General Information of Target

Target ID LDTP03474
Target Name Ephrin type-A receptor 2 (EPHA2)
Gene Name EPHA2
Gene ID 1969
Synonyms
ECK; Ephrin type-A receptor 2; EC 2.7.10.1; Epithelial cell kinase; Tyrosine-protein kinase receptor ECK
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MELQAARACFALLWGCALAAAAAAQGKEVVLLDFAAAGGELGWLTHPYGKGWDLMQNIMN
DMPIYMYSVCNVMSGDQDNWLRTNWVYRGEAERIFIELKFTVRDCNSFPGGASSCKETFN
LYYAESDLDYGTNFQKRLFTKIDTIAPDEITVSSDFEARHVKLNVEERSVGPLTRKGFYL
AFQDIGACVALLSVRVYYKKCPELLQGLAHFPETIAGSDAPSLATVAGTCVDHAVVPPGG
EEPRMHCAVDGEWLVPIGQCLCQAGYEKVEDACQACSPGFFKFEASESPCLECPEHTLPS
PEGATSCECEEGFFRAPQDPASMPCTRPPSAPHYLTAVGMGAKVELRWTPPQDSGGREDI
VYSVTCEQCWPESGECGPCEASVRYSEPPHGLTRTSVTVSDLEPHMNYTFTVEARNGVSG
LVTSRSFRTASVSINQTEPPKVRLEGRSTTSLSVSWSIPPPQQSRVWKYEVTYRKKGDSN
SYNVRRTEGFSVTLDDLAPDTTYLVQVQALTQEGQGAGSKVHEFQTLSPEGSGNLAVIGG
VAVGVVLLLVLAGVGFFIHRRRKNQRARQSPEDVYFSKSEQLKPLKTYVDPHTYEDPNQA
VLKFTTEIHPSCVTRQKVIGAGEFGEVYKGMLKTSSGKKEVPVAIKTLKAGYTEKQRVDF
LGEAGIMGQFSHHNIIRLEGVISKYKPMMIITEYMENGALDKFLREKDGEFSVLQLVGML
RGIAAGMKYLANMNYVHRDLAARNILVNSNLVCKVSDFGLSRVLEDDPEATYTTSGGKIP
IRWTAPEAISYRKFTSASDVWSFGIVMWEVMTYGERPYWELSNHEVMKAINDGFRLPTPM
DCPSAIYQLMMQCWQQERARRPKFADIVSILDKLIRAPDSLKTLADFDPRVSIRLPSTSG
SEGVPFRTVSEWLESIKMQQYTEHFMAAGYTAIEKVVQMTNDDIKRIGVRLPGHQKRIAY
SLLGLKDQVNTVGIPI
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, Ephrin receptor subfamily
Subcellular location
Cell membrane
Function
Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin-A family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Activated by the ligand ephrin-A1/EFNA1 regulates migration, integrin-mediated adhesion, proliferation and differentiation of cells. Regulates cell adhesion and differentiation through DSG1/desmoglein-1 and inhibition of the ERK1/ERK2 (MAPK3/MAPK1, respectively) signaling pathway. May also participate in UV radiation-induced apoptosis and have a ligand-independent stimulatory effect on chemotactic cell migration. During development, may function in distinctive aspects of pattern formation and subsequently in development of several fetal tissues. Involved for instance in angiogenesis, in early hindbrain development and epithelial proliferation and branching morphogenesis during mammary gland development. Engaged by the ligand ephrin-A5/EFNA5 may regulate lens fiber cells shape and interactions and be important for lens transparency development and maintenance. With ephrin-A2/EFNA2 may play a role in bone remodeling through regulation of osteoclastogenesis and osteoblastogenesis.; (Microbial infection) Acts as a receptor for hepatitis C virus (HCV) in hepatocytes and facilitates its cell entry. Mediates HCV entry by promoting the formation of the CD81-CLDN1 receptor complexes that are essential for HCV entry and by enhancing membrane fusion of cells expressing HCV envelope glycoproteins.; Acts as a receptor for human cytomegalovirus (HCMV) to mediate viral entry and fusion in glioblastoma cells.
TTD ID
T57278
Uniprot ID
P29317
DrugMap ID
TTRJB2G
Ensemble ID
ENST00000358432.8
HGNC ID
HGNC:3386
ChEMBL ID
CHEMBL2068

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA Deletion: p.P460RfsTer33 DBIA    Probe Info 
CCK81 SNV: p.S749N DBIA    Probe Info 
CFPAC1 Insertion: p.P461AfsTer135 DBIA    Probe Info 
COLO792 SNV: p.E825D DBIA    Probe Info 
EFO27 SNV: p.S354N DBIA    Probe Info 
HCT15 SNV: p.Y87C; p.Q715Ter .
HEC1B SNV: p.R561M; p.C842R .
IGROV1 Deletion: p.G240VfsTer153; p.P460RfsTer33 DBIA    Probe Info 
IM95 SNV: p.R561M DBIA    Probe Info 
JURKAT SNV: p.R782H .
KYSE510 SNV: p.H390Y DBIA    Probe Info 
LS123 SNV: p.A209D DBIA    Probe Info 
MCC13 SNV: p.L704F DBIA    Probe Info 
MEWO SNV: p.L836R DBIA    Probe Info 
MFE319 Deletion: p.P460RfsTer33
SNV: p.P896R
DBIA    Probe Info 
RL952 SNV: p.R950W DBIA    Probe Info 
SNU1079 SNV: p.T614P .
WM1552C SNV: p.S579T DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 21 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info 
5.40  LDD0402  [1]
CY-1
 Probe Info 
100.00  LDD0243  [2]
CY4
 Probe Info 
100.00  LDD0244  [2]
N1
 Probe Info 
100.00  LDD0242  [2]
YN-1
 Probe Info 
100.00  LDD0444  [3]
STPyne
 Probe Info 
K162(3.06); K468(0.28); K578(5.74); K583(4.10)  LDD0277  [4]
OPA-S-S-alkyne
 Probe Info 
K475(2.38); K468(3.11); K476(3.45); K162(5.99)  LDD3494  [5]
JZ128-DTB
 Probe Info 
N.A.  LDD0462  [6]
BTD
 Probe Info 
C753(2.51); C612(1.96)  LDD1700  [7]
DBIA
 Probe Info 
C105(1.53); C115(1.53); C753(1.01); C842(0.80)  LDD0531  [8]
ATP probe
 Probe Info 
N.A.  LDD0199  [9]
IA-alkyne
 Probe Info 
C753(0.00); C325(0.00); C612(0.00); C842(0.00)  LDD0162  [10]
ATP probe
 Probe Info 
K778(0.00); K873(0.00)  LDD0035  [11]
NAIA_4
 Probe Info 
C612(0.00); C753(0.00)  LDD2226  [12]
WYneN
 Probe Info 
N.A.  LDD0021  [13]
WYneO
 Probe Info 
C753(0.00); C612(0.00)  LDD0022  [13]
IPM
 Probe Info 
C753(0.00); C612(0.00)  LDD0147  [14]
PF-06672131
 Probe Info 
N.A.  LDD0017  [15]
TFBX
 Probe Info 
N.A.  LDD0148  [14]
Phosphinate-6
 Probe Info 
N.A.  LDD0018  [16]
W1
 Probe Info 
N.A.  LDD0236  [17]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C170
 Probe Info 
9.06  LDD1850  [18]
DFG-out-3
 Probe Info 
15.00  LDD0074  [19]
DFG-out-4
 Probe Info 
5.00  LDD0075  [19]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C612(0.76)  LDD2142  [7]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C612(0.92)  LDD2112  [7]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C612(0.62)  LDD2095  [7]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C612(1.18); C753(1.06)  LDD2117  [7]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C612(1.52)  LDD2152  [7]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C612(1.04); C753(0.90)  LDD2103  [7]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C612(0.59)  LDD2132  [7]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C612(0.58); C753(0.77)  LDD2131  [7]
 LDCM0214  AC1 HCT 116 C105(1.53); C115(1.53); C753(1.01); C842(0.80)  LDD0531  [8]
 LDCM0215  AC10 HCT 116 C105(0.93); C115(0.93); C842(0.53); C853(0.53)  LDD0532  [8]
 LDCM0216  AC100 HCT 116 C105(1.05); C115(0.94)  LDD0533  [8]
 LDCM0217  AC101 HCT 116 C105(0.72); C115(0.65)  LDD0534  [8]
 LDCM0218  AC102 HCT 116 C105(0.78); C115(0.74)  LDD0535  [8]
 LDCM0219  AC103 HCT 116 C105(0.69); C115(0.60)  LDD0536  [8]
 LDCM0220  AC104 HCT 116 C105(0.92); C115(0.85)  LDD0537  [8]
 LDCM0221  AC105 HCT 116 C105(0.76); C115(0.66)  LDD0538  [8]
 LDCM0222  AC106 HCT 116 C105(0.80); C115(0.72)  LDD0539  [8]
 LDCM0223  AC107 HCT 116 C105(0.72); C115(0.58)  LDD0540  [8]
 LDCM0224  AC108 HCT 116 C105(0.71); C115(0.68)  LDD0541  [8]
 LDCM0225  AC109 HCT 116 C105(0.74); C115(0.82)  LDD0542  [8]
 LDCM0226  AC11 HCT 116 C105(0.67); C115(0.67); C842(0.52); C853(0.52)  LDD0543  [8]
 LDCM0227  AC110 HCT 116 C105(0.71); C115(0.66)  LDD0544  [8]
 LDCM0228  AC111 HCT 116 C105(0.75); C115(0.72)  LDD0545  [8]
 LDCM0229  AC112 HCT 116 C105(0.67); C115(0.63)  LDD0546  [8]
 LDCM0230  AC113 HCT 116 C105(0.98); C115(0.98); C753(0.83)  LDD0547  [8]
 LDCM0231  AC114 HCT 116 C105(1.08); C115(0.99); C753(1.19)  LDD0548  [8]
 LDCM0232  AC115 HCT 116 C105(1.04); C115(1.02); C753(0.77)  LDD0549  [8]
 LDCM0233  AC116 HCT 116 C105(1.06); C115(1.00); C753(1.17)  LDD0550  [8]
 LDCM0234  AC117 HCT 116 C105(1.08); C115(1.12); C753(1.17)  LDD0551  [8]
 LDCM0235  AC118 HCT 116 C105(1.19); C115(1.09); C753(1.38)  LDD0552  [8]
 LDCM0236  AC119 HCT 116 C105(1.19); C115(1.15); C753(0.82)  LDD0553  [8]
 LDCM0237  AC12 HCT 116 C105(0.96); C115(0.96); C842(0.60); C853(0.60)  LDD0554  [8]
 LDCM0238  AC120 HCT 116 C105(1.03); C115(0.87); C753(1.59)  LDD0555  [8]
 LDCM0239  AC121 HCT 116 C105(1.16); C115(1.15); C753(1.14)  LDD0556  [8]
 LDCM0240  AC122 HCT 116 C105(1.28); C115(1.07); C753(1.23)  LDD0557  [8]
 LDCM0241  AC123 HCT 116 C105(1.33); C115(1.21); C753(0.91)  LDD0558  [8]
 LDCM0242  AC124 HCT 116 C105(1.26); C115(1.18); C753(1.27)  LDD0559  [8]
 LDCM0243  AC125 HCT 116 C105(1.20); C115(1.03); C753(1.23)  LDD0560  [8]
 LDCM0244  AC126 HCT 116 C105(1.13); C115(1.07); C753(1.01)  LDD0561  [8]
 LDCM0245  AC127 HCT 116 C105(1.35); C115(1.17); C753(1.44)  LDD0562  [8]
 LDCM0246  AC128 HCT 116 C105(1.08); C115(1.08); C842(0.64); C853(0.64)  LDD0563  [8]
 LDCM0247  AC129 HCT 116 C105(1.12); C115(1.12); C842(1.13); C853(1.13)  LDD0564  [8]
 LDCM0249  AC130 HCT 116 C105(0.93); C115(0.93); C842(0.78); C853(0.78)  LDD0566  [8]
 LDCM0250  AC131 HCT 116 C105(1.10); C115(1.10); C842(1.54); C853(1.54)  LDD0567  [8]
 LDCM0251  AC132 HCT 116 C105(1.04); C115(1.04); C842(1.09); C853(1.09)  LDD0568  [8]
 LDCM0252  AC133 HCT 116 C105(1.07); C115(1.07); C842(0.89); C853(0.89)  LDD0569  [8]
 LDCM0253  AC134 HCT 116 C105(0.97); C115(0.97); C842(0.73); C853(0.73)  LDD0570  [8]
 LDCM0254  AC135 HCT 116 C105(1.05); C115(1.05); C842(0.85); C853(0.85)  LDD0571  [8]
 LDCM0255  AC136 HCT 116 C105(0.95); C115(0.95); C842(0.86); C853(0.86)  LDD0572  [8]
 LDCM0256  AC137 HCT 116 C105(0.98); C115(0.98); C842(0.98); C853(0.98)  LDD0573  [8]
 LDCM0257  AC138 HCT 116 C105(0.93); C115(0.93); C842(0.89); C853(0.89)  LDD0574  [8]
 LDCM0258  AC139 HCT 116 C105(0.96); C115(0.96); C842(0.88); C853(0.88)  LDD0575  [8]
 LDCM0259  AC14 HCT 116 C105(0.78); C115(0.78); C842(0.56); C853(0.56)  LDD0576  [8]
 LDCM0260  AC140 HCT 116 C105(0.97); C115(0.97); C842(0.77); C853(0.77)  LDD0577  [8]
 LDCM0261  AC141 HCT 116 C105(1.01); C115(1.01); C842(0.84); C853(0.84)  LDD0578  [8]
 LDCM0262  AC142 HCT 116 C105(1.02); C115(1.02); C842(1.17); C853(1.17)  LDD0579  [8]
 LDCM0263  AC143 HCT 116 C105(1.04); C115(1.04); C612(0.84); C842(0.97)  LDD0580  [8]
 LDCM0264  AC144 HCT 116 C842(0.57); C853(0.57); C115(0.97); C612(0.99)  LDD0581  [8]
 LDCM0265  AC145 HCT 116 C842(0.80); C853(0.80); C115(0.95); C612(0.96)  LDD0582  [8]
 LDCM0266  AC146 HCT 116 C842(0.62); C853(0.62); C105(0.86); C115(0.91)  LDD0583  [8]
 LDCM0267  AC147 HCT 116 C842(0.52); C853(0.52); C115(1.02); C105(1.03)  LDD0584  [8]
 LDCM0268  AC148 HCT 116 C842(0.46); C853(0.46); C115(0.91); C105(0.93)  LDD0585  [8]
 LDCM0269  AC149 HCT 116 C842(0.50); C853(0.50); C105(0.79); C115(0.84)  LDD0586  [8]
 LDCM0270  AC15 HCT 116 C842(0.49); C853(0.49); C105(1.04); C115(1.04)  LDD0587  [8]
 LDCM0271  AC150 HCT 116 C842(0.80); C853(0.80); C105(1.07); C115(1.07)  LDD0588  [8]
 LDCM0272  AC151 HCT 116 C612(0.93); C115(0.96); C105(0.98); C842(1.00)  LDD0589  [8]
 LDCM0273  AC152 HCT 116 C842(0.56); C853(0.56); C105(0.93); C115(0.94)  LDD0590  [8]
 LDCM0274  AC153 HCT 116 C842(0.45); C853(0.45); C105(0.82); C115(0.85)  LDD0591  [8]
 LDCM0621  AC154 HCT 116 C105(1.04); C115(1.06); C612(1.16); C842(0.58)  LDD2158  [8]
 LDCM0622  AC155 HCT 116 C105(1.09); C115(1.11); C612(1.32); C842(0.57)  LDD2159  [8]
 LDCM0623  AC156 HCT 116 C105(1.06); C115(1.12); C612(0.80); C842(1.05)  LDD2160  [8]
 LDCM0624  AC157 HCT 116 C105(1.02); C115(1.02); C612(0.72); C842(1.30)  LDD2161  [8]
 LDCM0276  AC17 HCT 116 C105(1.18); C115(1.18); C842(1.20); C853(1.20)  LDD0593  [8]
 LDCM0277  AC18 HCT 116 C842(0.73); C853(0.73); C105(1.32); C115(1.32)  LDD0594  [8]
 LDCM0278  AC19 HCT 116 C842(0.91); C853(0.91); C105(1.24); C115(1.24)  LDD0595  [8]
 LDCM0279  AC2 HCT 116 C842(0.80); C853(0.80); C753(0.95); C105(1.28)  LDD0596  [8]
 LDCM0280  AC20 HCT 116 C105(0.94); C115(0.94); C842(1.59); C853(1.59)  LDD0597  [8]
 LDCM0281  AC21 HCT 116 C842(1.18); C853(1.18); C105(1.28); C115(1.28)  LDD0598  [8]
 LDCM0282  AC22 HCT 116 C105(0.97); C115(0.97); C842(1.38); C853(1.38)  LDD0599  [8]
 LDCM0283  AC23 HCT 116 C105(0.98); C115(0.98); C842(1.44); C853(1.44)  LDD0600  [8]
 LDCM0284  AC24 HCT 116 C105(1.04); C115(1.04); C842(2.37); C853(2.37)  LDD0601  [8]
 LDCM0285  AC25 HCT 116 C612(0.84); C753(0.87); C115(1.20); C105(1.34)  LDD0602  [8]
 LDCM0286  AC26 HCT 116 C612(0.79); C753(0.91); C105(1.00); C115(1.00)  LDD0603  [8]
 LDCM0287  AC27 HCT 116 C612(0.88); C753(0.92); C115(0.94); C105(0.99)  LDD0604  [8]
 LDCM0288  AC28 HCT 116 C612(0.84); C753(0.84); C115(0.99); C105(1.12)  LDD0605  [8]
 LDCM0289  AC29 HCT 116 C105(0.68); C115(0.75); C753(0.89); C612(1.17)  LDD0606  [8]
 LDCM0290  AC3 HCT 116 C753(0.99); C842(1.00); C853(1.00); C105(1.56)  LDD0607  [8]
 LDCM0291  AC30 HCT 116 C105(0.61); C115(0.70); C753(0.79); C612(1.24)  LDD0608  [8]
 LDCM0292  AC31 HCT 116 C105(0.78); C115(0.79); C612(0.85); C753(1.04)  LDD0609  [8]
 LDCM0293  AC32 HCT 116 C105(0.63); C753(0.66); C115(0.75); C612(0.99)  LDD0610  [8]
 LDCM0294  AC33 HCT 116 C753(0.66); C115(0.97); C105(1.05); C612(1.09)  LDD0611  [8]
 LDCM0295  AC34 HCT 116 C753(0.62); C115(0.90); C105(0.96); C612(1.32)  LDD0612  [8]
 LDCM0296  AC35 HCT 116 C105(1.02); C115(1.02); C842(1.11); C853(1.11)  LDD0613  [8]
 LDCM0297  AC36 HCT 116 C105(0.67); C115(0.67); C753(1.00); C842(1.63)  LDD0614  [8]
 LDCM0298  AC37 HCT 116 C753(0.87); C842(0.89); C853(0.89); C105(0.96)  LDD0615  [8]
 LDCM0299  AC38 HCT 116 C105(0.68); C115(0.68); C753(1.01); C842(1.22)  LDD0616  [8]
 LDCM0300  AC39 HCT 116 C105(0.78); C115(0.78); C842(0.99); C853(0.99)  LDD0617  [8]
 LDCM0301  AC4 HCT 116 C842(0.83); C853(0.83); C753(1.20); C105(1.79)  LDD0618  [8]
 LDCM0302  AC40 HCT 116 C105(0.68); C115(0.68); C842(0.84); C853(0.84)  LDD0619  [8]
 LDCM0303  AC41 HCT 116 C105(0.57); C115(0.57); C753(0.70); C842(1.02)  LDD0620  [8]
 LDCM0304  AC42 HCT 116 C105(0.61); C115(0.61); C753(0.86); C842(1.06)  LDD0621  [8]
 LDCM0305  AC43 HCT 116 C105(0.60); C115(0.60); C753(0.78); C842(0.93)  LDD0622  [8]
 LDCM0306  AC44 HCT 116 C753(0.68); C105(0.87); C115(0.87); C842(1.04)  LDD0623  [8]
 LDCM0307  AC45 HCT 116 C753(0.72); C842(0.87); C853(0.87); C105(0.88)  LDD0624  [8]
 LDCM0308  AC46 HCT 116 C105(0.74); C115(0.74)  LDD0625  [8]
 LDCM0309  AC47 HCT 116 C105(0.89); C115(0.89)  LDD0626  [8]
 LDCM0310  AC48 HCT 116 C105(0.56); C115(0.56)  LDD0627  [8]
 LDCM0311  AC49 HCT 116 C105(0.65); C115(0.65)  LDD0628  [8]
 LDCM0312  AC5 HCT 116 C842(0.78); C853(0.78); C753(1.05); C105(1.68)  LDD0629  [8]
 LDCM0313  AC50 HCT 116 C105(0.70); C115(0.70)  LDD0630  [8]
 LDCM0314  AC51 HCT 116 C105(0.85); C115(0.85)  LDD0631  [8]
 LDCM0315  AC52 HCT 116 C105(0.87); C115(0.87)  LDD0632  [8]
 LDCM0316  AC53 HCT 116 C105(0.73); C115(0.73)  LDD0633  [8]
 LDCM0317  AC54 HCT 116 C105(0.87); C115(0.87)  LDD0634  [8]
 LDCM0318  AC55 HCT 116 C105(0.71); C115(0.71)  LDD0635  [8]
 LDCM0319  AC56 HCT 116 C105(0.53); C115(0.53)  LDD0636  [8]
 LDCM0320  AC57 HCT 116 C842(0.74); C853(0.74); C105(0.89); C115(0.89)  LDD0637  [8]
 LDCM0321  AC58 HCT 116 C105(0.69); C115(0.69); C842(0.77); C853(0.77)  LDD0638  [8]
 LDCM0322  AC59 HCT 116 C842(0.72); C853(0.72); C105(1.10); C115(1.10)  LDD0639  [8]
 LDCM0323  AC6 HCT 116 C842(0.54); C853(0.54); C105(0.80); C115(0.80)  LDD0640  [8]
 LDCM0324  AC60 HCT 116 C842(0.55); C853(0.55); C105(0.78); C115(0.78)  LDD0641  [8]
 LDCM0325  AC61 HCT 116 C105(0.79); C115(0.79); C842(1.03); C853(1.03)  LDD0642  [8]
 LDCM0326  AC62 HCT 116 C842(0.80); C853(0.80); C105(0.99); C115(0.99)  LDD0643  [8]
 LDCM0327  AC63 HCT 116 C842(0.96); C853(0.96); C105(0.99); C115(0.99)  LDD0644  [8]
 LDCM0328  AC64 HCT 116 C842(0.97); C853(0.97); C105(1.01); C115(1.01)  LDD0645  [8]
 LDCM0329  AC65 HCT 116 C105(0.70); C115(0.70); C842(0.73); C853(0.73)  LDD0646  [8]
 LDCM0330  AC66 HCT 116 C842(0.63); C853(0.63); C105(0.74); C115(0.74)  LDD0647  [8]
 LDCM0331  AC67 HCT 116 C842(0.50); C853(0.50); C105(0.58); C115(0.58)  LDD0648  [8]
 LDCM0332  AC68 HCT 116 C842(0.83); C853(0.95); C105(1.06); C115(1.06)  LDD0649  [8]
 LDCM0333  AC69 HCT 116 C853(0.99); C842(1.07); C105(1.19); C115(1.19)  LDD0650  [8]
 LDCM0334  AC7 HCT 116 C842(0.62); C853(0.62); C105(0.86); C115(0.86)  LDD0651  [8]
 LDCM0335  AC70 HCT 116 C853(0.54); C842(0.68); C105(1.09); C115(1.09)  LDD0652  [8]
 LDCM0336  AC71 HCT 116 C105(1.29); C115(1.29); C853(1.32); C753(1.32)  LDD0653  [8]
 LDCM0337  AC72 HCT 116 C853(0.68); C842(0.91); C753(1.20); C105(1.22)  LDD0654  [8]
 LDCM0338  AC73 HCT 116 C853(0.65); C842(0.79); C105(0.97); C115(0.97)  LDD0655  [8]
 LDCM0339  AC74 HCT 116 C853(0.83); C105(0.98); C115(0.98); C842(1.11)  LDD0656  [8]
 LDCM0340  AC75 HCT 116 C853(0.83); C105(0.89); C115(0.89); C842(0.98)  LDD0657  [8]
 LDCM0341  AC76 HCT 116 C853(0.72); C842(0.81); C105(1.31); C115(1.31)  LDD0658  [8]
 LDCM0342  AC77 HCT 116 C842(0.66); C853(0.68); C753(1.10); C105(1.13)  LDD0659  [8]
 LDCM0343  AC78 HCT 116 C105(0.99); C115(0.99); C753(1.08); C842(1.25)  LDD0660  [8]
 LDCM0344  AC79 HCT 116 C853(0.88); C753(1.19); C105(1.25); C115(1.25)  LDD0661  [8]
 LDCM0345  AC8 HCT 116 C842(0.55); C853(0.55); C105(0.85); C115(0.85)  LDD0662  [8]
 LDCM0346  AC80 HCT 116 C853(0.78); C753(1.03); C842(1.05); C105(1.09)  LDD0663  [8]
 LDCM0347  AC81 HCT 116 C842(1.06); C105(1.34); C115(1.34); C753(1.38)  LDD0664  [8]
 LDCM0348  AC82 HCT 116 C853(0.72); C105(0.74); C115(0.74); C842(0.81)  LDD0665  [8]
 LDCM0349  AC83 HCT 116 C842(0.42); C853(0.42); C105(0.94); C115(0.94)  LDD0666  [8]
 LDCM0350  AC84 HCT 116 C753(0.43); C842(0.65); C853(0.65); C105(0.72)  LDD0667  [8]
 LDCM0351  AC85 HCT 116 C753(0.50); C105(0.78); C115(0.78); C842(1.63)  LDD0668  [8]
 LDCM0352  AC86 HCT 116 C753(0.54); C105(0.69); C115(0.69); C842(1.26)  LDD0669  [8]
 LDCM0353  AC87 HCT 116 C753(0.58); C105(0.86); C115(0.86); C842(1.13)  LDD0670  [8]
 LDCM0354  AC88 HCT 116 C753(0.57); C105(0.71); C115(0.71); C842(1.39)  LDD0671  [8]
 LDCM0355  AC89 HCT 116 C753(0.57); C105(0.83); C115(0.83); C842(0.84)  LDD0672  [8]
 LDCM0357  AC90 HCT 116 C753(0.62); C105(0.84); C115(0.84); C842(1.39)  LDD0674  [8]
 LDCM0358  AC91 HCT 116 C842(0.40); C853(0.40); C753(0.73); C105(1.06)  LDD0675  [8]
 LDCM0359  AC92 HCT 116 C842(0.41); C853(0.41); C753(0.46); C105(1.03)  LDD0676  [8]
 LDCM0360  AC93 HCT 116 C753(0.58); C105(0.87); C115(0.87); C842(0.94)  LDD0677  [8]
 LDCM0361  AC94 HCT 116 C753(0.68); C105(1.51); C115(1.51); C842(1.72)  LDD0678  [8]
 LDCM0362  AC95 HCT 116 C753(0.57); C842(0.83); C853(0.83); C105(0.86)  LDD0679  [8]
 LDCM0363  AC96 HCT 116 C753(0.66); C842(0.72); C853(0.72); C105(1.32)  LDD0680  [8]
 LDCM0364  AC97 HCT 116 C842(0.61); C853(0.61); C753(0.67); C105(0.76)  LDD0681  [8]
 LDCM0365  AC98 HCT 116 C115(0.24); C105(0.36)  LDD0682  [8]
 LDCM0366  AC99 HCT 116 C115(0.70); C105(0.81)  LDD0683  [8]
 LDCM0248  AKOS034007472 HCT 116 C105(0.91); C115(0.91); C842(0.70); C853(0.70)  LDD0565  [8]
 LDCM0356  AKOS034007680 HCT 116 C842(0.58); C853(0.58); C105(0.85); C115(0.85)  LDD0673  [8]
 LDCM0275  AKOS034007705 HCT 116 C842(0.33); C853(0.33); C105(0.89); C115(0.89)  LDD0592  [8]
 LDCM0498  BS-3668 MDA-MB-231 C753(0.96)  LDD2091  [7]
 LDCM0630  CCW28-3 231MFP C612(1.46)  LDD2214  [20]
 LDCM0367  CL1 HCT 116 C753(0.93); C105(0.99); C115(0.99); C612(1.29)  LDD0684  [8]
 LDCM0368  CL10 HCT 116 C753(0.72); C842(0.78); C853(0.81); C105(0.83)  LDD0685  [8]
 LDCM0369  CL100 HCT 116 C842(0.82); C853(0.82); C753(0.95); C105(1.50)  LDD0686  [8]
 LDCM0370  CL101 HCT 116 C842(0.50); C853(0.50); C105(1.08); C115(1.08)  LDD0687  [8]
 LDCM0371  CL102 HCT 116 C842(0.91); C853(0.91); C105(0.99); C115(0.99)  LDD0688  [8]
 LDCM0372  CL103 HCT 116 C842(0.69); C853(0.69); C105(1.01); C115(1.01)  LDD0689  [8]
 LDCM0373  CL104 HCT 116 C842(0.77); C853(0.77); C105(0.92); C115(0.92)  LDD0690  [8]
 LDCM0374  CL105 HCT 116 C842(1.04); C853(1.04); C105(1.40); C115(1.40)  LDD0691  [8]
 LDCM0375  CL106 HCT 116 C842(0.94); C853(0.94); C105(1.05); C115(1.05)  LDD0692  [8]
 LDCM0376  CL107 HCT 116 C842(1.02); C853(1.02); C105(1.13); C115(1.13)  LDD0693  [8]
 LDCM0377  CL108 HCT 116 C842(1.08); C853(1.08); C105(1.41); C115(1.41)  LDD0694  [8]
 LDCM0378  CL109 HCT 116 C842(1.01); C853(1.01); C105(1.14); C115(1.14)  LDD0695  [8]
 LDCM0379  CL11 HCT 116 C842(0.57); C853(0.63); C753(0.84); C105(0.90)  LDD0696  [8]
 LDCM0380  CL110 HCT 116 C842(0.72); C853(0.72); C105(0.98); C115(0.98)  LDD0697  [8]
 LDCM0381  CL111 HCT 116 C105(1.15); C115(1.15); C842(1.28); C853(1.28)  LDD0698  [8]
 LDCM0382  CL112 HCT 116 C612(0.90); C115(0.96); C753(1.05); C105(1.06)  LDD0699  [8]
 LDCM0383  CL113 HCT 116 C105(0.57); C115(0.66); C753(0.80); C612(1.27)  LDD0700  [8]
 LDCM0384  CL114 HCT 116 C105(0.51); C115(0.56); C753(0.70); C612(1.37)  LDD0701  [8]
 LDCM0385  CL115 HCT 116 C105(0.50); C115(0.69); C753(0.75); C612(1.03)  LDD0702  [8]
 LDCM0386  CL116 HCT 116 C753(0.64); C105(0.84); C115(0.85); C612(1.44)  LDD0703  [8]
 LDCM0387  CL117 HCT 116 C105(0.67); C115(0.67); C842(0.78); C853(0.78)  LDD0704  [8]
 LDCM0388  CL118 HCT 116 C105(0.77); C115(0.77); C753(0.89); C842(0.91)  LDD0705  [8]
 LDCM0389  CL119 HCT 116 C105(0.66); C115(0.66); C842(0.80); C853(0.80)  LDD0706  [8]
 LDCM0390  CL12 HCT 116 C842(0.60); C853(0.66); C753(0.92); C612(0.98)  LDD0707  [8]
 LDCM0391  CL120 HCT 116 C105(0.54); C115(0.54); C753(0.86); C842(0.88)  LDD0708  [8]
 LDCM0392  CL121 HCT 116 C105(0.96); C115(0.96)  LDD0709  [8]
 LDCM0393  CL122 HCT 116 C105(0.60); C115(0.60)  LDD0710  [8]
 LDCM0394  CL123 HCT 116 C105(0.77); C115(0.77)  LDD0711  [8]
 LDCM0395  CL124 HCT 116 C105(0.74); C115(0.74)  LDD0712  [8]
 LDCM0396  CL125 HCT 116 C842(0.89); C853(0.89); C105(0.90); C115(0.90)  LDD0713  [8]
 LDCM0397  CL126 HCT 116 C105(0.76); C115(0.76); C842(0.90); C853(0.90)  LDD0714  [8]
 LDCM0398  CL127 HCT 116 C105(0.89); C115(0.89); C842(1.23); C853(1.23)  LDD0715  [8]
 LDCM0399  CL128 HCT 116 C842(0.77); C853(0.77); C105(0.94); C115(0.94)  LDD0716  [8]
 LDCM0400  CL13 HCT 116 C105(0.73); C115(0.73); C842(0.75); C853(0.77)  LDD0717  [8]
 LDCM0401  CL14 HCT 116 C842(0.75); C753(0.80); C105(0.80); C115(0.80)  LDD0718  [8]
 LDCM0402  CL15 HCT 116 C612(0.63); C853(0.75); C842(0.77); C105(0.80)  LDD0719  [8]
 LDCM0403  CL16 HCT 116 C105(0.80); C115(0.80); C753(0.91); C842(1.18)  LDD0720  [8]
 LDCM0404  CL17 HCT 116 C105(0.79); C115(0.79); C842(0.81); C853(0.81)  LDD0721  [8]
 LDCM0405  CL18 HCT 116 C105(0.56); C115(0.56); C842(0.94); C853(0.94)  LDD0722  [8]
 LDCM0406  CL19 HCT 116 C105(0.65); C115(0.65); C842(0.73); C853(0.73)  LDD0723  [8]
 LDCM0407  CL2 HCT 116 C842(0.82); C753(0.83); C853(0.89); C612(0.89)  LDD0724  [8]
 LDCM0408  CL20 HCT 116 C842(0.63); C853(0.63); C105(0.74); C115(0.74)  LDD0725  [8]
 LDCM0409  CL21 HCT 116 C842(0.61); C853(0.61); C105(0.68); C115(0.68)  LDD0726  [8]
 LDCM0410  CL22 HCT 116 C842(0.59); C853(0.59); C105(0.67); C115(0.67)  LDD0727  [8]
 LDCM0411  CL23 HCT 116 C842(0.73); C853(0.73); C105(0.78); C115(0.78)  LDD0728  [8]
 LDCM0412  CL24 HCT 116 C842(0.52); C853(0.52); C105(0.79); C115(0.79)  LDD0729  [8]
 LDCM0413  CL25 HCT 116 C105(0.71); C115(0.71); C753(0.83); C842(0.51)  LDD0730  [8]
 LDCM0414  CL26 HCT 116 C105(0.76); C115(0.76); C753(0.79); C842(0.77)  LDD0731  [8]
 LDCM0415  CL27 HCT 116 C105(0.93); C115(0.93); C753(0.99); C842(0.89)  LDD0732  [8]
 LDCM0416  CL28 HCT 116 C105(0.67); C115(0.67); C753(0.93); C842(0.67)  LDD0733  [8]
 LDCM0417  CL29 HCT 116 C105(0.68); C115(0.68); C753(1.02); C842(0.66)  LDD0734  [8]
 LDCM0418  CL3 HCT 116 C105(0.95); C115(0.95); C612(1.27); C753(0.79)  LDD0735  [8]
 LDCM0419  CL30 HCT 116 C105(0.90); C115(0.90); C753(0.91); C842(1.63)  LDD0736  [8]
 LDCM0420  CL31 HCT 116 C105(0.93); C115(0.93); C842(0.86)  LDD0737  [8]
 LDCM0421  CL32 HCT 116 C105(0.52); C115(0.52); C753(0.81); C842(1.10)  LDD0738  [8]
 LDCM0422  CL33 HCT 116 C105(0.60); C115(0.60); C753(0.81); C842(1.34)  LDD0739  [8]
 LDCM0423  CL34 HCT 116 C105(0.62); C115(0.62); C753(1.00); C842(0.55)  LDD0740  [8]
 LDCM0424  CL35 HCT 116 C105(0.75); C115(0.75); C753(1.05); C842(0.82)  LDD0741  [8]
 LDCM0425  CL36 HCT 116 C105(0.78); C115(0.78); C753(0.99); C842(0.71)  LDD0742  [8]
 LDCM0426  CL37 HCT 116 C105(0.76); C115(0.76); C753(1.15); C842(0.80)  LDD0743  [8]
 LDCM0428  CL39 HCT 116 C105(0.74); C115(0.74); C753(0.94); C842(0.68)  LDD0745  [8]
 LDCM0429  CL4 HCT 116 C105(0.96); C115(0.96); C612(1.11); C753(0.91)  LDD0746  [8]
 LDCM0430  CL40 HCT 116 C105(0.78); C115(0.78); C753(0.93); C842(0.58)  LDD0747  [8]
 LDCM0431  CL41 HCT 116 C105(0.69); C115(0.69); C753(0.70); C842(1.10)  LDD0748  [8]
 LDCM0432  CL42 HCT 116 C105(0.60); C115(0.60); C753(1.12); C842(0.75)  LDD0749  [8]
 LDCM0433  CL43 HCT 116 C105(0.57); C115(0.57); C753(0.92); C842(0.91)  LDD0750  [8]
 LDCM0434  CL44 HCT 116 C105(0.64); C115(0.64); C753(1.14); C842(0.85)  LDD0751  [8]
 LDCM0435  CL45 HCT 116 C105(0.63); C115(0.63); C753(1.09); C842(0.76)  LDD0752  [8]
 LDCM0436  CL46 HCT 116 C105(0.75); C115(0.75); C612(0.55); C842(1.26)  LDD0753  [8]
 LDCM0437  CL47 HCT 116 C105(0.79); C115(0.79); C612(0.78); C842(1.23)  LDD0754  [8]
 LDCM0438  CL48 HCT 116 C105(0.75); C115(0.75); C612(0.61); C842(1.88)  LDD0755  [8]
 LDCM0439  CL49 HCT 116 C105(0.85); C115(0.85); C612(0.47); C842(1.19)  LDD0756  [8]
 LDCM0440  CL5 HCT 116 C105(0.92); C115(0.92); C612(0.70); C753(0.98)  LDD0757  [8]
 LDCM0441  CL50 HCT 116 C105(0.77); C115(0.77); C612(0.66); C842(1.06)  LDD0758  [8]
 LDCM0442  CL51 HCT 116 C105(0.87); C115(0.87); C612(0.44); C842(1.22)  LDD0759  [8]
 LDCM0443  CL52 HCT 116 C105(0.86); C115(0.86); C612(0.55); C842(1.24)  LDD0760  [8]
 LDCM0444  CL53 HCT 116 C105(0.62); C115(0.62); C612(1.36); C842(1.17)  LDD0761  [8]
 LDCM0445  CL54 HCT 116 C105(0.66); C115(0.66); C612(0.78); C842(1.32)  LDD0762  [8]
 LDCM0446  CL55 HCT 116 C105(0.68); C115(0.68); C612(1.00); C842(1.34)  LDD0763  [8]
 LDCM0447  CL56 HCT 116 C105(0.87); C115(0.87); C612(1.09); C842(0.97)  LDD0764  [8]
 LDCM0448  CL57 HCT 116 C105(0.82); C115(0.82); C612(0.91); C842(1.21)  LDD0765  [8]
 LDCM0449  CL58 HCT 116 C105(0.72); C115(0.72); C612(0.49); C842(1.36)  LDD0766  [8]
 LDCM0450  CL59 HCT 116 C105(0.94); C115(0.94); C612(0.82); C842(1.10)  LDD0767  [8]
 LDCM0451  CL6 HCT 116 C105(0.74); C115(0.74); C612(0.41); C753(0.76)  LDD0768  [8]
 LDCM0452  CL60 HCT 116 C105(0.82); C115(0.82); C612(0.49); C842(1.34)  LDD0769  [8]
 LDCM0453  CL61 HCT 116 C105(1.83); C115(1.83); C612(0.95); C842(0.64)  LDD0770  [8]
 LDCM0454  CL62 HCT 116 C105(1.74); C115(1.74); C612(0.96); C842(0.66)  LDD0771  [8]
 LDCM0455  CL63 HCT 116 C105(0.92); C115(0.92); C612(1.05); C842(0.44)  LDD0772  [8]
 LDCM0456  CL64 HCT 116 C105(1.44); C115(1.44); C612(1.01); C842(0.47)  LDD0773  [8]
 LDCM0457  CL65 HCT 116 C105(1.54); C115(1.54); C612(1.16); C842(0.53)  LDD0774  [8]
 LDCM0458  CL66 HCT 116 C105(1.33); C115(1.33); C612(1.30); C842(0.38)  LDD0775  [8]
 LDCM0459  CL67 HCT 116 C105(1.47); C115(1.47); C612(1.61); C842(0.42)  LDD0776  [8]
 LDCM0460  CL68 HCT 116 C105(2.95); C115(2.95); C612(1.83); C842(0.70)  LDD0777  [8]
 LDCM0461  CL69 HCT 116 C105(1.18); C115(1.18); C612(1.14); C842(0.49)  LDD0778  [8]
 LDCM0462  CL7 HCT 116 C105(1.07); C115(1.07); C612(0.42); C753(1.06)  LDD0779  [8]
 LDCM0463  CL70 HCT 116 C105(2.29); C115(2.29); C612(1.21); C842(1.07)  LDD0780  [8]
 LDCM0464  CL71 HCT 116 C105(1.58); C115(1.58); C612(1.31); C842(0.59)  LDD0781  [8]
 LDCM0465  CL72 HCT 116 C105(1.74); C115(1.74); C612(1.28); C842(0.90)  LDD0782  [8]
 LDCM0466  CL73 HCT 116 C105(1.54); C115(1.54); C612(1.20); C842(0.53)  LDD0783  [8]
 LDCM0467  CL74 HCT 116 C105(1.31); C115(1.31); C612(1.19); C842(0.34)  LDD0784  [8]
 LDCM0469  CL76 HCT 116 C105(0.81); C115(0.81); C753(1.30); C842(0.77)  LDD0786  [8]
 LDCM0470  CL77 HCT 116 C105(0.83); C115(0.83); C753(1.19); C842(2.18)  LDD0787  [8]
 LDCM0471  CL78 HCT 116 C105(0.80); C115(0.80); C753(0.97); C842(0.72)  LDD0788  [8]
 LDCM0472  CL79 HCT 116 C105(0.94); C115(0.94); C753(1.29); C842(0.51)  LDD0789  [8]
 LDCM0473  CL8 HCT 116 C105(0.73); C115(0.73); C612(1.09); C753(0.46)  LDD0790  [8]
 LDCM0474  CL80 HCT 116 C105(0.82); C115(0.82); C753(1.31); C842(0.96)  LDD0791  [8]
 LDCM0475  CL81 HCT 116 C105(0.97); C115(0.97); C753(1.35); C842(0.62)  LDD0792  [8]
 LDCM0476  CL82 HCT 116 C105(1.10); C115(1.10); C753(1.38); C842(0.49)  LDD0793  [8]
 LDCM0477  CL83 HCT 116 C105(0.91); C115(0.91); C753(1.52); C842(0.48)  LDD0794  [8]
 LDCM0478  CL84 HCT 116 C105(0.78); C115(0.78); C753(1.03); C842(0.60)  LDD0795  [8]
 LDCM0479  CL85 HCT 116 C105(0.97); C115(0.97); C753(1.02); C842(0.64)  LDD0796  [8]
 LDCM0480  CL86 HCT 116 C105(0.94); C115(0.94); C753(1.14); C842(0.87)  LDD0797  [8]
 LDCM0481  CL87 HCT 116 C105(0.88); C115(0.88); C753(1.65); C842(0.57)  LDD0798  [8]
 LDCM0482  CL88 HCT 116 C105(1.06); C115(1.06); C753(1.69); C842(0.51)  LDD0799  [8]
 LDCM0483  CL89 HCT 116 C105(0.75); C115(0.75); C753(1.17); C842(0.61)  LDD0800  [8]
 LDCM0484  CL9 HCT 116 C105(0.89); C115(0.89); C612(0.61); C753(0.86)  LDD0801  [8]
 LDCM0485  CL90 HCT 116 C105(0.81); C115(0.81); C753(1.09); C842(1.02)  LDD0802  [8]
 LDCM0486  CL91 HCT 116 C105(1.03); C115(1.03); C753(1.16); C842(1.03)  LDD0803  [8]
 LDCM0487  CL92 HCT 116 C105(0.88); C115(0.88); C753(1.28); C842(1.16)  LDD0804  [8]
 LDCM0488  CL93 HCT 116 C105(1.36); C115(1.36); C753(1.25); C842(0.82)  LDD0805  [8]
 LDCM0489  CL94 HCT 116 C105(1.65); C115(1.65); C753(0.98); C842(0.72)  LDD0806  [8]
 LDCM0490  CL95 HCT 116 C105(1.05); C115(1.05); C753(1.03); C842(1.01)  LDD0807  [8]
 LDCM0491  CL96 HCT 116 C105(1.11); C115(1.11); C753(1.06); C842(0.95)  LDD0808  [8]
 LDCM0492  CL97 HCT 116 C105(1.08); C115(1.08); C753(0.87); C842(0.89)  LDD0809  [8]
 LDCM0493  CL98 HCT 116 C105(1.13); C115(1.13); C753(0.96); C842(0.67)  LDD0810  [8]
 LDCM0494  CL99 HCT 116 C105(1.19); C115(1.19); C753(1.02); C842(0.76)  LDD0811  [8]
 LDCM0017  DFG-out-2 A431 5.00  LDD0075  [19]
 LDCM0495  E2913 HEK-293T C612(1.10)  LDD1698  [21]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C612(3.73)  LDD1702  [7]
 LDCM0468  Fragment33 HCT 116 C105(2.22); C115(2.22); C612(1.35); C842(0.48)  LDD0785  [8]
 LDCM0427  Fragment51 HCT 116 C105(0.75); C115(0.75); C753(1.21); C842(0.51)  LDD0744  [8]
 LDCM0179  JZ128 PC-3 N.A.  LDD0462  [6]
 LDCM0022  KB02 HEK-293T C612(0.93); C842(0.75); C853(0.75)  LDD1492  [21]
 LDCM0023  KB03 HEK-293T C612(1.00); C842(0.93); C853(0.93)  LDD1497  [21]
 LDCM0024  KB05 Hs 936.T C612(1.25)  LDD3313  [22]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C612(0.97); C753(0.92)  LDD2102  [7]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C612(1.00)  LDD2121  [7]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C612(1.34); C753(1.32)  LDD2090  [7]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C612(0.86)  LDD2092  [7]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C612(1.39); C753(1.33)  LDD2093  [7]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C612(1.29); C753(1.14)  LDD2094  [7]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C753(0.81)  LDD2097  [7]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C612(1.05)  LDD2098  [7]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C612(1.14); C753(1.06)  LDD2099  [7]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C612(1.05)  LDD2100  [7]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C612(1.08); C753(0.43)  LDD2104  [7]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C612(1.10)  LDD2105  [7]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C612(0.71)  LDD2106  [7]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C612(1.01); C753(1.04)  LDD2107  [7]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C612(1.05); C753(0.77)  LDD2109  [7]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C612(1.26); C753(1.30)  LDD2111  [7]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C612(1.15)  LDD2114  [7]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C612(0.70)  LDD2115  [7]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C612(2.19); C753(2.59)  LDD2119  [7]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C612(1.02); C753(1.01)  LDD2123  [7]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C612(0.99)  LDD2125  [7]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C612(1.06); C753(1.07)  LDD2127  [7]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C612(0.59)  LDD2128  [7]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C612(1.40)  LDD2129  [7]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C612(1.39); C753(1.41)  LDD2135  [7]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C612(1.34)  LDD2136  [7]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C753(0.97)  LDD2137  [7]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C753(2.51); C612(1.96)  LDD1700  [7]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C612(1.03); C753(0.91)  LDD2140  [7]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C612(0.85); C753(0.38)  LDD2141  [7]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C753(0.88)  LDD2143  [7]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C612(2.74)  LDD2144  [7]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C612(1.26); C753(1.05)  LDD2146  [7]
 LDCM0553  Nucleophilic fragment 6b MDA-MB-231 C753(2.01)  LDD2147  [7]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C612(0.68); C753(0.46)  LDD2150  [7]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C612(1.98)  LDD2153  [7]
 LDCM0016  Ranjitkar_cp1 A431 15.00  LDD0074  [19]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tyrosine-protein kinase receptor UFO (AXL) Tyr protein kinase family P30530
Ephrin type-A receptor 3 (EPHA3) Tyr protein kinase family P29320
Ephrin type-A receptor 5 (EPHA5) Tyr protein kinase family P54756
Ephrin type-A receptor 6 (EPHA6) Tyr protein kinase family Q9UF33
Ephrin type-A receptor 7 (EPHA7) Tyr protein kinase family Q15375
Focal adhesion kinase 1 (PTK2) Tyr protein kinase family Q05397
Leukocyte tyrosine kinase receptor (LTK) Tyr protein kinase family P29376
Tyrosine-protein phosphatase non-receptor type 11 (PTPN11) Protein-tyrosine phosphatase family Q06124
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock protein HSP 90-beta (HSP90AB1) Heat shock protein 90 family P08238
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Catenin beta-1 (CTNNB1) Beta-catenin family P35222
Ephrin-A1 (EFNA1) Ephrin family P20827
Ephrin-A5 (EFNA5) Ephrin family P52803

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dasatinib Small molecular drug DB01254
Fostamatinib Small molecular drug DB12010
Regorafenib Small molecular drug DB08896
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bt5528 Bicycle toxin conjugate DS5C0K
Car-t Cells Targeting Epha2 CAR T Cell Therapy D05OHY
Phase 1
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ds-8895 Antibody D03YBJ
Medi-547 Antibody D0B8MS
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Medi-543 Vaccine D0W8HP
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amp-pnp Small molecular drug D00ICA
Pmid19788238c66 Small molecular drug D05FXD
Pmid21561767c8h Small molecular drug D02BXJ
Pmid23489211c20 Small molecular drug D0X8BU
Phosphoaminophosphonic Acid-adenylate Ester . DB04395

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 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
3 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
4 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
5 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
6 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
7 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
8 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
9 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.
10 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
11 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
12 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
13 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
14 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
15 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
16 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
17 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.
18 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
19 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.
20 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.
21 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
22 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