Details of the Target

General Information of Target

Target ID LDTP03387
Target Name Mitogen-activated protein kinase 3 (MAPK3)
Gene Name MAPK3
Gene ID 5595
Synonyms
ERK1; PRKM3; Mitogen-activated protein kinase 3; MAP kinase 3; MAPK 3; EC 2.7.11.24; ERT2; Extracellular signal-regulated kinase 1; ERK-1; Insulin-stimulated MAP2 kinase; MAP kinase isoform p44; p44-MAPK; Microtubule-associated protein 2 kinase; p44-ERK1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAAAAAQGGGGGEPRRTEGVGPGVPGEVEMVKGQPFDVGPRYTQLQYIGEGAYGMVSSAY
DHVRKTRVAIKKISPFEHQTYCQRTLREIQILLRFRHENVIGIRDILRASTLEAMRDVYI
VQDLMETDLYKLLKSQQLSNDHICYFLYQILRGLKYIHSANVLHRDLKPSNLLINTTCDL
KICDFGLARIADPEHDHTGFLTEYVATRWYRAPEIMLNSKGYTKSIDIWSVGCILAEMLS
NRPIFPGKHYLDQLNHILGILGSPSQEDLNCIINMKARNYLQSLPSKTKVAWAKLFPKSD
SKALDLLDRMLTFNPNKRITVEEALAHPYLEQYYDPTDEPVAEEPFTFAMELDDLPKERL
KELIFQETARFQPGVLEAP
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, CMGC Ser/Thr protein kinase family, MAP kinase subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine kinase which acts as an essential component of the MAP kinase signal transduction pathway. MAPK1/ERK2 and MAPK3/ERK1 are the 2 MAPKs which play an important role in the MAPK/ERK cascade. They participate also in a signaling cascade initiated by activated KIT and KITLG/SCF. Depending on the cellular context, the MAPK/ERK cascade mediates diverse biological functions such as cell growth, adhesion, survival and differentiation through the regulation of transcription, translation, cytoskeletal rearrangements. The MAPK/ERK cascade also plays a role in initiation and regulation of meiosis, mitosis, and postmitotic functions in differentiated cells by phosphorylating a number of transcription factors. About 160 substrates have already been discovered for ERKs. Many of these substrates are localized in the nucleus, and seem to participate in the regulation of transcription upon stimulation. However, other substrates are found in the cytosol as well as in other cellular organelles, and those are responsible for processes such as translation, mitosis and apoptosis. Moreover, the MAPK/ERK cascade is also involved in the regulation of the endosomal dynamics, including lysosome processing and endosome cycling through the perinuclear recycling compartment (PNRC); as well as in the fragmentation of the Golgi apparatus during mitosis. The substrates include transcription factors (such as ATF2, BCL6, ELK1, ERF, FOS, HSF4 or SPZ1), cytoskeletal elements (such as CANX, CTTN, GJA1, MAP2, MAPT, PXN, SORBS3 or STMN1), regulators of apoptosis (such as BAD, BTG2, CASP9, DAPK1, IER3, MCL1 or PPARG), regulators of translation (such as EIF4EBP1) and a variety of other signaling-related molecules (like ARHGEF2, DEPTOR, FRS2 or GRB10). Protein kinases (such as RAF1, RPS6KA1/RSK1, RPS6KA3/RSK2, RPS6KA2/RSK3, RPS6KA6/RSK4, SYK, MKNK1/MNK1, MKNK2/MNK2, RPS6KA5/MSK1, RPS6KA4/MSK2, MAPKAPK3 or MAPKAPK5) and phosphatases (such as DUSP1, DUSP4, DUSP6 or DUSP16) are other substrates which enable the propagation the MAPK/ERK signal to additional cytosolic and nuclear targets, thereby extending the specificity of the cascade.
TTD ID
T23276
Uniprot ID
P27361
DrugMap ID
TT1MG9E
Ensemble ID
ENST00000263025.9
HGNC ID
HGNC:6877
ChEMBL ID
CHEMBL3385

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.P373S DBIA    Probe Info 
CHL1 SNV: p.I228V DBIA    Probe Info 
DU145 SNV: p.C271Y .
IM95 SNV: p.M275T .
Ishikawa (Heraklio) 02 ER Deletion: p.G9AfsTer23 .
JURKAT SNV: p.Q46Ter; p.M216I Compound 10    Probe Info 
MDST8 SNV: p.P25S DBIA    Probe Info 
MEWO SNV: p.P246S DBIA    Probe Info 
MOLT4 SNV: p.R318W IA-alkyne    Probe Info 
NCIH2052 SNV: p.A3E DBIA    Probe Info 
SNGM SNV: p.Q44P .
SW756 SNV: p.H197D .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 23 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
TH211
 Probe Info  		Y280(20.00); Y204(16.43)  LDD0257  [1]
YN-1
 Probe Info  		100.00  LDD0444  [2]
STPyne
 Probe Info  		K181(10.00); K287(1.21); K294(5.26)  LDD0277  [3]
Probe 1
 Probe Info  		Y130(23.93); Y156(15.98); Y204(13.48); Y280(10.56)  LDD3495  [4]
BTD
 Probe Info  		C178(0.94)  LDD2089  [5]
HHS-475
 Probe Info  		Y81(0.82)  LDD0264  [6]
IPM
 Probe Info  		C178(2.13); C82(1.79)  LDD1701  [5]
HHS-465
 Probe Info  		Y204(7.23); Y81(10.00)  LDD2237  [7]
DBIA
 Probe Info  		C82(1.45); C178(1.74)  LDD0080  [8]
5E-2FA
 Probe Info  		N.A.  LDD2235  [9]
m-APA
 Probe Info  		N.A.  LDD2231  [9]
4-Iodoacetamidophenylacetylene
 Probe Info  		C271(0.00); C144(0.00)  LDD0038  [10]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [11]
Lodoacetamide azide
 Probe Info  		C271(0.00); C183(0.00); C82(0.00); C233(0.00)  LDD0037  [10]
ATP probe
 Probe Info  		N.A.  LDD0035  [12]
Compound 10
 Probe Info  		N.A.  LDD2216  [13]
SF
 Probe Info  		Y81(0.00); Y204(0.00)  LDD0028  [14]
1c-yne
 Probe Info  		N.A.  LDD0228  [15]
1d-yne
 Probe Info  		N.A.  LDD0357  [15]
Acrolein
 Probe Info  		N.A.  LDD0217  [16]
AOyne
 Probe Info  		14.60  LDD0443  [17]
NAIA_5
 Probe Info  		C178(0.00); C233(0.00); C82(0.00); C144(0.00)  LDD2223  [18]
HHS-482
 Probe Info  		Y81(1.78)  LDD2239  [7]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe13
 Probe Info  		12.16  LDD0475  [19]
FFF probe14
 Probe Info  		7.48  LDD0477  [19]
FFF probe2
 Probe Info  		5.27  LDD0463  [19]
JN0003
 Probe Info  		12.64  LDD0469  [19]
STS-1
 Probe Info  		N.A.  LDD0137  [20]

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 C82(0.90); C178(0.83)  LDD2142  [5]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C82(0.93); C178(1.02)  LDD2112  [5]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C82(0.52)  LDD2095  [5]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C82(1.19)  LDD2130  [5]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C82(1.01)  LDD2117  [5]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C178(0.63)  LDD2152  [5]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C82(0.50); C178(0.95)  LDD2132  [5]
 LDCM0026  4SU-RNA+native RNA HEK-293T C271(2.02)  LDD0372  [21]
 LDCM0214  AC1 HEK-293T C233(0.88)  LDD0812  [8]
 LDCM0215  AC10 HEK-293T C233(0.50); C82(0.81)  LDD0813  [8]
 LDCM0216  AC100 HEK-293T C178(1.03)  LDD0814  [8]
 LDCM0217  AC101 HEK-293T C178(0.93)  LDD0815  [8]
 LDCM0218  AC102 HEK-293T C178(0.95)  LDD0816  [8]
 LDCM0219  AC103 HEK-293T C178(0.75)  LDD0817  [8]
 LDCM0220  AC104 HEK-293T C178(0.90)  LDD0818  [8]
 LDCM0221  AC105 HEK-293T C178(0.86)  LDD0819  [8]
 LDCM0222  AC106 HEK-293T C178(1.11)  LDD0820  [8]
 LDCM0223  AC107 HEK-293T C178(1.10)  LDD0821  [8]
 LDCM0224  AC108 HEK-293T C178(1.18)  LDD0822  [8]
 LDCM0225  AC109 HEK-293T C178(1.01)  LDD0823  [8]
 LDCM0226  AC11 HEK-293T C233(0.64); C82(0.67)  LDD0824  [8]
 LDCM0227  AC110 HEK-293T C178(1.09)  LDD0825  [8]
 LDCM0228  AC111 HEK-293T C178(1.13)  LDD0826  [8]
 LDCM0229  AC112 HEK-293T C178(1.05)  LDD0827  [8]
 LDCM0230  AC113 HEK-293T C144(1.03)  LDD0828  [8]
 LDCM0231  AC114 HEK-293T C144(1.00)  LDD0829  [8]
 LDCM0232  AC115 HEK-293T C144(1.14)  LDD0830  [8]
 LDCM0233  AC116 HEK-293T C144(1.27)  LDD0831  [8]
 LDCM0234  AC117 HEK-293T C144(1.23)  LDD0832  [8]
 LDCM0235  AC118 HEK-293T C144(1.38)  LDD0833  [8]
 LDCM0236  AC119 HEK-293T C144(1.44)  LDD0834  [8]
 LDCM0237  AC12 HEK-293T C233(0.74); C82(0.66)  LDD0835  [8]
 LDCM0238  AC120 HEK-293T C144(1.24)  LDD0836  [8]
 LDCM0239  AC121 HEK-293T C144(1.40)  LDD0837  [8]
 LDCM0240  AC122 HEK-293T C144(1.56)  LDD0838  [8]
 LDCM0241  AC123 HEK-293T C144(1.65)  LDD0839  [8]
 LDCM0242  AC124 HEK-293T C144(1.38)  LDD0840  [8]
 LDCM0243  AC125 HEK-293T C144(1.48)  LDD0841  [8]
 LDCM0244  AC126 HEK-293T C144(1.87)  LDD0842  [8]
 LDCM0245  AC127 HEK-293T C144(2.07)  LDD0843  [8]
 LDCM0246  AC128 HEK-293T C178(1.20); C233(0.95); C82(0.81)  LDD0844  [8]
 LDCM0247  AC129 HEK-293T C178(1.18); C233(1.00); C82(0.71)  LDD0845  [8]
 LDCM0249  AC130 HEK-293T C178(1.08); C233(0.96); C82(0.68)  LDD0847  [8]
 LDCM0250  AC131 HEK-293T C178(1.11); C233(1.01); C82(0.80)  LDD0848  [8]
 LDCM0251  AC132 HEK-293T C178(1.33); C233(0.95); C82(0.71)  LDD0849  [8]
 LDCM0252  AC133 HEK-293T C178(0.95); C233(0.90); C82(1.10)  LDD0850  [8]
 LDCM0253  AC134 HEK-293T C178(1.12); C233(0.85); C82(0.89)  LDD0851  [8]
 LDCM0254  AC135 HEK-293T C178(0.95); C233(1.37); C82(0.86)  LDD0852  [8]
 LDCM0255  AC136 HEK-293T C178(1.08); C233(1.01); C82(0.86)  LDD0853  [8]
 LDCM0256  AC137 HEK-293T C178(1.27); C233(1.14); C82(0.78)  LDD0854  [8]
 LDCM0257  AC138 HEK-293T C178(1.20); C233(1.25); C82(0.86)  LDD0855  [8]
 LDCM0258  AC139 HEK-293T C178(1.26); C233(1.21); C82(0.80)  LDD0856  [8]
 LDCM0259  AC14 HEK-293T C233(0.67); C82(0.68)  LDD0857  [8]
 LDCM0260  AC140 HEK-293T C178(1.12); C233(1.07); C82(0.88)  LDD0858  [8]
 LDCM0261  AC141 HEK-293T C178(1.21); C233(1.19); C82(0.89)  LDD0859  [8]
 LDCM0262  AC142 HEK-293T C178(1.27); C233(1.02); C82(0.78)  LDD0860  [8]
 LDCM0263  AC143 HEK-293T C144(1.22); C178(0.98); C82(0.92)  LDD0861  [8]
 LDCM0264  AC144 HEK-293T C144(1.30); C178(1.06); C82(0.99)  LDD0862  [8]
 LDCM0265  AC145 HEK-293T C144(1.21); C178(1.01); C82(0.99)  LDD0863  [8]
 LDCM0266  AC146 HEK-293T C144(1.48); C178(1.07); C82(1.13)  LDD0864  [8]
 LDCM0267  AC147 HEK-293T C144(1.36); C178(0.95); C82(1.26)  LDD0865  [8]
 LDCM0268  AC148 HEK-293T C144(1.00); C178(0.81); C82(1.25)  LDD0866  [8]
 LDCM0269  AC149 HEK-293T C144(1.15); C178(0.90); C82(1.14)  LDD0867  [8]
 LDCM0270  AC15 HEK-293T C233(0.74); C82(0.75)  LDD0868  [8]
 LDCM0271  AC150 HEK-293T C144(1.14); C178(0.74); C82(1.06)  LDD0869  [8]
 LDCM0272  AC151 HEK-293T C144(1.04); C178(1.04); C82(1.20)  LDD0870  [8]
 LDCM0273  AC152 HEK-293T C144(1.26); C178(1.04); C82(1.09)  LDD0871  [8]
 LDCM0274  AC153 HEK-293T C144(1.15); C178(0.94); C82(1.03)  LDD0872  [8]
 LDCM0621  AC154 HEK-293T C144(1.18); C178(0.89); C82(1.21)  LDD2162  [8]
 LDCM0622  AC155 HEK-293T C144(1.08); C178(0.99); C82(1.06)  LDD2163  [8]
 LDCM0623  AC156 HEK-293T C144(1.41); C178(1.09); C82(0.99)  LDD2164  [8]
 LDCM0624  AC157 HEK-293T C144(1.66); C178(0.86); C82(1.15)  LDD2165  [8]
 LDCM0276  AC17 PaTu 8988t C178(0.59); C233(1.00); C183(0.84)  LDD1155  [8]
 LDCM0277  AC18 PaTu 8988t C178(0.81); C233(0.95); C183(0.92)  LDD1156  [8]
 LDCM0278  AC19 PaTu 8988t C178(0.66); C233(1.25); C183(0.83)  LDD1157  [8]
 LDCM0279  AC2 HEK-293T C233(1.16)  LDD0877  [8]
 LDCM0280  AC20 PaTu 8988t C178(1.00); C233(0.93); C183(1.18)  LDD1159  [8]
 LDCM0281  AC21 PaTu 8988t C178(0.74); C233(0.86); C183(0.89)  LDD1160  [8]
 LDCM0282  AC22 PaTu 8988t C178(1.17); C233(1.02); C183(1.33)  LDD1161  [8]
 LDCM0283  AC23 PaTu 8988t C178(1.16); C233(0.92); C183(1.24)  LDD1162  [8]
 LDCM0284  AC24 PaTu 8988t C178(0.79); C233(0.60); C183(0.96)  LDD1163  [8]
 LDCM0285  AC25 HEK-293T C144(1.17)  LDD0883  [8]
 LDCM0286  AC26 HEK-293T C144(1.30)  LDD0884  [8]
 LDCM0287  AC27 HEK-293T C144(1.40)  LDD0885  [8]
 LDCM0288  AC28 HEK-293T C144(1.08)  LDD0886  [8]
 LDCM0289  AC29 HEK-293T C144(1.23)  LDD0887  [8]
 LDCM0290  AC3 HEK-293T C233(1.13)  LDD0888  [8]
 LDCM0291  AC30 HEK-293T C144(1.32)  LDD0889  [8]
 LDCM0292  AC31 HEK-293T C144(1.00)  LDD0890  [8]
 LDCM0293  AC32 HEK-293T C144(1.19)  LDD0891  [8]
 LDCM0294  AC33 HEK-293T C144(1.35)  LDD0892  [8]
 LDCM0295  AC34 HEK-293T C144(1.12)  LDD0893  [8]
 LDCM0296  AC35 HEK-293T C178(1.01); C233(1.05); C82(0.91)  LDD0894  [8]
 LDCM0297  AC36 HEK-293T C178(0.92); C233(1.47); C82(0.66)  LDD0895  [8]
 LDCM0298  AC37 HEK-293T C178(0.88); C233(1.76); C82(0.84)  LDD0896  [8]
 LDCM0299  AC38 HEK-293T C178(1.02); C233(1.66); C82(0.88)  LDD0897  [8]
 LDCM0300  AC39 HEK-293T C178(1.32); C233(0.95); C82(0.74)  LDD0898  [8]
 LDCM0301  AC4 HEK-293T C233(0.98)  LDD0899  [8]
 LDCM0302  AC40 HEK-293T C178(0.88); C233(1.05); C82(0.77)  LDD0900  [8]
 LDCM0303  AC41 HEK-293T C178(1.00); C233(0.85); C82(0.84)  LDD0901  [8]
 LDCM0304  AC42 HEK-293T C178(1.09); C233(1.22); C82(0.92)  LDD0902  [8]
 LDCM0305  AC43 HEK-293T C178(1.04); C233(1.05); C82(0.79)  LDD0903  [8]
 LDCM0306  AC44 HEK-293T C178(1.19); C233(1.00); C82(0.82)  LDD0904  [8]
 LDCM0307  AC45 HEK-293T C178(1.16); C233(1.19); C82(0.80)  LDD0905  [8]
 LDCM0308  AC46 HEK-293T C178(1.02); C233(1.19)  LDD0906  [8]
 LDCM0309  AC47 HEK-293T C178(0.97); C233(1.35)  LDD0907  [8]
 LDCM0310  AC48 HEK-293T C178(1.01); C233(1.21)  LDD0908  [8]
 LDCM0311  AC49 HEK-293T C178(0.89); C233(1.19)  LDD0909  [8]
 LDCM0312  AC5 HEK-293T C233(1.10)  LDD0910  [8]
 LDCM0313  AC50 HEK-293T C178(1.07); C233(1.38)  LDD0911  [8]
 LDCM0314  AC51 HEK-293T C178(1.14); C233(1.28)  LDD0912  [8]
 LDCM0315  AC52 HEK-293T C178(0.95); C233(1.37)  LDD0913  [8]
 LDCM0316  AC53 HEK-293T C178(0.95); C233(1.24)  LDD0914  [8]
 LDCM0317  AC54 HEK-293T C178(1.05); C233(1.28)  LDD0915  [8]
 LDCM0318  AC55 HEK-293T C178(1.17); C233(1.36)  LDD0916  [8]
 LDCM0319  AC56 HEK-293T C178(1.03); C233(1.45)  LDD0917  [8]
 LDCM0320  AC57 HEK-293T C178(0.88); C233(0.91)  LDD0918  [8]
 LDCM0321  AC58 HEK-293T C178(1.09); C233(1.14)  LDD0919  [8]
 LDCM0322  AC59 HEK-293T C178(1.02); C233(1.12)  LDD0920  [8]
 LDCM0323  AC6 HEK-293T C233(0.63); C82(0.81)  LDD0921  [8]
 LDCM0324  AC60 HEK-293T C178(0.96); C233(0.99)  LDD0922  [8]
 LDCM0325  AC61 HEK-293T C178(1.08); C233(1.16)  LDD0923  [8]
 LDCM0326  AC62 HEK-293T C178(1.25); C233(1.17)  LDD0924  [8]
 LDCM0327  AC63 HEK-293T C178(1.04); C233(1.11)  LDD0925  [8]
 LDCM0328  AC64 HEK-293T C178(1.37); C233(1.30)  LDD0926  [8]
 LDCM0329  AC65 HEK-293T C178(1.09); C233(1.37)  LDD0927  [8]
 LDCM0330  AC66 HEK-293T C178(1.20); C233(1.32)  LDD0928  [8]
 LDCM0331  AC67 HEK-293T C178(1.03); C233(1.08)  LDD0929  [8]
 LDCM0332  AC68 HEK-293T C178(1.11); C233(0.83)  LDD0930  [8]
 LDCM0333  AC69 HEK-293T C178(1.17); C233(0.86)  LDD0931  [8]
 LDCM0334  AC7 HEK-293T C233(0.67); C82(0.96)  LDD0932  [8]
 LDCM0335  AC70 HEK-293T C178(0.94); C233(0.84)  LDD0933  [8]
 LDCM0336  AC71 HEK-293T C178(0.97); C233(0.85)  LDD0934  [8]
 LDCM0337  AC72 HEK-293T C178(1.11); C233(0.80)  LDD0935  [8]
 LDCM0338  AC73 HEK-293T C178(0.92); C233(0.81)  LDD0936  [8]
 LDCM0339  AC74 HEK-293T C178(0.90); C233(1.07)  LDD0937  [8]
 LDCM0340  AC75 HEK-293T C178(0.89); C233(0.89)  LDD0938  [8]
 LDCM0341  AC76 HEK-293T C178(0.99); C233(0.98)  LDD0939  [8]
 LDCM0342  AC77 HEK-293T C178(1.08); C233(0.81)  LDD0940  [8]
 LDCM0343  AC78 HEK-293T C178(1.08); C233(0.81)  LDD0941  [8]
 LDCM0344  AC79 HEK-293T C178(1.00); C233(0.91)  LDD0942  [8]
 LDCM0345  AC8 HEK-293T C233(0.84); C82(0.79)  LDD0943  [8]
 LDCM0346  AC80 HEK-293T C178(1.10); C233(0.99)  LDD0944  [8]
 LDCM0347  AC81 HEK-293T C178(1.15); C233(1.01)  LDD0945  [8]
 LDCM0348  AC82 HEK-293T C178(1.17); C233(0.89)  LDD0946  [8]
 LDCM0349  AC83 HEK-293T C144(1.09); C178(1.16)  LDD0947  [8]
 LDCM0350  AC84 HEK-293T C144(1.38); C178(1.35)  LDD0948  [8]
 LDCM0351  AC85 HEK-293T C144(1.21); C178(1.01)  LDD0949  [8]
 LDCM0352  AC86 HEK-293T C144(1.30); C178(0.98)  LDD0950  [8]
 LDCM0353  AC87 HEK-293T C144(1.27); C178(1.03)  LDD0951  [8]
 LDCM0354  AC88 HEK-293T C144(1.29); C178(0.86)  LDD0952  [8]
 LDCM0355  AC89 HEK-293T C144(1.24); C178(1.13)  LDD0953  [8]
 LDCM0357  AC90 HEK-293T C144(1.11); C178(0.90)  LDD0955  [8]
 LDCM0358  AC91 HEK-293T C144(1.11); C178(1.01)  LDD0956  [8]
 LDCM0359  AC92 HEK-293T C144(1.07); C178(1.18)  LDD0957  [8]
 LDCM0360  AC93 HEK-293T C144(1.08); C178(1.06)  LDD0958  [8]
 LDCM0361  AC94 HEK-293T C144(1.18); C178(1.11)  LDD0959  [8]
 LDCM0362  AC95 HEK-293T C144(1.32); C178(0.99)  LDD0960  [8]
 LDCM0363  AC96 HEK-293T C144(1.32); C178(1.11)  LDD0961  [8]
 LDCM0364  AC97 HEK-293T C144(1.69); C178(1.01)  LDD0962  [8]
 LDCM0365  AC98 HEK-293T C178(0.98)  LDD0963  [8]
 LDCM0366  AC99 HEK-293T C178(1.00)  LDD0964  [8]
 LDCM0545  Acetamide MDA-MB-231 C82(0.53)  LDD2138  [5]
 LDCM0248  AKOS034007472 HEK-293T C233(0.72); C82(0.80)  LDD0846  [8]
 LDCM0356  AKOS034007680 HEK-293T C233(0.82); C82(0.78)  LDD0954  [8]
 LDCM0275  AKOS034007705 HEK-293T C233(0.71); C82(0.67)  LDD0873  [8]
 LDCM0020  ARS-1620 HCC44 C183(1.19); C178(0.77)  LDD2171  [8]
 LDCM0498  BS-3668 MDA-MB-231 C82(0.74); C178(0.87)  LDD2091  [5]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [16]
 LDCM0632  CL-Sc Hep-G2 C82(2.36)  LDD2227  [18]
 LDCM0367  CL1 HEK-293T C178(1.35); C233(1.22)  LDD0965  [8]
 LDCM0368  CL10 HEK-293T C178(1.18); C233(1.43)  LDD0966  [8]
 LDCM0369  CL100 HEK-293T C233(0.96)  LDD0967  [8]
 LDCM0370  CL101 HEK-293T C233(0.81); C82(0.93)  LDD0968  [8]
 LDCM0371  CL102 HEK-293T C233(0.76); C82(0.70)  LDD0969  [8]
 LDCM0372  CL103 HEK-293T C233(0.69); C82(0.88)  LDD0970  [8]
 LDCM0373  CL104 HEK-293T C233(0.62); C82(1.00)  LDD0971  [8]
 LDCM0374  CL105 PaTu 8988t C178(0.96); C233(1.08); C183(0.96)  LDD1253  [8]
 LDCM0375  CL106 PaTu 8988t C178(0.73); C233(1.05); C183(0.90)  LDD1254  [8]
 LDCM0376  CL107 PaTu 8988t C178(0.54); C233(1.26); C183(0.78)  LDD1255  [8]
 LDCM0377  CL108 PaTu 8988t C178(0.57); C233(0.82); C183(0.85)  LDD1256  [8]
 LDCM0378  CL109 PaTu 8988t C178(0.94); C233(1.25); C183(0.97)  LDD1257  [8]
 LDCM0379  CL11 HEK-293T C178(1.12); C233(1.25)  LDD0977  [8]
 LDCM0380  CL110 PaTu 8988t C178(1.28); C233(0.86); C183(0.94)  LDD1259  [8]
 LDCM0381  CL111 PaTu 8988t C178(1.22); C233(0.85); C183(1.08)  LDD1260  [8]
 LDCM0382  CL112 HEK-293T C144(1.34)  LDD0980  [8]
 LDCM0383  CL113 HEK-293T C144(1.23)  LDD0981  [8]
 LDCM0384  CL114 HEK-293T C144(1.30)  LDD0982  [8]
 LDCM0385  CL115 HEK-293T C144(1.43)  LDD0983  [8]
 LDCM0386  CL116 HEK-293T C144(1.42)  LDD0984  [8]
 LDCM0387  CL117 HEK-293T C178(1.15); C233(1.91); C82(0.73)  LDD0985  [8]
 LDCM0388  CL118 HEK-293T C178(0.85); C233(1.20); C82(0.77)  LDD0986  [8]
 LDCM0389  CL119 HEK-293T C178(0.91); C233(1.11); C82(0.77)  LDD0987  [8]
 LDCM0390  CL12 HEK-293T C178(1.02); C233(0.94)  LDD0988  [8]
 LDCM0391  CL120 HEK-293T C178(1.37); C233(1.01); C82(0.76)  LDD0989  [8]
 LDCM0392  CL121 HEK-293T C178(0.90); C233(1.42)  LDD0990  [8]
 LDCM0393  CL122 HEK-293T C178(0.96); C233(1.28)  LDD0991  [8]
 LDCM0394  CL123 HEK-293T C178(0.77); C233(1.36)  LDD0992  [8]
 LDCM0395  CL124 HEK-293T C178(0.89); C233(1.31)  LDD0993  [8]
 LDCM0396  CL125 HEK-293T C178(0.99); C233(1.04)  LDD0994  [8]
 LDCM0397  CL126 HEK-293T C178(0.86); C233(1.06)  LDD0995  [8]
 LDCM0398  CL127 HEK-293T C178(0.97); C233(0.95)  LDD0996  [8]
 LDCM0399  CL128 HEK-293T C178(1.02); C233(1.03)  LDD0997  [8]
 LDCM0400  CL13 HEK-293T C178(0.91); C233(0.91)  LDD0998  [8]
 LDCM0401  CL14 HEK-293T C178(1.20); C233(0.81)  LDD0999  [8]
 LDCM0402  CL15 HEK-293T C178(0.95); C233(1.77)  LDD1000  [8]
 LDCM0403  CL16 HEK-293T C144(1.01); C178(1.18)  LDD1001  [8]
 LDCM0404  CL17 HEK-293T C144(1.54); C178(1.05)  LDD1002  [8]
 LDCM0405  CL18 HEK-293T C144(1.20); C178(0.89)  LDD1003  [8]
 LDCM0406  CL19 HEK-293T C144(1.18); C178(0.96)  LDD1004  [8]
 LDCM0407  CL2 HEK-293T C178(1.01); C233(0.92)  LDD1005  [8]
 LDCM0408  CL20 HEK-293T C144(1.10); C178(0.94)  LDD1006  [8]
 LDCM0409  CL21 HEK-293T C144(1.34); C178(1.68)  LDD1007  [8]
 LDCM0410  CL22 HEK-293T C144(1.02); C178(1.18)  LDD1008  [8]
 LDCM0411  CL23 HEK-293T C144(0.88); C178(0.87)  LDD1009  [8]
 LDCM0412  CL24 HEK-293T C144(0.91); C178(0.98)  LDD1010  [8]
 LDCM0413  CL25 HEK-293T C144(1.30); C178(1.15)  LDD1011  [8]
 LDCM0414  CL26 HEK-293T C144(1.05); C178(0.94)  LDD1012  [8]
 LDCM0415  CL27 HEK-293T C144(1.11); C178(1.00)  LDD1013  [8]
 LDCM0416  CL28 HEK-293T C144(1.06); C178(0.78)  LDD1014  [8]
 LDCM0417  CL29 HEK-293T C144(1.05); C178(0.99)  LDD1015  [8]
 LDCM0418  CL3 HEK-293T C178(1.23); C233(1.10)  LDD1016  [8]
 LDCM0419  CL30 HEK-293T C144(1.18); C178(0.90)  LDD1017  [8]
 LDCM0420  CL31 HEK-293T C144(1.29); C178(1.24); C233(0.93)  LDD1018  [8]
 LDCM0421  CL32 HEK-293T C144(1.22); C178(1.18); C233(0.98)  LDD1019  [8]
 LDCM0422  CL33 HEK-293T C144(2.55); C178(0.94); C233(1.47)  LDD1020  [8]
 LDCM0423  CL34 HEK-293T C144(1.24); C178(1.10); C233(1.19)  LDD1021  [8]
 LDCM0424  CL35 HEK-293T C144(1.24); C178(0.99); C233(1.04)  LDD1022  [8]
 LDCM0425  CL36 HEK-293T C144(1.27); C178(1.15); C233(1.19)  LDD1023  [8]
 LDCM0426  CL37 HEK-293T C144(1.32); C178(1.16); C233(1.08)  LDD1024  [8]
 LDCM0428  CL39 HEK-293T C144(1.73); C178(1.04); C233(1.47)  LDD1026  [8]
 LDCM0429  CL4 HEK-293T C178(1.35); C233(0.98)  LDD1027  [8]
 LDCM0430  CL40 HEK-293T C144(1.17); C178(1.12); C233(1.11)  LDD1028  [8]
 LDCM0431  CL41 HEK-293T C144(1.52); C178(0.94); C233(1.13)  LDD1029  [8]
 LDCM0432  CL42 HEK-293T C144(1.36); C178(1.04); C233(1.20)  LDD1030  [8]
 LDCM0433  CL43 HEK-293T C144(1.52); C178(1.11); C233(1.09)  LDD1031  [8]
 LDCM0434  CL44 HEK-293T C144(1.25); C178(1.08); C233(1.17)  LDD1032  [8]
 LDCM0435  CL45 HEK-293T C144(1.73); C178(0.91); C233(1.20)  LDD1033  [8]
 LDCM0436  CL46 HEK-293T C233(1.14)  LDD1034  [8]
 LDCM0437  CL47 HEK-293T C233(1.22)  LDD1035  [8]
 LDCM0438  CL48 HEK-293T C233(1.24)  LDD1036  [8]
 LDCM0439  CL49 HEK-293T C233(1.02)  LDD1037  [8]
 LDCM0440  CL5 HEK-293T C178(1.10); C233(1.11)  LDD1038  [8]
 LDCM0441  CL50 HEK-293T C233(1.16)  LDD1039  [8]
 LDCM0442  CL51 HEK-293T C233(1.23)  LDD1040  [8]
 LDCM0443  CL52 HEK-293T C233(0.94)  LDD1041  [8]
 LDCM0444  CL53 HEK-293T C233(0.89)  LDD1042  [8]
 LDCM0445  CL54 HEK-293T C233(1.13)  LDD1043  [8]
 LDCM0446  CL55 HEK-293T C233(0.94)  LDD1044  [8]
 LDCM0447  CL56 HEK-293T C233(1.20)  LDD1045  [8]
 LDCM0448  CL57 HEK-293T C233(0.90)  LDD1046  [8]
 LDCM0449  CL58 HEK-293T C233(0.82)  LDD1047  [8]
 LDCM0450  CL59 HEK-293T C233(1.21)  LDD1048  [8]
 LDCM0451  CL6 HEK-293T C178(1.36); C233(1.29)  LDD1049  [8]
 LDCM0452  CL60 HEK-293T C233(0.96)  LDD1050  [8]
 LDCM0453  CL61 HEK-293T C178(0.88); C233(1.18)  LDD1051  [8]
 LDCM0454  CL62 HEK-293T C178(1.02); C233(1.18)  LDD1052  [8]
 LDCM0455  CL63 HEK-293T C178(0.89); C233(1.06)  LDD1053  [8]
 LDCM0456  CL64 HEK-293T C178(0.81); C233(0.98)  LDD1054  [8]
 LDCM0457  CL65 HEK-293T C178(1.00); C233(0.81)  LDD1055  [8]
 LDCM0458  CL66 HEK-293T C178(1.05); C233(0.94)  LDD1056  [8]
 LDCM0459  CL67 HEK-293T C178(0.89); C233(0.96)  LDD1057  [8]
 LDCM0460  CL68 HEK-293T C178(1.13); C233(1.07)  LDD1058  [8]
 LDCM0461  CL69 HEK-293T C178(0.87); C233(1.01)  LDD1059  [8]
 LDCM0462  CL7 HEK-293T C178(1.03); C233(1.29)  LDD1060  [8]
 LDCM0463  CL70 HEK-293T C178(0.90); C233(0.94)  LDD1061  [8]
 LDCM0464  CL71 HEK-293T C178(0.85); C233(1.09)  LDD1062  [8]
 LDCM0465  CL72 HEK-293T C178(0.92); C233(1.38)  LDD1063  [8]
 LDCM0466  CL73 HEK-293T C178(0.72); C233(1.00)  LDD1064  [8]
 LDCM0467  CL74 HEK-293T C178(0.91); C233(1.18)  LDD1065  [8]
 LDCM0469  CL76 HEK-293T C178(1.10)  LDD1067  [8]
 LDCM0470  CL77 HEK-293T C178(1.09)  LDD1068  [8]
 LDCM0471  CL78 HEK-293T C178(0.94)  LDD1069  [8]
 LDCM0472  CL79 HEK-293T C178(0.85)  LDD1070  [8]
 LDCM0473  CL8 HEK-293T C178(0.96); C233(0.99)  LDD1071  [8]
 LDCM0474  CL80 HEK-293T C178(1.00)  LDD1072  [8]
 LDCM0475  CL81 HEK-293T C178(1.34)  LDD1073  [8]
 LDCM0476  CL82 HEK-293T C178(1.13)  LDD1074  [8]
 LDCM0477  CL83 HEK-293T C178(0.84)  LDD1075  [8]
 LDCM0478  CL84 HEK-293T C178(1.32)  LDD1076  [8]
 LDCM0479  CL85 HEK-293T C178(1.44)  LDD1077  [8]
 LDCM0480  CL86 HEK-293T C178(1.08)  LDD1078  [8]
 LDCM0481  CL87 HEK-293T C178(1.19)  LDD1079  [8]
 LDCM0482  CL88 HEK-293T C178(1.46)  LDD1080  [8]
 LDCM0483  CL89 HEK-293T C178(1.18)  LDD1081  [8]
 LDCM0484  CL9 HEK-293T C178(0.92); C233(0.84)  LDD1082  [8]
 LDCM0485  CL90 HEK-293T C178(0.81)  LDD1083  [8]
 LDCM0486  CL91 HEK-293T C233(0.85)  LDD1084  [8]
 LDCM0487  CL92 HEK-293T C233(0.92)  LDD1085  [8]
 LDCM0488  CL93 HEK-293T C233(1.23)  LDD1086  [8]
 LDCM0489  CL94 HEK-293T C233(1.01)  LDD1087  [8]
 LDCM0490  CL95 HEK-293T C233(1.38)  LDD1088  [8]
 LDCM0491  CL96 HEK-293T C233(1.02)  LDD1089  [8]
 LDCM0492  CL97 HEK-293T C233(1.03)  LDD1090  [8]
 LDCM0493  CL98 HEK-293T C233(0.87)  LDD1091  [8]
 LDCM0494  CL99 HEK-293T C233(0.88)  LDD1092  [8]
 LDCM0634  CY-0357 Hep-G2 C82(1.14)  LDD2228  [18]
 LDCM0495  E2913 HEK-293T C82(0.93); C178(0.91); C144(1.01); C271(1.09)  LDD1698  [22]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C82(1.44); C178(1.06)  LDD1702  [5]
 LDCM0625  F8 Ramos C82(1.45)  LDD2187  [23]
 LDCM0572  Fragment10 Ramos C82(0.68)  LDD2189  [23]
 LDCM0573  Fragment11 Ramos C82(0.15)  LDD2190  [23]
 LDCM0574  Fragment12 Ramos C82(0.59)  LDD2191  [23]
 LDCM0575  Fragment13 Ramos C82(0.96)  LDD2192  [23]
 LDCM0576  Fragment14 Ramos C82(1.11)  LDD2193  [23]
 LDCM0579  Fragment20 Ramos C82(0.53)  LDD2194  [23]
 LDCM0580  Fragment21 Ramos C82(0.99)  LDD2195  [23]
 LDCM0582  Fragment23 Ramos C82(1.09)  LDD2196  [23]
 LDCM0578  Fragment27 Ramos C82(1.03)  LDD2197  [23]
 LDCM0586  Fragment28 Ramos C82(0.76)  LDD2198  [23]
 LDCM0588  Fragment30 Ramos C82(1.12)  LDD2199  [23]
 LDCM0589  Fragment31 Ramos C82(1.08)  LDD2200  [23]
 LDCM0590  Fragment32 Ramos C82(0.65)  LDD2201  [23]
 LDCM0468  Fragment33 HEK-293T C178(0.81); C233(0.95)  LDD1066  [8]
 LDCM0596  Fragment38 Ramos C82(0.89)  LDD2203  [23]
 LDCM0566  Fragment4 Ramos C82(0.90)  LDD2184  [23]
 LDCM0427  Fragment51 HEK-293T C144(1.17); C178(1.06); C233(1.18)  LDD1025  [8]
 LDCM0610  Fragment52 Ramos C82(1.11)  LDD2204  [23]
 LDCM0614  Fragment56 Ramos C82(1.24)  LDD2205  [23]
 LDCM0569  Fragment7 Ramos C82(0.71)  LDD2186  [23]
 LDCM0571  Fragment9 Ramos C82(0.66)  LDD2188  [23]
 LDCM0116  HHS-0101 DM93 Y81(0.82)  LDD0264  [6]
 LDCM0117  HHS-0201 DM93 Y81(0.82)  LDD0265  [6]
 LDCM0118  HHS-0301 DM93 Y81(0.81)  LDD0266  [6]
 LDCM0119  HHS-0401 DM93 Y81(0.91)  LDD0267  [6]
 LDCM0120  HHS-0701 DM93 Y81(0.93)  LDD0268  [6]
 LDCM0022  KB02 HCT 116 C82(1.45); C178(1.74)  LDD0080  [8]
 LDCM0023  KB03 HCT 116 C82(1.29); C178(1.19)  LDD0081  [8]
 LDCM0024  KB05 HCT 116 C82(1.57); C178(1.55)  LDD0082  [8]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C178(1.06)  LDD2102  [5]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C178(0.94)  LDD2089  [5]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C178(1.19)  LDD2092  [5]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C82(1.08)  LDD2093  [5]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C178(0.69)  LDD2094  [5]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C178(0.96)  LDD2098  [5]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C178(1.22)  LDD2099  [5]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C178(0.72)  LDD2100  [5]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C82(0.74); C178(0.93)  LDD2104  [5]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C178(1.23)  LDD2105  [5]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C82(0.56); C178(0.98)  LDD2106  [5]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C82(0.96)  LDD2107  [5]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C82(0.94)  LDD2108  [5]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C82(0.74); C178(0.70)  LDD2109  [5]
 LDCM0517  Nucleophilic fragment 21b MDA-MB-231 C82(1.28)  LDD2110  [5]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C82(0.98); C183(1.31)  LDD2111  [5]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C82(0.99); C178(0.78)  LDD2114  [5]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C178(0.91)  LDD2118  [5]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C82(2.05)  LDD2119  [5]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C82(1.02)  LDD2120  [5]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C178(1.05)  LDD2124  [5]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C82(0.90); C178(0.91)  LDD2125  [5]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C178(1.01)  LDD2126  [5]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C82(1.18); C178(0.95)  LDD2127  [5]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C82(1.26)  LDD2129  [5]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C82(0.44)  LDD2134  [5]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C82(1.12)  LDD2135  [5]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C82(0.96); C178(0.95)  LDD2137  [5]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C178(0.98)  LDD2140  [5]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C82(0.49); C178(0.87)  LDD2141  [5]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C82(0.84)  LDD2143  [5]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C82(0.98)  LDD2146  [5]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C82(0.66)  LDD2148  [5]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C82(0.64)  LDD2150  [5]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C82(1.73)  LDD2153  [5]
 LDCM0628  OTUB2-COV-1 HEK-293T C178(0.89); C82(0.61)  LDD2207  [24]
 LDCM0021  THZ1 HCT 116 C183(1.19); C178(0.77)  LDD2173  [8]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 11 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Deoxyhypusine synthase (DHPS) Deoxyhypusine synthase family P49366
Probable hydrolase PNKD (PNKD) Glyoxalase II family Q8N490
Protein-arginine deiminase type-3 (PADI3) Protein arginine deiminase family Q9ULW8
Death-associated protein kinase 1 (DAPK1) CAMK Ser/Thr protein kinase family P53355
Mitogen-activated protein kinase 14 (MAPK14) CMGC Ser/Thr protein kinase family Q16539
Mitogen-activated protein kinase 3 (MAPK3) CMGC Ser/Thr protein kinase family P27361
Dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1) STE Ser/Thr protein kinase family Q02750
Dual specificity protein phosphatase 1 (DUSP1) Protein-tyrosine phosphatase family P28562
Dual specificity protein phosphatase 6 (DUSP6) Protein-tyrosine phosphatase family Q16828
Receptor-type tyrosine-protein phosphatase beta (PTPRB) Protein-tyrosine phosphatase family P23467
Receptor-type tyrosine-protein phosphatase eta (PTPRJ) Protein-tyrosine phosphatase family Q12913
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
ETS domain-containing protein Elk-1 (ELK1) ETS family P19419
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein scribble homolog (SCRIB) LAP (LRR and PDZ) protein family Q14160
MORF4 family-associated protein 1-like 1 (MRFAP1L1) MORF4 family-associated protein family Q96HT8
Astrocytic phosphoprotein PEA-15 (PEA15) . Q15121
Endosialin (CD248) . Q9HCU0
Kelch-like protein 32 (KLHL32) . Q96NJ5

The Drug(s) Related To This Target

Approved
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Acetylsalicylic Acid Small molecular drug DB00945
Arsenic Trioxide Small molecular drug DB01169
Minocycline Small molecular drug DB01017
Sulindac Small molecular drug DB00605
Cholecystokinin . DB08862
Phase 2
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Astx029 Small molecular drug DM1FD5
Bvd-523 . D01IED
Hh2710 . D1KIY9
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Jsi-1187 Small molecular drug DBU16T
Asn007 . D0D2XQ
Gdc-0994 . D0Q4IX
Van-10-4-eluting Stent . D08KNG
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cor-d Small molecular drug DOJ6D9
Investigative
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
6-[(E)-2-(4-fluoro-phenyl)-vinyl]-9h-purine Small molecular drug D02TYK
Colforsin Small molecular drug DB02587
Purvalanol Small molecular drug DB02733
Seliciclib Small molecular drug DB06195
5-iodotubercidin . DB04604
Ulixertinib . DB13930

References

1 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
2 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.
3 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
4 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.
5 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
6 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.
7 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
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 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
10 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
11 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
12 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
13 Multiplexed CuAAC Suzuki-Miyaura Labeling for Tandem Activity-Based Chemoproteomic Profiling. Anal Chem. 2021 Feb 2;93(4):2610-2618. doi: 10.1021/acs.analchem.0c04726. Epub 2021 Jan 20.
Mass spectrometry data entry: PXD022279
14 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
15 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
16 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.
17 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.
18 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
19 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.
20 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
21 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
22 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
23 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
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.