Details of the Target

General Information of Target

Target ID LDTP02852
Target Name Methylated-DNA--protein-cysteine methyltransferase (MGMT)
Gene Name MGMT
Gene ID 4255
Synonyms
Methylated-DNA--protein-cysteine methyltransferase; EC 2.1.1.63; 6-O-methylguanine-DNA methyltransferase; MGMT; O-6-methylguanine-DNA-alkyltransferase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDKDCEMKRTTLDSPLGKLELSGCEQGLHEIKLLGKGTSAADAVEVPAPAAVLGGPEPLM
QCTAWLNAYFHQPEAIEEFPVPALHHPVFQQESFTRQVLWKLLKVVKFGEVISYQQLAAL
AGNPKAARAVGGAMRGNPVPILIPCHRVVCSSGAVGNYSGGLAVKEWLLAHEGHRLGKPG
LGGSSGLAGAWLKGAGATSGSPPAGRN
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
MGMT family
Subcellular location
Nucleus
Function
Involved in the cellular defense against the biological effects of O6-methylguanine (O6-MeG) and O4-methylthymine (O4-MeT) in DNA. Repairs the methylated nucleobase in DNA by stoichiometrically transferring the methyl group to a cysteine residue in the enzyme. This is a suicide reaction: the enzyme is irreversibly inactivated.
TTD ID
T24587
Uniprot ID
P16455
DrugMap ID
TTJ8DV7
Ensemble ID
ENST00000651593.1
HGNC ID
HGNC:7059
ChEMBL ID
CHEMBL2864

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 15 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
BTD
 Probe Info  		C145(1.95)  LDD1699  [2]
Johansson_61
 Probe Info  		_(15.53)  LDD1485  [3]
YY4-yne
 Probe Info  		3.70  LDD0400  [4]
HPAP
 Probe Info  		3.30  LDD0064  [5]
EA-probe
 Probe Info  		C145(0.64)  LDD2210  [6]
DBIA
 Probe Info  		C150(1.05); C145(0.87)  LDD0078  [7]
IPM
 Probe Info  		C150(0.00); C145(0.00)  LDD0025  [8]
JW-RF-010
 Probe Info  		C150(0.00); C145(0.00)  LDD0026  [8]
TFBX
 Probe Info  		C150(0.00); C145(0.00)  LDD0027  [8]
WYneN
 Probe Info  		N.A.  LDD0021  [9]
IA-alkyne
 Probe Info  		C145(0.00); C150(0.00)  LDD0149  [10]
Acrolein
 Probe Info  		N.A.  LDD0217  [11]
W1
 Probe Info  		N.A.  LDD0236  [12]
NAIA_5
 Probe Info  		C145(0.00); C5(0.00); C24(0.00); C150(0.00)  LDD2223  [13]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C145(1.19); C150(1.19)  LDD0531  [7]
 LDCM0215  AC10 HCT 116 C145(1.14); C150(1.19)  LDD0532  [7]
 LDCM0216  AC100 HCT 116 C145(1.26); C150(1.03)  LDD0533  [7]
 LDCM0217  AC101 HCT 116 C145(1.33); C150(1.08)  LDD0534  [7]
 LDCM0218  AC102 HCT 116 C145(1.19); C150(1.07)  LDD0535  [7]
 LDCM0219  AC103 HCT 116 C145(1.69); C150(1.29)  LDD0536  [7]
 LDCM0220  AC104 HCT 116 C145(1.30); C150(1.21)  LDD0537  [7]
 LDCM0221  AC105 HCT 116 C145(1.37); C150(1.08)  LDD0538  [7]
 LDCM0222  AC106 HCT 116 C145(1.33); C150(1.14)  LDD0539  [7]
 LDCM0223  AC107 HCT 116 C145(1.41); C150(1.28)  LDD0540  [7]
 LDCM0224  AC108 HCT 116 C145(1.12); C150(0.97)  LDD0541  [7]
 LDCM0225  AC109 HCT 116 C145(0.90); C150(0.96)  LDD0542  [7]
 LDCM0226  AC11 HCT 116 C145(1.19); C150(1.30)  LDD0543  [7]
 LDCM0227  AC110 HCT 116 C145(1.20); C150(0.96)  LDD0544  [7]
 LDCM0228  AC111 HCT 116 C145(1.12); C150(1.06)  LDD0545  [7]
 LDCM0229  AC112 HCT 116 C145(1.23); C150(1.34)  LDD0546  [7]
 LDCM0230  AC113 HCT 116 C145(1.10); C150(0.95)  LDD0547  [7]
 LDCM0231  AC114 HCT 116 C145(1.09); C150(1.04)  LDD0548  [7]
 LDCM0232  AC115 HCT 116 C145(1.12); C150(1.06)  LDD0549  [7]
 LDCM0233  AC116 HCT 116 C145(1.04); C150(1.10)  LDD0550  [7]
 LDCM0234  AC117 HCT 116 C145(0.94); C150(1.07)  LDD0551  [7]
 LDCM0235  AC118 HCT 116 C145(0.96); C150(1.01)  LDD0552  [7]
 LDCM0236  AC119 HCT 116 C145(1.14); C150(1.07)  LDD0553  [7]
 LDCM0237  AC12 HCT 116 C145(1.14); C150(1.02)  LDD0554  [7]
 LDCM0238  AC120 HCT 116 C145(1.12); C150(1.17)  LDD0555  [7]
 LDCM0239  AC121 HCT 116 C145(0.80); C150(0.89)  LDD0556  [7]
 LDCM0240  AC122 HCT 116 C145(1.01); C150(0.95)  LDD0557  [7]
 LDCM0241  AC123 HCT 116 C145(0.94); C150(0.89)  LDD0558  [7]
 LDCM0242  AC124 HCT 116 C145(0.85); C150(0.90)  LDD0559  [7]
 LDCM0243  AC125 HCT 116 C145(1.01); C150(1.02)  LDD0560  [7]
 LDCM0244  AC126 HCT 116 C145(0.93); C150(0.95)  LDD0561  [7]
 LDCM0245  AC127 HCT 116 C145(0.89); C150(1.04)  LDD0562  [7]
 LDCM0246  AC128 HCT 116 C145(1.18)  LDD0563  [7]
 LDCM0247  AC129 HCT 116 C145(0.97)  LDD0564  [7]
 LDCM0249  AC130 HCT 116 C145(1.15)  LDD0566  [7]
 LDCM0250  AC131 HCT 116 C145(1.04)  LDD0567  [7]
 LDCM0251  AC132 HCT 116 C145(1.03)  LDD0568  [7]
 LDCM0252  AC133 HCT 116 C145(1.09)  LDD0569  [7]
 LDCM0253  AC134 HCT 116 C145(1.33)  LDD0570  [7]
 LDCM0254  AC135 HCT 116 C145(1.18)  LDD0571  [7]
 LDCM0255  AC136 HCT 116 C145(1.17)  LDD0572  [7]
 LDCM0256  AC137 HCT 116 C145(1.16)  LDD0573  [7]
 LDCM0257  AC138 HCT 116 C145(1.37)  LDD0574  [7]
 LDCM0258  AC139 HCT 116 C145(1.32)  LDD0575  [7]
 LDCM0259  AC14 HCT 116 C145(1.02); C150(1.01)  LDD0576  [7]
 LDCM0260  AC140 HCT 116 C145(1.49)  LDD0577  [7]
 LDCM0261  AC141 HCT 116 C145(1.31)  LDD0578  [7]
 LDCM0262  AC142 HCT 116 C145(1.04)  LDD0579  [7]
 LDCM0263  AC143 HCT 116 C145(1.11); C150(1.31)  LDD0580  [7]
 LDCM0264  AC144 HCT 116 C145(1.05); C150(1.36)  LDD0581  [7]
 LDCM0265  AC145 HCT 116 C145(1.01); C150(1.12)  LDD0582  [7]
 LDCM0266  AC146 HCT 116 C145(1.02); C150(1.42)  LDD0583  [7]
 LDCM0267  AC147 HCT 116 C145(0.97); C150(1.50)  LDD0584  [7]
 LDCM0268  AC148 HCT 116 C150(1.71); C145(2.01)  LDD0585  [7]
 LDCM0269  AC149 HCT 116 C150(1.52); C145(2.10)  LDD0586  [7]
 LDCM0270  AC15 HCT 116 C145(1.12); C150(1.17)  LDD0587  [7]
 LDCM0271  AC150 HCT 116 C150(1.11); C145(1.13)  LDD0588  [7]
 LDCM0272  AC151 HCT 116 C145(1.13); C150(1.35)  LDD0589  [7]
 LDCM0273  AC152 HCT 116 C145(1.16); C150(1.38)  LDD0590  [7]
 LDCM0274  AC153 HCT 116 C145(1.54); C150(2.02)  LDD0591  [7]
 LDCM0621  AC154 HCT 116 C145(0.89); C150(1.41)  LDD2158  [7]
 LDCM0622  AC155 HCT 116 C145(1.12); C150(1.41)  LDD2159  [7]
 LDCM0623  AC156 HCT 116 C145(1.01); C150(1.18)  LDD2160  [7]
 LDCM0624  AC157 HCT 116 C145(1.01); C150(1.06)  LDD2161  [7]
 LDCM0276  AC17 HCT 116 C145(1.12); C150(1.12)  LDD0593  [7]
 LDCM0277  AC18 HCT 116 C145(1.37); C150(1.53)  LDD0594  [7]
 LDCM0278  AC19 HCT 116 C145(1.08); C150(1.11)  LDD0595  [7]
 LDCM0279  AC2 HCT 116 C150(1.09); C145(1.14)  LDD0596  [7]
 LDCM0280  AC20 HCT 116 C145(1.14); C150(1.24)  LDD0597  [7]
 LDCM0281  AC21 HCT 116 C145(1.05); C150(1.15)  LDD0598  [7]
 LDCM0282  AC22 HCT 116 C150(1.04); C145(1.05)  LDD0599  [7]
 LDCM0283  AC23 HCT 116 C145(1.00); C150(1.21)  LDD0600  [7]
 LDCM0284  AC24 HCT 116 C145(1.00); C150(1.02)  LDD0601  [7]
 LDCM0285  AC25 HCT 116 C150(1.08); C145(1.12)  LDD0602  [7]
 LDCM0286  AC26 HCT 116 C150(1.11); C145(1.22)  LDD0603  [7]
 LDCM0287  AC27 HCT 116 C150(1.11); C145(1.31)  LDD0604  [7]
 LDCM0288  AC28 HCT 116 C145(1.28); C150(1.30)  LDD0605  [7]
 LDCM0289  AC29 HCT 116 C150(1.22); C145(1.34)  LDD0606  [7]
 LDCM0290  AC3 HCT 116 C150(1.08); C145(1.17)  LDD0607  [7]
 LDCM0291  AC30 HCT 116 C150(1.20); C145(1.41)  LDD0608  [7]
 LDCM0292  AC31 HCT 116 C150(1.22); C145(1.27)  LDD0609  [7]
 LDCM0293  AC32 HCT 116 C150(1.44); C145(1.53)  LDD0610  [7]
 LDCM0294  AC33 HCT 116 C150(1.33); C145(1.34)  LDD0611  [7]
 LDCM0295  AC34 HCT 116 C150(1.53); C145(1.62)  LDD0612  [7]
 LDCM0296  AC35 HCT 116 C145(0.90); C150(1.01)  LDD0613  [7]
 LDCM0297  AC36 HCT 116 C145(0.98); C150(1.09)  LDD0614  [7]
 LDCM0298  AC37 HCT 116 C145(0.88); C150(1.34)  LDD0615  [7]
 LDCM0299  AC38 HCT 116 C145(1.05); C150(1.20)  LDD0616  [7]
 LDCM0300  AC39 HCT 116 C145(1.01); C150(1.03)  LDD0617  [7]
 LDCM0301  AC4 HCT 116 C150(1.27); C145(1.31)  LDD0618  [7]
 LDCM0302  AC40 HCT 116 C145(1.12); C150(1.41)  LDD0619  [7]
 LDCM0303  AC41 HCT 116 C145(1.13); C150(1.51)  LDD0620  [7]
 LDCM0304  AC42 HCT 116 C145(1.09); C150(1.20)  LDD0621  [7]
 LDCM0305  AC43 HCT 116 C145(1.21); C150(1.30)  LDD0622  [7]
 LDCM0306  AC44 HCT 116 C145(1.02); C150(1.32)  LDD0623  [7]
 LDCM0307  AC45 HCT 116 C145(1.17); C150(1.47)  LDD0624  [7]
 LDCM0308  AC46 HCT 116 C145(1.08); C150(1.31)  LDD0625  [7]
 LDCM0309  AC47 HCT 116 C145(1.07); C150(1.11)  LDD0626  [7]
 LDCM0310  AC48 HCT 116 C145(1.12); C150(1.12)  LDD0627  [7]
 LDCM0311  AC49 HCT 116 C150(1.37); C145(1.44)  LDD0628  [7]
 LDCM0312  AC5 HCT 116 C150(1.26); C145(1.37)  LDD0629  [7]
 LDCM0313  AC50 HCT 116 C150(1.22); C145(1.51)  LDD0630  [7]
 LDCM0314  AC51 HCT 116 C145(0.97); C150(1.16)  LDD0631  [7]
 LDCM0315  AC52 HCT 116 C145(1.09); C150(1.11)  LDD0632  [7]
 LDCM0316  AC53 HCT 116 C150(1.19); C145(1.24)  LDD0633  [7]
 LDCM0317  AC54 HCT 116 C150(1.05); C145(1.13)  LDD0634  [7]
 LDCM0318  AC55 HCT 116 C150(1.35); C145(1.46)  LDD0635  [7]
 LDCM0319  AC56 HCT 116 C150(1.24); C145(2.09)  LDD0636  [7]
 LDCM0320  AC57 HCT 116 C145(1.01); C150(1.23)  LDD0637  [7]
 LDCM0321  AC58 HCT 116 C145(1.06); C150(1.62)  LDD0638  [7]
 LDCM0322  AC59 HCT 116 C145(1.12); C150(1.55)  LDD0639  [7]
 LDCM0323  AC6 HCT 116 C145(1.16); C150(1.18)  LDD0640  [7]
 LDCM0324  AC60 HCT 116 C145(1.03); C150(1.47)  LDD0641  [7]
 LDCM0325  AC61 HCT 116 C145(0.94); C150(1.32)  LDD0642  [7]
 LDCM0326  AC62 HCT 116 C145(1.06); C150(1.31)  LDD0643  [7]
 LDCM0327  AC63 HCT 116 C145(1.09); C150(1.16)  LDD0644  [7]
 LDCM0328  AC64 HCT 116 C145(1.01); C150(1.36)  LDD0645  [7]
 LDCM0329  AC65 HCT 116 C145(1.14); C150(1.64)  LDD0646  [7]
 LDCM0330  AC66 HCT 116 C145(1.03); C150(1.61)  LDD0647  [7]
 LDCM0331  AC67 HCT 116 C145(1.14); C150(1.62)  LDD0648  [7]
 LDCM0332  AC68 HCT 116 C150(1.14); C145(1.16)  LDD0649  [7]
 LDCM0333  AC69 HCT 116 C150(1.02); C145(1.17)  LDD0650  [7]
 LDCM0334  AC7 HCT 116 C145(1.01); C150(1.22)  LDD0651  [7]
 LDCM0335  AC70 HCT 116 C145(1.31); C150(1.37)  LDD0652  [7]
 LDCM0336  AC71 HCT 116 C150(1.04); C145(1.09)  LDD0653  [7]
 LDCM0337  AC72 HCT 116 C150(1.21); C145(1.28)  LDD0654  [7]
 LDCM0338  AC73 HCT 116 C150(1.43); C145(1.84)  LDD0655  [7]
 LDCM0339  AC74 HCT 116 C150(1.39); C145(1.78)  LDD0656  [7]
 LDCM0340  AC75 HCT 116 C150(1.74); C145(1.91)  LDD0657  [7]
 LDCM0341  AC76 HCT 116 C150(0.99); C145(1.25)  LDD0658  [7]
 LDCM0342  AC77 HCT 116 C150(1.16); C145(1.34)  LDD0659  [7]
 LDCM0343  AC78 HCT 116 C150(1.02); C145(1.08)  LDD0660  [7]
 LDCM0344  AC79 HCT 116 C145(1.22); C150(1.24)  LDD0661  [7]
 LDCM0345  AC8 HCT 116 C145(1.06); C150(1.40)  LDD0662  [7]
 LDCM0346  AC80 HCT 116 C150(0.93); C145(1.14)  LDD0663  [7]
 LDCM0347  AC81 HCT 116 C145(1.02); C150(1.21)  LDD0664  [7]
 LDCM0348  AC82 HCT 116 C150(1.63); C145(2.02)  LDD0665  [7]
 LDCM0349  AC83 HCT 116 C145(1.83); C150(1.86)  LDD0666  [7]
 LDCM0350  AC84 HCT 116 C145(1.63); C150(1.90)  LDD0667  [7]
 LDCM0351  AC85 HCT 116 C145(1.45); C150(1.59)  LDD0668  [7]
 LDCM0352  AC86 HCT 116 C145(1.20); C150(1.41)  LDD0669  [7]
 LDCM0353  AC87 HCT 116 C145(1.05); C150(1.09)  LDD0670  [7]
 LDCM0354  AC88 HCT 116 C145(1.16); C150(1.44)  LDD0671  [7]
 LDCM0355  AC89 HCT 116 C145(1.38); C150(1.44)  LDD0672  [7]
 LDCM0357  AC90 HCT 116 C145(0.92); C150(1.01)  LDD0674  [7]
 LDCM0358  AC91 HCT 116 C145(1.80); C150(1.93)  LDD0675  [7]
 LDCM0359  AC92 HCT 116 C145(1.62); C150(1.76)  LDD0676  [7]
 LDCM0360  AC93 HCT 116 C145(1.25); C150(1.36)  LDD0677  [7]
 LDCM0361  AC94 HCT 116 C145(1.25); C150(1.62)  LDD0678  [7]
 LDCM0362  AC95 HCT 116 C145(1.21); C150(1.32)  LDD0679  [7]
 LDCM0363  AC96 HCT 116 C145(1.34); C150(1.56)  LDD0680  [7]
 LDCM0364  AC97 HCT 116 C145(1.60); C150(1.89)  LDD0681  [7]
 LDCM0365  AC98 HCT 116 C150(1.54); C145(1.91)  LDD0682  [7]
 LDCM0366  AC99 HCT 116 C150(1.09); C145(1.26)  LDD0683  [7]
 LDCM0248  AKOS034007472 HCT 116 C145(0.95); C150(1.02)  LDD0565  [7]
 LDCM0356  AKOS034007680 HCT 116 C145(1.12); C150(1.20)  LDD0673  [7]
 LDCM0275  AKOS034007705 HCT 116 C150(1.49); C145(1.55)  LDD0592  [7]
 LDCM0156  Aniline NCI-H1299 12.93  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C150(1.05); C145(0.87)  LDD0078  [7]
 LDCM0108  Chloroacetamide HeLa C24(0.00); C150(0.00)  LDD0222  [11]
 LDCM0632  CL-Sc Hep-G2 C5(4.25); C145(1.22); C24(0.28)  LDD2227  [13]
 LDCM0367  CL1 HCT 116 C150(1.40); C145(7.93)  LDD0684  [7]
 LDCM0368  CL10 HCT 116 C145(1.02); C150(1.40)  LDD0685  [7]
 LDCM0369  CL100 HCT 116 C150(2.14); C145(14.93)  LDD0686  [7]
 LDCM0370  CL101 HCT 116 C150(1.58); C145(2.45)  LDD0687  [7]
 LDCM0371  CL102 HCT 116 C150(2.37); C145(2.84)  LDD0688  [7]
 LDCM0372  CL103 HCT 116 C145(1.48); C150(1.79)  LDD0689  [7]
 LDCM0373  CL104 HCT 116 C150(1.25); C145(2.66)  LDD0690  [7]
 LDCM0374  CL105 HCT 116 C150(1.78); C145(15.33)  LDD0691  [7]
 LDCM0375  CL106 HCT 116 C150(1.96); C145(17.91)  LDD0692  [7]
 LDCM0376  CL107 HCT 116 C145(1.45); C150(1.48)  LDD0693  [7]
 LDCM0377  CL108 HCT 116 C150(2.01); C145(3.88)  LDD0694  [7]
 LDCM0378  CL109 HCT 116 C150(2.11); C145(17.37)  LDD0695  [7]
 LDCM0379  CL11 HCT 116 C150(3.68); C145(7.94)  LDD0696  [7]
 LDCM0380  CL110 HCT 116 C150(4.59); C145(18.61)  LDD0697  [7]
 LDCM0381  CL111 HCT 116 C150(2.61); C145(16.04)  LDD0698  [7]
 LDCM0382  CL112 HCT 116 C150(1.75); C145(10.47)  LDD0699  [7]
 LDCM0383  CL113 HCT 116 C150(1.38); C145(1.44)  LDD0700  [7]
 LDCM0384  CL114 HCT 116 C150(4.57); C145(16.65)  LDD0701  [7]
 LDCM0385  CL115 HCT 116 C150(1.59); C145(5.62)  LDD0702  [7]
 LDCM0386  CL116 HCT 116 C150(1.30); C145(1.73)  LDD0703  [7]
 LDCM0387  CL117 HCT 116 C150(1.94); C145(12.66)  LDD0704  [7]
 LDCM0388  CL118 HCT 116 C150(1.58); C145(2.42)  LDD0705  [7]
 LDCM0389  CL119 HCT 116 C150(1.27); C145(1.47)  LDD0706  [7]
 LDCM0390  CL12 HCT 116 C150(1.19); C145(2.05)  LDD0707  [7]
 LDCM0391  CL120 HCT 116 C145(1.16); C150(1.30)  LDD0708  [7]
 LDCM0392  CL121 HCT 116 C150(1.67); C145(5.76)  LDD0709  [7]
 LDCM0393  CL122 HCT 116 C150(1.80); C145(4.81)  LDD0710  [7]
 LDCM0394  CL123 HCT 116 C150(2.29); C145(10.42)  LDD0711  [7]
 LDCM0395  CL124 HCT 116 C150(2.16); C145(12.63)  LDD0712  [7]
 LDCM0396  CL125 HCT 116 C150(1.93); C145(6.73)  LDD0713  [7]
 LDCM0397  CL126 HCT 116 C150(1.68); C145(18.46)  LDD0714  [7]
 LDCM0398  CL127 HCT 116 C150(1.30); C145(2.90)  LDD0715  [7]
 LDCM0399  CL128 HCT 116 C145(1.03); C150(1.48)  LDD0716  [7]
 LDCM0400  CL13 HCT 116 C150(1.09); C145(1.49)  LDD0717  [7]
 LDCM0401  CL14 HCT 116 C150(1.20); C145(2.91)  LDD0718  [7]
 LDCM0402  CL15 HCT 116 C150(2.97); C145(20.00)  LDD0719  [7]
 LDCM0403  CL16 HCT 116 C150(1.44); C145(3.64)  LDD0720  [7]
 LDCM0404  CL17 HCT 116 C150(5.47); C145(20.00)  LDD0721  [7]
 LDCM0405  CL18 HCT 116 C150(0.94); C145(1.15)  LDD0722  [7]
 LDCM0406  CL19 HCT 116 C150(0.85); C145(2.48)  LDD0723  [7]
 LDCM0407  CL2 HCT 116 C150(1.16); C145(5.77)  LDD0724  [7]
 LDCM0408  CL20 HCT 116 C150(0.84); C145(0.90)  LDD0725  [7]
 LDCM0409  CL21 HCT 116 C150(2.52); C145(17.69)  LDD0726  [7]
 LDCM0410  CL22 HCT 116 C150(1.09); C145(5.38)  LDD0727  [7]
 LDCM0411  CL23 HCT 116 C150(1.14); C145(1.48)  LDD0728  [7]
 LDCM0412  CL24 HCT 116 C150(0.86); C145(1.41)  LDD0729  [7]
 LDCM0413  CL25 HCT 116 C145(1.38); C150(1.80)  LDD0730  [7]
 LDCM0414  CL26 HCT 116 C145(1.94); C150(0.98)  LDD0731  [7]
 LDCM0415  CL27 HCT 116 C145(2.62); C150(1.02)  LDD0732  [7]
 LDCM0416  CL28 HCT 116 C145(20.00); C150(1.47)  LDD0733  [7]
 LDCM0417  CL29 HCT 116 C145(0.88); C150(0.81)  LDD0734  [7]
 LDCM0418  CL3 HCT 116 C145(13.60); C150(1.11)  LDD0735  [7]
 LDCM0419  CL30 HCT 116 C145(0.91); C150(0.79)  LDD0736  [7]
 LDCM0420  CL31 HCT 116 C150(1.33)  LDD0737  [7]
 LDCM0421  CL32 HCT 116 C145(0.81); C150(1.38)  LDD0738  [7]
 LDCM0422  CL33 HCT 116 C145(1.19); C150(1.68)  LDD0739  [7]
 LDCM0423  CL34 HCT 116 C145(0.91); C150(1.72)  LDD0740  [7]
 LDCM0424  CL35 HCT 116 C145(0.46); C150(1.34)  LDD0741  [7]
 LDCM0425  CL36 HCT 116 C145(0.57); C150(2.99)  LDD0742  [7]
 LDCM0426  CL37 HCT 116 C145(0.24); C150(1.54)  LDD0743  [7]
 LDCM0428  CL39 HCT 116 C145(0.74); C150(1.30)  LDD0745  [7]
 LDCM0429  CL4 HCT 116 C145(20.00); C150(1.22)  LDD0746  [7]
 LDCM0430  CL40 HCT 116 C145(0.66); C150(6.32)  LDD0747  [7]
 LDCM0431  CL41 HCT 116 C145(0.77); C150(1.80)  LDD0748  [7]
 LDCM0432  CL42 HCT 116 C145(0.24); C150(2.50)  LDD0749  [7]
 LDCM0433  CL43 HCT 116 C145(0.45); C150(1.58)  LDD0750  [7]
 LDCM0434  CL44 HCT 116 C145(0.29); C150(1.81)  LDD0751  [7]
 LDCM0435  CL45 HCT 116 C145(0.56); C150(6.96)  LDD0752  [7]
 LDCM0436  CL46 HCT 116 C145(6.34)  LDD0753  [7]
 LDCM0437  CL47 HCT 116 C145(1.89)  LDD0754  [7]
 LDCM0438  CL48 HCT 116 C145(2.77)  LDD0755  [7]
 LDCM0439  CL49 HCT 116 C145(9.19)  LDD0756  [7]
 LDCM0440  CL5 HCT 116 C145(1.79); C150(0.75)  LDD0757  [7]
 LDCM0441  CL50 HCT 116 C145(9.01)  LDD0758  [7]
 LDCM0442  CL51 HCT 116 C145(1.13)  LDD0759  [7]
 LDCM0443  CL52 HCT 116 C145(2.54)  LDD0760  [7]
 LDCM0444  CL53 HCT 116 C145(5.26)  LDD0761  [7]
 LDCM0445  CL54 HCT 116 C145(9.14)  LDD0762  [7]
 LDCM0446  CL55 HCT 116 C145(3.48)  LDD0763  [7]
 LDCM0447  CL56 HCT 116 C145(2.16)  LDD0764  [7]
 LDCM0448  CL57 HCT 116 C145(5.87)  LDD0765  [7]
 LDCM0449  CL58 HCT 116 C145(1.51)  LDD0766  [7]
 LDCM0450  CL59 HCT 116 C145(6.26)  LDD0767  [7]
 LDCM0451  CL6 HCT 116 C145(4.41); C150(1.60)  LDD0768  [7]
 LDCM0452  CL60 HCT 116 C145(4.15)  LDD0769  [7]
 LDCM0453  CL61 HCT 116 C145(3.34); C150(1.44)  LDD0770  [7]
 LDCM0454  CL62 HCT 116 C145(20.00); C150(1.42)  LDD0771  [7]
 LDCM0455  CL63 HCT 116 C145(20.00); C150(2.91)  LDD0772  [7]
 LDCM0456  CL64 HCT 116 C145(4.24); C150(3.10)  LDD0773  [7]
 LDCM0457  CL65 HCT 116 C145(2.15); C150(1.32)  LDD0774  [7]
 LDCM0458  CL66 HCT 116 C145(10.95); C150(2.14)  LDD0775  [7]
 LDCM0459  CL67 HCT 116 C145(1.50); C150(1.45)  LDD0776  [7]
 LDCM0460  CL68 HCT 116 C145(20.00); C150(2.03)  LDD0777  [7]
 LDCM0461  CL69 HCT 116 C145(20.00); C150(2.35)  LDD0778  [7]
 LDCM0462  CL7 HCT 116 C145(20.00); C150(0.96)  LDD0779  [7]
 LDCM0463  CL70 HCT 116 C145(2.72); C150(1.45)  LDD0780  [7]
 LDCM0464  CL71 HCT 116 C145(20.00); C150(3.40)  LDD0781  [7]
 LDCM0465  CL72 HCT 116 C145(2.22); C150(1.33)  LDD0782  [7]
 LDCM0466  CL73 HCT 116 C145(20.00); C150(2.91)  LDD0783  [7]
 LDCM0467  CL74 HCT 116 C145(15.14); C150(2.39)  LDD0784  [7]
 LDCM0469  CL76 HCT 116 C145(1.99); C150(1.12)  LDD0786  [7]
 LDCM0470  CL77 HCT 116 C145(16.99); C150(2.22)  LDD0787  [7]
 LDCM0471  CL78 HCT 116 C145(2.96); C150(1.12)  LDD0788  [7]
 LDCM0472  CL79 HCT 116 C145(5.88); C150(1.70)  LDD0789  [7]
 LDCM0473  CL8 HCT 116 C145(3.56); C150(5.05)  LDD0790  [7]
 LDCM0474  CL80 HCT 116 C145(1.38); C150(1.11)  LDD0791  [7]
 LDCM0475  CL81 HCT 116 C145(3.64); C150(1.47)  LDD0792  [7]
 LDCM0476  CL82 HCT 116 C145(8.11); C150(1.95)  LDD0793  [7]
 LDCM0477  CL83 HCT 116 C145(10.90); C150(3.31)  LDD0794  [7]
 LDCM0478  CL84 HCT 116 C145(17.31); C150(3.99)  LDD0795  [7]
 LDCM0479  CL85 HCT 116 C145(4.31); C150(1.49)  LDD0796  [7]
 LDCM0480  CL86 HCT 116 C145(1.52); C150(1.09)  LDD0797  [7]
 LDCM0481  CL87 HCT 116 C145(15.75); C150(2.01)  LDD0798  [7]
 LDCM0482  CL88 HCT 116 C145(3.38); C150(1.75)  LDD0799  [7]
 LDCM0483  CL89 HCT 116 C145(4.73); C150(2.52)  LDD0800  [7]
 LDCM0484  CL9 HCT 116 C145(12.31); C150(1.17)  LDD0801  [7]
 LDCM0485  CL90 HCT 116 C145(16.11); C150(4.20)  LDD0802  [7]
 LDCM0486  CL91 HCT 116 C145(4.70); C150(1.14)  LDD0803  [7]
 LDCM0487  CL92 HCT 116 C145(16.87); C150(1.71)  LDD0804  [7]
 LDCM0488  CL93 HCT 116 C145(9.71); C150(1.75)  LDD0805  [7]
 LDCM0489  CL94 HCT 116 C145(15.83); C150(2.30)  LDD0806  [7]
 LDCM0490  CL95 HCT 116 C145(18.22); C150(3.81)  LDD0807  [7]
 LDCM0491  CL96 HCT 116 C145(16.40); C150(3.15)  LDD0808  [7]
 LDCM0492  CL97 HCT 116 C145(17.06); C150(1.94)  LDD0809  [7]
 LDCM0493  CL98 HCT 116 C145(16.25); C150(1.74)  LDD0810  [7]
 LDCM0494  CL99 HCT 116 C145(16.06); C150(1.60)  LDD0811  [7]
 LDCM0175  Ethacrynic acid HeLa C145(0.64)  LDD2210  [6]
 LDCM0201  EV-3 T cell C145(6.42)  LDD0515  [14]
 LDCM0625  F8 Ramos C145(20.00); C150(2.50)  LDD2187  [15]
 LDCM0572  Fragment10 Ramos C145(20.00)  LDD1466  [3]
 LDCM0573  Fragment11 Ramos C150(2.04)  LDD2190  [15]
 LDCM0575  Fragment13 Ramos C145(20.00); C150(1.77)  LDD2192  [15]
 LDCM0576  Fragment14 Ramos C145(0.86); C150(0.94)  LDD2193  [15]
 LDCM0579  Fragment20 Ramos C150(3.96)  LDD2194  [15]
 LDCM0580  Fragment21 Ramos C145(20.00); C150(2.99)  LDD2195  [15]
 LDCM0582  Fragment23 Ramos C145(0.69); C150(0.56)  LDD2196  [15]
 LDCM0578  Fragment27 Ramos C145(20.00); C150(0.97)  LDD2197  [15]
 LDCM0586  Fragment28 Ramos C145(20.00); C150(1.12)  LDD2198  [15]
 LDCM0588  Fragment30 Ramos C145(20.00); C150(2.14)  LDD2199  [15]
 LDCM0589  Fragment31 Ramos C145(1.15)  LDD1478  [3]
 LDCM0590  Fragment32 Ramos C145(20.00); C150(2.79)  LDD2201  [15]
 LDCM0468  Fragment33 HCT 116 C145(8.33); C150(1.78)  LDD0785  [7]
 LDCM0596  Fragment38 Ramos C145(0.64); C150(0.80)  LDD2203  [15]
 LDCM0566  Fragment4 Ramos C145(20.00); C150(3.96)  LDD2184  [15]
 LDCM0427  Fragment51 HCT 116 C145(0.98); C150(19.59)  LDD0744  [7]
 LDCM0610  Fragment52 Ramos C145(12.96); C150(1.37)  LDD2204  [15]
 LDCM0614  Fragment56 Ramos C145(0.82); C150(0.91)  LDD2205  [15]
 LDCM0616  Fragment61 Jurkat _(20.00)  LDD1489  [3]
 LDCM0617  Fragment63-S Jurkat _(8.23)  LDD1490  [3]
 LDCM0569  Fragment7 Jurkat _(15.53)  LDD1485  [3]
 LDCM0571  Fragment9 Ramos C145(20.00)  LDD1464  [3]
 LDCM0107  IAA HeLa N.A.  LDD0221  [11]
 LDCM0022  KB02 T cell C145(19.44); C150(20.00)  LDD1703  [14]
 LDCM0023  KB03 Ramos C145(20.00); C150(8.45)  LDD2183  [15]
 LDCM0024  KB05 COLO792 C24(1.10)  LDD3310  [16]
 LDCM0169  KB63 Ramos 7.59  LDD0432  [17]
 LDCM0014  Panhematin hPBMC 3.30  LDD0064  [5]
 LDCM0131  RA190 MM1.R C150(1.35)  LDD0304  [18]
 LDCM0021  THZ1 HCT 116 C145(0.89)  LDD2173  [7]
 LDCM0112  W16 Hep-G2 C145(1.47)  LDD0239  [12]
 LDCM0154  YY4 T cell 3.70  LDD0400  [4]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cysteine Small molecular drug DB00151
Zinc . DB01593
Zinc Acetate . DB14487
Zinc Chloride . DB14533
Zinc Sulfate Unspecified Form . DB14548
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
O6-benzylguanine Alkylade . D0S0HA
Investigative
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
6-allyloxy-9h-purin-2-ylamine Small molecular drug D0Z8EI
6-benzyloxy-5-nitro-pyrimidine-2,4-diamine Small molecular drug D07BTU
6-benzyloxy-5-nitroso-pyrimidine-2,4-diamine Small molecular drug D04RNU
6-benzyloxy-9h-purin-2-ylamine Small molecular drug D0B5BG
Benzylcysteine Small molecular drug D0S0JL
Dinitrochlorobenzene Small molecular drug DB11831
S-benzylcysteine Small molecular drug DB04531
S-methylcysteine Small molecular drug D0CU4Q

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 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
3 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
4 A Chemical Proteomic Probe for the Mitochondrial Pyruvate Carrier Complex. Angew Chem Int Ed Engl. 2020 Mar 2;59(10):3896-3899. doi: 10.1002/anie.201914391. Epub 2020 Feb 11.
5 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
6 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.
7 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.
8 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
9 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
10 Sequence-Based Prediction of Cysteine Reactivity Using Machine Learning. Biochemistry. 2018 Jan 30;57(4):451-460. doi: 10.1021/acs.biochem.7b00897. Epub 2017 Oct 26.
11 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.
12 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.
13 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
14 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
15 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
16 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
17 2-Sulfonylpyridines as Tunable, Cysteine-Reactive Electrophiles. J Am Chem Soc. 2020 May 13;142(19):8972-8979. doi: 10.1021/jacs.0c02721. Epub 2020 Apr 29.
18 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.