD2193  [10]
 LDCM0580  Fragment21 Ramos C109(0.76)  LDD2195  [10]
 LDCM0582  Fragment23 Ramos C109(0.78)  LDD2196  [10]
 LDCM0578  Fragment27 Ramos C109(0.73)  LDD2197  [10]
 LDCM0586  Fragment28 Ramos C109(0.53)  LDD2198  [10]
 LDCM0588  Fragment30 Ramos C109(2.35)  LDD2199  [10]
 LDCM0589  Fragment31 Ramos C109(0.67)  LDD2200  [10]
 LDCM0590  Fragment32 Ramos C109(1.69)  LDD2201  [10]
 LDCM0468  Fragment33 HCT 116 C300(1.03)  LDD0785  [8]
 LDCM0596  Fragment38 Ramos C109(0.76)  LDD2203  [10]
 LDCM0566  Fragment4 Ramos C109(0.80)  LDD2184  [10]
 LDCM0427  Fragment51 HCT 116 C300(1.09)  LDD0744  [8]
 LDCM0610  Fragment52 Ramos C109(0.96)  LDD2204  [10]
 LDCM0614  Fragment56 Ramos C109(0.89)  LDD2205  [10]
 LDCM0569  Fragment7 Ramos C109(1.25)  LDD2186  [10]
 LDCM0571  Fragment9 Ramos C109(1.66)  LDD2188  [10]
 LDCM0022  KB02 HEK-293T C300(0.94); C109(1.03)  LDD1492  [9]
 LDCM0023  KB03 Jurkat C109(14.31)  LDD0209  [2]
 LDCM0024  KB05 NCI-H1792 C73(5.54)  LDD3348  [11]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Mitogen-activated protein kinase 7 (MAPK7) CMGC Ser/Thr protein kinase family Q13164
Mitogen-activated protein kinase kinase kinase 2 (MAP3K2) STE Ser/Thr protein kinase family Q9Y2U5
Mitogen-activated protein kinase kinase kinase 3 (MAP3K3) STE Ser/Thr protein kinase family Q99759
Dual specificity protein phosphatase 21 (DUSP21) Protein-tyrosine phosphatase family Q9H596
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein 620 (ZNF620) Krueppel C2H2-type zinc-finger protein family Q6ZNG0
Zinc finger protein 426 (ZNF426) . Q9BUY5
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
Prefoldin subunit 5 (PFDN5) Prefoldin subunit alpha family Q99471
Ligand of Numb protein X 2 (LNX2) . Q8N448
Sequestosome-1 (SQSTM1) . Q13501
Uncharacterized protein C3orf36 (C3orf36) . Q3SXR2

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bix 02188 Small molecular drug D0R6JG

References

1 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
2 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.
3 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.
4 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
5 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
6 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
7 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.
8 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
9 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
10 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
11 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