Details of the Target

General Information of Target

Target ID LDTP05776
Target Name Serine/threonine-protein kinase PAK 2 (PAK2)
Gene Name PAK2
Gene ID 5062
Synonyms
Serine/threonine-protein kinase PAK 2; EC 2.7.11.1; Gamma-PAK; PAK65; S6/H4 kinase; p21-activated kinase 2; PAK-2; p58) [Cleaved into: PAK-2p27; p27; PAK-2p34; p34; C-t-PAK2)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSDNGELEDKPPAPPVRMSSTIFSTGGKDPLSANHSLKPLPSVPEEKKPRHKIISIFSGT
EKGSKKKEKERPEISPPSDFEHTIHVGFDAVTGEFTGMPEQWARLLQTSNITKLEQKKNP
QAVLDVLKFYDSNTVKQKYLSFTPPEKDGFPSGTPALNAKGTEAPAVVTEEEDDDEETAP
PVIAPRPDHTKSIYTRSVIDPVPAPVGDSHVDGAAKSLDKQKKKTKMTDEEIMEKLRTIV
SIGDPKKKYTRYEKIGQGASGTVFTATDVALGQEVAIKQINLQKQPKKELIINEILVMKE
LKNPNIVNFLDSYLVGDELFVVMEYLAGGSLTDVVTETCMDEAQIAAVCRECLQALEFLH
ANQVIHRDIKSDNVLLGMEGSVKLTDFGFCAQITPEQSKRSTMVGTPYWMAPEVVTRKAY
GPKVDIWSLGIMAIEMVEGEPPYLNENPLRALYLIATNGTPELQNPEKLSPIFRDFLNRC
LEMDVEKRGSAKELLQHPFLKLAKPLSSLTPLIMAAKEAMKSNR
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, STE20 subfamily
Subcellular location
Cytoplasm; Nucleus
Function
Serine/threonine protein kinase that plays a role in a variety of different signaling pathways including cytoskeleton regulation, cell motility, cell cycle progression, apoptosis or proliferation. Acts as a downstream effector of the small GTPases CDC42 and RAC1. Activation by the binding of active CDC42 and RAC1 results in a conformational change and a subsequent autophosphorylation on several serine and/or threonine residues. Full-length PAK2 stimulates cell survival and cell growth. Phosphorylates MAPK4 and MAPK6 and activates the downstream target MAPKAPK5, a regulator of F-actin polymerization and cell migration. Phosphorylates JUN and plays an important role in EGF-induced cell proliferation. Phosphorylates many other substrates including histone H4 to promote assembly of H3.3 and H4 into nucleosomes, BAD, ribosomal protein S6, or MBP. Phosphorylates CASP7, thereby preventing its activity. Additionally, associates with ARHGEF7 and GIT1 to perform kinase-independent functions such as spindle orientation control during mitosis. On the other hand, apoptotic stimuli such as DNA damage lead to caspase-mediated cleavage of PAK2, generating PAK-2p34, an active p34 fragment that translocates to the nucleus and promotes cellular apoptosis involving the JNK signaling pathway. Caspase-activated PAK2 phosphorylates MKNK1 and reduces cellular translation.
TTD ID
T07766
Uniprot ID
Q13177
DrugMap ID
TT279WO
Ensemble ID
ENST00000327134.7
HGNC ID
HGNC:8591
ChEMBL ID
CHEMBL4487

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  		5.56  LDD0402  [1]
TH211
 Probe Info  		Y130(11.92); Y408(9.69)  LDD0260  [2]
ONAyne
 Probe Info  		K191(2.38); K246(0.42)  LDD0274  [3]
STPyne
 Probe Info  		K128(7.22); K136(3.52); K147(0.10); K235(10.00)  LDD0277  [3]
Probe 1
 Probe Info  		Y130(77.89); Y252(41.45)  LDD3495  [4]
HHS-482
 Probe Info  		Y130(1.16)  LDD0285  [5]
HHS-475
 Probe Info  		Y130(0.90)  LDD0264  [6]
HHS-465
 Probe Info  		Y130(1.76)  LDD2237  [7]
Acrolein
 Probe Info  		N.A.  LDD0223  [8]
DBIA
 Probe Info  		C390(0.84)  LDD0078  [9]
5E-2FA
 Probe Info  		H35(0.00); H210(0.00)  LDD2235  [10]
ATP probe
 Probe Info  		K38(0.00); K246(0.00); K247(0.00); K216(0.00)  LDD0199  [11]
4-Iodoacetamidophenylacetylene
 Probe Info  		C480(0.00); C352(0.00); C390(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [13]
IPIAA_H
 Probe Info  		N.A.  LDD0030  [14]
IPIAA_L
 Probe Info  		C390(0.00); C352(0.00)  LDD0031  [14]
Lodoacetamide azide
 Probe Info  		C480(0.00); C352(0.00); C390(0.00)  LDD0037  [12]
NAIA_5
 Probe Info  		C390(0.00); C411(0.00); C424(0.00)  LDD2224  [15]
PF-06672131
 Probe Info  		N.A.  LDD0017  [16]
1c-yne
 Probe Info  		N.A.  LDD0228  [17]
PAL-AfBPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C277
 Probe Info  		9.65  LDD1947  [18]
C289
 Probe Info  		47.50  LDD1959  [18]
FFF probe14
 Probe Info  		20.00  LDD0477  [19]
FFF probe2
 Probe Info  		6.51  LDD0463  [19]
STS-2
 Probe Info  		N.A.  LDD0139  [20]
VE-P
 Probe Info  		N.A.  LDD0396  [21]
DFG-out-4
 Probe Info  		2.30  LDD0075  [22]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C352(0.98); C390(1.00)  LDD0531  [9]
 LDCM0215  AC10 HCT 116 C352(1.07)  LDD0532  [9]
 LDCM0216  AC100 HCT 116 C390(1.04)  LDD0533  [9]
 LDCM0217  AC101 HCT 116 C390(1.18)  LDD0534  [9]
 LDCM0218  AC102 HCT 116 C390(1.22)  LDD0535  [9]
 LDCM0219  AC103 HCT 116 C390(1.15)  LDD0536  [9]
 LDCM0220  AC104 HCT 116 C390(1.12)  LDD0537  [9]
 LDCM0221  AC105 HCT 116 C390(0.98)  LDD0538  [9]
 LDCM0222  AC106 HCT 116 C390(1.08)  LDD0539  [9]
 LDCM0223  AC107 HCT 116 C390(1.14)  LDD0540  [9]
 LDCM0224  AC108 HCT 116 C390(0.97)  LDD0541  [9]
 LDCM0225  AC109 HCT 116 C390(1.08)  LDD0542  [9]
 LDCM0226  AC11 HCT 116 C352(1.17)  LDD0543  [9]
 LDCM0227  AC110 HCT 116 C390(0.96)  LDD0544  [9]
 LDCM0228  AC111 HCT 116 C390(1.45)  LDD0545  [9]
 LDCM0229  AC112 HCT 116 C390(1.29)  LDD0546  [9]
 LDCM0230  AC113 HCT 116 C352(1.24)  LDD0547  [9]
 LDCM0231  AC114 HCT 116 C352(1.00)  LDD0548  [9]
 LDCM0232  AC115 HCT 116 C352(1.02)  LDD0549  [9]
 LDCM0233  AC116 HCT 116 C352(1.14)  LDD0550  [9]
 LDCM0234  AC117 HCT 116 C352(1.06)  LDD0551  [9]
 LDCM0235  AC118 HCT 116 C352(1.22)  LDD0552  [9]
 LDCM0236  AC119 HCT 116 C352(1.10)  LDD0553  [9]
 LDCM0237  AC12 HCT 116 C352(0.91)  LDD0554  [9]
 LDCM0238  AC120 HCT 116 C352(0.88)  LDD0555  [9]
 LDCM0239  AC121 HCT 116 C352(1.25)  LDD0556  [9]
 LDCM0240  AC122 HCT 116 C352(1.02)  LDD0557  [9]
 LDCM0241  AC123 HCT 116 C352(1.06)  LDD0558  [9]
 LDCM0242  AC124 HCT 116 C352(1.27)  LDD0559  [9]
 LDCM0243  AC125 HCT 116 C352(1.13)  LDD0560  [9]
 LDCM0244  AC126 HCT 116 C352(1.06)  LDD0561  [9]
 LDCM0245  AC127 HCT 116 C352(1.02)  LDD0562  [9]
 LDCM0246  AC128 HCT 116 C352(0.89)  LDD0563  [9]
 LDCM0247  AC129 HCT 116 C352(0.85)  LDD0564  [9]
 LDCM0249  AC130 HCT 116 C352(0.81)  LDD0566  [9]
 LDCM0250  AC131 HCT 116 C352(0.88)  LDD0567  [9]
 LDCM0251  AC132 HCT 116 C352(1.00)  LDD0568  [9]
 LDCM0252  AC133 HCT 116 C352(0.91)  LDD0569  [9]
 LDCM0253  AC134 HCT 116 C352(0.88)  LDD0570  [9]
 LDCM0254  AC135 HCT 116 C352(0.93)  LDD0571  [9]
 LDCM0255  AC136 HCT 116 C352(0.91)  LDD0572  [9]
 LDCM0256  AC137 HCT 116 C352(1.01)  LDD0573  [9]
 LDCM0257  AC138 HCT 116 C352(0.97)  LDD0574  [9]
 LDCM0258  AC139 HCT 116 C352(1.05)  LDD0575  [9]
 LDCM0259  AC14 HCT 116 C352(0.89)  LDD0576  [9]
 LDCM0260  AC140 HCT 116 C352(1.02)  LDD0577  [9]
 LDCM0261  AC141 HCT 116 C352(0.95)  LDD0578  [9]
 LDCM0262  AC142 HCT 116 C352(1.00)  LDD0579  [9]
 LDCM0263  AC143 HCT 116 C352(1.03)  LDD0580  [9]
 LDCM0264  AC144 HCT 116 C352(0.93)  LDD0581  [9]
 LDCM0265  AC145 HCT 116 C352(0.89)  LDD0582  [9]
 LDCM0266  AC146 HCT 116 C352(0.76)  LDD0583  [9]
 LDCM0267  AC147 HCT 116 C352(0.90)  LDD0584  [9]
 LDCM0268  AC148 HCT 116 C352(0.97)  LDD0585  [9]
 LDCM0269  AC149 HCT 116 C352(0.91)  LDD0586  [9]
 LDCM0270  AC15 HCT 116 C352(1.04)  LDD0587  [9]
 LDCM0271  AC150 HCT 116 C352(1.19)  LDD0588  [9]
 LDCM0272  AC151 HCT 116 C352(1.06)  LDD0589  [9]
 LDCM0273  AC152 HCT 116 C352(0.87)  LDD0590  [9]
 LDCM0274  AC153 HCT 116 C352(0.89)  LDD0591  [9]
 LDCM0621  AC154 HCT 116 C352(1.04)  LDD2158  [9]
 LDCM0622  AC155 HCT 116 C352(1.02)  LDD2159  [9]
 LDCM0623  AC156 HCT 116 C352(1.04)  LDD2160  [9]
 LDCM0624  AC157 HCT 116 C352(1.12)  LDD2161  [9]
 LDCM0276  AC17 HCT 116 C352(0.99); C390(1.25)  LDD0593  [9]
 LDCM0277  AC18 HCT 116 C352(0.78); C390(1.25)  LDD0594  [9]
 LDCM0278  AC19 HCT 116 C352(1.02); C390(1.26)  LDD0595  [9]
 LDCM0279  AC2 HCT 116 C390(0.99); C352(1.10)  LDD0596  [9]
 LDCM0280  AC20 HCT 116 C352(0.92); C390(1.30)  LDD0597  [9]
 LDCM0281  AC21 HCT 116 C352(1.00); C390(1.41)  LDD0598  [9]
 LDCM0282  AC22 HCT 116 C352(1.09); C390(1.53)  LDD0599  [9]
 LDCM0283  AC23 HCT 116 C352(1.01); C390(1.49)  LDD0600  [9]
 LDCM0284  AC24 HCT 116 C352(1.03); C390(1.37)  LDD0601  [9]
 LDCM0285  AC25 HCT 116 C390(0.60); C352(1.03)  LDD0602  [9]
 LDCM0286  AC26 HCT 116 C390(0.49); C352(0.89)  LDD0603  [9]
 LDCM0287  AC27 HCT 116 C390(0.55); C352(0.92)  LDD0604  [9]
 LDCM0288  AC28 HCT 116 C352(0.52); C390(0.54)  LDD0605  [9]
 LDCM0289  AC29 HCT 116 C390(0.55); C352(1.07)  LDD0606  [9]
 LDCM0290  AC3 HCT 116 C390(1.03); C352(1.07)  LDD0607  [9]
 LDCM0291  AC30 HCT 116 C390(0.57); C352(0.99)  LDD0608  [9]
 LDCM0292  AC31 HCT 116 C390(0.57); C352(1.17)  LDD0609  [9]
 LDCM0293  AC32 HCT 116 C390(0.58); C352(0.95)  LDD0610  [9]
 LDCM0294  AC33 HCT 116 C390(0.53); C352(1.14)  LDD0611  [9]
 LDCM0295  AC34 HCT 116 C390(0.60); C352(1.01)  LDD0612  [9]
 LDCM0296  AC35 HCT 116 C390(0.76); C352(1.30)  LDD0613  [9]
 LDCM0297  AC36 HCT 116 C390(0.78); C352(1.34)  LDD0614  [9]
 LDCM0298  AC37 HCT 116 C390(0.86); C352(1.35)  LDD0615  [9]
 LDCM0299  AC38 HCT 116 C390(0.88); C352(1.16)  LDD0616  [9]
 LDCM0300  AC39 HCT 116 C390(0.80); C352(0.97)  LDD0617  [9]
 LDCM0301  AC4 HCT 116 C390(0.98); C352(1.10)  LDD0618  [9]
 LDCM0302  AC40 HCT 116 C390(0.92); C352(1.15)  LDD0619  [9]
 LDCM0303  AC41 HCT 116 C390(1.01); C352(1.32)  LDD0620  [9]
 LDCM0304  AC42 HCT 116 C390(0.86); C352(1.09)  LDD0621  [9]
 LDCM0305  AC43 HCT 116 C390(0.99); C352(1.08)  LDD0622  [9]
 LDCM0306  AC44 HCT 116 C390(0.95); C352(1.28)  LDD0623  [9]
 LDCM0307  AC45 HCT 116 C352(1.03); C390(1.05)  LDD0624  [9]
 LDCM0308  AC46 HCT 116 C352(0.90); C390(1.14)  LDD0625  [9]
 LDCM0309  AC47 HCT 116 C352(0.91); C390(0.93)  LDD0626  [9]
 LDCM0310  AC48 HCT 116 C352(0.82); C390(0.90)  LDD0627  [9]
 LDCM0311  AC49 HCT 116 C352(0.90); C390(1.01)  LDD0628  [9]
 LDCM0312  AC5 HCT 116 C390(1.03); C352(1.19)  LDD0629  [9]
 LDCM0313  AC50 HCT 116 C352(0.85); C390(0.93)  LDD0630  [9]
 LDCM0314  AC51 HCT 116 C390(0.93); C352(1.06)  LDD0631  [9]
 LDCM0315  AC52 HCT 116 C352(0.97); C390(0.99)  LDD0632  [9]
 LDCM0316  AC53 HCT 116 C352(0.84); C390(1.02)  LDD0633  [9]
 LDCM0317  AC54 HCT 116 C390(0.83); C352(1.04)  LDD0634  [9]
 LDCM0318  AC55 HCT 116 C352(0.89); C390(1.14)  LDD0635  [9]
 LDCM0319  AC56 HCT 116 C352(0.82); C390(1.02)  LDD0636  [9]
 LDCM0320  AC57 HCT 116 C390(1.11); C352(1.11)  LDD0637  [9]
 LDCM0321  AC58 HCT 116 C390(1.03); C352(1.17)  LDD0638  [9]
 LDCM0322  AC59 HCT 116 C390(1.11); C352(1.17)  LDD0639  [9]
 LDCM0323  AC6 HCT 116 C352(1.13)  LDD0640  [9]
 LDCM0324  AC60 HCT 116 C352(1.06); C390(1.25)  LDD0641  [9]
 LDCM0325  AC61 HCT 116 C352(0.96); C390(1.12)  LDD0642  [9]
 LDCM0326  AC62 HCT 116 C352(1.01); C390(1.26)  LDD0643  [9]
 LDCM0327  AC63 HCT 116 C352(1.00); C390(1.22)  LDD0644  [9]
 LDCM0328  AC64 HCT 116 C352(0.99); C390(1.21)  LDD0645  [9]
 LDCM0329  AC65 HCT 116 C390(1.14); C352(1.14)  LDD0646  [9]
 LDCM0330  AC66 HCT 116 C390(1.08); C352(1.13)  LDD0647  [9]
 LDCM0331  AC67 HCT 116 C352(1.01); C390(1.25)  LDD0648  [9]
 LDCM0332  AC68 HCT 116 C352(0.84); C390(1.13)  LDD0649  [9]
 LDCM0333  AC69 HCT 116 C352(0.83); C390(1.17)  LDD0650  [9]
 LDCM0334  AC7 HCT 116 C352(0.99)  LDD0651  [9]
 LDCM0335  AC70 HCT 116 C390(0.68); C352(0.74)  LDD0652  [9]
 LDCM0336  AC71 HCT 116 C352(0.89); C390(1.22)  LDD0653  [9]
 LDCM0337  AC72 HCT 116 C390(0.77); C352(0.87)  LDD0654  [9]
 LDCM0338  AC73 HCT 116 C352(0.81); C390(0.91)  LDD0655  [9]
 LDCM0339  AC74 HCT 116 C352(0.80); C390(1.23)  LDD0656  [9]
 LDCM0340  AC75 HCT 116 C352(0.79); C390(0.87)  LDD0657  [9]
 LDCM0341  AC76 HCT 116 C352(0.87); C390(0.94)  LDD0658  [9]
 LDCM0342  AC77 HCT 116 C352(0.90); C390(1.19)  LDD0659  [9]
 LDCM0343  AC78 HCT 116 C352(0.81); C390(1.41)  LDD0660  [9]
 LDCM0344  AC79 HCT 116 C352(0.89); C390(0.94)  LDD0661  [9]
 LDCM0345  AC8 HCT 116 C352(1.03)  LDD0662  [9]
 LDCM0346  AC80 HCT 116 C352(0.92); C390(1.19)  LDD0663  [9]
 LDCM0347  AC81 HCT 116 C390(0.85); C352(0.90)  LDD0664  [9]
 LDCM0348  AC82 HCT 116 C352(0.75); C390(0.80)  LDD0665  [9]
 LDCM0349  AC83 HCT 116 C390(0.96)  LDD0666  [9]
 LDCM0350  AC84 HCT 116 C390(0.97)  LDD0667  [9]
 LDCM0351  AC85 HCT 116 C390(1.13)  LDD0668  [9]
 LDCM0352  AC86 HCT 116 C390(1.08)  LDD0669  [9]
 LDCM0353  AC87 HCT 116 C390(0.92)  LDD0670  [9]
 LDCM0354  AC88 HCT 116 C390(0.92)  LDD0671  [9]
 LDCM0355  AC89 HCT 116 C390(0.94)  LDD0672  [9]
 LDCM0357  AC90 HCT 116 C390(1.07)  LDD0674  [9]
 LDCM0358  AC91 HCT 116 C390(0.88)  LDD0675  [9]
 LDCM0359  AC92 HCT 116 C390(1.19)  LDD0676  [9]
 LDCM0360  AC93 HCT 116 C390(1.10)  LDD0677  [9]
 LDCM0361  AC94 HCT 116 C390(1.05)  LDD0678  [9]
 LDCM0362  AC95 HCT 116 C390(0.92)  LDD0679  [9]
 LDCM0363  AC96 HCT 116 C390(1.07)  LDD0680  [9]
 LDCM0364  AC97 HCT 116 C390(1.06)  LDD0681  [9]
 LDCM0365  AC98 HCT 116 C390(0.99)  LDD0682  [9]
 LDCM0366  AC99 HCT 116 C390(0.88)  LDD0683  [9]
 LDCM0248  AKOS034007472 HCT 116 C352(1.09)  LDD0565  [9]
 LDCM0356  AKOS034007680 HCT 116 C352(1.05)  LDD0673  [9]
 LDCM0275  AKOS034007705 HCT 116 C352(0.92)  LDD0592  [9]
 LDCM0020  ARS-1620 HCC44 C390(0.84)  LDD0078  [9]
 LDCM0632  CL-Sc Hep-G2 C390(1.05)  LDD2227  [15]
 LDCM0367  CL1 HCT 116 C390(1.04); C352(1.13)  LDD0684  [9]
 LDCM0368  CL10 HCT 116 C352(0.79); C390(1.06)  LDD0685  [9]
 LDCM0369  CL100 HCT 116 C352(0.94); C390(1.00)  LDD0686  [9]
 LDCM0370  CL101 HCT 116 C352(1.08)  LDD0687  [9]
 LDCM0371  CL102 HCT 116 C352(0.96)  LDD0688  [9]
 LDCM0372  CL103 HCT 116 C352(1.23)  LDD0689  [9]
 LDCM0373  CL104 HCT 116 C352(1.03)  LDD0690  [9]
 LDCM0374  CL105 HCT 116 C352(0.92); C390(1.36)  LDD0691  [9]
 LDCM0375  CL106 HCT 116 C352(0.95); C390(1.44)  LDD0692  [9]
 LDCM0376  CL107 HCT 116 C352(0.81); C390(1.58)  LDD0693  [9]
 LDCM0377  CL108 HCT 116 C352(0.86); C390(1.43)  LDD0694  [9]
 LDCM0378  CL109 HCT 116 C352(0.88); C390(1.52)  LDD0695  [9]
 LDCM0379  CL11 HCT 116 C352(0.80); C390(0.95)  LDD0696  [9]
 LDCM0380  CL110 HCT 116 C352(0.88); C390(1.27)  LDD0697  [9]
 LDCM0381  CL111 HCT 116 C352(0.90); C390(1.19)  LDD0698  [9]
 LDCM0382  CL112 HCT 116 C390(0.53); C352(0.99)  LDD0699  [9]
 LDCM0383  CL113 HCT 116 C390(0.54); C352(1.07)  LDD0700  [9]
 LDCM0384  CL114 HCT 116 C390(0.48); C352(0.95)  LDD0701  [9]
 LDCM0385  CL115 HCT 116 C390(0.58); C352(1.08)  LDD0702  [9]
 LDCM0386  CL116 HCT 116 C390(0.60); C352(1.05)  LDD0703  [9]
 LDCM0387  CL117 HCT 116 C390(0.85); C352(0.92)  LDD0704  [9]
 LDCM0388  CL118 HCT 116 C390(0.94); C352(1.18)  LDD0705  [9]
 LDCM0389  CL119 HCT 116 C390(0.83); C352(0.91)  LDD0706  [9]
 LDCM0390  CL12 HCT 116 C352(0.87); C390(1.05)  LDD0707  [9]
 LDCM0391  CL120 HCT 116 C390(0.88); C352(1.18)  LDD0708  [9]
 LDCM0392  CL121 HCT 116 C390(1.06); C352(1.25)  LDD0709  [9]
 LDCM0393  CL122 HCT 116 C352(0.89); C390(0.93)  LDD0710  [9]
 LDCM0394  CL123 HCT 116 C352(0.83); C390(0.99)  LDD0711  [9]
 LDCM0395  CL124 HCT 116 C352(0.91); C390(1.13)  LDD0712  [9]
 LDCM0396  CL125 HCT 116 C390(1.11); C352(1.11)  LDD0713  [9]
 LDCM0397  CL126 HCT 116 C390(1.11); C352(1.17)  LDD0714  [9]
 LDCM0398  CL127 HCT 116 C390(1.12); C352(1.15)  LDD0715  [9]
 LDCM0399  CL128 HCT 116 C390(1.08); C352(1.14)  LDD0716  [9]
 LDCM0400  CL13 HCT 116 C352(0.72); C390(0.81)  LDD0717  [9]
 LDCM0401  CL14 HCT 116 C352(0.86); C390(0.98)  LDD0718  [9]
 LDCM0402  CL15 HCT 116 C352(0.63); C390(0.83)  LDD0719  [9]
 LDCM0403  CL16 HCT 116 C390(1.04)  LDD0720  [9]
 LDCM0404  CL17 HCT 116 C390(0.98)  LDD0721  [9]
 LDCM0405  CL18 HCT 116 C390(0.88)  LDD0722  [9]
 LDCM0406  CL19 HCT 116 C390(0.98)  LDD0723  [9]
 LDCM0407  CL2 HCT 116 C390(0.98); C352(1.06)  LDD0724  [9]
 LDCM0408  CL20 HCT 116 C390(0.97)  LDD0725  [9]
 LDCM0409  CL21 HCT 116 C390(0.98)  LDD0726  [9]
 LDCM0410  CL22 HCT 116 C390(1.04)  LDD0727  [9]
 LDCM0411  CL23 HCT 116 C390(0.97)  LDD0728  [9]
 LDCM0412  CL24 HCT 116 C390(1.02)  LDD0729  [9]
 LDCM0413  CL25 HCT 116 C390(0.90)  LDD0730  [9]
 LDCM0414  CL26 HCT 116 C390(0.91)  LDD0731  [9]
 LDCM0415  CL27 HCT 116 C390(1.00)  LDD0732  [9]
 LDCM0416  CL28 HCT 116 C390(0.89)  LDD0733  [9]
 LDCM0417  CL29 HCT 116 C390(1.10)  LDD0734  [9]
 LDCM0418  CL3 HCT 116 C352(1.02); C390(0.99)  LDD0735  [9]
 LDCM0419  CL30 HCT 116 C390(0.95)  LDD0736  [9]
 LDCM0420  CL31 HCT 116 C352(1.11)  LDD0737  [9]
 LDCM0421  CL32 HCT 116 C352(0.95); C390(1.15)  LDD0738  [9]
 LDCM0422  CL33 HCT 116 C352(0.84); C390(0.97)  LDD0739  [9]
 LDCM0423  CL34 HCT 116 C352(1.04); C390(0.94)  LDD0740  [9]
 LDCM0424  CL35 HCT 116 C352(0.93); C390(1.07)  LDD0741  [9]
 LDCM0425  CL36 HCT 116 C352(0.95); C390(0.99)  LDD0742  [9]
 LDCM0426  CL37 HCT 116 C352(0.79); C390(1.09)  LDD0743  [9]
 LDCM0428  CL39 HCT 116 C352(1.12); C390(1.24)  LDD0745  [9]
 LDCM0429  CL4 HCT 116 C352(1.04); C390(0.90)  LDD0746  [9]
 LDCM0430  CL40 HCT 116 C352(0.99); C390(1.05)  LDD0747  [9]
 LDCM0431  CL41 HCT 116 C352(0.98); C390(0.93)  LDD0748  [9]
 LDCM0432  CL42 HCT 116 C352(0.97); C390(1.33)  LDD0749  [9]
 LDCM0433  CL43 HCT 116 C352(1.08); C390(1.04)  LDD0750  [9]
 LDCM0434  CL44 HCT 116 C352(0.92); C390(1.00)  LDD0751  [9]
 LDCM0435  CL45 HCT 116 C352(1.23); C390(1.11)  LDD0752  [9]
 LDCM0436  CL46 HCT 116 C352(0.92)  LDD0753  [9]
 LDCM0437  CL47 HCT 116 C352(0.98)  LDD0754  [9]
 LDCM0438  CL48 HCT 116 C352(1.02)  LDD0755  [9]
 LDCM0439  CL49 HCT 116 C352(0.91)  LDD0756  [9]
 LDCM0440  CL5 HCT 116 C352(0.94); C390(1.08)  LDD0757  [9]
 LDCM0441  CL50 HCT 116 C352(0.95)  LDD0758  [9]
 LDCM0442  CL51 HCT 116 C352(0.96)  LDD0759  [9]
 LDCM0443  CL52 HCT 116 C352(1.07)  LDD0760  [9]
 LDCM0444  CL53 HCT 116 C352(0.94)  LDD0761  [9]
 LDCM0445  CL54 HCT 116 C352(0.88)  LDD0762  [9]
 LDCM0446  CL55 HCT 116 C352(1.05)  LDD0763  [9]
 LDCM0447  CL56 HCT 116 C352(1.02)  LDD0764  [9]
 LDCM0448  CL57 HCT 116 C352(0.87)  LDD0765  [9]
 LDCM0449  CL58 HCT 116 C352(1.00)  LDD0766  [9]
 LDCM0450  CL59 HCT 116 C352(0.99)  LDD0767  [9]
 LDCM0451  CL6 HCT 116 C352(0.71); C390(0.79)  LDD0768  [9]
 LDCM0452  CL60 HCT 116 C352(1.01)  LDD0769  [9]
 LDCM0453  CL61 HCT 116 C352(1.06)  LDD0770  [9]
 LDCM0454  CL62 HCT 116 C352(1.09)  LDD0771  [9]
 LDCM0455  CL63 HCT 116 C352(0.95)  LDD0772  [9]
 LDCM0456  CL64 HCT 116 C352(0.97)  LDD0773  [9]
 LDCM0457  CL65 HCT 116 C352(1.08)  LDD0774  [9]
 LDCM0458  CL66 HCT 116 C352(0.98)  LDD0775  [9]
 LDCM0459  CL67 HCT 116 C352(1.00)  LDD0776  [9]
 LDCM0460  CL68 HCT 116 C352(1.02)  LDD0777  [9]
 LDCM0461  CL69 HCT 116 C352(0.85)  LDD0778  [9]
 LDCM0462  CL7 HCT 116 C352(0.83); C390(0.96)  LDD0779  [9]
 LDCM0463  CL70 HCT 116 C352(0.98)  LDD0780  [9]
 LDCM0464  CL71 HCT 116 C352(1.01)  LDD0781  [9]
 LDCM0465  CL72 HCT 116 C352(1.09)  LDD0782  [9]
 LDCM0466  CL73 HCT 116 C352(1.02)  LDD0783  [9]
 LDCM0467  CL74 HCT 116 C352(0.98)  LDD0784  [9]
 LDCM0469  CL76 HCT 116 C352(0.77); C390(1.04)  LDD0786  [9]
 LDCM0470  CL77 HCT 116 C352(0.87); C390(1.05)  LDD0787  [9]
 LDCM0471  CL78 HCT 116 C352(0.89); C390(0.98)  LDD0788  [9]
 LDCM0472  CL79 HCT 116 C352(0.87); C390(1.11)  LDD0789  [9]
 LDCM0473  CL8 HCT 116 C352(0.74); C390(0.80)  LDD0790  [9]
 LDCM0474  CL80 HCT 116 C352(0.81); C390(0.95)  LDD0791  [9]
 LDCM0475  CL81 HCT 116 C352(0.83); C390(0.98)  LDD0792  [9]
 LDCM0476  CL82 HCT 116 C352(0.86); C390(1.05)  LDD0793  [9]
 LDCM0477  CL83 HCT 116 C352(0.78); C390(1.14)  LDD0794  [9]
 LDCM0478  CL84 HCT 116 C352(0.81); C390(1.39)  LDD0795  [9]
 LDCM0479  CL85 HCT 116 C352(0.94); C390(1.10)  LDD0796  [9]
 LDCM0480  CL86 HCT 116 C352(1.09); C390(0.96)  LDD0797  [9]
 LDCM0481  CL87 HCT 116 C352(0.97); C390(0.94)  LDD0798  [9]
 LDCM0482  CL88 HCT 116 C352(0.78); C390(0.99)  LDD0799  [9]
 LDCM0483  CL89 HCT 116 C352(0.88); C390(1.04)  LDD0800  [9]
 LDCM0484  CL9 HCT 116 C352(0.82); C390(1.04)  LDD0801  [9]
 LDCM0485  CL90 HCT 116 C352(0.99); C390(1.06)  LDD0802  [9]
 LDCM0486  CL91 HCT 116 C352(1.06); C390(0.94)  LDD0803  [9]
 LDCM0487  CL92 HCT 116 C352(0.99); C390(0.94)  LDD0804  [9]
 LDCM0488  CL93 HCT 116 C352(0.90); C390(1.10)  LDD0805  [9]
 LDCM0489  CL94 HCT 116 C352(0.93); C390(0.94)  LDD0806  [9]
 LDCM0490  CL95 HCT 116 C352(0.98); C390(0.83)  LDD0807  [9]
 LDCM0491  CL96 HCT 116 C352(0.98); C390(0.92)  LDD0808  [9]
 LDCM0492  CL97 HCT 116 C352(0.98); C390(0.94)  LDD0809  [9]
 LDCM0493  CL98 HCT 116 C352(1.00); C390(1.04)  LDD0810  [9]
 LDCM0494  CL99 HCT 116 C352(1.01); C390(0.91)  LDD0811  [9]
 LDCM0017  DFG-out-2 A431 2.30  LDD0075  [22]
 LDCM0495  E2913 HEK-293T C480(0.93); C352(1.21); C390(1.26)  LDD1698  [23]
 LDCM0468  Fragment33 HCT 116 C352(1.01)  LDD0785  [9]
 LDCM0427  Fragment51 HCT 116 C352(0.94); C390(1.09)  LDD0744  [9]
 LDCM0116  HHS-0101 DM93 Y130(0.90)  LDD0264  [6]
 LDCM0117  HHS-0201 DM93 Y130(0.81)  LDD0265  [6]
 LDCM0118  HHS-0301 DM93 Y130(0.80)  LDD0266  [6]
 LDCM0119  HHS-0401 DM93 Y130(0.94)  LDD0267  [6]
 LDCM0120  HHS-0701 DM93 Y130(0.89)  LDD0268  [6]
 LDCM0123  JWB131 DM93 Y130(1.16)  LDD0285  [5]
 LDCM0124  JWB142 DM93 Y130(0.71)  LDD0286  [5]
 LDCM0125  JWB146 DM93 Y130(1.15)  LDD0287  [5]
 LDCM0126  JWB150 DM93 Y130(3.14)  LDD0288  [5]
 LDCM0127  JWB152 DM93 Y130(2.10)  LDD0289  [5]
 LDCM0128  JWB198 DM93 Y130(0.96)  LDD0290  [5]
 LDCM0129  JWB202 DM93 Y130(0.62)  LDD0291  [5]
 LDCM0130  JWB211 DM93 Y130(0.91)  LDD0292  [5]
 LDCM0022  KB02 HEK-293T C352(0.98)  LDD1492  [23]
 LDCM0023  KB03 HEK-293T C352(0.91)  LDD1497  [23]
 LDCM0024  KB05 G361 C501(1.27); C352(1.31)  LDD3311  [24]
 LDCM0109  NEM HeLa N.A.  LDD0223  [8]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 10 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Caspase-7 (CASP7) Peptidase C14A family P55210
Serine/threonine-protein kinase PAK 2 (PAK2) STE Ser/Thr protein kinase family Q13177
LIM domain kinase 1 (LIMK1) TKL Ser/Thr protein kinase family P53667
RAF proto-oncogene serine/threonine-protein kinase (RAF1) TKL Ser/Thr protein kinase family P04049
Proto-oncogene tyrosine-protein kinase Src (SRC) Tyr protein kinase family P12931
Tyrosine-protein kinase HCK (HCK) Tyr protein kinase family P08631
E3 ubiquitin-protein ligase SH3RF3 (SH3RF3) SH3RF family Q8TEJ3
Ras-related C3 botulinum toxin substrate 1 (RAC1) Rho family P63000
Rho-related GTP-binding protein RhoJ (RHOJ) Rho family Q9H4E5
Cell division control protein 42 homolog (CDC42) Rho family P60953
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
Cytoplasmic protein NCK2 (NCK2) . O43639
Rho guanine nucleotide exchange factor 6 (ARHGEF6) . Q15052
Rho guanine nucleotide exchange factor 7 (ARHGEF7) . Q14155
SH2/SH3 adapter protein NCK1 (NCK1) . P16333
Sorbin and SH3 domain-containing protein 1 (SORBS1) . Q9BX66
Sorbin and SH3 domain-containing protein 2 (SORBS2) . O94875
Vinexin (SORBS3) . O60504

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
Il-94 Small molecular drug D07ORL

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 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.
3 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
4 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.
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 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.
7 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.
8 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.
9 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.
10 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
11 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.
12 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
13 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
14 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
15 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
16 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
17 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.
18 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
19 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.
20 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
21 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
22 Affinity-based probes based on type II kinase inhibitors. J Am Chem Soc. 2012 Nov 21;134(46):19017-25. doi: 10.1021/ja306035v. Epub 2012 Nov 6.
23 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
24 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