Details of the Target

General Information of Target

Target ID LDTP02231
Target Name Tyrosine-protein kinase Yes (YES1)
Gene Name YES1
Gene ID 7525
Synonyms
YES; Tyrosine-protein kinase Yes; EC 2.7.10.2; Proto-oncogene c-Yes; p61-Yes
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MGCIKSKENKSPAIKYRPENTPEPVSTSVSHYGAEPTTVSPCPSSSAKGTAVNFSSLSMT
PFGGSSGVTPFGGASSSFSVVPSSYPAGLTGGVTIFVALYDYEARTTEDLSFKKGERFQI
INNTEGDWWEARSIATGKNGYIPSNYVAPADSIQAEEWYFGKMGRKDAERLLLNPGNQRG
IFLVRESETTKGAYSLSIRDWDEIRGDNVKHYKIRKLDNGGYYITTRAQFDTLQKLVKHY
TEHADGLCHKLTTVCPTVKPQTQGLAKDAWEIPRESLRLEVKLGQGCFGEVWMGTWNGTT
KVAIKTLKPGTMMPEAFLQEAQIMKKLRHDKLVPLYAVVSEEPIYIVTEFMSKGSLLDFL
KEGDGKYLKLPQLVDMAAQIADGMAYIERMNYIHRDLRAANILVGENLVCKIADFGLARL
IEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILQTELVTKGRVPYPGMVNRE
VLEQVERGYRMPCPQGCPESLHELMNLCWKKDPDERPTFEYIQSFLEDYFTATEPQYQPG
ENL
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, SRC subfamily
Subcellular location
Cell membrane
Function
Non-receptor protein tyrosine kinase that is involved in the regulation of cell growth and survival, apoptosis, cell-cell adhesion, cytoskeleton remodeling, and differentiation. Stimulation by receptor tyrosine kinases (RTKs) including EGFR, PDGFR, CSF1R and FGFR leads to recruitment of YES1 to the phosphorylated receptor, and activation and phosphorylation of downstream substrates. Upon EGFR activation, promotes the phosphorylation of PARD3 to favor epithelial tight junction assembly. Participates in the phosphorylation of specific junctional components such as CTNND1 by stimulating the FYN and FER tyrosine kinases at cell-cell contacts. Upon T-cell stimulation by CXCL12, phosphorylates collapsin response mediator protein 2/DPYSL2 and induces T-cell migration. Participates in CD95L/FASLG signaling pathway and mediates AKT-mediated cell migration. Plays a role in cell cycle progression by phosphorylating the cyclin-dependent kinase 4/CDK4 thus regulating the G1 phase. Also involved in G2/M progression and cytokinesis. Catalyzes phosphorylation of organic cation transporter OCT2 which induces its transport activity.
TTD ID
T75570
Uniprot ID
P07947
DrugMap ID
TT0SQ8J
Ensemble ID
ENST00000314574.5
HGNC ID
HGNC:12841
ChEMBL ID
CHEMBL2073

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 17 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		13.59  LDD0402  [1]
BTD
 Probe Info  		C255(0.73)  LDD2089  [2]
AHL-Pu-1
 Probe Info  		C42(2.03)  LDD0169  [3]
Acrolein
 Probe Info  		C255(0.00); C410(0.00)  LDD0222  [4]
DBIA
 Probe Info  		C287(3.70)  LDD0080  [5]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [6]
IA-alkyne
 Probe Info  		C248(0.00); C410(0.00)  LDD0162  [7]
Lodoacetamide azide
 Probe Info  		C410(0.00); C255(0.00)  LDD0037  [6]
JW-RF-010
 Probe Info  		N.A.  LDD0026  [8]
NAIA_4
 Probe Info  		C42(0.00); C287(0.00); C410(0.00)  LDD2226  [9]
TFBX
 Probe Info  		C42(0.00); C410(0.00)  LDD0027  [8]
IPM
 Probe Info  		N.A.  LDD0005  [10]
PF-06672131
 Probe Info  		N.A.  LDD0152  [11]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [12]
W1
 Probe Info  		C255(0.00); C410(0.00)  LDD0236  [13]
AOyne
 Probe Info  		9.90  LDD0443  [14]
NAIA_5
 Probe Info  		C410(0.00); C248(0.00); C255(0.00); C42(0.00)  LDD2223  [9]
PAL-AfBPP Probe
Click To Hide/Show 8 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe11
 Probe Info  		13.65  LDD0472  [15]
FFF probe15
 Probe Info  		12.10  LDD0478  [15]
Dasatinib-CA-3PAP
 Probe Info  		N.A.  LDD0365  [16]
DFG-out-3
 Probe Info  		5.50  LDD0076  [17]
Alk-rapa
 Probe Info  		2.93  LDD0213  [18]
Staurosporine capture compound
 Probe Info  		N.A.  LDD0083  [19]
DA-2
 Probe Info  		N.A.  LDD0070  [20]
STS-1
 Probe Info  		N.A.  LDD0068  [21]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C255(0.44)  LDD2095  [2]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C255(1.03)  LDD2152  [2]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C255(0.98)  LDD2103  [2]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C255(0.56)  LDD2132  [2]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C255(0.82)  LDD2131  [2]
 LDCM0026  4SU-RNA+native RNA HEK-293T C42(2.03)  LDD0169  [3]
 LDCM0214  AC1 HCT 116 C287(1.11)  LDD0531  [5]
 LDCM0215  AC10 HCT 116 C287(1.08)  LDD0532  [5]
 LDCM0216  AC100 HCT 116 C287(1.00)  LDD0533  [5]
 LDCM0217  AC101 HCT 116 C287(1.12)  LDD0534  [5]
 LDCM0218  AC102 HCT 116 C287(1.00)  LDD0535  [5]
 LDCM0219  AC103 HCT 116 C287(1.38)  LDD0536  [5]
 LDCM0220  AC104 HCT 116 C287(1.17)  LDD0537  [5]
 LDCM0221  AC105 HCT 116 C287(1.18)  LDD0538  [5]
 LDCM0222  AC106 HCT 116 C287(1.25)  LDD0539  [5]
 LDCM0223  AC107 HCT 116 C287(1.34)  LDD0540  [5]
 LDCM0224  AC108 HCT 116 C287(1.01)  LDD0541  [5]
 LDCM0225  AC109 HCT 116 C287(0.98)  LDD0542  [5]
 LDCM0226  AC11 HCT 116 C287(1.30)  LDD0543  [5]
 LDCM0227  AC110 HCT 116 C287(0.97)  LDD0544  [5]
 LDCM0228  AC111 HCT 116 C287(1.01)  LDD0545  [5]
 LDCM0229  AC112 HCT 116 C287(1.20)  LDD0546  [5]
 LDCM0230  AC113 HCT 116 C287(1.07)  LDD0547  [5]
 LDCM0231  AC114 HCT 116 C287(1.16)  LDD0548  [5]
 LDCM0232  AC115 HCT 116 C287(1.24)  LDD0549  [5]
 LDCM0233  AC116 HCT 116 C287(1.22)  LDD0550  [5]
 LDCM0234  AC117 HCT 116 C287(1.13)  LDD0551  [5]
 LDCM0235  AC118 HCT 116 C287(1.00)  LDD0552  [5]
 LDCM0236  AC119 HCT 116 C287(1.13)  LDD0553  [5]
 LDCM0237  AC12 HCT 116 C287(1.07)  LDD0554  [5]
 LDCM0238  AC120 HCT 116 C287(1.20)  LDD0555  [5]
 LDCM0239  AC121 HCT 116 C287(1.07)  LDD0556  [5]
 LDCM0240  AC122 HCT 116 C287(1.07)  LDD0557  [5]
 LDCM0241  AC123 HCT 116 C287(1.04)  LDD0558  [5]
 LDCM0242  AC124 HCT 116 C287(0.95)  LDD0559  [5]
 LDCM0243  AC125 HCT 116 C287(1.05)  LDD0560  [5]
 LDCM0244  AC126 HCT 116 C287(1.22)  LDD0561  [5]
 LDCM0245  AC127 HCT 116 C287(1.17)  LDD0562  [5]
 LDCM0246  AC128 HCT 116 C287(1.33)  LDD0563  [5]
 LDCM0247  AC129 HCT 116 C287(0.92)  LDD0564  [5]
 LDCM0249  AC130 HCT 116 C287(1.19)  LDD0566  [5]
 LDCM0250  AC131 HCT 116 C287(1.12)  LDD0567  [5]
 LDCM0251  AC132 HCT 116 C287(1.16)  LDD0568  [5]
 LDCM0252  AC133 HCT 116 C287(1.05)  LDD0569  [5]
 LDCM0253  AC134 HCT 116 C287(1.25)  LDD0570  [5]
 LDCM0254  AC135 HCT 116 C287(1.18)  LDD0571  [5]
 LDCM0255  AC136 HCT 116 C287(1.22)  LDD0572  [5]
 LDCM0256  AC137 HCT 116 C287(1.02)  LDD0573  [5]
 LDCM0257  AC138 HCT 116 C287(1.16)  LDD0574  [5]
 LDCM0258  AC139 HCT 116 C287(1.12)  LDD0575  [5]
 LDCM0259  AC14 HCT 116 C287(1.14)  LDD0576  [5]
 LDCM0260  AC140 HCT 116 C287(1.45)  LDD0577  [5]
 LDCM0261  AC141 HCT 116 C287(1.39)  LDD0578  [5]
 LDCM0262  AC142 HCT 116 C287(1.03)  LDD0579  [5]
 LDCM0263  AC143 HCT 116 C287(1.18)  LDD0580  [5]
 LDCM0264  AC144 HCT 116 C287(1.48)  LDD0581  [5]
 LDCM0265  AC145 HCT 116 C287(1.24)  LDD0582  [5]
 LDCM0266  AC146 HCT 116 C287(1.49)  LDD0583  [5]
 LDCM0267  AC147 HCT 116 C287(1.60)  LDD0584  [5]
 LDCM0268  AC148 HCT 116 C287(2.93)  LDD0585  [5]
 LDCM0269  AC149 HCT 116 C287(2.06)  LDD0586  [5]
 LDCM0270  AC15 HCT 116 C287(1.22)  LDD0587  [5]
 LDCM0271  AC150 HCT 116 C287(1.24)  LDD0588  [5]
 LDCM0272  AC151 HCT 116 C287(1.02)  LDD0589  [5]
 LDCM0273  AC152 HCT 116 C287(1.55)  LDD0590  [5]
 LDCM0274  AC153 HCT 116 C287(2.89)  LDD0591  [5]
 LDCM0621  AC154 HCT 116 C287(1.31)  LDD2158  [5]
 LDCM0622  AC155 HCT 116 C287(1.41)  LDD2159  [5]
 LDCM0623  AC156 HCT 116 C287(1.07)  LDD2160  [5]
 LDCM0624  AC157 HCT 116 C287(1.07)  LDD2161  [5]
 LDCM0276  AC17 HCT 116 C287(1.10)  LDD0593  [5]
 LDCM0277  AC18 HCT 116 C287(1.55)  LDD0594  [5]
 LDCM0278  AC19 HCT 116 C287(1.13)  LDD0595  [5]
 LDCM0279  AC2 HCT 116 C287(1.13)  LDD0596  [5]
 LDCM0280  AC20 HCT 116 C287(1.11)  LDD0597  [5]
 LDCM0281  AC21 HCT 116 C287(1.18)  LDD0598  [5]
 LDCM0282  AC22 HCT 116 C287(1.08)  LDD0599  [5]
 LDCM0283  AC23 HCT 116 C287(1.07)  LDD0600  [5]
 LDCM0284  AC24 HCT 116 C287(0.98)  LDD0601  [5]
 LDCM0285  AC25 HCT 116 C287(1.07)  LDD0602  [5]
 LDCM0286  AC26 HCT 116 C287(1.17)  LDD0603  [5]
 LDCM0287  AC27 HCT 116 C287(1.20)  LDD0604  [5]
 LDCM0288  AC28 HCT 116 C287(1.20)  LDD0605  [5]
 LDCM0289  AC29 HCT 116 C287(1.23)  LDD0606  [5]
 LDCM0290  AC3 HCT 116 C287(1.14)  LDD0607  [5]
 LDCM0291  AC30 HCT 116 C287(1.29)  LDD0608  [5]
 LDCM0292  AC31 HCT 116 C287(1.23)  LDD0609  [5]
 LDCM0293  AC32 HCT 116 C287(1.51)  LDD0610  [5]
 LDCM0294  AC33 HCT 116 C287(1.31)  LDD0611  [5]
 LDCM0295  AC34 HCT 116 C287(1.48)  LDD0612  [5]
 LDCM0296  AC35 HCT 116 C287(0.96)  LDD0613  [5]
 LDCM0297  AC36 HCT 116 C287(1.04)  LDD0614  [5]
 LDCM0298  AC37 HCT 116 C287(0.84)  LDD0615  [5]
 LDCM0299  AC38 HCT 116 C287(0.95)  LDD0616  [5]
 LDCM0300  AC39 HCT 116 C287(1.00)  LDD0617  [5]
 LDCM0301  AC4 HCT 116 C287(1.23)  LDD0618  [5]
 LDCM0302  AC40 HCT 116 C287(1.13)  LDD0619  [5]
 LDCM0303  AC41 HCT 116 C287(1.00)  LDD0620  [5]
 LDCM0304  AC42 HCT 116 C287(1.03)  LDD0621  [5]
 LDCM0305  AC43 HCT 116 C287(1.03)  LDD0622  [5]
 LDCM0306  AC44 HCT 116 C287(1.08)  LDD0623  [5]
 LDCM0307  AC45 HCT 116 C287(1.33)  LDD0624  [5]
 LDCM0308  AC46 HCT 116 C287(1.07)  LDD0625  [5]
 LDCM0309  AC47 HCT 116 C287(1.07)  LDD0626  [5]
 LDCM0310  AC48 HCT 116 C287(1.07)  LDD0627  [5]
 LDCM0311  AC49 HCT 116 C287(1.73)  LDD0628  [5]
 LDCM0312  AC5 HCT 116 C287(1.33)  LDD0629  [5]
 LDCM0313  AC50 HCT 116 C287(1.61)  LDD0630  [5]
 LDCM0314  AC51 HCT 116 C287(0.89)  LDD0631  [5]
 LDCM0315  AC52 HCT 116 C287(1.02)  LDD0632  [5]
 LDCM0316  AC53 HCT 116 C287(1.19)  LDD0633  [5]
 LDCM0317  AC54 HCT 116 C287(1.30)  LDD0634  [5]
 LDCM0318  AC55 HCT 116 C287(1.49)  LDD0635  [5]
 LDCM0319  AC56 HCT 116 C287(1.91)  LDD0636  [5]
 LDCM0320  AC57 HCT 116 C287(1.27)  LDD0637  [5]
 LDCM0321  AC58 HCT 116 C287(1.49)  LDD0638  [5]
 LDCM0322  AC59 HCT 116 C287(1.56)  LDD0639  [5]
 LDCM0323  AC6 HCT 116 C287(1.20)  LDD0640  [5]
 LDCM0324  AC60 HCT 116 C287(1.43)  LDD0641  [5]
 LDCM0325  AC61 HCT 116 C287(1.31)  LDD0642  [5]
 LDCM0326  AC62 HCT 116 C287(1.67)  LDD0643  [5]
 LDCM0327  AC63 HCT 116 C287(1.42)  LDD0644  [5]
 LDCM0328  AC64 HCT 116 C287(1.90)  LDD0645  [5]
 LDCM0329  AC65 HCT 116 C287(1.68)  LDD0646  [5]
 LDCM0330  AC66 HCT 116 C287(1.69)  LDD0647  [5]
 LDCM0331  AC67 HCT 116 C287(2.05)  LDD0648  [5]
 LDCM0332  AC68 HCT 116 C287(1.20)  LDD0649  [5]
 LDCM0333  AC69 HCT 116 C287(1.19)  LDD0650  [5]
 LDCM0334  AC7 HCT 116 C287(1.07)  LDD0651  [5]
 LDCM0335  AC70 HCT 116 C287(1.51)  LDD0652  [5]
 LDCM0336  AC71 HCT 116 C287(1.11)  LDD0653  [5]
 LDCM0337  AC72 HCT 116 C287(1.26)  LDD0654  [5]
 LDCM0338  AC73 HCT 116 C287(2.09)  LDD0655  [5]
 LDCM0339  AC74 HCT 116 C287(1.81)  LDD0656  [5]
 LDCM0340  AC75 HCT 116 C287(2.12)  LDD0657  [5]
 LDCM0341  AC76 HCT 116 C287(1.43)  LDD0658  [5]
 LDCM0342  AC77 HCT 116 C287(1.46)  LDD0659  [5]
 LDCM0343  AC78 HCT 116 C287(1.11)  LDD0660  [5]
 LDCM0344  AC79 HCT 116 C287(1.30)  LDD0661  [5]
 LDCM0345  AC8 HCT 116 C287(1.24)  LDD0662  [5]
 LDCM0346  AC80 HCT 116 C287(1.42)  LDD0663  [5]
 LDCM0347  AC81 HCT 116 C287(1.12)  LDD0664  [5]
 LDCM0348  AC82 HCT 116 C287(2.03)  LDD0665  [5]
 LDCM0349  AC83 HCT 116 C287(1.65)  LDD0666  [5]
 LDCM0350  AC84 HCT 116 C287(1.49)  LDD0667  [5]
 LDCM0351  AC85 HCT 116 C287(1.17)  LDD0668  [5]
 LDCM0352  AC86 HCT 116 C287(1.06)  LDD0669  [5]
 LDCM0353  AC87 HCT 116 C287(1.08)  LDD0670  [5]
 LDCM0354  AC88 HCT 116 C287(1.07)  LDD0671  [5]
 LDCM0355  AC89 HCT 116 C287(1.25)  LDD0672  [5]
 LDCM0357  AC90 HCT 116 C287(0.93)  LDD0674  [5]
 LDCM0358  AC91 HCT 116 C287(1.58)  LDD0675  [5]
 LDCM0359  AC92 HCT 116 C287(1.46)  LDD0676  [5]
 LDCM0360  AC93 HCT 116 C287(1.10)  LDD0677  [5]
 LDCM0361  AC94 HCT 116 C287(1.10)  LDD0678  [5]
 LDCM0362  AC95 HCT 116 C287(1.04)  LDD0679  [5]
 LDCM0363  AC96 HCT 116 C287(1.20)  LDD0680  [5]
 LDCM0364  AC97 HCT 116 C287(1.36)  LDD0681  [5]
 LDCM0365  AC98 HCT 116 C287(1.71)  LDD0682  [5]
 LDCM0366  AC99 HCT 116 C287(0.97)  LDD0683  [5]
 LDCM0520  AKOS000195272 MDA-MB-231 C255(0.71)  LDD2113  [2]
 LDCM0248  AKOS034007472 HCT 116 C287(1.07)  LDD0565  [5]
 LDCM0356  AKOS034007680 HCT 116 C287(1.14)  LDD0673  [5]
 LDCM0275  AKOS034007705 HCT 116 C287(1.86)  LDD0592  [5]
 LDCM0156  Aniline NCI-H1299 12.69  LDD0403  [1]
 LDCM0020  ARS-1620 HCC44 C287(1.09)  LDD2171  [5]
 LDCM0498  BS-3668 MDA-MB-231 C255(0.56)  LDD2091  [2]
 LDCM0630  CCW28-3 231MFP C42(1.14)  LDD2214  [22]
 LDCM0108  Chloroacetamide HeLa C255(0.00); C410(0.00)  LDD0222  [4]
 LDCM0632  CL-Sc Hep-G2 C287(1.63); C410(0.95); C42(0.59)  LDD2227  [9]
 LDCM0367  CL1 HCT 116 C287(0.89)  LDD0684  [5]
 LDCM0368  CL10 HCT 116 C287(1.23)  LDD0685  [5]
 LDCM0369  CL100 HCT 116 C287(1.19)  LDD0686  [5]
 LDCM0370  CL101 HCT 116 C287(1.18)  LDD0687  [5]
 LDCM0371  CL102 HCT 116 C287(1.01)  LDD0688  [5]
 LDCM0372  CL103 HCT 116 C287(0.99)  LDD0689  [5]
 LDCM0373  CL104 HCT 116 C287(1.11)  LDD0690  [5]
 LDCM0374  CL105 HCT 116 C287(1.26)  LDD0691  [5]
 LDCM0375  CL106 HCT 116 C287(1.52)  LDD0692  [5]
 LDCM0376  CL107 HCT 116 C287(1.59)  LDD0693  [5]
 LDCM0377  CL108 HCT 116 C287(1.59)  LDD0694  [5]
 LDCM0378  CL109 HCT 116 C287(1.12)  LDD0695  [5]
 LDCM0379  CL11 HCT 116 C287(1.36)  LDD0696  [5]
 LDCM0380  CL110 HCT 116 C287(1.22)  LDD0697  [5]
 LDCM0381  CL111 HCT 116 C287(1.19)  LDD0698  [5]
 LDCM0382  CL112 HCT 116 C287(1.02)  LDD0699  [5]
 LDCM0383  CL113 HCT 116 C287(1.38)  LDD0700  [5]
 LDCM0384  CL114 HCT 116 C287(1.14)  LDD0701  [5]
 LDCM0385  CL115 HCT 116 C287(1.20)  LDD0702  [5]
 LDCM0386  CL116 HCT 116 C287(1.23)  LDD0703  [5]
 LDCM0387  CL117 HCT 116 C287(1.57)  LDD0704  [5]
 LDCM0388  CL118 HCT 116 C287(1.05)  LDD0705  [5]
 LDCM0389  CL119 HCT 116 C287(1.11)  LDD0706  [5]
 LDCM0390  CL12 HCT 116 C287(1.46)  LDD0707  [5]
 LDCM0391  CL120 HCT 116 C287(0.98)  LDD0708  [5]
 LDCM0392  CL121 HCT 116 C287(0.74)  LDD0709  [5]
 LDCM0393  CL122 HCT 116 C287(1.11)  LDD0710  [5]
 LDCM0394  CL123 HCT 116 C287(1.27)  LDD0711  [5]
 LDCM0395  CL124 HCT 116 C287(1.46)  LDD0712  [5]
 LDCM0396  CL125 HCT 116 C287(1.13)  LDD0713  [5]
 LDCM0397  CL126 HCT 116 C287(11.03)  LDD0714  [5]
 LDCM0398  CL127 HCT 116 C287(1.17)  LDD0715  [5]
 LDCM0399  CL128 HCT 116 C287(1.34)  LDD0716  [5]
 LDCM0400  CL13 HCT 116 C287(1.18)  LDD0717  [5]
 LDCM0401  CL14 HCT 116 C287(1.04)  LDD0718  [5]
 LDCM0402  CL15 HCT 116 C287(1.12)  LDD0719  [5]
 LDCM0403  CL16 HCT 116 C287(0.90)  LDD0720  [5]
 LDCM0404  CL17 HCT 116 C287(0.90)  LDD0721  [5]
 LDCM0405  CL18 HCT 116 C287(1.04)  LDD0722  [5]
 LDCM0406  CL19 HCT 116 C287(1.03)  LDD0723  [5]
 LDCM0407  CL2 HCT 116 C287(0.98)  LDD0724  [5]
 LDCM0408  CL20 HCT 116 C287(1.16)  LDD0725  [5]
 LDCM0409  CL21 HCT 116 C287(1.28)  LDD0726  [5]
 LDCM0410  CL22 HCT 116 C287(1.89)  LDD0727  [5]
 LDCM0411  CL23 HCT 116 C287(1.12)  LDD0728  [5]
 LDCM0412  CL24 HCT 116 C287(1.35)  LDD0729  [5]
 LDCM0413  CL25 HCT 116 C287(1.21)  LDD0730  [5]
 LDCM0414  CL26 HCT 116 C287(1.04)  LDD0731  [5]
 LDCM0415  CL27 HCT 116 C287(1.02)  LDD0732  [5]
 LDCM0416  CL28 HCT 116 C287(1.07)  LDD0733  [5]
 LDCM0417  CL29 HCT 116 C287(1.19)  LDD0734  [5]
 LDCM0418  CL3 HCT 116 C287(0.97)  LDD0735  [5]
 LDCM0419  CL30 HCT 116 C287(1.02)  LDD0736  [5]
 LDCM0420  CL31 HCT 116 C287(1.04)  LDD0737  [5]
 LDCM0421  CL32 HCT 116 C287(1.10)  LDD0738  [5]
 LDCM0422  CL33 HCT 116 C287(1.03)  LDD0739  [5]
 LDCM0423  CL34 HCT 116 C287(1.38)  LDD0740  [5]
 LDCM0424  CL35 HCT 116 C287(1.18)  LDD0741  [5]
 LDCM0425  CL36 HCT 116 C287(1.20)  LDD0742  [5]
 LDCM0426  CL37 HCT 116 C287(1.35)  LDD0743  [5]
 LDCM0428  CL39 HCT 116 C287(1.21)  LDD0745  [5]
 LDCM0429  CL4 HCT 116 C287(0.94)  LDD0746  [5]
 LDCM0430  CL40 HCT 116 C287(1.19)  LDD0747  [5]
 LDCM0431  CL41 HCT 116 C287(1.05)  LDD0748  [5]
 LDCM0432  CL42 HCT 116 C287(1.66)  LDD0749  [5]
 LDCM0433  CL43 HCT 116 C287(1.38)  LDD0750  [5]
 LDCM0434  CL44 HCT 116 C287(1.25)  LDD0751  [5]
 LDCM0435  CL45 HCT 116 C287(1.28)  LDD0752  [5]
 LDCM0436  CL46 HCT 116 C287(0.91)  LDD0753  [5]
 LDCM0437  CL47 HCT 116 C287(0.96)  LDD0754  [5]
 LDCM0438  CL48 HCT 116 C287(0.91)  LDD0755  [5]
 LDCM0439  CL49 HCT 116 C287(0.91)  LDD0756  [5]
 LDCM0440  CL5 HCT 116 C287(1.00)  LDD0757  [5]
 LDCM0441  CL50 HCT 116 C287(0.94)  LDD0758  [5]
 LDCM0442  CL51 HCT 116 C287(0.85)  LDD0759  [5]
 LDCM0443  CL52 HCT 116 C287(0.92)  LDD0760  [5]
 LDCM0444  CL53 HCT 116 C287(0.90)  LDD0761  [5]
 LDCM0445  CL54 HCT 116 C287(0.89)  LDD0762  [5]
 LDCM0446  CL55 HCT 116 C287(0.87)  LDD0763  [5]
 LDCM0447  CL56 HCT 116 C287(0.90)  LDD0764  [5]
 LDCM0448  CL57 HCT 116 C287(0.86)  LDD0765  [5]
 LDCM0449  CL58 HCT 116 C287(0.97)  LDD0766  [5]
 LDCM0450  CL59 HCT 116 C287(0.95)  LDD0767  [5]
 LDCM0451  CL6 HCT 116 C287(1.04)  LDD0768  [5]
 LDCM0452  CL60 HCT 116 C287(1.02)  LDD0769  [5]
 LDCM0453  CL61 HCT 116 C287(1.13)  LDD0770  [5]
 LDCM0454  CL62 HCT 116 C287(1.05)  LDD0771  [5]
 LDCM0455  CL63 HCT 116 C287(1.13)  LDD0772  [5]
 LDCM0456  CL64 HCT 116 C287(1.32)  LDD0773  [5]
 LDCM0457  CL65 HCT 116 C287(1.18)  LDD0774  [5]
 LDCM0458  CL66 HCT 116 C287(1.55)  LDD0775  [5]
 LDCM0459  CL67 HCT 116 C287(1.39)  LDD0776  [5]
 LDCM0460  CL68 HCT 116 C287(1.25)  LDD0777  [5]
 LDCM0461  CL69 HCT 116 C287(1.10)  LDD0778  [5]
 LDCM0462  CL7 HCT 116 C287(1.21)  LDD0779  [5]
 LDCM0463  CL70 HCT 116 C287(1.19)  LDD0780  [5]
 LDCM0464  CL71 HCT 116 C287(1.29)  LDD0781  [5]
 LDCM0465  CL72 HCT 116 C287(1.12)  LDD0782  [5]
 LDCM0466  CL73 HCT 116 C287(1.26)  LDD0783  [5]
 LDCM0467  CL74 HCT 116 C287(1.14)  LDD0784  [5]
 LDCM0469  CL76 HCT 116 C287(1.07)  LDD0786  [5]
 LDCM0470  CL77 HCT 116 C287(1.00)  LDD0787  [5]
 LDCM0471  CL78 HCT 116 C287(1.17)  LDD0788  [5]
 LDCM0472  CL79 HCT 116 C287(1.36)  LDD0789  [5]
 LDCM0473  CL8 HCT 116 C287(1.35)  LDD0790  [5]
 LDCM0474  CL80 HCT 116 C287(1.04)  LDD0791  [5]
 LDCM0475  CL81 HCT 116 C287(1.16)  LDD0792  [5]
 LDCM0476  CL82 HCT 116 C287(1.57)  LDD0793  [5]
 LDCM0477  CL83 HCT 116 C287(1.66)  LDD0794  [5]
 LDCM0478  CL84 HCT 116 C287(1.94)  LDD0795  [5]
 LDCM0479  CL85 HCT 116 C287(1.19)  LDD0796  [5]
 LDCM0480  CL86 HCT 116 C287(1.10)  LDD0797  [5]
 LDCM0481  CL87 HCT 116 C287(1.18)  LDD0798  [5]
 LDCM0482  CL88 HCT 116 C287(1.53)  LDD0799  [5]
 LDCM0483  CL89 HCT 116 C287(2.20)  LDD0800  [5]
 LDCM0484  CL9 HCT 116 C287(1.10)  LDD0801  [5]
 LDCM0485  CL90 HCT 116 C287(0.92)  LDD0802  [5]
 LDCM0486  CL91 HCT 116 C287(1.11)  LDD0803  [5]
 LDCM0487  CL92 HCT 116 C287(1.04)  LDD0804  [5]
 LDCM0488  CL93 HCT 116 C287(1.02)  LDD0805  [5]
 LDCM0489  CL94 HCT 116 C287(1.17)  LDD0806  [5]
 LDCM0490  CL95 HCT 116 C287(1.19)  LDD0807  [5]
 LDCM0491  CL96 HCT 116 C287(1.01)  LDD0808  [5]
 LDCM0492  CL97 HCT 116 C287(1.02)  LDD0809  [5]
 LDCM0493  CL98 HCT 116 C287(1.22)  LDD0810  [5]
 LDCM0494  CL99 HCT 116 C287(1.16)  LDD0811  [5]
 LDCM0097  Dasatinib K562 N.A.  LDD0365  [16]
 LDCM0495  E2913 HEK-293T C287(1.33); C255(1.27); C410(1.03); C508(1.08)  LDD1698  [23]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C42(4.82)  LDD1702  [2]
 LDCM0468  Fragment33 HCT 116 C287(1.20)  LDD0785  [5]
 LDCM0427  Fragment51 HCT 116 C287(1.41)  LDD0744  [5]
 LDCM0022  KB02 HCT 116 C287(3.70)  LDD0080  [5]
 LDCM0023  KB03 HCT 116 C287(1.41)  LDD0081  [5]
 LDCM0024  KB05 HCT 116 C287(6.97)  LDD0082  [5]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C255(0.95)  LDD2102  [2]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C255(0.46)  LDD2121  [2]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C255(0.73)  LDD2089  [2]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C255(1.18)  LDD2090  [2]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C255(0.83)  LDD2092  [2]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C255(0.94)  LDD2094  [2]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C255(0.88)  LDD2098  [2]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C255(0.88)  LDD2099  [2]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C255(0.74)  LDD2100  [2]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C255(1.22)  LDD2105  [2]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C255(0.57); C410(0.90)  LDD2106  [2]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C255(0.83)  LDD2107  [2]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C255(0.65)  LDD2108  [2]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C255(0.67)  LDD2109  [2]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C255(0.77)  LDD2111  [2]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C255(0.65)  LDD2114  [2]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C255(0.62)  LDD2125  [2]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C255(0.80)  LDD2127  [2]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C255(0.79)  LDD2128  [2]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C255(1.06)  LDD2129  [2]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C255(0.92)  LDD2136  [2]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C255(0.53)  LDD2140  [2]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C255(0.43)  LDD2141  [2]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C255(2.94); C410(0.85)  LDD2144  [2]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C255(0.76)  LDD2146  [2]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C255(2.01)  LDD2153  [2]
 LDCM0627  NUDT7-COV-1 HEK-293T C287(1.28)  LDD2206  [24]
 LDCM0628  OTUB2-COV-1 HEK-293T C287(1.31)  LDD2207  [24]
 LDCM0016  Ranjitkar_cp1 A431 5.50  LDD0076  [17]
 LDCM0090  Rapamycin JHH-7 2.93  LDD0213  [18]
 LDCM0019  Staurosporine Hep-G2 N.A.  LDD0083  [19]
 LDCM0021  THZ1 HCT 116 C287(1.09)  LDD2173  [5]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 12 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Probable E3 ubiquitin-protein ligase DTX3 (DTX3) Deltex family Q8N9I9
NIF3-like protein 1 (NIF3L1) GTP cyclohydrolase I type 2/NIF3 family Q9GZT8
Polyunsaturated fatty acid 5-lipoxygenase (ALOX5) Lipoxygenase family P09917
Hepatocyte growth factor receptor (MET) Tyr protein kinase family P08581
Mast/stem cell growth factor receptor Kit (KIT) Tyr protein kinase family P10721
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Focal adhesion kinase 1 (PTK2) Tyr protein kinase family Q05397
TNF receptor-associated factor 2 (TRAF2) TNF receptor-associated factor family Q12933
TNF receptor-associated factor 6 (TRAF6) TNF receptor-associated factor family Q9Y4K3
Disintegrin and metalloproteinase domain-containing protein 10 (ADAM10) . O14672
E3 ubiquitin-protein ligase CBL-B (CBLB) . Q13191
E3 ubiquitin-protein ligase CBL-C (CBLC) . Q9ULV8
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Hsp90 co-chaperone Cdc37 (CDC37) CDC37 family Q16543
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Transcription factor
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Zinc finger protein Aiolos (IKZF3) Ikaros C2H2-type zinc-finger protein family Q9UKT9
Zinc finger protein 438 (ZNF438) Krueppel C2H2-type zinc-finger protein family Q7Z4V0
Androgen receptor (AR) Nuclear hormone receptor family P10275
THAP domain-containing protein 1 (THAP1) THAP1 family Q9NVV9
Zinc finger C2HC domain-containing protein 1A (ZC2HC1A) ZC2HC1 family Q96GY0
Oligodendrocyte transcription factor 1 (OLIG1) . Q8TAK6
Zinc finger and BTB domain-containing protein 8A (ZBTB8A) . Q96BR9
Other
Click To Hide/Show 32 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Angiomotin-like protein 2 (AMOTL2) Angiomotin family Q9Y2J4
Breast cancer anti-estrogen resistance protein 1 (BCAR1) CAS family P56945
Crk-like protein (CRKL) CRK family P46109
Cysteine-rich tail protein 1 (CYSRT1) CYSRT1 family A8MQ03
DNA damage-inducible transcript 4-like protein (DDIT4L) DDIT4 family Q96D03
Docking protein 2 (DOK2) DOK family O60496
Dynein regulatory complex subunit 4 (GAS8) DRC4 family O95995
Endophilin-B2 (SH3GLB2) Endophilin family Q9NR46
RNA-binding protein FXR2 (FXR2) FMR1 family P51116
FUN14 domain-containing protein 1 (FUNDC1) FUN14 family Q8IVP5
GRB2-associated-binding protein 1 (GAB1) GAB family Q13480
Desmin (DES) Intermediate filament family P17661
Glial fibrillary acidic protein (GFAP) Intermediate filament family P14136
Janus kinase and microtubule-interacting protein 1 (JAKMIP1) JAKMIP family Q96N16
Protein lin-7 homolog C (LIN7C) Lin-7 family Q9NUP9
Mediator of RNA polymerase II transcription subunit 28 (MED28) Mediator complex subunit 28 family Q9H204
Periaxin (PRX) Periaxin family Q9BXM0
Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) PI3K p85 subunit family Q92569
Splicing factor 3A subunit 2 (SF3A2) SF3A2 family Q15428
Charged multivesicular body protein 1a (CHMP1A) SNF7 family Q9HD42
Centrosomal protein CEP57L1 (CEP57L1) Translokin family Q8IYX8
Arf-GAP with SH3 domain, ANK repeat and PH domain-containing protein 1 (ASAP1) . Q9ULH1
CUB domain-containing protein 1 (CDCP1) . Q9H5V8
PRKCA-binding protein (PICK1) . Q9NRD5
Rho guanine nucleotide exchange factor 5 (ARHGEF5) . Q12774
Signal-transducing adaptor protein 2 (STAP2) . Q9UGK3
Single-stranded DNA-binding protein 3 (SSBP3) . Q9BWW4
Suppressor of cytokine signaling 2 (SOCS2) . O14508
Suppressor of cytokine signaling 3 (SOCS3) . O14543
Suppressor of cytokine signaling 7 (SOCS7) . O14512
Testis-specific protein 10-interacting protein (TSGA10IP) . Q3SY00
Uncharacterized protein C1orf94 (C1orf94) . Q6P1W5

The Drug(s) Related To This Target

Approved
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dasatinib Small molecular drug DB01254
Fostamatinib Small molecular drug DB12010
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jnj-26483327 . D0U3XL
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tg-100435 Small molecular drug D0H1OK

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 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 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.
5 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.
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 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
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 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 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
11 Site-Specific Activity-Based Protein Profiling Using Phosphonate Handles. Mol Cell Proteomics. 2023 Jan;22(1):100455. doi: 10.1016/j.mcpro.2022.100455. Epub 2022 Nov 24.
Mass spectrometry data entry: PXD036569
12 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
13 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.
14 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
15 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
16 Streamlined Target Deconvolution Approach Utilizing a Single Photoreactive Chloroalkane Capture Tag. ACS Chem Biol. 2021 Feb 19;16(2):404-413. doi: 10.1021/acschembio.0c00987. Epub 2021 Feb 5.
17 Affinity-based probes based on type II kinase inhibitors. J Am Chem Soc. 2012 Nov 21;134(46):19017-25. doi: 10.1021/ja306035v. Epub 2012 Nov 6.
18 Rapamycin targets STAT3 and impacts c-Myc to suppress tumor growth. Cell Chem Biol. 2022 Mar 17;29(3):373-385.e6. doi: 10.1016/j.chembiol.2021.10.006. Epub 2021 Oct 26.
19 Comprehensive identification of staurosporine-binding kinases in the hepatocyte cell line HepG2 using Capture Compound Mass Spectrometry (CCMS). J Proteome Res. 2010 Feb 5;9(2):806-17. doi: 10.1021/pr9007333.
20 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
21 Proteome profiling reveals potential cellular targets of staurosporine using a clickable cell-permeable probe. Chem Commun (Camb). 2011 Oct 28;47(40):11306-8. doi: 10.1039/c1cc14824a. Epub 2011 Sep 16.
22 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
23 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
24 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.