Details of the Target

General Information of Target

Target ID LDTP11045
Target Name Target of rapamycin complex 2 subunit MAPKAP1 (MAPKAP1)
Gene Name MAPKAP1
Gene ID 79109
Synonyms
MIP1; SIN1; Target of rapamycin complex 2 subunit MAPKAP1; TORC2 subunit MAPKAP1; Mitogen-activated protein kinase 2-associated protein 1; Stress-activated map kinase-interacting protein 1; SAPK-interacting protein 1; mSIN1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKDPSRSSTSPSIINEDVIINGHSHEDDNPFAEYMWMENEEEFNRQIEEELWEEEFIERC
FQEMLEEEEEHEWFIPARDLPQTMDQIQDQFNDLVISDGSSLEDLVVKSNLNPNAKEFVP
GVKYGNI
Target Type
Clinical trial
Target Bioclass
Other
Family
SIN1 family
Subcellular location
Cell membrane
Function
Subunit of mTORC2, which regulates cell growth and survival in response to hormonal signals. mTORC2 is activated by growth factors, but, in contrast to mTORC1, seems to be nutrient-insensitive. mTORC2 seems to function upstream of Rho GTPases to regulate the actin cytoskeleton, probably by activating one or more Rho-type guanine nucleotide exchange factors. mTORC2 promotes the serum-induced formation of stress-fibers or F-actin. mTORC2 plays a critical role in AKT1 'Ser-473' phosphorylation, which may facilitate the phosphorylation of the activation loop of AKT1 on 'Thr-308' by PDK1 which is a prerequisite for full activation. mTORC2 regulates the phosphorylation of SGK1 at 'Ser-422'. mTORC2 also modulates the phosphorylation of PRKCA on 'Ser-657'. Within mTORC2, MAPKAP1 is required for complex formation and mTORC2 kinase activity. MAPKAP1 inhibits MAP3K2 by preventing its dimerization and autophosphorylation. Inhibits HRAS and KRAS signaling. Enhances osmotic stress-induced phosphorylation of ATF2 and ATF2-mediated transcription. Involved in ciliogenesis, regulates cilia length through its interaction with CCDC28B independently of mTORC2 complex.
TTD ID
T85544
Uniprot ID
Q9BPZ7
DrugMap ID
TTWDKCL
Ensemble ID
ENST00000265960.8
HGNC ID
HGNC:18752
ChEMBL ID
CHEMBL4523999

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL120 SNV: p.T492S .
HEC1 SNV: p.K276N DBIA    Probe Info 

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  		14.10  LDD0402  [1]
STPyne
 Probe Info  		K302(10.00); K501(1.14)  LDD0277  [2]
AHL-Pu-1
 Probe Info  		C149(2.44)  LDD0168  [3]
DBIA
 Probe Info  		C149(4.39)  LDD0209  [4]
IA-alkyne
 Probe Info  		C149(2.77)  LDD2182  [5]
IPM
 Probe Info  		N.A.  LDD0025  [6]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [6]
NAIA_5
 Probe Info  		N.A.  LDD2224  [7]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA HEK-293T C149(2.44)  LDD0168  [3]
 LDCM0026  4SU-RNA+native RNA HEK-293T C149(2.05)  LDD0169  [3]
 LDCM0214  AC1 HCT 116 C149(0.88)  LDD0531  [8]
 LDCM0215  AC10 PaTu 8988t C438(0.82); C440(0.82)  LDD1094  [8]
 LDCM0216  AC100 HCT 116 C149(0.87)  LDD0533  [8]
 LDCM0217  AC101 HCT 116 C149(0.95)  LDD0534  [8]
 LDCM0218  AC102 HCT 116 C149(1.01)  LDD0535  [8]
 LDCM0219  AC103 HCT 116 C149(1.00)  LDD0536  [8]
 LDCM0220  AC104 HCT 116 C149(1.05)  LDD0537  [8]
 LDCM0221  AC105 HCT 116 C149(1.11)  LDD0538  [8]
 LDCM0222  AC106 HCT 116 C149(0.95)  LDD0539  [8]
 LDCM0223  AC107 HCT 116 C149(1.07)  LDD0540  [8]
 LDCM0224  AC108 HCT 116 C149(0.88)  LDD0541  [8]
 LDCM0225  AC109 HCT 116 C149(0.94)  LDD0542  [8]
 LDCM0226  AC11 PaTu 8988t C438(0.83); C440(0.83)  LDD1105  [8]
 LDCM0227  AC110 HCT 116 C149(0.93)  LDD0544  [8]
 LDCM0228  AC111 HCT 116 C149(0.91)  LDD0545  [8]
 LDCM0229  AC112 HCT 116 C149(1.10)  LDD0546  [8]
 LDCM0230  AC113 HCT 116 C149(1.08)  LDD0547  [8]
 LDCM0231  AC114 HCT 116 C149(0.98)  LDD0548  [8]
 LDCM0232  AC115 HCT 116 C149(0.95)  LDD0549  [8]
 LDCM0233  AC116 HCT 116 C149(1.23)  LDD0550  [8]
 LDCM0234  AC117 HCT 116 C149(1.04)  LDD0551  [8]
 LDCM0235  AC118 HCT 116 C149(0.95)  LDD0552  [8]
 LDCM0236  AC119 HCT 116 C149(1.11)  LDD0553  [8]
 LDCM0237  AC12 PaTu 8988t C438(0.75); C440(0.75)  LDD1116  [8]
 LDCM0238  AC120 HCT 116 C149(1.04)  LDD0555  [8]
 LDCM0239  AC121 HCT 116 C149(0.79)  LDD0556  [8]
 LDCM0240  AC122 HCT 116 C149(1.21)  LDD0557  [8]
 LDCM0241  AC123 HCT 116 C149(0.75)  LDD0558  [8]
 LDCM0242  AC124 HCT 116 C149(0.92)  LDD0559  [8]
 LDCM0243  AC125 HCT 116 C149(1.02)  LDD0560  [8]
 LDCM0244  AC126 HCT 116 C149(0.94)  LDD0561  [8]
 LDCM0245  AC127 HCT 116 C149(0.84)  LDD0562  [8]
 LDCM0246  AC128 PaTu 8988t C149(0.99)  LDD1125  [8]
 LDCM0247  AC129 PaTu 8988t C149(1.16)  LDD1126  [8]
 LDCM0249  AC130 PaTu 8988t C149(1.08)  LDD1128  [8]
 LDCM0250  AC131 PaTu 8988t C149(0.98)  LDD1129  [8]
 LDCM0251  AC132 PaTu 8988t C149(0.89)  LDD1130  [8]
 LDCM0252  AC133 PaTu 8988t C149(1.37)  LDD1131  [8]
 LDCM0253  AC134 PaTu 8988t C149(1.06)  LDD1132  [8]
 LDCM0254  AC135 PaTu 8988t C149(1.18)  LDD1133  [8]
 LDCM0255  AC136 PaTu 8988t C149(1.24)  LDD1134  [8]
 LDCM0256  AC137 PaTu 8988t C149(1.11)  LDD1135  [8]
 LDCM0257  AC138 PaTu 8988t C149(1.00)  LDD1136  [8]
 LDCM0258  AC139 PaTu 8988t C149(1.21)  LDD1137  [8]
 LDCM0259  AC14 PaTu 8988t C438(0.99); C440(0.99)  LDD1138  [8]
 LDCM0260  AC140 PaTu 8988t C149(1.17)  LDD1139  [8]
 LDCM0261  AC141 PaTu 8988t C149(1.13)  LDD1140  [8]
 LDCM0262  AC142 PaTu 8988t C149(1.28)  LDD1141  [8]
 LDCM0263  AC143 HCT 116 C149(0.90)  LDD0580  [8]
 LDCM0264  AC144 HCT 116 C149(0.94)  LDD0581  [8]
 LDCM0265  AC145 HCT 116 C149(0.94)  LDD0582  [8]
 LDCM0266  AC146 HCT 116 C149(1.06)  LDD0583  [8]
 LDCM0267  AC147 HCT 116 C149(0.88)  LDD0584  [8]
 LDCM0268  AC148 HCT 116 C149(1.25)  LDD0585  [8]
 LDCM0269  AC149 HCT 116 C149(1.10)  LDD0586  [8]
 LDCM0270  AC15 PaTu 8988t C438(0.94); C440(0.94)  LDD1149  [8]
 LDCM0271  AC150 HCT 116 C149(1.50)  LDD0588  [8]
 LDCM0272  AC151 HCT 116 C149(1.15)  LDD0589  [8]
 LDCM0273  AC152 HCT 116 C149(0.96)  LDD0590  [8]
 LDCM0274  AC153 HCT 116 C149(1.01)  LDD0591  [8]
 LDCM0621  AC154 HCT 116 C149(0.90)  LDD2158  [8]
 LDCM0622  AC155 HCT 116 C149(0.93)  LDD2159  [8]
 LDCM0623  AC156 HCT 116 C149(0.90)  LDD2160  [8]
 LDCM0624  AC157 HCT 116 C149(0.87)  LDD2161  [8]
 LDCM0276  AC17 HCT 116 C149(0.98)  LDD0593  [8]
 LDCM0277  AC18 HCT 116 C149(0.87)  LDD0594  [8]
 LDCM0278  AC19 HCT 116 C149(0.87)  LDD0595  [8]
 LDCM0279  AC2 HCT 116 C149(0.95)  LDD0596  [8]
 LDCM0280  AC20 HCT 116 C149(0.94)  LDD0597  [8]
 LDCM0281  AC21 HCT 116 C149(0.75)  LDD0598  [8]
 LDCM0282  AC22 HCT 116 C149(0.88)  LDD0599  [8]
 LDCM0283  AC23 HCT 116 C149(0.86)  LDD0600  [8]
 LDCM0284  AC24 HCT 116 C149(1.00)  LDD0601  [8]
 LDCM0285  AC25 HEK-293T C149(0.97)  LDD1524  [9]
 LDCM0286  AC26 HEK-293T C149(0.92)  LDD1525  [9]
 LDCM0287  AC27 HEK-293T C149(0.95)  LDD1526  [9]
 LDCM0288  AC28 HEK-293T C149(1.12)  LDD1527  [9]
 LDCM0289  AC29 HEK-293T C149(0.92)  LDD1528  [9]
 LDCM0290  AC3 HCT 116 C149(0.88)  LDD0607  [8]
 LDCM0291  AC30 HEK-293T C149(0.89)  LDD1530  [9]
 LDCM0292  AC31 HEK-293T C149(1.12)  LDD1531  [9]
 LDCM0293  AC32 HEK-293T C149(1.00)  LDD1532  [9]
 LDCM0294  AC33 HEK-293T C149(1.10)  LDD1533  [9]
 LDCM0295  AC34 HEK-293T C149(0.94)  LDD1534  [9]
 LDCM0296  AC35 HCT 116 C149(0.86)  LDD0613  [8]
 LDCM0297  AC36 HCT 116 C149(0.95)  LDD0614  [8]
 LDCM0298  AC37 HCT 116 C149(1.06)  LDD0615  [8]
 LDCM0299  AC38 HCT 116 C149(1.09)  LDD0616  [8]
 LDCM0300  AC39 HCT 116 C149(0.98)  LDD0617  [8]
 LDCM0301  AC4 HCT 116 C149(0.93)  LDD0618  [8]
 LDCM0302  AC40 HCT 116 C149(1.14)  LDD0619  [8]
 LDCM0303  AC41 HCT 116 C149(1.15)  LDD0620  [8]
 LDCM0304  AC42 HCT 116 C149(1.02)  LDD0621  [8]
 LDCM0305  AC43 HCT 116 C149(1.22)  LDD0622  [8]
 LDCM0306  AC44 HCT 116 C149(1.05)  LDD0623  [8]
 LDCM0307  AC45 HCT 116 C149(1.21)  LDD0624  [8]
 LDCM0308  AC46 PaTu 8988t C211(0.93); C438(0.93); C440(0.93)  LDD1187  [8]
 LDCM0309  AC47 PaTu 8988t C211(0.78); C438(0.96); C440(0.96)  LDD1188  [8]
 LDCM0310  AC48 PaTu 8988t C211(0.70); C438(0.93); C440(0.93)  LDD1189  [8]
 LDCM0311  AC49 PaTu 8988t C211(0.80); C438(0.94); C440(0.94)  LDD1190  [8]
 LDCM0312  AC5 HCT 116 C149(0.97)  LDD0629  [8]
 LDCM0313  AC50 PaTu 8988t C211(0.86); C438(0.80); C440(0.80)  LDD1192  [8]
 LDCM0314  AC51 PaTu 8988t C211(0.90); C438(0.88); C440(0.88)  LDD1193  [8]
 LDCM0315  AC52 PaTu 8988t C211(0.70); C438(0.79); C440(0.79)  LDD1194  [8]
 LDCM0316  AC53 PaTu 8988t C211(0.59); C438(0.97); C440(0.97)  LDD1195  [8]
 LDCM0317  AC54 PaTu 8988t C211(0.75); C438(0.94); C440(0.94)  LDD1196  [8]
 LDCM0318  AC55 PaTu 8988t C211(0.68); C438(1.12); C440(1.12)  LDD1197  [8]
 LDCM0319  AC56 PaTu 8988t C211(0.67); C438(0.85); C440(0.85)  LDD1198  [8]
 LDCM0320  AC57 HEK-293T C149(1.12)  LDD1559  [9]
 LDCM0321  AC58 HEK-293T C149(0.95)  LDD1560  [9]
 LDCM0322  AC59 HEK-293T C149(0.91)  LDD1561  [9]
 LDCM0323  AC6 PaTu 8988t C438(0.79); C440(0.79)  LDD1202  [8]
 LDCM0324  AC60 HEK-293T C149(1.02)  LDD1563  [9]
 LDCM0325  AC61 HEK-293T C149(1.16)  LDD1564  [9]
 LDCM0326  AC62 HEK-293T C149(0.92)  LDD1565  [9]
 LDCM0327  AC63 HEK-293T C149(1.08)  LDD1566  [9]
 LDCM0328  AC64 HEK-293T C149(0.99)  LDD1567  [9]
 LDCM0332  AC68 HCT 116 C149(0.77)  LDD0649  [8]
 LDCM0333  AC69 HCT 116 C149(0.86)  LDD0650  [8]
 LDCM0334  AC7 PaTu 8988t C438(0.86); C440(0.86)  LDD1213  [8]
 LDCM0335  AC70 HCT 116 C149(0.92)  LDD0652  [8]
 LDCM0336  AC71 HCT 116 C149(0.77)  LDD0653  [8]
 LDCM0337  AC72 HCT 116 C149(1.08)  LDD0654  [8]
 LDCM0338  AC73 HCT 116 C149(1.11)  LDD0655  [8]
 LDCM0339  AC74 HCT 116 C149(0.84)  LDD0656  [8]
 LDCM0340  AC75 HCT 116 C149(0.89)  LDD0657  [8]
 LDCM0341  AC76 HCT 116 C149(0.85)  LDD0658  [8]
 LDCM0342  AC77 HCT 116 C149(0.87)  LDD0659  [8]
 LDCM0343  AC78 HCT 116 C149(0.83)  LDD0660  [8]
 LDCM0344  AC79 HCT 116 C149(1.10)  LDD0661  [8]
 LDCM0345  AC8 PaTu 8988t C438(1.06); C440(1.06)  LDD1224  [8]
 LDCM0346  AC80 HCT 116 C149(0.95)  LDD0663  [8]
 LDCM0347  AC81 HCT 116 C149(0.79)  LDD0664  [8]
 LDCM0348  AC82 HCT 116 C149(0.89)  LDD0665  [8]
 LDCM0349  AC83 HCT 116 C149(1.19)  LDD0666  [8]
 LDCM0350  AC84 HCT 116 C149(1.23)  LDD0667  [8]
 LDCM0351  AC85 HCT 116 C149(1.24)  LDD0668  [8]
 LDCM0352  AC86 HCT 116 C149(1.18)  LDD0669  [8]
 LDCM0353  AC87 HCT 116 C149(1.03)  LDD0670  [8]
 LDCM0354  AC88 HCT 116 C149(1.19)  LDD0671  [8]
 LDCM0355  AC89 HCT 116 C149(1.15)  LDD0672  [8]
 LDCM0357  AC90 HCT 116 C149(1.38)  LDD0674  [8]
 LDCM0358  AC91 HCT 116 C149(0.89)  LDD0675  [8]
 LDCM0359  AC92 HCT 116 C149(1.18)  LDD0676  [8]
 LDCM0360  AC93 HCT 116 C149(1.27)  LDD0677  [8]
 LDCM0361  AC94 HCT 116 C149(0.95)  LDD0678  [8]
 LDCM0362  AC95 HCT 116 C149(1.43)  LDD0679  [8]
 LDCM0363  AC96 HCT 116 C149(0.96)  LDD0680  [8]
 LDCM0364  AC97 HCT 116 C149(1.25)  LDD0681  [8]
 LDCM0365  AC98 HCT 116 C149(1.03)  LDD0682  [8]
 LDCM0366  AC99 HCT 116 C149(0.95)  LDD0683  [8]
 LDCM0248  AKOS034007472 PaTu 8988t C438(0.97); C440(0.97)  LDD1127  [8]
 LDCM0356  AKOS034007680 PaTu 8988t C438(0.89); C440(0.89)  LDD1235  [8]
 LDCM0275  AKOS034007705 PaTu 8988t C438(0.87); C440(0.87)  LDD1154  [8]
 LDCM0367  CL1 HCT 116 C149(0.92)  LDD0684  [8]
 LDCM0368  CL10 HCT 116 C149(1.42)  LDD0685  [8]
 LDCM0369  CL100 HCT 116 C149(0.85)  LDD0686  [8]
 LDCM0370  CL101 PaTu 8988t C438(0.91); C440(0.91)  LDD1249  [8]
 LDCM0371  CL102 PaTu 8988t C438(0.75); C440(0.75)  LDD1250  [8]
 LDCM0372  CL103 PaTu 8988t C438(0.80); C440(0.80)  LDD1251  [8]
 LDCM0373  CL104 PaTu 8988t C438(0.95); C440(0.95)  LDD1252  [8]
 LDCM0374  CL105 HCT 116 C149(0.82)  LDD0691  [8]
 LDCM0375  CL106 HCT 116 C149(0.77)  LDD0692  [8]
 LDCM0376  CL107 HCT 116 C149(0.79)  LDD0693  [8]
 LDCM0377  CL108 HCT 116 C149(0.85)  LDD0694  [8]
 LDCM0378  CL109 HCT 116 C149(1.00)  LDD0695  [8]
 LDCM0379  CL11 HCT 116 C149(1.25)  LDD0696  [8]
 LDCM0380  CL110 HCT 116 C149(1.05)  LDD0697  [8]
 LDCM0381  CL111 HCT 116 C149(1.06)  LDD0698  [8]
 LDCM0382  CL112 HEK-293T C149(1.16)  LDD1586  [9]
 LDCM0383  CL113 HEK-293T C149(1.03)  LDD1587  [9]
 LDCM0384  CL114 HEK-293T C149(1.11)  LDD1588  [9]
 LDCM0385  CL115 HEK-293T C149(1.04)  LDD1589  [9]
 LDCM0386  CL116 HEK-293T C149(1.09)  LDD1590  [9]
 LDCM0387  CL117 HCT 116 C149(1.50)  LDD0704  [8]
 LDCM0388  CL118 HCT 116 C149(1.19)  LDD0705  [8]
 LDCM0389  CL119 HCT 116 C149(1.01)  LDD0706  [8]
 LDCM0390  CL12 HCT 116 C149(1.76)  LDD0707  [8]
 LDCM0391  CL120 HCT 116 C149(1.05)  LDD0708  [8]
 LDCM0392  CL121 PaTu 8988t C211(0.69); C438(1.14); C440(1.14)  LDD1271  [8]
 LDCM0393  CL122 PaTu 8988t C211(0.89); C438(0.87); C440(0.87)  LDD1272  [8]
 LDCM0394  CL123 PaTu 8988t C211(0.67); C438(1.00); C440(1.00)  LDD1273  [8]
 LDCM0395  CL124 PaTu 8988t C211(0.68); C438(0.79); C440(0.79)  LDD1274  [8]
 LDCM0396  CL125 HEK-293T C149(0.99)  LDD1600  [9]
 LDCM0397  CL126 HEK-293T C149(0.98)  LDD1601  [9]
 LDCM0398  CL127 HEK-293T C149(1.02)  LDD1602  [9]
 LDCM0399  CL128 HEK-293T C149(1.01)  LDD1603  [9]
 LDCM0400  CL13 HCT 116 C149(1.27)  LDD0717  [8]
 LDCM0401  CL14 HCT 116 C149(1.15)  LDD0718  [8]
 LDCM0402  CL15 HCT 116 C149(1.36)  LDD0719  [8]
 LDCM0403  CL16 PaTu 8988t C211(1.46); C149(1.19); C438(0.82); C440(0.82)  LDD1282  [8]
 LDCM0404  CL17 PaTu 8988t C211(2.07); C149(1.56); C438(1.00); C440(1.00)  LDD1283  [8]
 LDCM0405  CL18 PaTu 8988t C211(0.55); C149(1.52); C438(0.73); C440(0.73)  LDD1284  [8]
 LDCM0406  CL19 PaTu 8988t C211(1.42); C149(1.37); C438(0.69); C440(0.69)  LDD1285  [8]
 LDCM0407  CL2 HCT 116 C149(0.77)  LDD0724  [8]
 LDCM0408  CL20 PaTu 8988t C211(1.43); C149(1.32); C438(0.82); C440(0.82)  LDD1287  [8]
 LDCM0409  CL21 PaTu 8988t C211(0.61); C149(1.74); C438(0.69); C440(0.69)  LDD1288  [8]
 LDCM0410  CL22 PaTu 8988t C211(1.27); C149(1.59); C438(0.71); C440(0.71)  LDD1289  [8]
 LDCM0411  CL23 PaTu 8988t C211(1.23); C149(1.43); C438(0.87); C440(0.87)  LDD1290  [8]
 LDCM0412  CL24 PaTu 8988t C211(0.88); C149(1.27); C438(0.95); C440(0.95)  LDD1291  [8]
 LDCM0413  CL25 PaTu 8988t C211(1.01); C149(1.49); C438(0.85); C440(0.85)  LDD1292  [8]
 LDCM0414  CL26 PaTu 8988t C211(0.98); C149(1.25); C438(0.76); C440(0.76)  LDD1293  [8]
 LDCM0415  CL27 PaTu 8988t C211(1.75); C149(1.65); C438(0.82); C440(0.82)  LDD1294  [8]
 LDCM0416  CL28 PaTu 8988t C211(1.28); C149(1.80); C438(0.85); C440(0.85)  LDD1295  [8]
 LDCM0417  CL29 PaTu 8988t C211(1.92); C149(1.35); C438(0.78); C440(0.78)  LDD1296  [8]
 LDCM0418  CL3 HCT 116 C149(0.79)  LDD0735  [8]
 LDCM0419  CL30 PaTu 8988t C211(1.80); C149(1.63); C438(0.72); C440(0.72)  LDD1298  [8]
 LDCM0420  CL31 HCT 116 C149(1.32)  LDD0737  [8]
 LDCM0421  CL32 HCT 116 C149(1.15)  LDD0738  [8]
 LDCM0422  CL33 HCT 116 C149(1.09)  LDD0739  [8]
 LDCM0423  CL34 HCT 116 C149(1.09)  LDD0740  [8]
 LDCM0424  CL35 HCT 116 C149(1.22)  LDD0741  [8]
 LDCM0425  CL36 HCT 116 C149(1.26)  LDD0742  [8]
 LDCM0426  CL37 HCT 116 C149(1.24)  LDD0743  [8]
 LDCM0428  CL39 HCT 116 C149(1.12)  LDD0745  [8]
 LDCM0429  CL4 HCT 116 C149(1.02)  LDD0746  [8]
 LDCM0430  CL40 HCT 116 C149(1.52)  LDD0747  [8]
 LDCM0431  CL41 HCT 116 C149(1.04)  LDD0748  [8]
 LDCM0432  CL42 HCT 116 C149(1.21)  LDD0749  [8]
 LDCM0433  CL43 HCT 116 C149(1.14)  LDD0750  [8]
 LDCM0434  CL44 HCT 116 C149(1.21)  LDD0751  [8]
 LDCM0435  CL45 HCT 116 C149(1.44)  LDD0752  [8]
 LDCM0436  CL46 HCT 116 C149(1.31)  LDD0753  [8]
 LDCM0437  CL47 HCT 116 C149(1.05)  LDD0754  [8]
 LDCM0438  CL48 HCT 116 C149(1.22)  LDD0755  [8]
 LDCM0439  CL49 HCT 116 C149(1.13)  LDD0756  [8]
 LDCM0440  CL5 HCT 116 C149(0.94)  LDD0757  [8]
 LDCM0441  CL50 HCT 116 C149(1.23)  LDD0758  [8]
 LDCM0442  CL51 HCT 116 C149(1.24)  LDD0759  [8]
 LDCM0443  CL52 HCT 116 C149(1.26)  LDD0760  [8]
 LDCM0444  CL53 HCT 116 C149(1.10)  LDD0761  [8]
 LDCM0445  CL54 HCT 116 C149(0.83)  LDD0762  [8]
 LDCM0446  CL55 HCT 116 C149(1.12)  LDD0763  [8]
 LDCM0447  CL56 HCT 116 C149(1.12)  LDD0764  [8]
 LDCM0448  CL57 HCT 116 C149(1.03)  LDD0765  [8]
 LDCM0449  CL58 HCT 116 C149(1.18)  LDD0766  [8]
 LDCM0450  CL59 HCT 116 C149(1.32)  LDD0767  [8]
 LDCM0451  CL6 HCT 116 C149(1.24)  LDD0768  [8]
 LDCM0452  CL60 HCT 116 C149(1.14)  LDD0769  [8]
 LDCM0453  CL61 HCT 116 C149(1.19)  LDD0770  [8]
 LDCM0454  CL62 HCT 116 C149(0.95)  LDD0771  [8]
 LDCM0455  CL63 HCT 116 C149(1.00)  LDD0772  [8]
 LDCM0456  CL64 HCT 116 C149(1.12)  LDD0773  [8]
 LDCM0457  CL65 HCT 116 C149(1.12)  LDD0774  [8]
 LDCM0458  CL66 HCT 116 C149(1.12)  LDD0775  [8]
 LDCM0459  CL67 HCT 116 C149(1.09)  LDD0776  [8]
 LDCM0460  CL68 HCT 116 C149(1.00)  LDD0777  [8]
 LDCM0461  CL69 HCT 116 C149(0.93)  LDD0778  [8]
 LDCM0462  CL7 HCT 116 C149(1.19)  LDD0779  [8]
 LDCM0463  CL70 HCT 116 C149(0.79)  LDD0780  [8]
 LDCM0464  CL71 HCT 116 C149(0.93)  LDD0781  [8]
 LDCM0465  CL72 HCT 116 C149(1.19)  LDD0782  [8]
 LDCM0466  CL73 HCT 116 C149(1.09)  LDD0783  [8]
 LDCM0467  CL74 HCT 116 C149(0.99)  LDD0784  [8]
 LDCM0469  CL76 HCT 116 C149(0.99)  LDD0786  [8]
 LDCM0470  CL77 HCT 116 C149(1.10)  LDD0787  [8]
 LDCM0471  CL78 HCT 116 C149(1.20)  LDD0788  [8]
 LDCM0472  CL79 HCT 116 C149(1.39)  LDD0789  [8]
 LDCM0473  CL8 HCT 116 C149(1.76)  LDD0790  [8]
 LDCM0474  CL80 HCT 116 C149(1.20)  LDD0791  [8]
 LDCM0475  CL81 HCT 116 C149(1.40)  LDD0792  [8]
 LDCM0476  CL82 HCT 116 C149(1.66)  LDD0793  [8]
 LDCM0477  CL83 HCT 116 C149(1.70)  LDD0794  [8]
 LDCM0478  CL84 HCT 116 C149(2.04)  LDD0795  [8]
 LDCM0479  CL85 HCT 116 C149(1.08)  LDD0796  [8]
 LDCM0480  CL86 HCT 116 C149(1.08)  LDD0797  [8]
 LDCM0481  CL87 HCT 116 C149(1.59)  LDD0798  [8]
 LDCM0482  CL88 HCT 116 C149(1.35)  LDD0799  [8]
 LDCM0483  CL89 HCT 116 C149(2.12)  LDD0800  [8]
 LDCM0484  CL9 HCT 116 C149(1.17)  LDD0801  [8]
 LDCM0485  CL90 HCT 116 C149(1.57)  LDD0802  [8]
 LDCM0486  CL91 HCT 116 C149(1.11)  LDD0803  [8]
 LDCM0487  CL92 HCT 116 C149(1.01)  LDD0804  [8]
 LDCM0488  CL93 HCT 116 C149(0.82)  LDD0805  [8]
 LDCM0489  CL94 HCT 116 C149(0.99)  LDD0806  [8]
 LDCM0490  CL95 HCT 116 C149(1.02)  LDD0807  [8]
 LDCM0491  CL96 HCT 116 C149(1.04)  LDD0808  [8]
 LDCM0492  CL97 HCT 116 C149(1.09)  LDD0809  [8]
 LDCM0493  CL98 HCT 116 C149(0.99)  LDD0810  [8]
 LDCM0494  CL99 HCT 116 C149(0.97)  LDD0811  [8]
 LDCM0495  E2913 HEK-293T C149(1.40)  LDD1698  [9]
 LDCM0625  F8 Ramos C149(0.67)  LDD2187  [5]
 LDCM0572  Fragment10 Ramos C149(0.56)  LDD2189  [5]
 LDCM0575  Fragment13 Ramos C149(0.27)  LDD2192  [5]
 LDCM0576  Fragment14 Ramos C149(0.68)  LDD2193  [5]
 LDCM0580  Fragment21 Ramos C149(0.13)  LDD2195  [5]
 LDCM0578  Fragment27 Ramos C149(0.29)  LDD2197  [5]
 LDCM0586  Fragment28 Ramos C149(3.09)  LDD2198  [5]
 LDCM0588  Fragment30 Ramos C149(0.42)  LDD2199  [5]
 LDCM0589  Fragment31 Ramos C149(0.15)  LDD2200  [5]
 LDCM0590  Fragment32 Ramos C149(0.28)  LDD2201  [5]
 LDCM0468  Fragment33 HCT 116 C149(0.96)  LDD0785  [8]
 LDCM0596  Fragment38 Ramos C149(0.61)  LDD2203  [5]
 LDCM0566  Fragment4 Ramos C149(0.77)  LDD2184  [5]
 LDCM0427  Fragment51 HCT 116 C149(1.89)  LDD0744  [8]
 LDCM0614  Fragment56 Ramos C149(0.15)  LDD2205  [5]
 LDCM0569  Fragment7 Ramos C149(1.92)  LDD2186  [5]
 LDCM0022  KB02 HEK-293T C149(0.86)  LDD1492  [9]
 LDCM0023  KB03 Jurkat C149(4.39)  LDD0209  [4]
 LDCM0024  KB05 MSTO-211H C149(2.06)  LDD3337  [10]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
DNA-dependent protein kinase catalytic subunit (PRKDC) PI3/PI4-kinase family P78527
Protein kinase C epsilon type (PRKCE) AGC Ser/Thr protein kinase family Q02156

The Drug(s) Related To This Target

Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Azd2014 Small molecular drug D0Z2UQ
Me-344 Small molecular drug D03IXK
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Palomid-529 Small molecular drug DP17AI
Vs-5584 Small molecular drug D0U3DP

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
3 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
4 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.
5 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
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 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
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 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