Details of the Target

General Information of Target

Target ID LDTP06321
Target Name [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial (PDK2)
Gene Name PDK2
Gene ID 5164
Synonyms
PDHK2; [Pyruvate dehydrogenase; acetyl-transferring)] kinase isozyme 2, mitochondrial; EC 2.7.11.2; Pyruvate dehydrogenase kinase isoform 2; PDH kinase 2; PDKII
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRWVWALLKNASLAGAPKYIEHFSKFSPSPLSMKQFLDFGSSNACEKTSFTFLRQELPVR
LANIMKEINLLPDRVLSTPSVQLVQSWYVQSLLDIMEFLDKDPEDHRTLSQFTDALVTIR
NRHNDVVPTMAQGVLEYKDTYGDDPVSNQNIQYFLDRFYLSRISIRMLINQHTLIFDGST
NPAHPKHIGSIDPNCNVSEVVKDAYDMAKLLCDKYYMASPDLEIQEINAANSKQPIHMVY
VPSHLYHMLFELFKNAMRATVESHESSLILPPIKVMVALGEEDLSIKMSDRGGGVPLRKI
ERLFSYMYSTAPTPQPGTGGTPLAGFGYGLPISRLYAKYFQGDLQLFSMEGFGTDAVIYL
KALSTDSVERLPVYNKSAWRHYQTIQEAGDWCVPSTEPKNTSTYRVS
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
PDK/BCKDK protein kinase family
Subcellular location
Mitochondrion matrix
Function
Kinase that plays a key role in the regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Inhibition of pyruvate dehydrogenase decreases glucose utilization and increases fat metabolism. Mediates cellular responses to insulin. Plays an important role in maintaining normal blood glucose levels and in metabolic adaptation to nutrient availability. Via its regulation of pyruvate dehydrogenase activity, plays an important role in maintaining normal blood pH and in preventing the accumulation of ketone bodies under starvation. Plays a role in the regulation of cell proliferation and in resistance to apoptosis under oxidative stress. Plays a role in p53/TP53-mediated apoptosis.
TTD ID
T17967
Uniprot ID
Q15119
DrugMap ID
TTJGCKM
Ensemble ID
ENST00000007708.7
HGNC ID
HGNC:8810
ChEMBL ID
CHEMBL3861

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
TOV21G SNV: p.S232Y; p.G293W .
UACC257 Substitution: p.R166C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		14.89  LDD0402  [1]
AHL-Pu-1
 Probe Info  		C392(3.49)  LDD0169  [2]
DBIA
 Probe Info  		C45(2.27)  LDD0080  [3]
IA-alkyne
 Probe Info  		C392(0.00); C45(0.00)  LDD0165  [4]
Compound 10
 Probe Info  		N.A.  LDD2216  [5]
Compound 11
 Probe Info  		N.A.  LDD2213  [5]
IPM
 Probe Info  		N.A.  LDD0147  [6]
Phosphinate-6
 Probe Info  		C392(0.00); C45(0.00)  LDD0018  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0026  4SU-RNA+native RNA HEK-293T C392(3.49)  LDD0169  [2]
 LDCM0214  AC1 HCT 116 C45(0.95)  LDD0531  [3]
 LDCM0215  AC10 HEK-293T C45(1.12)  LDD0813  [3]
 LDCM0216  AC100 HCT 116 C45(0.81)  LDD0533  [3]
 LDCM0217  AC101 HCT 116 C45(0.71)  LDD0534  [3]
 LDCM0218  AC102 HCT 116 C45(0.89)  LDD0535  [3]
 LDCM0219  AC103 HCT 116 C45(1.35)  LDD0536  [3]
 LDCM0220  AC104 HCT 116 C45(1.16)  LDD0537  [3]
 LDCM0221  AC105 HCT 116 C45(0.99)  LDD0538  [3]
 LDCM0222  AC106 HCT 116 C45(0.94)  LDD0539  [3]
 LDCM0223  AC107 HCT 116 C45(0.98)  LDD0540  [3]
 LDCM0224  AC108 HCT 116 C45(0.57)  LDD0541  [3]
 LDCM0225  AC109 HCT 116 C45(1.51)  LDD0542  [3]
 LDCM0226  AC11 HEK-293T C45(0.74)  LDD0824  [3]
 LDCM0227  AC110 HCT 116 C45(0.66)  LDD0544  [3]
 LDCM0228  AC111 HCT 116 C45(0.79)  LDD0545  [3]
 LDCM0229  AC112 HCT 116 C45(0.81)  LDD0546  [3]
 LDCM0230  AC113 HCT 116 C45(0.83)  LDD0547  [3]
 LDCM0231  AC114 HCT 116 C45(1.23)  LDD0548  [3]
 LDCM0232  AC115 HCT 116 C45(1.43)  LDD0549  [3]
 LDCM0233  AC116 HCT 116 C45(1.50)  LDD0550  [3]
 LDCM0234  AC117 HCT 116 C45(1.24)  LDD0551  [3]
 LDCM0235  AC118 HCT 116 C45(1.46)  LDD0552  [3]
 LDCM0236  AC119 HCT 116 C45(0.96)  LDD0553  [3]
 LDCM0237  AC12 HEK-293T C45(1.14)  LDD0835  [3]
 LDCM0238  AC120 HCT 116 C45(1.00)  LDD0555  [3]
 LDCM0239  AC121 HCT 116 C45(0.83)  LDD0556  [3]
 LDCM0240  AC122 HCT 116 C45(0.87)  LDD0557  [3]
 LDCM0241  AC123 HCT 116 C45(0.74)  LDD0558  [3]
 LDCM0242  AC124 HCT 116 C45(0.91)  LDD0559  [3]
 LDCM0243  AC125 HCT 116 C45(0.99)  LDD0560  [3]
 LDCM0244  AC126 HCT 116 C45(1.28)  LDD0561  [3]
 LDCM0245  AC127 HCT 116 C45(0.95)  LDD0562  [3]
 LDCM0246  AC128 PaTu 8988t C45(1.25)  LDD1125  [3]
 LDCM0247  AC129 PaTu 8988t C45(1.31)  LDD1126  [3]
 LDCM0249  AC130 PaTu 8988t C45(1.20)  LDD1128  [3]
 LDCM0250  AC131 PaTu 8988t C45(1.04)  LDD1129  [3]
 LDCM0251  AC132 PaTu 8988t C45(1.14)  LDD1130  [3]
 LDCM0252  AC133 PaTu 8988t C45(1.20)  LDD1131  [3]
 LDCM0253  AC134 PaTu 8988t C45(1.22)  LDD1132  [3]
 LDCM0254  AC135 PaTu 8988t C45(1.20)  LDD1133  [3]
 LDCM0255  AC136 PaTu 8988t C45(1.21)  LDD1134  [3]
 LDCM0256  AC137 PaTu 8988t C45(1.18)  LDD1135  [3]
 LDCM0257  AC138 PaTu 8988t C45(1.28)  LDD1136  [3]
 LDCM0258  AC139 PaTu 8988t C45(1.10)  LDD1137  [3]
 LDCM0259  AC14 HEK-293T C45(0.75)  LDD0857  [3]
 LDCM0260  AC140 PaTu 8988t C45(1.28)  LDD1139  [3]
 LDCM0261  AC141 PaTu 8988t C45(1.27)  LDD1140  [3]
 LDCM0262  AC142 PaTu 8988t C45(1.18)  LDD1141  [3]
 LDCM0263  AC143 HEK-293T C45(1.18)  LDD0861  [3]
 LDCM0264  AC144 HEK-293T C45(0.91)  LDD0862  [3]
 LDCM0265  AC145 HEK-293T C45(0.99)  LDD0863  [3]
 LDCM0266  AC146 HEK-293T C45(1.08)  LDD0864  [3]
 LDCM0267  AC147 HEK-293T C45(1.07)  LDD0865  [3]
 LDCM0268  AC148 HEK-293T C45(1.15)  LDD0866  [3]
 LDCM0269  AC149 HEK-293T C45(0.91)  LDD0867  [3]
 LDCM0270  AC15 HEK-293T C45(0.99)  LDD0868  [3]
 LDCM0271  AC150 HEK-293T C45(1.12)  LDD0869  [3]
 LDCM0272  AC151 HEK-293T C45(0.88)  LDD0870  [3]
 LDCM0273  AC152 HEK-293T C45(0.91)  LDD0871  [3]
 LDCM0274  AC153 HEK-293T C45(0.91)  LDD0872  [3]
 LDCM0621  AC154 HEK-293T C45(0.94)  LDD2162  [3]
 LDCM0622  AC155 HEK-293T C45(1.06)  LDD2163  [3]
 LDCM0623  AC156 HEK-293T C45(1.12)  LDD2164  [3]
 LDCM0624  AC157 HEK-293T C45(1.43)  LDD2165  [3]
 LDCM0276  AC17 HCT 116 C45(1.12)  LDD0593  [3]
 LDCM0277  AC18 HCT 116 C45(1.64)  LDD0594  [3]
 LDCM0278  AC19 HCT 116 C45(1.02)  LDD0595  [3]
 LDCM0279  AC2 HCT 116 C45(1.14)  LDD0596  [3]
 LDCM0280  AC20 HCT 116 C45(1.01)  LDD0597  [3]
 LDCM0281  AC21 HCT 116 C45(1.03)  LDD0598  [3]
 LDCM0282  AC22 HCT 116 C45(0.97)  LDD0599  [3]
 LDCM0283  AC23 HCT 116 C45(1.06)  LDD0600  [3]
 LDCM0284  AC24 HCT 116 C45(0.90)  LDD0601  [3]
 LDCM0285  AC25 HCT 116 C45(1.15)  LDD0602  [3]
 LDCM0286  AC26 HCT 116 C45(1.24)  LDD0603  [3]
 LDCM0287  AC27 HCT 116 C45(1.41)  LDD0604  [3]
 LDCM0288  AC28 HCT 116 C45(1.35)  LDD0605  [3]
 LDCM0289  AC29 HCT 116 C45(1.12)  LDD0606  [3]
 LDCM0290  AC3 HCT 116 C45(1.04)  LDD0607  [3]
 LDCM0291  AC30 HCT 116 C45(1.32)  LDD0608  [3]
 LDCM0292  AC31 HCT 116 C45(1.31)  LDD0609  [3]
 LDCM0293  AC32 HCT 116 C45(1.68)  LDD0610  [3]
 LDCM0294  AC33 HCT 116 C45(1.39)  LDD0611  [3]
 LDCM0295  AC34 HCT 116 C45(1.71)  LDD0612  [3]
 LDCM0296  AC35 HCT 116 C45(0.93)  LDD0613  [3]
 LDCM0297  AC36 HCT 116 C45(1.19)  LDD0614  [3]
 LDCM0298  AC37 HCT 116 C45(0.79)  LDD0615  [3]
 LDCM0299  AC38 HCT 116 C45(1.13)  LDD0616  [3]
 LDCM0300  AC39 HCT 116 C45(1.06)  LDD0617  [3]
 LDCM0301  AC4 HCT 116 C45(1.11)  LDD0618  [3]
 LDCM0302  AC40 HCT 116 C45(1.02)  LDD0619  [3]
 LDCM0303  AC41 HCT 116 C45(1.10)  LDD0620  [3]
 LDCM0304  AC42 HCT 116 C45(1.18)  LDD0621  [3]
 LDCM0305  AC43 HCT 116 C45(1.11)  LDD0622  [3]
 LDCM0306  AC44 HCT 116 C45(0.86)  LDD0623  [3]
 LDCM0307  AC45 HCT 116 C45(0.84)  LDD0624  [3]
 LDCM0308  AC46 HEK-293T C195(1.06); C392(1.08); C45(1.04)  LDD1547  [8]
 LDCM0310  AC48 HEK-293T C195(1.08); C392(1.05); C45(1.10)  LDD1549  [8]
 LDCM0311  AC49 HEK-293T C195(0.84); C392(0.93)  LDD1550  [8]
 LDCM0312  AC5 HCT 116 C45(1.25)  LDD0629  [3]
 LDCM0313  AC50 HEK-293T C195(0.89); C392(1.11)  LDD1552  [8]
 LDCM0314  AC51 HEK-293T C195(1.07); C45(1.04)  LDD1553  [8]
 LDCM0315  AC52 HEK-293T C195(0.99); C392(1.03)  LDD1554  [8]
 LDCM0316  AC53 HEK-293T C392(1.11)  LDD1555  [8]
 LDCM0317  AC54 HEK-293T C195(1.08); C392(1.13); C45(1.01)  LDD1556  [8]
 LDCM0319  AC56 HEK-293T C195(0.98); C392(0.99); C45(1.06)  LDD1558  [8]
 LDCM0320  AC57 HEK-293T C195(0.96); C392(0.93)  LDD1559  [8]
 LDCM0321  AC58 HEK-293T C195(0.88); C392(1.08)  LDD1560  [8]
 LDCM0322  AC59 HEK-293T C195(0.92); C45(1.07)  LDD1561  [8]
 LDCM0323  AC6 HEK-293T C45(0.85)  LDD0921  [3]
 LDCM0324  AC60 HEK-293T C195(1.20); C392(0.88)  LDD1563  [8]
 LDCM0325  AC61 HEK-293T C392(1.08)  LDD1564  [8]
 LDCM0326  AC62 HEK-293T C195(0.98); C392(1.09); C45(1.04)  LDD1565  [8]
 LDCM0328  AC64 HEK-293T C195(1.07); C392(0.87); C45(1.04)  LDD1567  [8]
 LDCM0332  AC68 PaTu 8988t C45(0.65)  LDD1211  [3]
 LDCM0333  AC69 PaTu 8988t C45(0.88)  LDD1212  [3]
 LDCM0334  AC7 HEK-293T C45(1.06)  LDD0932  [3]
 LDCM0335  AC70 PaTu 8988t C45(0.76)  LDD1214  [3]
 LDCM0336  AC71 PaTu 8988t C45(0.89)  LDD1215  [3]
 LDCM0337  AC72 PaTu 8988t C45(0.75)  LDD1216  [3]
 LDCM0338  AC73 PaTu 8988t C45(0.66)  LDD1217  [3]
 LDCM0339  AC74 PaTu 8988t C45(0.73)  LDD1218  [3]
 LDCM0340  AC75 PaTu 8988t C45(0.85)  LDD1219  [3]
 LDCM0341  AC76 PaTu 8988t C45(0.72)  LDD1220  [3]
 LDCM0342  AC77 PaTu 8988t C45(0.76)  LDD1221  [3]
 LDCM0343  AC78 PaTu 8988t C45(0.83)  LDD1222  [3]
 LDCM0344  AC79 PaTu 8988t C45(0.81)  LDD1223  [3]
 LDCM0345  AC8 HEK-293T C45(0.66)  LDD0943  [3]
 LDCM0346  AC80 PaTu 8988t C45(0.67)  LDD1225  [3]
 LDCM0347  AC81 PaTu 8988t C45(0.71)  LDD1226  [3]
 LDCM0348  AC82 PaTu 8988t C45(0.76)  LDD1227  [3]
 LDCM0365  AC98 HCT 116 C45(1.41)  LDD0682  [3]
 LDCM0366  AC99 HCT 116 C45(0.89)  LDD0683  [3]
 LDCM0248  AKOS034007472 HEK-293T C45(0.99)  LDD0846  [3]
 LDCM0356  AKOS034007680 HEK-293T C45(0.89)  LDD0954  [3]
 LDCM0275  AKOS034007705 HEK-293T C45(0.90)  LDD0873  [3]
 LDCM0367  CL1 HCT 116 C45(1.11)  LDD0684  [3]
 LDCM0368  CL10 HCT 116 C45(0.95)  LDD0685  [3]
 LDCM0369  CL100 HCT 116 C45(1.10)  LDD0686  [3]
 LDCM0370  CL101 HEK-293T C45(0.95)  LDD0968  [3]
 LDCM0371  CL102 HEK-293T C45(0.80)  LDD0969  [3]
 LDCM0372  CL103 HEK-293T C45(0.78)  LDD0970  [3]
 LDCM0373  CL104 HEK-293T C45(0.88)  LDD0971  [3]
 LDCM0374  CL105 HCT 116 C45(1.45)  LDD0691  [3]
 LDCM0375  CL106 HCT 116 C45(1.72)  LDD0692  [3]
 LDCM0376  CL107 HCT 116 C45(1.57)  LDD0693  [3]
 LDCM0377  CL108 HCT 116 C45(1.79)  LDD0694  [3]
 LDCM0378  CL109 HCT 116 C45(1.23)  LDD0695  [3]
 LDCM0379  CL11 HCT 116 C45(1.05)  LDD0696  [3]
 LDCM0380  CL110 HCT 116 C45(1.62)  LDD0697  [3]
 LDCM0381  CL111 HCT 116 C45(1.30)  LDD0698  [3]
 LDCM0382  CL112 HCT 116 C45(1.09)  LDD0699  [3]
 LDCM0383  CL113 HCT 116 C45(1.52)  LDD0700  [3]
 LDCM0384  CL114 HCT 116 C45(1.32)  LDD0701  [3]
 LDCM0385  CL115 HCT 116 C45(1.38)  LDD0702  [3]
 LDCM0386  CL116 HCT 116 C45(1.24)  LDD0703  [3]
 LDCM0387  CL117 HCT 116 C45(1.44)  LDD0704  [3]
 LDCM0388  CL118 HCT 116 C45(1.15)  LDD0705  [3]
 LDCM0389  CL119 HCT 116 C45(1.13)  LDD0706  [3]
 LDCM0390  CL12 HCT 116 C45(1.06)  LDD0707  [3]
 LDCM0391  CL120 HCT 116 C45(1.34)  LDD0708  [3]
 LDCM0392  CL121 HEK-293T C195(0.95); C392(1.16); C45(1.11)  LDD1596  [8]
 LDCM0393  CL122 HEK-293T C195(0.89); C392(0.73)  LDD1597  [8]
 LDCM0394  CL123 HEK-293T C195(1.15); C45(1.02)  LDD1598  [8]
 LDCM0395  CL124 HEK-293T C195(0.89); C392(1.09)  LDD1599  [8]
 LDCM0396  CL125 HEK-293T C195(0.90); C392(0.99); C45(1.04)  LDD1600  [8]
 LDCM0397  CL126 HEK-293T C195(0.93); C392(0.78)  LDD1601  [8]
 LDCM0398  CL127 HEK-293T C195(0.80); C45(1.07)  LDD1602  [8]
 LDCM0399  CL128 HEK-293T C195(0.95); C392(1.14)  LDD1603  [8]
 LDCM0400  CL13 HCT 116 C45(1.10)  LDD0717  [3]
 LDCM0401  CL14 HCT 116 C45(0.98)  LDD0718  [3]
 LDCM0402  CL15 HCT 116 C45(1.87)  LDD0719  [3]
 LDCM0403  CL16 HCT 116 C45(0.85)  LDD0720  [3]
 LDCM0404  CL17 HCT 116 C45(0.71)  LDD0721  [3]
 LDCM0405  CL18 HCT 116 C45(0.98)  LDD0722  [3]
 LDCM0406  CL19 HCT 116 C45(1.26)  LDD0723  [3]
 LDCM0407  CL2 HCT 116 C45(1.07)  LDD0724  [3]
 LDCM0408  CL20 HCT 116 C45(1.50)  LDD0725  [3]
 LDCM0409  CL21 HCT 116 C45(1.66)  LDD0726  [3]
 LDCM0410  CL22 HCT 116 C45(1.81)  LDD0727  [3]
 LDCM0411  CL23 HCT 116 C45(0.89)  LDD0728  [3]
 LDCM0412  CL24 HCT 116 C45(1.20)  LDD0729  [3]
 LDCM0413  CL25 HCT 116 C45(1.10)  LDD0730  [3]
 LDCM0414  CL26 HCT 116 C45(1.18)  LDD0731  [3]
 LDCM0415  CL27 HCT 116 C45(1.12)  LDD0732  [3]
 LDCM0416  CL28 HCT 116 C45(1.05)  LDD0733  [3]
 LDCM0417  CL29 HCT 116 C45(1.12)  LDD0734  [3]
 LDCM0418  CL3 HCT 116 C45(1.01)  LDD0735  [3]
 LDCM0419  CL30 HCT 116 C45(0.86)  LDD0736  [3]
 LDCM0420  CL31 HCT 116 C45(1.27)  LDD0737  [3]
 LDCM0421  CL32 HCT 116 C45(1.30)  LDD0738  [3]
 LDCM0422  CL33 HCT 116 C45(2.34)  LDD0739  [3]
 LDCM0423  CL34 HCT 116 C45(1.85)  LDD0740  [3]
 LDCM0424  CL35 HCT 116 C45(1.50)  LDD0741  [3]
 LDCM0425  CL36 HCT 116 C45(1.64)  LDD0742  [3]
 LDCM0426  CL37 HCT 116 C45(1.93)  LDD0743  [3]
 LDCM0428  CL39 HCT 116 C45(2.38)  LDD0745  [3]
 LDCM0429  CL4 HCT 116 C45(2.23)  LDD0746  [3]
 LDCM0430  CL40 HCT 116 C45(1.56)  LDD0747  [3]
 LDCM0431  CL41 HCT 116 C45(1.56)  LDD0748  [3]
 LDCM0432  CL42 HCT 116 C45(2.09)  LDD0749  [3]
 LDCM0433  CL43 HCT 116 C45(2.10)  LDD0750  [3]
 LDCM0434  CL44 HCT 116 C45(1.89)  LDD0751  [3]
 LDCM0435  CL45 HCT 116 C45(2.44)  LDD0752  [3]
 LDCM0436  CL46 HEK-293T C45(1.07)  LDD1034  [3]
 LDCM0437  CL47 HEK-293T C45(1.01)  LDD1035  [3]
 LDCM0438  CL48 HEK-293T C45(0.87)  LDD1036  [3]
 LDCM0439  CL49 HEK-293T C45(1.03)  LDD1037  [3]
 LDCM0440  CL5 HCT 116 C45(0.93)  LDD0757  [3]
 LDCM0441  CL50 HEK-293T C45(0.97)  LDD1039  [3]
 LDCM0442  CL51 HEK-293T C45(1.20)  LDD1040  [3]
 LDCM0443  CL52 HEK-293T C45(0.86)  LDD1041  [3]
 LDCM0444  CL53 HEK-293T C45(1.21)  LDD1042  [3]
 LDCM0445  CL54 HEK-293T C45(1.27)  LDD1043  [3]
 LDCM0446  CL55 HEK-293T C45(0.99)  LDD1044  [3]
 LDCM0447  CL56 HEK-293T C45(1.13)  LDD1045  [3]
 LDCM0448  CL57 HEK-293T C45(1.39)  LDD1046  [3]
 LDCM0449  CL58 HEK-293T C45(1.12)  LDD1047  [3]
 LDCM0450  CL59 HEK-293T C45(1.00)  LDD1048  [3]
 LDCM0451  CL6 HCT 116 C45(1.09)  LDD0768  [3]
 LDCM0452  CL60 HEK-293T C45(0.97)  LDD1050  [3]
 LDCM0453  CL61 HCT 116 C45(1.12)  LDD0770  [3]
 LDCM0454  CL62 HCT 116 C45(1.45)  LDD0771  [3]
 LDCM0455  CL63 HCT 116 C45(1.13)  LDD0772  [3]
 LDCM0456  CL64 HCT 116 C45(1.76)  LDD0773  [3]
 LDCM0457  CL65 HCT 116 C45(1.42)  LDD0774  [3]
 LDCM0458  CL66 HCT 116 C45(1.67)  LDD0775  [3]
 LDCM0459  CL67 HCT 116 C45(2.27)  LDD0776  [3]
 LDCM0460  CL68 HCT 116 C45(1.76)  LDD0777  [3]
 LDCM0461  CL69 HCT 116 C45(1.02)  LDD0778  [3]
 LDCM0462  CL7 HCT 116 C45(1.09)  LDD0779  [3]
 LDCM0463  CL70 HCT 116 C45(1.41)  LDD0780  [3]
 LDCM0464  CL71 HCT 116 C45(1.66)  LDD0781  [3]
 LDCM0465  CL72 HCT 116 C45(1.28)  LDD0782  [3]
 LDCM0466  CL73 HCT 116 C45(1.61)  LDD0783  [3]
 LDCM0467  CL74 HCT 116 C45(1.31)  LDD0784  [3]
 LDCM0469  CL76 PaTu 8988t C45(1.49)  LDD1348  [3]
 LDCM0470  CL77 PaTu 8988t C45(1.31)  LDD1349  [3]
 LDCM0471  CL78 PaTu 8988t C45(1.43)  LDD1350  [3]
 LDCM0472  CL79 PaTu 8988t C45(1.12)  LDD1351  [3]
 LDCM0473  CL8 HCT 116 C45(0.99)  LDD0790  [3]
 LDCM0474  CL80 PaTu 8988t C45(1.46)  LDD1353  [3]
 LDCM0475  CL81 PaTu 8988t C45(1.38)  LDD1354  [3]
 LDCM0476  CL82 PaTu 8988t C45(1.53)  LDD1355  [3]
 LDCM0477  CL83 PaTu 8988t C45(1.14)  LDD1356  [3]
 LDCM0478  CL84 PaTu 8988t C45(1.92)  LDD1357  [3]
 LDCM0479  CL85 PaTu 8988t C45(1.61)  LDD1358  [3]
 LDCM0480  CL86 PaTu 8988t C45(1.55)  LDD1359  [3]
 LDCM0481  CL87 PaTu 8988t C45(1.96)  LDD1360  [3]
 LDCM0482  CL88 PaTu 8988t C45(1.96)  LDD1361  [3]
 LDCM0483  CL89 PaTu 8988t C45(1.57)  LDD1362  [3]
 LDCM0484  CL9 HCT 116 C45(1.47)  LDD0801  [3]
 LDCM0485  CL90 PaTu 8988t C45(2.10)  LDD1364  [3]
 LDCM0486  CL91 HCT 116 C45(1.23)  LDD0803  [3]
 LDCM0487  CL92 HCT 116 C45(1.34)  LDD0804  [3]
 LDCM0488  CL93 HCT 116 C45(1.13)  LDD0805  [3]
 LDCM0489  CL94 HCT 116 C45(1.44)  LDD0806  [3]
 LDCM0490  CL95 HCT 116 C45(1.54)  LDD0807  [3]
 LDCM0491  CL96 HCT 116 C45(1.21)  LDD0808  [3]
 LDCM0492  CL97 HCT 116 C45(1.15)  LDD0809  [3]
 LDCM0493  CL98 HCT 116 C45(1.23)  LDD0810  [3]
 LDCM0494  CL99 HCT 116 C45(1.20)  LDD0811  [3]
 LDCM0495  E2913 HEK-293T C195(1.18); C45(1.52)  LDD1698  [8]
 LDCM0468  Fragment33 HCT 116 C45(1.69)  LDD0785  [3]
 LDCM0427  Fragment51 HCT 116 C45(2.03)  LDD0744  [3]
 LDCM0022  KB02 HCT 116 C45(2.27)  LDD0080  [3]
 LDCM0023  KB03 HCT 116 C45(1.65)  LDD0081  [3]
 LDCM0024  KB05 HCT 116 C45(1.43)  LDD0082  [3]
 LDCM0628  OTUB2-COV-1 HEK-293T C45(1.11)  LDD2207  [9]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(2r)-n-{4-[Ethyl(Phenyl)Sulfamoyl]-2-methylphenyl}-333-trifluoro-2-hydroxy-2-methylpropanamide . DB08609
4-({(2r5s)-25-dimethyl-4-[(2r)-333-trifluoro-2-hydroxy-2-methylpropanoyl]Piperazin-1-yl}Carbonyl)Benzonitrile . DB08608
N-(2-aminoethyl)-2-{3-chloro-4-[(4-isopropylbenzyl)Oxy]Phenyl} Acetamide . DB08610
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd-7545 Small molecular drug D03GFC

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 capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
3 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.
4 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
5 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
6 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
7 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
8 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
9 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.