General Information of Target

Target ID LDTP01751
Target Name Serine/threonine-protein kinase PAK 4 (PAK4)
Gene Name PAK4
Gene ID 10298
Synonyms
KIAA1142; Serine/threonine-protein kinase PAK 4; EC 2.7.11.1; p21-activated kinase 4; PAK-4
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MFGKRKKRVEISAPSNFEHRVHTGFDQHEQKFTGLPRQWQSLIEESARRPKPLVDPACIT
SIQPGAPKTIVRGSKGAKDGALTLLLDEFENMSVTRSNSLRRDSPPPPARARQENGMPEE
PATTARGGPGKAGSRGRFAGHSEAGGGSGDRRRAGPEKRPKSSREGSGGPQESSRDKRPL
SGPDVGTPQPAGLASGAKLAAGRPFNTYPRADTDHPSRGAQGEPHDVAPNGPSAGGLAIP
QSSSSSSRPPTRARGAPSPGVLGPHASEPQLAPPACTPAAPAVPGPPGPRSPQREPQRVS
HEQFRAALQLVVDPGDPRSYLDNFIKIGEGSTGIVCIATVRSSGKLVAVKKMDLRKQQRR
ELLFNEVVIMRDYQHENVVEMYNSYLVGDELWVVMEFLEGGALTDIVTHTRMNEEQIAAV
CLAVLQALSVLHAQGVIHRDIKSDSILLTHDGRVKLSDFGFCAQVSKEVPRRKSLVGTPY
WMAPELISRLPYGPEVDIWSLGIMVIEMVDGEPPYFNEPPLKAMKMIRDNLPPRLKNLHK
VSPSLKGFLDRLLVRDPAQRATAAELLKHPFLAKAGPPASIVPLMRQNRTR
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, STE20 subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine protein kinase that plays a role in a variety of different signaling pathways including cytoskeleton regulation, cell migration, growth, proliferation or cell survival. Activation by various effectors including growth factor receptors or active CDC42 and RAC1 results in a conformational change and a subsequent autophosphorylation on several serine and/or threonine residues. Phosphorylates and inactivates the protein phosphatase SSH1, leading to increased inhibitory phosphorylation of the actin binding/depolymerizing factor cofilin. Decreased cofilin activity may lead to stabilization of actin filaments. Phosphorylates LIMK1, a kinase that also inhibits the activity of cofilin. Phosphorylates integrin beta5/ITGB5 and thus regulates cell motility. Phosphorylates ARHGEF2 and activates the downstream target RHOA that plays a role in the regulation of assembly of focal adhesions and actin stress fibers. Stimulates cell survival by phosphorylating the BCL2 antagonist of cell death BAD. Alternatively, inhibits apoptosis by preventing caspase-8 binding to death domain receptors in a kinase independent manner. Plays a role in cell-cycle progression by controlling levels of the cell-cycle regulatory protein CDKN1A and by phosphorylating RAN.
TTD ID
T98293
Uniprot ID
O96013
DrugMap ID
TT7Y3BZ
Ensemble ID
ENST00000321944.8
HGNC ID
HGNC:16059
ChEMBL ID
CHEMBL4482

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
FUOV1 SNV: p.D389Y .
GB1 Substitution: p.S300F .
IGROV1 Deletion: p.A81PfsTer14 .
NB4 SNV: p.A427S .
RL952 SNV: p.K31R .
TE4 SNV: p.T33R .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 21 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
15.00  LDD0402  [1]
ONAyne
 Probe Info 
K31(4.25)  LDD0274  [2]
STPyne
 Probe Info 
K158(0.11); K31(7.22); K540(9.42); K546(5.19)  LDD0277  [2]
BTD
 Probe Info 
C58(0.91)  LDD2099  [3]
AHL-Pu-1
 Probe Info 
C276(2.11)  LDD0168  [4]
EA-probe
 Probe Info 
N.A.  LDD0440  [5]
HHS-475
 Probe Info 
Y320(0.71)  LDD0264  [6]
Acrolein
 Probe Info 
N.A.  LDD0223  [7]
DBIA
 Probe Info 
C462(0.75); C58(0.82)  LDD0531  [8]
5E-2FA
 Probe Info 
N.A.  LDD2235  [9]
1d-yne
 Probe Info 
N.A.  LDD0358  [10]
4-Iodoacetamidophenylacetylene
 Probe Info 
C462(0.00); C421(0.00)  LDD0038  [11]
IA-alkyne
 Probe Info 
C421(0.00); C462(0.00)  LDD0036  [11]
Lodoacetamide azide
 Probe Info 
N.A.  LDD0037  [11]
IPM
 Probe Info 
C276(0.00); C58(0.00)  LDD0025  [12]
JW-RF-010
 Probe Info 
N.A.  LDD0026  [12]
TFBX
 Probe Info 
N.A.  LDD0027  [12]
VSF
 Probe Info 
N.A.  LDD0007  [13]
Phosphinate-6
 Probe Info 
N.A.  LDD0018  [14]
W1
 Probe Info 
N.A.  LDD0236  [15]
NAIA_5
 Probe Info 
C462(0.00); C421(0.00)  LDD2223  [16]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Staurosporine capture compound
 Probe Info 
N.A.  LDD0083  [17]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C276(2.11)  LDD0168  [4]
 LDCM0026  4SU-RNA+native RNA HEK-293T C276(4.20); C58(2.90)  LDD0169  [4]
 LDCM0214  AC1 HCT 116 C462(0.75); C58(0.82)  LDD0531  [8]
 LDCM0215  AC10 HCT 116 C462(1.12)  LDD0532  [8]
 LDCM0226  AC11 HCT 116 C462(0.79)  LDD0543  [8]
 LDCM0237  AC12 HCT 116 C462(1.00)  LDD0554  [8]
 LDCM0246  AC128 PaTu 8988t C462(0.86)  LDD1125  [8]
 LDCM0247  AC129 PaTu 8988t C462(0.87)  LDD1126  [8]
 LDCM0249  AC130 PaTu 8988t C462(0.87)  LDD1128  [8]
 LDCM0250  AC131 PaTu 8988t C462(0.87)  LDD1129  [8]
 LDCM0251  AC132 PaTu 8988t C462(0.98)  LDD1130  [8]
 LDCM0252  AC133 PaTu 8988t C462(0.87)  LDD1131  [8]
 LDCM0253  AC134 PaTu 8988t C462(0.86)  LDD1132  [8]
 LDCM0254  AC135 PaTu 8988t C462(0.85)  LDD1133  [8]
 LDCM0255  AC136 PaTu 8988t C462(0.89)  LDD1134  [8]
 LDCM0256  AC137 PaTu 8988t C462(0.83)  LDD1135  [8]
 LDCM0257  AC138 PaTu 8988t C462(0.87)  LDD1136  [8]
 LDCM0258  AC139 PaTu 8988t C462(0.82)  LDD1137  [8]
 LDCM0259  AC14 HCT 116 C462(0.82)  LDD0576  [8]
 LDCM0260  AC140 PaTu 8988t C462(0.84)  LDD1139  [8]
 LDCM0261  AC141 PaTu 8988t C462(0.92)  LDD1140  [8]
 LDCM0262  AC142 PaTu 8988t C462(0.92)  LDD1141  [8]
 LDCM0263  AC143 PaTu 8988t C462(0.79)  LDD1142  [8]
 LDCM0264  AC144 PaTu 8988t C462(0.68)  LDD1143  [8]
 LDCM0265  AC145 PaTu 8988t C462(0.75)  LDD1144  [8]
 LDCM0266  AC146 PaTu 8988t C462(0.60)  LDD1145  [8]
 LDCM0267  AC147 PaTu 8988t C462(0.64)  LDD1146  [8]
 LDCM0268  AC148 PaTu 8988t C462(0.64)  LDD1147  [8]
 LDCM0269  AC149 PaTu 8988t C462(0.65)  LDD1148  [8]
 LDCM0270  AC15 HCT 116 C462(1.16)  LDD0587  [8]
 LDCM0271  AC150 PaTu 8988t C462(0.73)  LDD1150  [8]
 LDCM0272  AC151 PaTu 8988t C462(0.62)  LDD1151  [8]
 LDCM0273  AC152 PaTu 8988t C462(0.58)  LDD1152  [8]
 LDCM0274  AC153 PaTu 8988t C462(0.59)  LDD1153  [8]
 LDCM0621  AC154 PaTu 8988t C462(0.58)  LDD2166  [8]
 LDCM0622  AC155 PaTu 8988t C462(0.67)  LDD2167  [8]
 LDCM0623  AC156 PaTu 8988t C462(0.59)  LDD2168  [8]
 LDCM0624  AC157 PaTu 8988t C462(0.63)  LDD2169  [8]
 LDCM0276  AC17 PaTu 8988t C462(0.97)  LDD1155  [8]
 LDCM0277  AC18 PaTu 8988t C462(0.60)  LDD1156  [8]
 LDCM0278  AC19 PaTu 8988t C462(0.82)  LDD1157  [8]
 LDCM0279  AC2 HCT 116 C58(0.79); C462(0.81)  LDD0596  [8]
 LDCM0280  AC20 PaTu 8988t C462(0.66)  LDD1159  [8]
 LDCM0281  AC21 PaTu 8988t C462(0.74)  LDD1160  [8]
 LDCM0282  AC22 PaTu 8988t C462(0.61)  LDD1161  [8]
 LDCM0283  AC23 PaTu 8988t C462(0.56)  LDD1162  [8]
 LDCM0284  AC24 PaTu 8988t C462(0.56)  LDD1163  [8]
 LDCM0285  AC25 HCT 116 C462(0.63)  LDD0602  [8]
 LDCM0286  AC26 HCT 116 C462(0.66)  LDD0603  [8]
 LDCM0287  AC27 HCT 116 C462(0.77)  LDD0604  [8]
 LDCM0288  AC28 HCT 116 C462(0.83)  LDD0605  [8]
 LDCM0289  AC29 HCT 116 C462(0.67)  LDD0606  [8]
 LDCM0290  AC3 HCT 116 C462(0.77); C58(0.77)  LDD0607  [8]
 LDCM0291  AC30 HCT 116 C462(0.71)  LDD0608  [8]
 LDCM0292  AC31 HCT 116 C462(0.97)  LDD0609  [8]
 LDCM0293  AC32 HCT 116 C462(0.60)  LDD0610  [8]
 LDCM0294  AC33 HCT 116 C462(0.56)  LDD0611  [8]
 LDCM0295  AC34 HCT 116 C462(0.59)  LDD0612  [8]
 LDCM0296  AC35 HCT 116 C58(1.34); C462(1.41)  LDD0613  [8]
 LDCM0297  AC36 HCT 116 C462(0.83); C58(1.61)  LDD0614  [8]
 LDCM0298  AC37 HCT 116 C462(0.86); C58(1.85)  LDD0615  [8]
 LDCM0299  AC38 HCT 116 C462(0.89); C58(1.57)  LDD0616  [8]
 LDCM0300  AC39 HCT 116 C462(1.04); C58(1.44)  LDD0617  [8]
 LDCM0301  AC4 HCT 116 C462(0.89); C58(0.90)  LDD0618  [8]
 LDCM0302  AC40 HCT 116 C462(0.98); C58(2.07)  LDD0619  [8]
 LDCM0303  AC41 HCT 116 C462(0.84); C58(1.70)  LDD0620  [8]
 LDCM0304  AC42 HCT 116 C462(0.88); C58(1.52)  LDD0621  [8]
 LDCM0305  AC43 HCT 116 C462(0.70); C58(2.04)  LDD0622  [8]
 LDCM0306  AC44 HCT 116 C462(0.69); C58(2.24)  LDD0623  [8]
 LDCM0307  AC45 HCT 116 C462(0.72); C58(2.04)  LDD0624  [8]
 LDCM0308  AC46 PaTu 8988t C462(0.79)  LDD1187  [8]
 LDCM0309  AC47 PaTu 8988t C462(0.64)  LDD1188  [8]
 LDCM0310  AC48 PaTu 8988t C462(0.61)  LDD1189  [8]
 LDCM0311  AC49 PaTu 8988t C462(0.62)  LDD1190  [8]
 LDCM0312  AC5 HCT 116 C58(0.73); C462(0.90)  LDD0629  [8]
 LDCM0313  AC50 PaTu 8988t C462(0.62)  LDD1192  [8]
 LDCM0314  AC51 PaTu 8988t C462(0.75)  LDD1193  [8]
 LDCM0315  AC52 PaTu 8988t C462(0.62)  LDD1194  [8]
 LDCM0316  AC53 PaTu 8988t C462(0.53)  LDD1195  [8]
 LDCM0317  AC54 PaTu 8988t C462(0.53)  LDD1196  [8]
 LDCM0318  AC55 PaTu 8988t C462(0.68)  LDD1197  [8]
 LDCM0319  AC56 PaTu 8988t C462(0.62)  LDD1198  [8]
 LDCM0320  AC57 HCT 116 C58(1.03)  LDD0637  [8]
 LDCM0321  AC58 HCT 116 C58(1.05)  LDD0638  [8]
 LDCM0322  AC59 HCT 116 C58(1.19)  LDD0639  [8]
 LDCM0323  AC6 HCT 116 C462(1.03)  LDD0640  [8]
 LDCM0324  AC60 HCT 116 C58(1.26)  LDD0641  [8]
 LDCM0325  AC61 HCT 116 C58(0.92)  LDD0642  [8]
 LDCM0326  AC62 HCT 116 C58(1.25)  LDD0643  [8]
 LDCM0327  AC63 HCT 116 C58(1.24)  LDD0644  [8]
 LDCM0328  AC64 HCT 116 C58(1.31)  LDD0645  [8]
 LDCM0329  AC65 HCT 116 C58(1.09)  LDD0646  [8]
 LDCM0330  AC66 HCT 116 C58(1.48)  LDD0647  [8]
 LDCM0331  AC67 HCT 116 C58(1.36)  LDD0648  [8]
 LDCM0332  AC68 PaTu 8988t C462(1.03)  LDD1211  [8]
 LDCM0333  AC69 PaTu 8988t C462(0.83)  LDD1212  [8]
 LDCM0334  AC7 HCT 116 C462(0.99)  LDD0651  [8]
 LDCM0335  AC70 PaTu 8988t C462(0.84)  LDD1214  [8]
 LDCM0336  AC71 PaTu 8988t C462(0.83)  LDD1215  [8]
 LDCM0337  AC72 PaTu 8988t C462(1.21)  LDD1216  [8]
 LDCM0338  AC73 PaTu 8988t C462(1.10)  LDD1217  [8]
 LDCM0339  AC74 PaTu 8988t C462(1.00)  LDD1218  [8]
 LDCM0340  AC75 PaTu 8988t C462(0.75)  LDD1219  [8]
 LDCM0341  AC76 PaTu 8988t C462(0.90)  LDD1220  [8]
 LDCM0342  AC77 PaTu 8988t C462(0.79)  LDD1221  [8]
 LDCM0343  AC78 PaTu 8988t C462(1.09)  LDD1222  [8]
 LDCM0344  AC79 PaTu 8988t C462(0.69)  LDD1223  [8]
 LDCM0345  AC8 HCT 116 C462(0.95)  LDD0662  [8]
 LDCM0346  AC80 PaTu 8988t C462(1.03)  LDD1225  [8]
 LDCM0347  AC81 PaTu 8988t C462(1.01)  LDD1226  [8]
 LDCM0348  AC82 PaTu 8988t C462(0.99)  LDD1227  [8]
 LDCM0349  AC83 PaTu 8988t C462(1.21)  LDD1228  [8]
 LDCM0350  AC84 PaTu 8988t C462(1.11)  LDD1229  [8]
 LDCM0351  AC85 PaTu 8988t C462(1.16)  LDD1230  [8]
 LDCM0352  AC86 PaTu 8988t C462(1.20)  LDD1231  [8]
 LDCM0353  AC87 PaTu 8988t C462(1.40)  LDD1232  [8]
 LDCM0354  AC88 PaTu 8988t C462(1.40)  LDD1233  [8]
 LDCM0355  AC89 PaTu 8988t C462(1.33)  LDD1234  [8]
 LDCM0357  AC90 PaTu 8988t C462(1.60)  LDD1236  [8]
 LDCM0358  AC91 PaTu 8988t C462(1.30)  LDD1237  [8]
 LDCM0359  AC92 PaTu 8988t C462(1.22)  LDD1238  [8]
 LDCM0360  AC93 PaTu 8988t C462(1.95)  LDD1239  [8]
 LDCM0361  AC94 PaTu 8988t C462(1.26)  LDD1240  [8]
 LDCM0362  AC95 PaTu 8988t C462(1.26)  LDD1241  [8]
 LDCM0363  AC96 PaTu 8988t C462(2.30)  LDD1242  [8]
 LDCM0364  AC97 PaTu 8988t C462(1.38)  LDD1243  [8]
 LDCM0248  AKOS034007472 HCT 116 C462(1.04)  LDD0565  [8]
 LDCM0356  AKOS034007680 HCT 116 C462(0.84)  LDD0673  [8]
 LDCM0275  AKOS034007705 HCT 116 C462(0.98)  LDD0592  [8]
 LDCM0156  Aniline NCI-H1299 11.83  LDD0403  [1]
 LDCM0632  CL-Sc Hep-G2 C462(20.00); C336(0.31)  LDD2227  [16]
 LDCM0367  CL1 PaTu 8988t C462(0.91)  LDD1246  [8]
 LDCM0368  CL10 PaTu 8988t C462(0.58)  LDD1247  [8]
 LDCM0369  CL100 HCT 116 C462(0.73); C58(0.97)  LDD0686  [8]
 LDCM0370  CL101 HCT 116 C462(0.97)  LDD0687  [8]
 LDCM0371  CL102 HCT 116 C462(0.96)  LDD0688  [8]
 LDCM0372  CL103 HCT 116 C462(0.85)  LDD0689  [8]
 LDCM0373  CL104 HCT 116 C462(0.90)  LDD0690  [8]
 LDCM0374  CL105 PaTu 8988t C462(0.74)  LDD1253  [8]
 LDCM0375  CL106 PaTu 8988t C462(0.74)  LDD1254  [8]
 LDCM0376  CL107 PaTu 8988t C462(0.78)  LDD1255  [8]
 LDCM0377  CL108 PaTu 8988t C462(0.78)  LDD1256  [8]
 LDCM0378  CL109 PaTu 8988t C462(0.70)  LDD1257  [8]
 LDCM0379  CL11 PaTu 8988t C462(0.81)  LDD1258  [8]
 LDCM0380  CL110 PaTu 8988t C462(0.57)  LDD1259  [8]
 LDCM0381  CL111 PaTu 8988t C462(0.50)  LDD1260  [8]
 LDCM0382  CL112 HCT 116 C462(0.90)  LDD0699  [8]
 LDCM0383  CL113 HCT 116 C462(0.72)  LDD0700  [8]
 LDCM0384  CL114 HCT 116 C462(0.52)  LDD0701  [8]
 LDCM0385  CL115 HCT 116 C462(0.63)  LDD0702  [8]
 LDCM0386  CL116 HCT 116 C462(0.55)  LDD0703  [8]
 LDCM0387  CL117 HCT 116 C462(1.70); C58(1.85)  LDD0704  [8]
 LDCM0388  CL118 HCT 116 C462(0.81); C58(1.07)  LDD0705  [8]
 LDCM0389  CL119 HCT 116 C462(0.95); C58(1.17)  LDD0706  [8]
 LDCM0390  CL12 PaTu 8988t C462(0.73)  LDD1269  [8]
 LDCM0391  CL120 HCT 116 C462(0.95); C58(1.93)  LDD0708  [8]
 LDCM0392  CL121 PaTu 8988t C462(0.65)  LDD1271  [8]
 LDCM0393  CL122 PaTu 8988t C462(0.67)  LDD1272  [8]
 LDCM0394  CL123 PaTu 8988t C462(0.50)  LDD1273  [8]
 LDCM0395  CL124 PaTu 8988t C462(0.54)  LDD1274  [8]
 LDCM0396  CL125 HCT 116 C58(1.17)  LDD0713  [8]
 LDCM0397  CL126 HCT 116 C58(1.02)  LDD0714  [8]
 LDCM0398  CL127 HCT 116 C58(1.14)  LDD0715  [8]
 LDCM0399  CL128 HCT 116 C58(1.13)  LDD0716  [8]
 LDCM0400  CL13 PaTu 8988t C462(0.61)  LDD1279  [8]
 LDCM0401  CL14 PaTu 8988t C462(0.60)  LDD1280  [8]
 LDCM0402  CL15 PaTu 8988t C462(0.59)  LDD1281  [8]
 LDCM0403  CL16 HCT 116 C58(0.54); C462(0.72)  LDD0720  [8]
 LDCM0404  CL17 HCT 116 C58(0.98); C462(1.16)  LDD0721  [8]
 LDCM0405  CL18 HCT 116 C462(0.78); C58(0.91)  LDD0722  [8]
 LDCM0406  CL19 HCT 116 C462(0.96); C58(1.06)  LDD0723  [8]
 LDCM0407  CL2 PaTu 8988t C462(0.81)  LDD1286  [8]
 LDCM0408  CL20 HCT 116 C462(0.82); C58(1.22)  LDD0725  [8]
 LDCM0409  CL21 HCT 116 C58(1.04); C462(1.06)  LDD0726  [8]
 LDCM0410  CL22 HCT 116 C462(0.84); C58(0.87)  LDD0727  [8]
 LDCM0411  CL23 HCT 116 C462(0.74); C58(1.21)  LDD0728  [8]
 LDCM0412  CL24 HCT 116 C462(0.71); C58(0.92)  LDD0729  [8]
 LDCM0413  CL25 HCT 116 C462(0.66); C58(0.99)  LDD0730  [8]
 LDCM0414  CL26 HCT 116 C462(0.72); C58(1.03)  LDD0731  [8]
 LDCM0415  CL27 HCT 116 C462(0.82); C58(0.94)  LDD0732  [8]
 LDCM0416  CL28 HCT 116 C462(0.62); C58(1.17)  LDD0733  [8]
 LDCM0417  CL29 HCT 116 C462(0.71); C58(1.07)  LDD0734  [8]
 LDCM0418  CL3 PaTu 8988t C462(0.65)  LDD1297  [8]
 LDCM0419  CL30 HCT 116 C462(0.69); C58(1.08)  LDD0736  [8]
 LDCM0420  CL31 HEK-293T C58(0.99)  LDD1624  [18]
 LDCM0421  CL32 HCT 116 C462(0.64)  LDD0738  [8]
 LDCM0422  CL33 HCT 116 C462(0.63)  LDD0739  [8]
 LDCM0423  CL34 HCT 116 C462(0.88)  LDD0740  [8]
 LDCM0424  CL35 HCT 116 C462(0.78)  LDD0741  [8]
 LDCM0425  CL36 HCT 116 C462(0.92)  LDD0742  [8]
 LDCM0426  CL37 HCT 116 C462(0.92)  LDD0743  [8]
 LDCM0428  CL39 HCT 116 C462(0.73)  LDD0745  [8]
 LDCM0429  CL4 PaTu 8988t C462(0.63)  LDD1308  [8]
 LDCM0430  CL40 HCT 116 C462(0.73)  LDD0747  [8]
 LDCM0431  CL41 HCT 116 C462(0.71)  LDD0748  [8]
 LDCM0432  CL42 HCT 116 C462(1.02)  LDD0749  [8]
 LDCM0433  CL43 HCT 116 C462(0.65)  LDD0750  [8]
 LDCM0434  CL44 HCT 116 C462(0.73)  LDD0751  [8]
 LDCM0435  CL45 HCT 116 C462(0.76)  LDD0752  [8]
 LDCM0436  CL46 HCT 116 C462(0.79); C58(0.99)  LDD0753  [8]
 LDCM0437  CL47 HCT 116 C462(1.01); C58(1.00)  LDD0754  [8]
 LDCM0438  CL48 HCT 116 C462(0.88); C58(0.80)  LDD0755  [8]
 LDCM0439  CL49 HCT 116 C462(1.00); C58(0.91)  LDD0756  [8]
 LDCM0440  CL5 PaTu 8988t C462(0.56)  LDD1319  [8]
 LDCM0441  CL50 HCT 116 C462(0.87); C58(1.01)  LDD0758  [8]
 LDCM0442  CL51 HCT 116 C462(0.92); C58(0.85)  LDD0759  [8]
 LDCM0443  CL52 HCT 116 C462(0.73); C58(1.01)  LDD0760  [8]
 LDCM0444  CL53 HCT 116 C462(1.01); C58(1.02)  LDD0761  [8]
 LDCM0445  CL54 HCT 116 C462(0.88); C58(1.03)  LDD0762  [8]
 LDCM0446  CL55 HCT 116 C462(1.19); C58(0.96)  LDD0763  [8]
 LDCM0447  CL56 HCT 116 C462(1.06); C58(0.90)  LDD0764  [8]
 LDCM0448  CL57 HCT 116 C462(1.01); C58(0.92)  LDD0765  [8]
 LDCM0449  CL58 HCT 116 C462(0.82); C58(0.95)  LDD0766  [8]
 LDCM0450  CL59 HCT 116 C462(0.94); C58(0.91)  LDD0767  [8]
 LDCM0451  CL6 PaTu 8988t C462(0.59)  LDD1330  [8]
 LDCM0452  CL60 HCT 116 C462(0.77); C58(0.87)  LDD0769  [8]
 LDCM0453  CL61 PaTu 8988t C462(0.86)  LDD1332  [8]
 LDCM0454  CL62 PaTu 8988t C462(0.77)  LDD1333  [8]
 LDCM0455  CL63 PaTu 8988t C462(0.88)  LDD1334  [8]
 LDCM0456  CL64 PaTu 8988t C462(0.72)  LDD1335  [8]
 LDCM0457  CL65 PaTu 8988t C462(0.79)  LDD1336  [8]
 LDCM0458  CL66 PaTu 8988t C462(0.77)  LDD1337  [8]
 LDCM0459  CL67 PaTu 8988t C462(0.72)  LDD1338  [8]
 LDCM0460  CL68 PaTu 8988t C462(0.69)  LDD1339  [8]
 LDCM0461  CL69 PaTu 8988t C462(0.66)  LDD1340  [8]
 LDCM0462  CL7 PaTu 8988t C462(0.59)  LDD1341  [8]
 LDCM0463  CL70 PaTu 8988t C462(0.77)  LDD1342  [8]
 LDCM0464  CL71 PaTu 8988t C462(0.84)  LDD1343  [8]
 LDCM0465  CL72 PaTu 8988t C462(0.85)  LDD1344  [8]
 LDCM0466  CL73 PaTu 8988t C462(0.62)  LDD1345  [8]
 LDCM0467  CL74 PaTu 8988t C462(0.68)  LDD1346  [8]
 LDCM0469  CL76 HCT 116 C58(0.88)  LDD0786  [8]
 LDCM0470  CL77 HCT 116 C58(0.91)  LDD0787  [8]
 LDCM0471  CL78 HCT 116 C58(0.88)  LDD0788  [8]
 LDCM0472  CL79 HCT 116 C58(0.91)  LDD0789  [8]
 LDCM0473  CL8 PaTu 8988t C462(0.58)  LDD1352  [8]
 LDCM0474  CL80 HCT 116 C58(0.85)  LDD0791  [8]
 LDCM0475  CL81 HCT 116 C58(0.81)  LDD0792  [8]
 LDCM0476  CL82 HCT 116 C58(0.84)  LDD0793  [8]
 LDCM0477  CL83 HCT 116 C58(0.87)  LDD0794  [8]
 LDCM0478  CL84 HCT 116 C58(0.89)  LDD0795  [8]
 LDCM0479  CL85 HCT 116 C58(0.90)  LDD0796  [8]
 LDCM0480  CL86 HCT 116 C58(0.87)  LDD0797  [8]
 LDCM0481  CL87 HCT 116 C58(0.88)  LDD0798  [8]
 LDCM0482  CL88 HCT 116 C58(0.73)  LDD0799  [8]
 LDCM0483  CL89 HCT 116 C58(0.92)  LDD0800  [8]
 LDCM0484  CL9 PaTu 8988t C462(0.68)  LDD1363  [8]
 LDCM0485  CL90 HCT 116 C58(0.80)  LDD0802  [8]
 LDCM0486  CL91 HCT 116 C462(0.84); C58(0.87)  LDD0803  [8]
 LDCM0487  CL92 HCT 116 C462(1.14); C58(0.81)  LDD0804  [8]
 LDCM0488  CL93 HCT 116 C462(1.17); C58(0.75)  LDD0805  [8]
 LDCM0489  CL94 HCT 116 C462(0.74); C58(0.93)  LDD0806  [8]
 LDCM0490  CL95 HCT 116 C462(0.95); C58(0.68)  LDD0807  [8]
 LDCM0491  CL96 HCT 116 C462(0.80); C58(0.75)  LDD0808  [8]
 LDCM0492  CL97 HCT 116 C462(0.75); C58(0.81)  LDD0809  [8]
 LDCM0493  CL98 HCT 116 C462(0.79); C58(0.87)  LDD0810  [8]
 LDCM0494  CL99 HCT 116 C462(0.85); C58(0.76)  LDD0811  [8]
 LDCM0634  CY-0357 Hep-G2 C276(0.59)  LDD2228  [16]
 LDCM0495  E2913 HEK-293T C276(1.10); C462(0.85); C58(0.87)  LDD1698  [18]
 LDCM0175  Ethacrynic acid HeLa N.A.  LDD0440  [5]
 LDCM0625  F8 Ramos C276(0.99)  LDD2187  [19]
 LDCM0572  Fragment10 Ramos C276(1.03)  LDD2189  [19]
 LDCM0573  Fragment11 Ramos C58(1.31); C276(5.29)  LDD2190  [19]
 LDCM0574  Fragment12 Ramos C276(0.55)  LDD2191  [19]
 LDCM0575  Fragment13 Ramos C276(0.73)  LDD2192  [19]
 LDCM0576  Fragment14 Ramos C58(0.48); C276(0.51)  LDD2193  [19]
 LDCM0579  Fragment20 Ramos C276(0.50)  LDD2194  [19]
 LDCM0580  Fragment21 Ramos C276(0.56)  LDD2195  [19]
 LDCM0578  Fragment27 Ramos C276(0.57)  LDD2197  [19]
 LDCM0586  Fragment28 Ramos C276(0.47)  LDD2198  [19]
 LDCM0588  Fragment30 Ramos C276(0.69)  LDD2199  [19]
 LDCM0590  Fragment32 Ramos C276(0.67)  LDD2201  [19]
 LDCM0468  Fragment33 PaTu 8988t C462(0.74)  LDD1347  [8]
 LDCM0596  Fragment38 Ramos C276(1.81)  LDD2203  [19]
 LDCM0566  Fragment4 Ramos C58(0.89); C276(2.09)  LDD2184  [19]
 LDCM0427  Fragment51 HCT 116 C462(0.99)  LDD0744  [8]
 LDCM0610  Fragment52 Ramos C276(0.56)  LDD2204  [19]
 LDCM0614  Fragment56 Ramos C276(0.82)  LDD2205  [19]
 LDCM0569  Fragment7 Ramos C58(0.67); C276(1.06)  LDD2186  [19]
 LDCM0571  Fragment9 Ramos C276(0.65)  LDD2188  [19]
 LDCM0116  HHS-0101 DM93 Y320(0.71)  LDD0264  [6]
 LDCM0117  HHS-0201 DM93 Y320(1.06)  LDD0265  [6]
 LDCM0118  HHS-0301 DM93 Y320(0.71)  LDD0266  [6]
 LDCM0119  HHS-0401 DM93 Y320(0.94)  LDD0267  [6]
 LDCM0120  HHS-0701 DM93 Y320(0.87)  LDD0268  [6]
 LDCM0022  KB02 HEK-293T C276(0.98); C58(1.10)  LDD1492  [18]
 LDCM0023  KB03 HEK-293T C276(1.05); C58(1.12)  LDD1497  [18]
 LDCM0024  KB05 COLO792 C336(1.38)  LDD3310  [20]
 LDCM0109  NEM HeLa N.A.  LDD0223  [7]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C58(0.91)  LDD2099  [3]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C276(1.21)  LDD2118  [3]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C276(0.95)  LDD2124  [3]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C58(1.05); C336(1.11)  LDD2125  [3]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C276(0.82)  LDD2126  [3]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C58(0.75)  LDD2135  [3]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C58(1.01)  LDD2136  [3]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C336(0.88)  LDD2137  [3]
 LDCM0019  Staurosporine Hep-G2 N.A.  LDD0083  [17]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cell division control protein 42 homolog (CDC42) Rho family P60953
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
Amyloid-beta precursor protein (APP) APP family P05067
Alpha-synuclein (SNCA) Synuclein family P37840
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
PAK4-inhibitor INKA1 (INKA1) INKA family Q96EL1
Actin nucleation-promoting factor WASL (WASL) . O00401
Telomeric repeat-binding factor 1 (TERF1) . P54274

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
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pf-3758309 Small molecular drug D08MHM
Kpt-9274 . D04ZQB

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 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 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
5 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.
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 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.
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 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
10 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.
11 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
12 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
13 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
14 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
15 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
16 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
17 Comprehensive identification of staurosporine-binding kinases in the hepatocyte cell line HepG2 using Capture Compound Mass Spectrometry (CCMS). J Proteome Res. 2010 Feb 5;9(2):806-17. doi: 10.1021/pr9007333.
18 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
19 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
20 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