Details of the Target

General Information of Target

Target ID LDTP05953
Target Name Dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A)
Gene Name DYRK1A
Gene ID 1859
Synonyms
DYRK; MNB; MNBH; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; EC 2.7.11.23; EC 2.7.12.1; Dual specificity YAK1-related kinase; HP86; Protein kinase minibrain homolog; MNBH; hMNB
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAGQMPHSHQYSDRRQPNISDQQVSALSYSD
QIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQ
QGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRV
EQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEM
LSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKR
SAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPL
FSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWNLKKTKDGKREYKPPGT
RKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFK
KTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGG
HFTAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHH
HHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSS
STTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTY
QFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, MNB/DYRK subfamily
Subcellular location
Nucleus
Function
Dual-specificity kinase which possesses both serine/threonine and tyrosine kinase activities. Exhibits a substrate preference for proline at position P+1 and arginine at position P-3. Plays an important role in double-strand breaks (DSBs) repair following DNA damage. Mechanistically, phosphorylates RNF169 and increases its ability to block accumulation of TP53BP1 at the DSB sites thereby promoting homologous recombination repair (HRR). Also acts as a positive regulator of transcription by acting as a CTD kinase that mediates phosphorylation of the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAP II) POLR2A. May play a role in a signaling pathway regulating nuclear functions of cell proliferation. Modulates alternative splicing by phosphorylating the splice factor SRSF6. Has pro-survival function and negatively regulates the apoptotic process. Promotes cell survival upon genotoxic stress through phosphorylation of SIRT1. This in turn inhibits p53/TP53 activity and apoptosis. Phosphorylates SEPTIN4, SEPTIN5 and SF3B1 at 'Thr-434'.
TTD ID
T92803
Uniprot ID
Q13627
DrugMap ID
TTSBVFO
Ensemble ID
ENST00000338785.8
HGNC ID
HGNC:3091
ChEMBL ID
CHEMBL2292

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 12 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K453(10.00)  LDD0277  [1]
Probe 1
 Probe Info  		Y145(10.21)  LDD3495  [2]
m-APA
 Probe Info  		10.43  LDD0403  [3]
Johansson_61
 Probe Info  		_(20.00)  LDD1485  [4]
HHS-475
 Probe Info  		Y472(0.38)  LDD0264  [5]
DBIA
 Probe Info  		C312(1.21)  LDD0531  [6]
ATP probe
 Probe Info  		N.A.  LDD0199  [7]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [8]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [8]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [8]
NAIA_5
 Probe Info  		N.A.  LDD2224  [9]
IPM
 Probe Info  		N.A.  LDD2156  [10]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Probe 12
 Probe Info  		N.A.  LDD0420  [11]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C312(1.21)  LDD0531  [6]
 LDCM0215  AC10 HCT 116 C312(0.88)  LDD0532  [6]
 LDCM0216  AC100 HCT 116 C312(0.68)  LDD0533  [6]
 LDCM0217  AC101 HCT 116 C312(0.77)  LDD0534  [6]
 LDCM0218  AC102 HCT 116 C312(0.65)  LDD0535  [6]
 LDCM0219  AC103 HCT 116 C312(0.69)  LDD0536  [6]
 LDCM0220  AC104 HCT 116 C312(0.74)  LDD0537  [6]
 LDCM0221  AC105 HCT 116 C312(0.69)  LDD0538  [6]
 LDCM0222  AC106 HCT 116 C312(0.75)  LDD0539  [6]
 LDCM0223  AC107 HCT 116 C312(0.70)  LDD0540  [6]
 LDCM0224  AC108 HCT 116 C312(0.79)  LDD0541  [6]
 LDCM0225  AC109 HCT 116 C312(0.73)  LDD0542  [6]
 LDCM0226  AC11 HCT 116 C312(1.11)  LDD0543  [6]
 LDCM0227  AC110 HCT 116 C312(0.78)  LDD0544  [6]
 LDCM0228  AC111 HCT 116 C312(0.95)  LDD0545  [6]
 LDCM0229  AC112 HCT 116 C312(0.72)  LDD0546  [6]
 LDCM0230  AC113 HCT 116 C312(1.13)  LDD0547  [6]
 LDCM0231  AC114 HCT 116 C312(0.99)  LDD0548  [6]
 LDCM0232  AC115 HCT 116 C312(1.01)  LDD0549  [6]
 LDCM0233  AC116 HCT 116 C312(1.10)  LDD0550  [6]
 LDCM0234  AC117 HCT 116 C312(1.11)  LDD0551  [6]
 LDCM0235  AC118 HCT 116 C312(0.88)  LDD0552  [6]
 LDCM0236  AC119 HCT 116 C312(0.97)  LDD0553  [6]
 LDCM0237  AC12 HCT 116 C312(1.03)  LDD0554  [6]
 LDCM0238  AC120 HCT 116 C312(0.98)  LDD0555  [6]
 LDCM0239  AC121 HCT 116 C312(1.23)  LDD0556  [6]
 LDCM0240  AC122 HCT 116 C312(1.09)  LDD0557  [6]
 LDCM0241  AC123 HCT 116 C312(1.13)  LDD0558  [6]
 LDCM0242  AC124 HCT 116 C312(1.09)  LDD0559  [6]
 LDCM0243  AC125 HCT 116 C312(1.04)  LDD0560  [6]
 LDCM0244  AC126 HCT 116 C312(1.28)  LDD0561  [6]
 LDCM0245  AC127 HCT 116 C312(1.22)  LDD0562  [6]
 LDCM0246  AC128 HCT 116 C312(1.33)  LDD0563  [6]
 LDCM0247  AC129 HCT 116 C312(1.36)  LDD0564  [6]
 LDCM0249  AC130 HCT 116 C312(1.24)  LDD0566  [6]
 LDCM0250  AC131 HCT 116 C312(1.30)  LDD0567  [6]
 LDCM0251  AC132 HCT 116 C312(1.08)  LDD0568  [6]
 LDCM0252  AC133 HCT 116 C312(1.02)  LDD0569  [6]
 LDCM0253  AC134 HCT 116 C312(0.97)  LDD0570  [6]
 LDCM0254  AC135 HCT 116 C312(1.09)  LDD0571  [6]
 LDCM0255  AC136 HCT 116 C312(1.06)  LDD0572  [6]
 LDCM0256  AC137 HCT 116 C312(0.97)  LDD0573  [6]
 LDCM0257  AC138 HCT 116 C312(0.69)  LDD0574  [6]
 LDCM0258  AC139 HCT 116 C312(0.88)  LDD0575  [6]
 LDCM0259  AC14 HCT 116 C312(1.00)  LDD0576  [6]
 LDCM0260  AC140 HCT 116 C312(0.80)  LDD0577  [6]
 LDCM0261  AC141 HCT 116 C312(0.85)  LDD0578  [6]
 LDCM0262  AC142 HCT 116 C312(1.01)  LDD0579  [6]
 LDCM0263  AC143 HCT 116 C312(0.85)  LDD0580  [6]
 LDCM0264  AC144 HCT 116 C312(0.90)  LDD0581  [6]
 LDCM0265  AC145 HCT 116 C312(0.96)  LDD0582  [6]
 LDCM0266  AC146 HCT 116 C312(1.19)  LDD0583  [6]
 LDCM0267  AC147 HCT 116 C312(0.95)  LDD0584  [6]
 LDCM0268  AC148 HCT 116 C312(1.05)  LDD0585  [6]
 LDCM0269  AC149 HCT 116 C312(0.91)  LDD0586  [6]
 LDCM0270  AC15 HCT 116 C312(0.93)  LDD0587  [6]
 LDCM0271  AC150 HCT 116 C312(1.22)  LDD0588  [6]
 LDCM0272  AC151 HCT 116 C312(1.05)  LDD0589  [6]
 LDCM0273  AC152 HCT 116 C312(0.96)  LDD0590  [6]
 LDCM0274  AC153 HCT 116 C312(0.93)  LDD0591  [6]
 LDCM0621  AC154 HCT 116 C312(1.02)  LDD2158  [6]
 LDCM0622  AC155 HCT 116 C312(0.88)  LDD2159  [6]
 LDCM0623  AC156 HCT 116 C312(0.91)  LDD2160  [6]
 LDCM0624  AC157 HCT 116 C312(0.79)  LDD2161  [6]
 LDCM0276  AC17 HCT 116 C312(1.05)  LDD0593  [6]
 LDCM0277  AC18 HCT 116 C312(1.01)  LDD0594  [6]
 LDCM0278  AC19 HCT 116 C312(1.15)  LDD0595  [6]
 LDCM0279  AC2 HCT 116 C312(1.21)  LDD0596  [6]
 LDCM0280  AC20 HCT 116 C312(0.82)  LDD0597  [6]
 LDCM0281  AC21 HCT 116 C312(1.00)  LDD0598  [6]
 LDCM0282  AC22 HCT 116 C312(0.99)  LDD0599  [6]
 LDCM0283  AC23 HCT 116 C312(0.91)  LDD0600  [6]
 LDCM0284  AC24 HCT 116 C312(1.01)  LDD0601  [6]
 LDCM0285  AC25 HCT 116 C312(0.87)  LDD0602  [6]
 LDCM0286  AC26 HCT 116 C312(0.85)  LDD0603  [6]
 LDCM0287  AC27 HCT 116 C312(0.85)  LDD0604  [6]
 LDCM0288  AC28 HCT 116 C312(0.84)  LDD0605  [6]
 LDCM0289  AC29 HCT 116 C312(0.78)  LDD0606  [6]
 LDCM0290  AC3 HCT 116 C312(1.20)  LDD0607  [6]
 LDCM0291  AC30 HCT 116 C312(0.75)  LDD0608  [6]
 LDCM0292  AC31 HCT 116 C312(0.84)  LDD0609  [6]
 LDCM0293  AC32 HCT 116 C312(0.77)  LDD0610  [6]
 LDCM0294  AC33 HCT 116 C312(0.92)  LDD0611  [6]
 LDCM0295  AC34 HCT 116 C312(0.89)  LDD0612  [6]
 LDCM0296  AC35 HCT 116 C312(0.97)  LDD0613  [6]
 LDCM0297  AC36 HCT 116 C312(0.90)  LDD0614  [6]
 LDCM0298  AC37 HCT 116 C312(0.94)  LDD0615  [6]
 LDCM0299  AC38 HCT 116 C312(0.90)  LDD0616  [6]
 LDCM0300  AC39 HCT 116 C312(0.97)  LDD0617  [6]
 LDCM0301  AC4 HCT 116 C312(1.06)  LDD0618  [6]
 LDCM0302  AC40 HCT 116 C312(0.97)  LDD0619  [6]
 LDCM0303  AC41 HCT 116 C312(0.95)  LDD0620  [6]
 LDCM0304  AC42 HCT 116 C312(0.87)  LDD0621  [6]
 LDCM0305  AC43 HCT 116 C312(1.01)  LDD0622  [6]
 LDCM0306  AC44 HCT 116 C312(1.08)  LDD0623  [6]
 LDCM0307  AC45 HCT 116 C312(1.08)  LDD0624  [6]
 LDCM0308  AC46 HCT 116 C312(1.01)  LDD0625  [6]
 LDCM0309  AC47 HCT 116 C312(1.04)  LDD0626  [6]
 LDCM0310  AC48 HCT 116 C312(1.18)  LDD0627  [6]
 LDCM0311  AC49 HCT 116 C312(1.08)  LDD0628  [6]
 LDCM0312  AC5 HCT 116 C312(1.06)  LDD0629  [6]
 LDCM0313  AC50 HCT 116 C312(1.08)  LDD0630  [6]
 LDCM0314  AC51 HCT 116 C312(1.07)  LDD0631  [6]
 LDCM0315  AC52 HCT 116 C312(1.12)  LDD0632  [6]
 LDCM0316  AC53 HCT 116 C312(1.13)  LDD0633  [6]
 LDCM0317  AC54 HCT 116 C312(1.00)  LDD0634  [6]
 LDCM0318  AC55 HCT 116 C312(1.11)  LDD0635  [6]
 LDCM0319  AC56 HCT 116 C312(1.11)  LDD0636  [6]
 LDCM0320  AC57 HCT 116 C312(1.14)  LDD0637  [6]
 LDCM0321  AC58 HCT 116 C312(1.22)  LDD0638  [6]
 LDCM0322  AC59 HCT 116 C312(1.09)  LDD0639  [6]
 LDCM0323  AC6 HCT 116 C312(0.98)  LDD0640  [6]
 LDCM0324  AC60 HCT 116 C312(1.11)  LDD0641  [6]
 LDCM0325  AC61 HCT 116 C312(1.25)  LDD0642  [6]
 LDCM0326  AC62 HCT 116 C312(1.18)  LDD0643  [6]
 LDCM0327  AC63 HCT 116 C312(1.21)  LDD0644  [6]
 LDCM0328  AC64 HCT 116 C312(1.17)  LDD0645  [6]
 LDCM0329  AC65 HCT 116 C312(1.51)  LDD0646  [6]
 LDCM0330  AC66 HCT 116 C312(1.46)  LDD0647  [6]
 LDCM0331  AC67 HCT 116 C312(1.23)  LDD0648  [6]
 LDCM0332  AC68 HCT 116 C312(1.10)  LDD0649  [6]
 LDCM0333  AC69 HCT 116 C312(1.09)  LDD0650  [6]
 LDCM0334  AC7 HCT 116 C312(1.22)  LDD0651  [6]
 LDCM0335  AC70 HCT 116 C312(0.99)  LDD0652  [6]
 LDCM0336  AC71 HCT 116 C312(1.16)  LDD0653  [6]
 LDCM0337  AC72 HCT 116 C312(1.13)  LDD0654  [6]
 LDCM0338  AC73 HCT 116 C312(1.07)  LDD0655  [6]
 LDCM0339  AC74 HCT 116 C312(1.14)  LDD0656  [6]
 LDCM0340  AC75 HCT 116 C312(1.17)  LDD0657  [6]
 LDCM0341  AC76 HCT 116 C312(1.15)  LDD0658  [6]
 LDCM0342  AC77 HCT 116 C312(1.00)  LDD0659  [6]
 LDCM0343  AC78 HCT 116 C312(1.12)  LDD0660  [6]
 LDCM0344  AC79 HCT 116 C312(1.23)  LDD0661  [6]
 LDCM0345  AC8 HCT 116 C312(1.14)  LDD0662  [6]
 LDCM0346  AC80 HCT 116 C312(1.05)  LDD0663  [6]
 LDCM0347  AC81 HCT 116 C312(1.14)  LDD0664  [6]
 LDCM0348  AC82 HCT 116 C312(1.11)  LDD0665  [6]
 LDCM0349  AC83 HCT 116 C312(1.09)  LDD0666  [6]
 LDCM0350  AC84 HCT 116 C312(1.09)  LDD0667  [6]
 LDCM0351  AC85 HCT 116 C312(0.97)  LDD0668  [6]
 LDCM0352  AC86 HCT 116 C312(0.94)  LDD0669  [6]
 LDCM0353  AC87 HCT 116 C312(1.01)  LDD0670  [6]
 LDCM0354  AC88 HCT 116 C312(0.92)  LDD0671  [6]
 LDCM0355  AC89 HCT 116 C312(0.90)  LDD0672  [6]
 LDCM0357  AC90 HCT 116 C312(0.87)  LDD0674  [6]
 LDCM0358  AC91 HCT 116 C312(1.00)  LDD0675  [6]
 LDCM0359  AC92 HCT 116 C312(0.97)  LDD0676  [6]
 LDCM0360  AC93 HCT 116 C312(0.96)  LDD0677  [6]
 LDCM0361  AC94 HCT 116 C312(1.10)  LDD0678  [6]
 LDCM0362  AC95 HCT 116 C312(1.02)  LDD0679  [6]
 LDCM0363  AC96 HCT 116 C312(0.96)  LDD0680  [6]
 LDCM0364  AC97 HCT 116 C312(0.90)  LDD0681  [6]
 LDCM0365  AC98 HCT 116 C312(0.71)  LDD0682  [6]
 LDCM0366  AC99 HCT 116 C312(0.78)  LDD0683  [6]
 LDCM0248  AKOS034007472 HCT 116 C312(1.10)  LDD0565  [6]
 LDCM0356  AKOS034007680 HCT 116 C312(1.12)  LDD0673  [6]
 LDCM0275  AKOS034007705 HCT 116 C312(1.01)  LDD0592  [6]
 LDCM0156  Aniline NCI-H1299 10.43  LDD0403  [3]
 LDCM0367  CL1 HCT 116 C312(1.08)  LDD0684  [6]
 LDCM0368  CL10 HCT 116 C312(1.12)  LDD0685  [6]
 LDCM0369  CL100 HCT 116 C312(1.08)  LDD0686  [6]
 LDCM0370  CL101 HCT 116 C312(1.09)  LDD0687  [6]
 LDCM0371  CL102 HCT 116 C312(1.05)  LDD0688  [6]
 LDCM0372  CL103 HCT 116 C312(1.03)  LDD0689  [6]
 LDCM0373  CL104 HCT 116 C312(0.93)  LDD0690  [6]
 LDCM0374  CL105 HCT 116 C312(1.06)  LDD0691  [6]
 LDCM0375  CL106 HCT 116 C312(1.03)  LDD0692  [6]
 LDCM0376  CL107 HCT 116 C312(0.98)  LDD0693  [6]
 LDCM0377  CL108 HCT 116 C312(1.00)  LDD0694  [6]
 LDCM0378  CL109 HCT 116 C312(1.09)  LDD0695  [6]
 LDCM0379  CL11 HCT 116 C312(1.18)  LDD0696  [6]
 LDCM0380  CL110 HCT 116 C312(0.96)  LDD0697  [6]
 LDCM0381  CL111 HCT 116 C312(0.92)  LDD0698  [6]
 LDCM0382  CL112 HCT 116 C312(0.84)  LDD0699  [6]
 LDCM0383  CL113 HCT 116 C312(0.75)  LDD0700  [6]
 LDCM0384  CL114 HCT 116 C312(0.74)  LDD0701  [6]
 LDCM0385  CL115 HCT 116 C312(0.78)  LDD0702  [6]
 LDCM0386  CL116 HCT 116 C312(0.90)  LDD0703  [6]
 LDCM0387  CL117 HCT 116 C312(0.97)  LDD0704  [6]
 LDCM0388  CL118 HCT 116 C312(0.95)  LDD0705  [6]
 LDCM0389  CL119 HCT 116 C312(0.96)  LDD0706  [6]
 LDCM0390  CL12 HCT 116 C312(1.10)  LDD0707  [6]
 LDCM0391  CL120 HCT 116 C312(0.95)  LDD0708  [6]
 LDCM0392  CL121 HCT 116 C312(0.70)  LDD0709  [6]
 LDCM0393  CL122 HCT 116 C312(0.99)  LDD0710  [6]
 LDCM0394  CL123 HCT 116 C312(1.06)  LDD0711  [6]
 LDCM0395  CL124 HCT 116 C312(1.10)  LDD0712  [6]
 LDCM0396  CL125 HCT 116 C312(1.08)  LDD0713  [6]
 LDCM0397  CL126 HCT 116 C312(0.93)  LDD0714  [6]
 LDCM0398  CL127 HCT 116 C312(0.99)  LDD0715  [6]
 LDCM0399  CL128 HCT 116 C312(1.04)  LDD0716  [6]
 LDCM0400  CL13 HCT 116 C312(1.15)  LDD0717  [6]
 LDCM0401  CL14 HCT 116 C312(1.00)  LDD0718  [6]
 LDCM0402  CL15 HCT 116 C312(1.11)  LDD0719  [6]
 LDCM0403  CL16 HCT 116 C312(0.93)  LDD0720  [6]
 LDCM0404  CL17 HCT 116 C312(0.94)  LDD0721  [6]
 LDCM0405  CL18 HCT 116 C312(1.39)  LDD0722  [6]
 LDCM0406  CL19 HCT 116 C312(0.84)  LDD0723  [6]
 LDCM0407  CL2 HCT 116 C312(1.12)  LDD0724  [6]
 LDCM0408  CL20 HCT 116 C312(0.71)  LDD0725  [6]
 LDCM0409  CL21 HCT 116 C312(0.95)  LDD0726  [6]
 LDCM0410  CL22 HCT 116 C312(0.96)  LDD0727  [6]
 LDCM0411  CL23 HCT 116 C312(0.99)  LDD0728  [6]
 LDCM0412  CL24 HCT 116 C312(0.91)  LDD0729  [6]
 LDCM0413  CL25 HCT 116 C312(1.01)  LDD0730  [6]
 LDCM0414  CL26 HCT 116 C312(0.84)  LDD0731  [6]
 LDCM0415  CL27 HCT 116 C312(0.87)  LDD0732  [6]
 LDCM0416  CL28 HCT 116 C312(0.84)  LDD0733  [6]
 LDCM0417  CL29 HCT 116 C312(0.93)  LDD0734  [6]
 LDCM0418  CL3 HCT 116 C312(1.04)  LDD0735  [6]
 LDCM0419  CL30 HCT 116 C312(1.43)  LDD0736  [6]
 LDCM0420  CL31 HCT 116 C312(0.66)  LDD0737  [6]
 LDCM0421  CL32 HCT 116 C312(1.06)  LDD0738  [6]
 LDCM0422  CL33 HCT 116 C312(1.06)  LDD0739  [6]
 LDCM0423  CL34 HCT 116 C312(0.72)  LDD0740  [6]
 LDCM0424  CL35 HCT 116 C312(0.86)  LDD0741  [6]
 LDCM0425  CL36 HCT 116 C312(0.73)  LDD0742  [6]
 LDCM0426  CL37 HCT 116 C312(0.65)  LDD0743  [6]
 LDCM0428  CL39 HCT 116 C312(0.75)  LDD0745  [6]
 LDCM0429  CL4 HCT 116 C312(1.04)  LDD0746  [6]
 LDCM0430  CL40 HCT 116 C312(0.66)  LDD0747  [6]
 LDCM0431  CL41 HCT 116 C312(0.81)  LDD0748  [6]
 LDCM0432  CL42 HCT 116 C312(0.76)  LDD0749  [6]
 LDCM0433  CL43 HCT 116 C312(1.14)  LDD0750  [6]
 LDCM0434  CL44 HCT 116 C312(0.82)  LDD0751  [6]
 LDCM0435  CL45 HCT 116 C312(0.97)  LDD0752  [6]
 LDCM0436  CL46 HCT 116 C312(0.73)  LDD0753  [6]
 LDCM0437  CL47 HCT 116 C312(0.72)  LDD0754  [6]
 LDCM0438  CL48 HCT 116 C312(0.76)  LDD0755  [6]
 LDCM0439  CL49 HCT 116 C312(0.82)  LDD0756  [6]
 LDCM0440  CL5 HCT 116 C312(1.03)  LDD0757  [6]
 LDCM0441  CL50 HCT 116 C312(0.75)  LDD0758  [6]
 LDCM0442  CL51 HCT 116 C312(0.95)  LDD0759  [6]
 LDCM0443  CL52 HCT 116 C312(0.70)  LDD0760  [6]
 LDCM0444  CL53 HCT 116 C312(0.82)  LDD0761  [6]
 LDCM0445  CL54 HCT 116 C312(0.90)  LDD0762  [6]
 LDCM0446  CL55 HCT 116 C312(1.00)  LDD0763  [6]
 LDCM0447  CL56 HCT 116 C312(0.72)  LDD0764  [6]
 LDCM0448  CL57 HCT 116 C312(0.75)  LDD0765  [6]
 LDCM0449  CL58 HCT 116 C312(1.14)  LDD0766  [6]
 LDCM0450  CL59 HCT 116 C312(1.08)  LDD0767  [6]
 LDCM0451  CL6 HCT 116 C312(1.16)  LDD0768  [6]
 LDCM0452  CL60 HCT 116 C312(0.79)  LDD0769  [6]
 LDCM0453  CL61 HCT 116 C312(1.03)  LDD0770  [6]
 LDCM0454  CL62 HCT 116 C312(1.05)  LDD0771  [6]
 LDCM0455  CL63 HCT 116 C312(1.03)  LDD0772  [6]
 LDCM0456  CL64 HCT 116 C312(1.11)  LDD0773  [6]
 LDCM0457  CL65 HCT 116 C312(1.04)  LDD0774  [6]
 LDCM0458  CL66 HCT 116 C312(1.09)  LDD0775  [6]
 LDCM0459  CL67 HCT 116 C312(1.11)  LDD0776  [6]
 LDCM0460  CL68 HCT 116 C312(1.10)  LDD0777  [6]
 LDCM0461  CL69 HCT 116 C312(1.15)  LDD0778  [6]
 LDCM0462  CL7 HCT 116 C312(1.10)  LDD0779  [6]
 LDCM0463  CL70 HCT 116 C312(1.04)  LDD0780  [6]
 LDCM0464  CL71 HCT 116 C312(1.04)  LDD0781  [6]
 LDCM0465  CL72 HCT 116 C312(1.09)  LDD0782  [6]
 LDCM0466  CL73 HCT 116 C312(1.04)  LDD0783  [6]
 LDCM0467  CL74 HCT 116 C312(0.99)  LDD0784  [6]
 LDCM0469  CL76 HCT 116 C312(1.11)  LDD0786  [6]
 LDCM0470  CL77 HCT 116 C312(1.00)  LDD0787  [6]
 LDCM0471  CL78 HCT 116 C312(0.98)  LDD0788  [6]
 LDCM0472  CL79 HCT 116 C312(0.99)  LDD0789  [6]
 LDCM0473  CL8 HCT 116 C312(1.15)  LDD0790  [6]
 LDCM0474  CL80 HCT 116 C312(1.66)  LDD0791  [6]
 LDCM0475  CL81 HCT 116 C312(1.08)  LDD0792  [6]
 LDCM0476  CL82 HCT 116 C312(0.99)  LDD0793  [6]
 LDCM0477  CL83 HCT 116 C312(1.26)  LDD0794  [6]
 LDCM0478  CL84 HCT 116 C312(1.21)  LDD0795  [6]
 LDCM0479  CL85 HCT 116 C312(1.12)  LDD0796  [6]
 LDCM0480  CL86 HCT 116 C312(1.03)  LDD0797  [6]
 LDCM0481  CL87 HCT 116 C312(1.10)  LDD0798  [6]
 LDCM0482  CL88 HCT 116 C312(1.05)  LDD0799  [6]
 LDCM0483  CL89 HCT 116 C312(1.42)  LDD0800  [6]
 LDCM0484  CL9 HCT 116 C312(1.08)  LDD0801  [6]
 LDCM0485  CL90 HCT 116 C312(1.45)  LDD0802  [6]
 LDCM0486  CL91 HCT 116 C312(1.02)  LDD0803  [6]
 LDCM0487  CL92 HCT 116 C312(1.06)  LDD0804  [6]
 LDCM0488  CL93 HCT 116 C312(1.26)  LDD0805  [6]
 LDCM0489  CL94 HCT 116 C312(1.08)  LDD0806  [6]
 LDCM0490  CL95 HCT 116 C312(0.91)  LDD0807  [6]
 LDCM0491  CL96 HCT 116 C312(1.03)  LDD0808  [6]
 LDCM0492  CL97 HCT 116 C312(0.92)  LDD0809  [6]
 LDCM0493  CL98 HCT 116 C312(0.96)  LDD0810  [6]
 LDCM0494  CL99 HCT 116 C312(1.02)  LDD0811  [6]
 LDCM0165  Compound 9 HL-60 N.A.  LDD0420  [11]
 LDCM0495  E2913 HEK-293T C312(1.09)  LDD1698  [12]
 LDCM0625  F8 Ramos C312(0.93)  LDD2187  [13]
 LDCM0572  Fragment10 Ramos C312(0.65)  LDD2189  [13]
 LDCM0573  Fragment11 Ramos C312(0.23)  LDD2190  [13]
 LDCM0574  Fragment12 Ramos C312(0.90)  LDD2191  [13]
 LDCM0575  Fragment13 Ramos C312(1.02)  LDD2192  [13]
 LDCM0576  Fragment14 Ramos C312(0.53)  LDD2193  [13]
 LDCM0579  Fragment20 Ramos C312(0.72)  LDD2194  [13]
 LDCM0580  Fragment21 Ramos C312(0.92)  LDD2195  [13]
 LDCM0582  Fragment23 Ramos C312(0.40)  LDD2196  [13]
 LDCM0578  Fragment27 Ramos C312(0.83)  LDD2197  [13]
 LDCM0586  Fragment28 Ramos C312(1.07)  LDD2198  [13]
 LDCM0588  Fragment30 Ramos C312(1.13)  LDD2199  [13]
 LDCM0589  Fragment31 Ramos C312(0.80)  LDD2200  [13]
 LDCM0590  Fragment32 Ramos C312(0.80)  LDD2201  [13]
 LDCM0468  Fragment33 HCT 116 C312(1.08)  LDD0785  [6]
 LDCM0596  Fragment38 Ramos C312(0.69)  LDD2203  [13]
 LDCM0566  Fragment4 Ramos C312(1.10)  LDD2184  [13]
 LDCM0427  Fragment51 HCT 116 C312(0.72)  LDD0744  [6]
 LDCM0610  Fragment52 Ramos C312(1.02)  LDD2204  [13]
 LDCM0614  Fragment56 Ramos C312(0.97)  LDD2205  [13]
 LDCM0569  Fragment7 Jurkat _(20.00)  LDD1485  [4]
 LDCM0571  Fragment9 Ramos C312(0.84)  LDD2188  [13]
 LDCM0116  HHS-0101 DM93 Y472(0.38)  LDD0264  [5]
 LDCM0117  HHS-0201 DM93 Y472(0.50)  LDD0265  [5]
 LDCM0118  HHS-0301 DM93 Y472(0.07)  LDD0266  [5]
 LDCM0120  HHS-0701 DM93 Y472(0.44)  LDD0268  [5]
 LDCM0022  KB02 HEK-293T C551(0.95); C754(1.16); C312(0.87)  LDD1492  [12]
 LDCM0023  KB03 HEK-293T C551(1.05); C754(1.21); C312(0.91)  LDD1497  [12]
 LDCM0024  KB05 HEK-293T C551(0.93); C754(0.92); C312(0.94)  LDD1502  [12]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein beta/alpha (YWHAB) 14-3-3 family P31946
Leucine zipper putative tumor suppressor 2 (LZTS2) LZTS2 family Q9BRK4
Retinoblastoma-associated protein (RB1) Retinoblastoma protein (RB) family P06400
Retinoblastoma-like protein 1 (RBL1) Retinoblastoma protein (RB) family P28749
DDB1- and CUL4-associated factor 7 (DCAF7) WD repeat DCAF7 family P61962
Keratinocyte proline-rich protein (KPRP) . Q5T749
Tastin (TROAP) . Q12815

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
Investigative
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Kh-cb19 Small molecular drug D00BAJ
Leucettine L41 Small molecular drug D04IMY
Ml315 Small molecular drug D0UI7U
Pmid23642479c17 Small molecular drug D06CXU
Pmid24900699c68 Small molecular drug D0X9PI
Wo2013026806c72 Small molecular drug D00AQR
N-(5-{[(2s)-4-amino-2-(3-chlorophenyl)Butanoyl]Amino}-1h-indazol-3-yl)Benzamide . DB07608
Patented
Click To Hide/Show 43 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Benzimidazole Small molecular drug D03TFJ
Harmine Small molecular drug D00OWF
Pmid28766366-compound-scheme11 Small molecular drug D0X8NN
Pmid28766366-compound-scheme12-1 Small molecular drug D06TIU
Pmid28766366-compound-scheme12-2 Small molecular drug D0PM1B
Pmid28766366-compound-scheme12-3 Small molecular drug D05ZHR
Pmid28766366-compound-scheme12-4 Small molecular drug D0K2BT
Pmid28766366-compound-scheme13indy Small molecular drug D0RG1T
Pmid28766366-compound-scheme14bindy Small molecular drug D04SYJ
Pmid28766366-compound-scheme15-1 Small molecular drug D0A7CE
Pmid28766366-compound-scheme15-2 Small molecular drug D0I8CT
Pmid28766366-compound-scheme15-3 Small molecular drug D0X0ZC
Pmid28766366-compound-scheme16dmat Small molecular drug D02GEJ
Pmid28766366-compound-scheme18 Small molecular drug D0L2XV
Pmid28766366-compound-scheme1wo2011135259 Small molecular drug D0X5MW
Pmid28766366-compound-scheme21left Small molecular drug D02DBH
Pmid28766366-compound-scheme21right Small molecular drug D07BWC
Pmid28766366-compound-scheme23mppderivatives Small molecular drug D0O9WA
Pmid28766366-compound-scheme24-11h-pyrido[4,3-a]Carbazole Small molecular drug D0GV3X
Pmid28766366-compound-scheme24paprotrain Small molecular drug D09UNF
Pmid28766366-compound-scheme25-2 Small molecular drug D09CDR
Pmid28766366-compound-scheme25-3 Small molecular drug D0CC7E
Pmid28766366-compound-scheme25-4 Small molecular drug D0GE4F
Pmid28766366-compound-scheme27leucettamineb Small molecular drug D0NS6I
Pmid28766366-compound-scheme27leucettinel41 Small molecular drug D0Q3VZ
Pmid28766366-compound-scheme27leucettinel41derivatives Small molecular drug D0B0AS
Pmid28766366-compound-scheme4bottom Small molecular drug D0SB1W
Pmid28766366-compound-scheme4upper Small molecular drug D0C0BP
Pmid28766366-compound-scheme5 Small molecular drug D0P7QO
Pmid28766366-compound-scheme6pyrrolo[2,3-d]Pyrimidines Small molecular drug D0YT1S
Pmid28766366-compound-scheme8ncgc-00010037 Small molecular drug D05BVP
Pmid28766366-compound-scheme8ncgc-00185981 Small molecular drug D0UY8K
Pmid28766366-compound-scheme8ncgc-00189310 Small molecular drug D0JQ0Z
Pmid28766366-compound-scheme9eht1610 Small molecular drug D08CUF
Pmid28766366-compound-scheme9eht3356 Small molecular drug D0DT5I
Pmid28766366-compound-scheme9eht5372 Small molecular drug D08DIJ
Pmid28766366-compound-scheme9eht6840 Small molecular drug D0O9BK
Pmid28766366-compound-scheme9eht9851 Small molecular drug D0PJ1W
Tg003 Small molecular drug D06MBI
Pmid28766366-compound-scheme2wo2012/098065bottom . D00TFF
Pmid28766366-compound-scheme2wo2012/098065upper . D0B8IQ
Pmid28766366-compound-scheme7wo2012/098070bottom . D0BP6J
Pmid28766366-compound-scheme7wo2012/098070upper . D05CLL

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 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
3 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.
4 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.
5 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.
6 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.
7 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
8 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
9 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
10 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
11 A Photoaffinity Displacement Assay and Probes to Study the Cyclin-Dependent Kinase Family. Angew Chem Int Ed Engl. 2019 Nov 25;58(48):17322-17327. doi: 10.1002/anie.201906321. Epub 2019 Oct 31.
12 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
13 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