Details of the Target

General Information of Target

Target ID LDTP09543
Target Name Histone-lysine N-methyltransferase SETD7 (SETD7)
Gene Name SETD7
Gene ID 80854
Synonyms
KIAA1717; KMT7; SET7; SET9; Histone-lysine N-methyltransferase SETD7; EC 2.1.1.364; Histone H3-K4 methyltransferase SETD7; H3-K4-HMTase SETD7; Lysine N-methyltransferase 7; SET domain-containing protein 7; SET7/9
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MDSDDEMVEEAVEGHLDDDGLPHGFCTVTYSSTDRFEGNFVHGEKNGRGKFFFFDGSTLE
GYYVDDALQGQGVYTYEDGGVLQGTYVDGELNGPAQEYDTDGRLIFKGQYKDNIRHGVCW
IYYPDGGSLVGEVNEDGEMTGEKIAYVYPDERTALYGKFIDGEMIEGKLATLMSTEEGRP
HFELMPGNSVYHFDKSTSSCISTNALLPDPYESERVYVAESLISSAGEGLFSKVAVGPNT
VMSFYNGVRITHQEVDSRDWALNGNTLSLDEETVIDVPEPYNHVSKYCASLGHKANHSFT
PNCIYDMFVHPRFGPIKCIRTLRAVEADEELTVAYGYDHSPPGKSGPEAPEWYQVELKAF
QATQQK
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Class V-like SAM-binding methyltransferase superfamily, Histone-lysine methyltransferase family, SET7 subfamily
Subcellular location
Nucleus
Function
Histone methyltransferase that specifically monomethylates 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. Plays a central role in the transcriptional activation of genes such as collagenase or insulin. Recruited by IPF1/PDX-1 to the insulin promoter, leading to activate transcription. Has also methyltransferase activity toward non-histone proteins such as CGAS, p53/TP53, TAF10, and possibly TAF7 by recognizing and binding the [KR]-[STA]-K in substrate proteins. Monomethylates 'Lys-189' of TAF10, leading to increase the affinity of TAF10 for RNA polymerase II. Monomethylates 'Lys-372' of p53/TP53, stabilizing p53/TP53 and increasing p53/TP53-mediated transcriptional activation. Monomethylates 'Lys-491' of CGAS, promoting interaction between SGF29 and CGAS.
TTD ID
T73184
Uniprot ID
Q8WTS6
DrugMap ID
TTJ0FSU
Ensemble ID
ENST00000274031.8
HGNC ID
HGNC:30412
ChEMBL ID
CHEMBL5523

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K111(2.38)  LDD0277  [1]
BTD
 Probe Info  		C288(3.93)  LDD1700  [2]
AHL-Pu-1
 Probe Info  		C200(2.90)  LDD0170  [3]
DBIA
 Probe Info  		C200(0.94)  LDD0531  [4]
5E-2FA
 Probe Info  		N.A.  LDD2235  [5]
m-APA
 Probe Info  		H181(0.00); H252(0.00)  LDD2231  [5]
IA-alkyne
 Probe Info  		C303(0.00); C119(0.00)  LDD0036  [6]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [6]
Acrolein
 Probe Info  		C200(0.00); C288(0.00)  LDD0217  [7]
Methacrolein
 Probe Info  		N.A.  LDD0218  [7]
NAIA_5
 Probe Info  		C303(0.00); C288(0.00)  LDD2223  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C288(1.66)  LDD2112  [2]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C288(0.54)  LDD2095  [2]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C288(1.14)  LDD2117  [2]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C288(2.46)  LDD2152  [2]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C288(0.63)  LDD2131  [2]
 LDCM0025  4SU-RNA DM93 C200(2.90)  LDD0170  [3]
 LDCM0026  4SU-RNA+native RNA DM93 C200(3.57)  LDD0171  [3]
 LDCM0214  AC1 HCT 116 C200(0.94)  LDD0531  [4]
 LDCM0215  AC10 HCT 116 C200(1.11)  LDD0532  [4]
 LDCM0216  AC100 HCT 116 C200(0.98)  LDD0533  [4]
 LDCM0217  AC101 HCT 116 C200(1.02)  LDD0534  [4]
 LDCM0218  AC102 HCT 116 C200(1.04)  LDD0535  [4]
 LDCM0219  AC103 HCT 116 C200(1.03)  LDD0536  [4]
 LDCM0220  AC104 HCT 116 C200(0.91)  LDD0537  [4]
 LDCM0221  AC105 HCT 116 C200(0.95)  LDD0538  [4]
 LDCM0222  AC106 HCT 116 C200(0.98)  LDD0539  [4]
 LDCM0223  AC107 HCT 116 C200(0.90)  LDD0540  [4]
 LDCM0224  AC108 HCT 116 C200(0.95)  LDD0541  [4]
 LDCM0225  AC109 HCT 116 C200(0.94)  LDD0542  [4]
 LDCM0226  AC11 HCT 116 C200(1.09)  LDD0543  [4]
 LDCM0227  AC110 HCT 116 C200(0.99)  LDD0544  [4]
 LDCM0228  AC111 HCT 116 C200(1.24)  LDD0545  [4]
 LDCM0229  AC112 HCT 116 C200(1.23)  LDD0546  [4]
 LDCM0230  AC113 HCT 116 C200(1.20)  LDD0547  [4]
 LDCM0231  AC114 HCT 116 C200(1.03)  LDD0548  [4]
 LDCM0232  AC115 HCT 116 C200(0.97)  LDD0549  [4]
 LDCM0233  AC116 HCT 116 C200(0.95)  LDD0550  [4]
 LDCM0234  AC117 HCT 116 C200(1.04)  LDD0551  [4]
 LDCM0235  AC118 HCT 116 C200(0.93)  LDD0552  [4]
 LDCM0236  AC119 HCT 116 C200(1.17)  LDD0553  [4]
 LDCM0237  AC12 HCT 116 C200(1.14)  LDD0554  [4]
 LDCM0238  AC120 HCT 116 C200(0.90)  LDD0555  [4]
 LDCM0239  AC121 HCT 116 C200(1.01)  LDD0556  [4]
 LDCM0240  AC122 HCT 116 C200(1.12)  LDD0557  [4]
 LDCM0241  AC123 HCT 116 C200(1.13)  LDD0558  [4]
 LDCM0242  AC124 HCT 116 C200(1.30)  LDD0559  [4]
 LDCM0243  AC125 HCT 116 C200(1.15)  LDD0560  [4]
 LDCM0244  AC126 HCT 116 C200(1.02)  LDD0561  [4]
 LDCM0245  AC127 HCT 116 C200(0.95)  LDD0562  [4]
 LDCM0246  AC128 HCT 116 C200(0.76)  LDD0563  [4]
 LDCM0247  AC129 HCT 116 C200(1.00)  LDD0564  [4]
 LDCM0249  AC130 HCT 116 C200(0.96)  LDD0566  [4]
 LDCM0250  AC131 HCT 116 C200(1.19)  LDD0567  [4]
 LDCM0251  AC132 HCT 116 C200(0.87)  LDD0568  [4]
 LDCM0252  AC133 HCT 116 C200(1.23)  LDD0569  [4]
 LDCM0253  AC134 HCT 116 C200(0.99)  LDD0570  [4]
 LDCM0254  AC135 HCT 116 C200(1.09)  LDD0571  [4]
 LDCM0255  AC136 HCT 116 C200(1.03)  LDD0572  [4]
 LDCM0256  AC137 HCT 116 C200(0.94)  LDD0573  [4]
 LDCM0257  AC138 HCT 116 C200(0.91)  LDD0574  [4]
 LDCM0258  AC139 HCT 116 C200(0.79)  LDD0575  [4]
 LDCM0259  AC14 HCT 116 C200(1.25)  LDD0576  [4]
 LDCM0260  AC140 HCT 116 C200(0.81)  LDD0577  [4]
 LDCM0261  AC141 HCT 116 C200(0.84)  LDD0578  [4]
 LDCM0262  AC142 HCT 116 C200(1.01)  LDD0579  [4]
 LDCM0270  AC15 HCT 116 C200(1.22)  LDD0587  [4]
 LDCM0276  AC17 HCT 116 C200(1.04)  LDD0593  [4]
 LDCM0277  AC18 HCT 116 C200(1.05)  LDD0594  [4]
 LDCM0278  AC19 HCT 116 C200(0.95)  LDD0595  [4]
 LDCM0279  AC2 HCT 116 C200(0.95)  LDD0596  [4]
 LDCM0280  AC20 HCT 116 C200(1.05)  LDD0597  [4]
 LDCM0281  AC21 HCT 116 C200(0.95)  LDD0598  [4]
 LDCM0282  AC22 HCT 116 C200(0.97)  LDD0599  [4]
 LDCM0283  AC23 HCT 116 C200(0.87)  LDD0600  [4]
 LDCM0284  AC24 HCT 116 C200(0.96)  LDD0601  [4]
 LDCM0285  AC25 HCT 116 C200(0.87)  LDD0602  [4]
 LDCM0286  AC26 HCT 116 C200(0.87)  LDD0603  [4]
 LDCM0287  AC27 HCT 116 C200(1.00)  LDD0604  [4]
 LDCM0288  AC28 HCT 116 C200(0.86)  LDD0605  [4]
 LDCM0289  AC29 HCT 116 C200(0.91)  LDD0606  [4]
 LDCM0290  AC3 HCT 116 C200(0.98)  LDD0607  [4]
 LDCM0291  AC30 HCT 116 C200(0.97)  LDD0608  [4]
 LDCM0292  AC31 HCT 116 C200(0.92)  LDD0609  [4]
 LDCM0293  AC32 HCT 116 C200(0.95)  LDD0610  [4]
 LDCM0294  AC33 HCT 116 C200(1.10)  LDD0611  [4]
 LDCM0295  AC34 HCT 116 C200(0.94)  LDD0612  [4]
 LDCM0296  AC35 HCT 116 C200(0.72)  LDD0613  [4]
 LDCM0297  AC36 HCT 116 C200(0.83)  LDD0614  [4]
 LDCM0298  AC37 HCT 116 C200(0.92)  LDD0615  [4]
 LDCM0299  AC38 HCT 116 C200(0.95)  LDD0616  [4]
 LDCM0300  AC39 HCT 116 C200(0.80)  LDD0617  [4]
 LDCM0301  AC4 HCT 116 C200(1.06)  LDD0618  [4]
 LDCM0302  AC40 HCT 116 C200(0.90)  LDD0619  [4]
 LDCM0303  AC41 HCT 116 C200(1.11)  LDD0620  [4]
 LDCM0304  AC42 HCT 116 C200(0.98)  LDD0621  [4]
 LDCM0305  AC43 HCT 116 C200(1.00)  LDD0622  [4]
 LDCM0306  AC44 HCT 116 C200(1.10)  LDD0623  [4]
 LDCM0307  AC45 HCT 116 C200(1.17)  LDD0624  [4]
 LDCM0308  AC46 HCT 116 C200(1.08)  LDD0625  [4]
 LDCM0309  AC47 HCT 116 C200(1.01)  LDD0626  [4]
 LDCM0310  AC48 HCT 116 C200(0.94)  LDD0627  [4]
 LDCM0311  AC49 HCT 116 C200(0.83)  LDD0628  [4]
 LDCM0312  AC5 HCT 116 C200(1.13)  LDD0629  [4]
 LDCM0313  AC50 HCT 116 C200(0.81)  LDD0630  [4]
 LDCM0314  AC51 HCT 116 C200(0.89)  LDD0631  [4]
 LDCM0315  AC52 HCT 116 C200(1.03)  LDD0632  [4]
 LDCM0316  AC53 HCT 116 C200(0.94)  LDD0633  [4]
 LDCM0317  AC54 HCT 116 C200(0.90)  LDD0634  [4]
 LDCM0318  AC55 HCT 116 C200(0.94)  LDD0635  [4]
 LDCM0319  AC56 HCT 116 C200(0.85)  LDD0636  [4]
 LDCM0320  AC57 HEK-293T C200(0.86)  LDD1559  [9]
 LDCM0321  AC58 HEK-293T C200(1.11)  LDD1560  [9]
 LDCM0322  AC59 HEK-293T C200(1.10)  LDD1561  [9]
 LDCM0323  AC6 HCT 116 C200(1.10)  LDD0640  [4]
 LDCM0324  AC60 HEK-293T C200(1.01)  LDD1563  [9]
 LDCM0325  AC61 HEK-293T C200(1.18)  LDD1564  [9]
 LDCM0326  AC62 HEK-293T C200(0.88)  LDD1565  [9]
 LDCM0327  AC63 HEK-293T C200(0.98)  LDD1566  [9]
 LDCM0328  AC64 HEK-293T C200(1.12)  LDD1567  [9]
 LDCM0332  AC68 HCT 116 C200(0.86)  LDD0649  [4]
 LDCM0333  AC69 HCT 116 C200(0.87)  LDD0650  [4]
 LDCM0334  AC7 HCT 116 C200(1.07)  LDD0651  [4]
 LDCM0335  AC70 HCT 116 C200(0.99)  LDD0652  [4]
 LDCM0336  AC71 HCT 116 C200(0.95)  LDD0653  [4]
 LDCM0337  AC72 HCT 116 C200(0.98)  LDD0654  [4]
 LDCM0338  AC73 HCT 116 C200(0.86)  LDD0655  [4]
 LDCM0339  AC74 HCT 116 C200(0.91)  LDD0656  [4]
 LDCM0340  AC75 HCT 116 C200(0.86)  LDD0657  [4]
 LDCM0341  AC76 HCT 116 C200(0.84)  LDD0658  [4]
 LDCM0342  AC77 HCT 116 C200(1.02)  LDD0659  [4]
 LDCM0343  AC78 HCT 116 C200(1.14)  LDD0660  [4]
 LDCM0344  AC79 HCT 116 C200(0.95)  LDD0661  [4]
 LDCM0345  AC8 HCT 116 C200(1.19)  LDD0662  [4]
 LDCM0346  AC80 HCT 116 C200(1.03)  LDD0663  [4]
 LDCM0347  AC81 HCT 116 C200(1.10)  LDD0664  [4]
 LDCM0348  AC82 HCT 116 C200(1.15)  LDD0665  [4]
 LDCM0349  AC83 HCT 116 C200(1.01)  LDD0666  [4]
 LDCM0350  AC84 HCT 116 C200(1.03)  LDD0667  [4]
 LDCM0351  AC85 HCT 116 C200(1.02)  LDD0668  [4]
 LDCM0352  AC86 HCT 116 C200(1.21)  LDD0669  [4]
 LDCM0353  AC87 HCT 116 C200(1.06)  LDD0670  [4]
 LDCM0354  AC88 HCT 116 C200(1.08)  LDD0671  [4]
 LDCM0355  AC89 HCT 116 C200(1.03)  LDD0672  [4]
 LDCM0357  AC90 HCT 116 C200(1.00)  LDD0674  [4]
 LDCM0358  AC91 HCT 116 C200(1.15)  LDD0675  [4]
 LDCM0359  AC92 HCT 116 C200(1.09)  LDD0676  [4]
 LDCM0360  AC93 HCT 116 C200(1.05)  LDD0677  [4]
 LDCM0361  AC94 HCT 116 C200(1.16)  LDD0678  [4]
 LDCM0362  AC95 HCT 116 C200(1.02)  LDD0679  [4]
 LDCM0363  AC96 HCT 116 C200(1.00)  LDD0680  [4]
 LDCM0364  AC97 HCT 116 C200(1.13)  LDD0681  [4]
 LDCM0365  AC98 HCT 116 C200(1.16)  LDD0682  [4]
 LDCM0366  AC99 HCT 116 C200(1.08)  LDD0683  [4]
 LDCM0545  Acetamide MDA-MB-231 C288(0.59)  LDD2138  [2]
 LDCM0248  AKOS034007472 HCT 116 C200(1.10)  LDD0565  [4]
 LDCM0356  AKOS034007680 HCT 116 C200(1.17)  LDD0673  [4]
 LDCM0275  AKOS034007705 HCT 116 C200(0.99)  LDD0592  [4]
 LDCM0498  BS-3668 MDA-MB-231 C288(0.88)  LDD2091  [2]
 LDCM0108  Chloroacetamide HeLa C200(0.00); C303(0.00)  LDD0222  [7]
 LDCM0367  CL1 HCT 116 C200(1.43)  LDD0684  [4]
 LDCM0368  CL10 HCT 116 C200(0.88)  LDD0685  [4]
 LDCM0369  CL100 HCT 116 C200(0.95)  LDD0686  [4]
 LDCM0370  CL101 HCT 116 C200(1.18)  LDD0687  [4]
 LDCM0371  CL102 HCT 116 C200(1.03)  LDD0688  [4]
 LDCM0372  CL103 HCT 116 C200(0.97)  LDD0689  [4]
 LDCM0373  CL104 HCT 116 C200(1.03)  LDD0690  [4]
 LDCM0374  CL105 HCT 116 C200(1.06)  LDD0691  [4]
 LDCM0375  CL106 HCT 116 C200(0.86)  LDD0692  [4]
 LDCM0376  CL107 HCT 116 C200(0.91)  LDD0693  [4]
 LDCM0377  CL108 HCT 116 C200(0.93)  LDD0694  [4]
 LDCM0378  CL109 HCT 116 C200(0.98)  LDD0695  [4]
 LDCM0379  CL11 HCT 116 C200(0.90)  LDD0696  [4]
 LDCM0380  CL110 HCT 116 C200(0.98)  LDD0697  [4]
 LDCM0381  CL111 HCT 116 C200(0.96)  LDD0698  [4]
 LDCM0382  CL112 HCT 116 C200(0.83)  LDD0699  [4]
 LDCM0383  CL113 HCT 116 C200(0.99)  LDD0700  [4]
 LDCM0384  CL114 HCT 116 C200(0.85)  LDD0701  [4]
 LDCM0385  CL115 HCT 116 C200(1.02)  LDD0702  [4]
 LDCM0386  CL116 HCT 116 C200(1.05)  LDD0703  [4]
 LDCM0387  CL117 HCT 116 C200(0.80)  LDD0704  [4]
 LDCM0388  CL118 HCT 116 C200(1.00)  LDD0705  [4]
 LDCM0389  CL119 HCT 116 C200(1.01)  LDD0706  [4]
 LDCM0390  CL12 HCT 116 C200(0.90)  LDD0707  [4]
 LDCM0391  CL120 HCT 116 C200(1.18)  LDD0708  [4]
 LDCM0392  CL121 HCT 116 C200(1.05)  LDD0709  [4]
 LDCM0393  CL122 HCT 116 C200(1.00)  LDD0710  [4]
 LDCM0394  CL123 HCT 116 C200(0.85)  LDD0711  [4]
 LDCM0395  CL124 HCT 116 C200(0.89)  LDD0712  [4]
 LDCM0396  CL125 HEK-293T C200(1.14)  LDD1600  [9]
 LDCM0397  CL126 HEK-293T C200(1.04)  LDD1601  [9]
 LDCM0398  CL127 HEK-293T C200(1.17)  LDD1602  [9]
 LDCM0399  CL128 HEK-293T C200(1.35)  LDD1603  [9]
 LDCM0400  CL13 HCT 116 C200(0.94)  LDD0717  [4]
 LDCM0401  CL14 HCT 116 C200(0.99)  LDD0718  [4]
 LDCM0402  CL15 HCT 116 C200(0.92)  LDD0719  [4]
 LDCM0403  CL16 HCT 116 C200(1.07)  LDD0720  [4]
 LDCM0404  CL17 HEK-293T C200(0.78)  LDD1608  [9]
 LDCM0405  CL18 HEK-293T C200(1.24)  LDD1609  [9]
 LDCM0406  CL19 HEK-293T C200(0.99)  LDD1610  [9]
 LDCM0407  CL2 HCT 116 C200(1.04)  LDD0724  [4]
 LDCM0408  CL20 HEK-293T C200(0.83)  LDD1612  [9]
 LDCM0409  CL21 HEK-293T C200(0.90)  LDD1613  [9]
 LDCM0410  CL22 HEK-293T C200(0.95)  LDD1614  [9]
 LDCM0411  CL23 HEK-293T C200(0.97)  LDD1615  [9]
 LDCM0412  CL24 HEK-293T C200(0.97)  LDD1616  [9]
 LDCM0413  CL25 HEK-293T C200(0.89)  LDD1617  [9]
 LDCM0414  CL26 HEK-293T C200(1.15)  LDD1618  [9]
 LDCM0415  CL27 HEK-293T C200(1.04)  LDD1619  [9]
 LDCM0416  CL28 HEK-293T C200(1.27)  LDD1620  [9]
 LDCM0417  CL29 HEK-293T C200(0.90)  LDD1621  [9]
 LDCM0418  CL3 HCT 116 C200(1.12)  LDD0735  [4]
 LDCM0419  CL30 HEK-293T C200(1.25)  LDD1623  [9]
 LDCM0420  CL31 HCT 116 C200(0.89)  LDD0737  [4]
 LDCM0421  CL32 HCT 116 C200(1.27)  LDD0738  [4]
 LDCM0422  CL33 HCT 116 C200(0.99)  LDD0739  [4]
 LDCM0423  CL34 HCT 116 C200(1.08)  LDD0740  [4]
 LDCM0424  CL35 HCT 116 C200(1.08)  LDD0741  [4]
 LDCM0425  CL36 HCT 116 C200(1.07)  LDD0742  [4]
 LDCM0426  CL37 HCT 116 C200(1.04)  LDD0743  [4]
 LDCM0428  CL39 HCT 116 C200(1.01)  LDD0745  [4]
 LDCM0429  CL4 HCT 116 C200(1.21)  LDD0746  [4]
 LDCM0430  CL40 HCT 116 C200(0.88)  LDD0747  [4]
 LDCM0431  CL41 HCT 116 C200(0.93)  LDD0748  [4]
 LDCM0432  CL42 HCT 116 C200(1.05)  LDD0749  [4]
 LDCM0433  CL43 HCT 116 C200(0.88)  LDD0750  [4]
 LDCM0434  CL44 HCT 116 C200(1.19)  LDD0751  [4]
 LDCM0435  CL45 HCT 116 C200(0.93)  LDD0752  [4]
 LDCM0436  CL46 HEK-293T C200(0.82)  LDD1640  [9]
 LDCM0437  CL47 HEK-293T C200(0.79)  LDD1641  [9]
 LDCM0438  CL48 HEK-293T C200(0.97)  LDD1642  [9]
 LDCM0439  CL49 HEK-293T C200(1.17)  LDD1643  [9]
 LDCM0440  CL5 HCT 116 C200(1.04)  LDD0757  [4]
 LDCM0441  CL50 HEK-293T C200(1.02)  LDD1645  [9]
 LDCM0443  CL52 HEK-293T C200(1.17)  LDD1646  [9]
 LDCM0444  CL53 HEK-293T C200(0.96)  LDD1647  [9]
 LDCM0445  CL54 HEK-293T C200(0.92)  LDD1648  [9]
 LDCM0446  CL55 HEK-293T C200(1.10)  LDD1649  [9]
 LDCM0447  CL56 HEK-293T C200(1.03)  LDD1650  [9]
 LDCM0448  CL57 HEK-293T C200(0.94)  LDD1651  [9]
 LDCM0449  CL58 HEK-293T C200(1.05)  LDD1652  [9]
 LDCM0450  CL59 HEK-293T C200(0.97)  LDD1653  [9]
 LDCM0451  CL6 HCT 116 C200(0.99)  LDD0768  [4]
 LDCM0452  CL60 HEK-293T C200(0.94)  LDD1655  [9]
 LDCM0453  CL61 HEK-293T C200(1.11)  LDD1656  [9]
 LDCM0454  CL62 HEK-293T C200(1.08)  LDD1657  [9]
 LDCM0455  CL63 HEK-293T C200(1.18)  LDD1658  [9]
 LDCM0456  CL64 HEK-293T C200(1.08)  LDD1659  [9]
 LDCM0457  CL65 HEK-293T C200(0.95)  LDD1660  [9]
 LDCM0458  CL66 HEK-293T C200(1.18)  LDD1661  [9]
 LDCM0459  CL67 HEK-293T C200(0.98)  LDD1662  [9]
 LDCM0460  CL68 HEK-293T C200(0.95)  LDD1663  [9]
 LDCM0461  CL69 HEK-293T C200(0.90)  LDD1664  [9]
 LDCM0462  CL7 HCT 116 C200(0.96)  LDD0779  [4]
 LDCM0463  CL70 HEK-293T C200(1.09)  LDD1666  [9]
 LDCM0464  CL71 HEK-293T C200(0.92)  LDD1667  [9]
 LDCM0465  CL72 HEK-293T C200(1.03)  LDD1668  [9]
 LDCM0466  CL73 HEK-293T C200(1.06)  LDD1669  [9]
 LDCM0467  CL74 HEK-293T C200(1.02)  LDD1670  [9]
 LDCM0469  CL76 HCT 116 C200(0.85)  LDD0786  [4]
 LDCM0470  CL77 HCT 116 C200(0.81)  LDD0787  [4]
 LDCM0471  CL78 HCT 116 C200(0.75)  LDD0788  [4]
 LDCM0472  CL79 HCT 116 C200(0.84)  LDD0789  [4]
 LDCM0473  CL8 HCT 116 C200(0.93)  LDD0790  [4]
 LDCM0474  CL80 HCT 116 C200(0.80)  LDD0791  [4]
 LDCM0475  CL81 HCT 116 C200(0.75)  LDD0792  [4]
 LDCM0476  CL82 HCT 116 C200(0.76)  LDD0793  [4]
 LDCM0477  CL83 HCT 116 C200(0.67)  LDD0794  [4]
 LDCM0478  CL84 HCT 116 C200(0.82)  LDD0795  [4]
 LDCM0479  CL85 HCT 116 C200(0.77)  LDD0796  [4]
 LDCM0480  CL86 HCT 116 C200(0.83)  LDD0797  [4]
 LDCM0481  CL87 HCT 116 C200(0.77)  LDD0798  [4]
 LDCM0482  CL88 HCT 116 C200(0.77)  LDD0799  [4]
 LDCM0483  CL89 HCT 116 C200(0.73)  LDD0800  [4]
 LDCM0484  CL9 HCT 116 C200(0.93)  LDD0801  [4]
 LDCM0485  CL90 HCT 116 C200(0.68)  LDD0802  [4]
 LDCM0486  CL91 HCT 116 C200(0.89)  LDD0803  [4]
 LDCM0487  CL92 HCT 116 C200(0.80)  LDD0804  [4]
 LDCM0488  CL93 HCT 116 C200(0.92)  LDD0805  [4]
 LDCM0489  CL94 HCT 116 C200(0.85)  LDD0806  [4]
 LDCM0490  CL95 HCT 116 C200(0.89)  LDD0807  [4]
 LDCM0491  CL96 HCT 116 C200(0.88)  LDD0808  [4]
 LDCM0492  CL97 HCT 116 C200(1.04)  LDD0809  [4]
 LDCM0493  CL98 HCT 116 C200(1.04)  LDD0810  [4]
 LDCM0494  CL99 HCT 116 C200(1.01)  LDD0811  [4]
 LDCM0495  E2913 HEK-293T C200(1.07)  LDD1698  [9]
 LDCM0468  Fragment33 HEK-293T C200(1.10)  LDD1671  [9]
 LDCM0427  Fragment51 HCT 116 C200(1.07)  LDD0744  [4]
 LDCM0107  IAA HeLa N.A.  LDD0221  [7]
 LDCM0022  KB02 HEK-293T C200(1.07)  LDD1492  [9]
 LDCM0023  KB03 HEK-293T C200(0.90)  LDD1497  [9]
 LDCM0024  KB05 HMCB C200(1.01)  LDD3312  [10]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C288(0.97)  LDD2121  [2]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C288(1.04)  LDD2089  [2]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C288(1.22); C318(1.01)  LDD2093  [2]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C288(0.41); C318(0.41)  LDD2096  [2]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C288(1.34)  LDD2097  [2]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C288(1.86)  LDD2099  [2]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C288(0.89); C318(0.46)  LDD2100  [2]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C288(1.11)  LDD2101  [2]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C288(1.00)  LDD2104  [2]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C318(0.39)  LDD2106  [2]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C288(1.21); C318(0.92)  LDD2107  [2]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C288(1.04); C318(0.43)  LDD2109  [2]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C288(1.40)  LDD2111  [2]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C288(1.01)  LDD2114  [2]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C288(0.73)  LDD2116  [2]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C288(1.46); C318(2.65)  LDD2119  [2]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C288(0.77)  LDD2122  [2]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C288(1.03)  LDD2123  [2]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C288(0.75)  LDD2124  [2]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C288(1.12); C318(0.78)  LDD2125  [2]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C288(0.94)  LDD2126  [2]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C318(0.98)  LDD2127  [2]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C288(0.82)  LDD2128  [2]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C288(2.02); C318(1.21)  LDD2129  [2]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C288(0.58)  LDD2133  [2]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C288(1.50)  LDD2134  [2]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C288(3.93)  LDD1700  [2]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C318(1.16)  LDD2140  [2]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C288(1.00)  LDD2143  [2]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C288(1.26)  LDD2145  [2]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C288(0.81); C318(0.87)  LDD2146  [2]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C288(0.82)  LDD2149  [2]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C288(0.64)  LDD2150  [2]
 LDCM0557  Nucleophilic fragment 8b MDA-MB-231 C288(0.51)  LDD2151  [2]

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 (cytosine-5)-methyltransferase 1 (DNMT1) C5-methyltransferase family P26358
NAD-dependent protein deacetylase sirtuin-1 (SIRT1) Sirtuin family Q96EB6
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cellular tumor antigen p53 (TP53) P53 family P04637
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Bile acid receptor (NR1H4) Nuclear hormone receptor family Q96RI1
Transcription factor p65 (RELA) . Q04206
Other
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone H3.1 (H3C1; H3C2; H3C3; H3C4; H3C6; H3C7; H3C8; H3C10; H3C11; H3C12) Histone H3 family P68431
Retinoblastoma-associated protein (RB1) Retinoblastoma protein (RB) family P06400
Transcription initiation factor TFIID subunit 10 (TAF10) TAF10 family Q12962
SERTA domain-containing protein 1 (SERTAD1) . Q9UHV2

The Drug(s) Related To This Target

Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(R)-pfi-2 Small molecular drug D0J6OV
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
S-adenosyl-l-homocysteine Small molecular drug DB01752

References

1 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
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 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 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.
5 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
6 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
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 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
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