General Information of Target

Target ID LDTP03170
Target Name Ectonucleotide pyrophosphatase/phosphodiesterase family member 1 (ENPP1)
Gene Name ENPP1
Gene ID 5167
Synonyms
M6S1; NPPS; PC1; PDNP1; Ectonucleotide pyrophosphatase/phosphodiesterase family member 1; E-NPP 1; Membrane component chromosome 6 surface marker 1; Phosphodiesterase I/nucleotide pyrophosphatase 1; Plasma-cell membrane glycoprotein PC-1) [Cleaved into: Ectonucleotide pyrophosphatase/phosphodiesterase family member 1, secreted form] [Includes: Alkaline phosphodiesterase I; EC 3.1.4.1; Nucleotide pyrophosphatase; NPPase; EC 3.6.1.9; Nucleotide diphosphatase)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MERDGCAGGGSRGGEGGRAPREGPAGNGRDRGRSHAAEAPGDPQAAASLLAPMDVGEEPL
EKAARARTAKDPNTYKVLSLVLSVCVLTTILGCIFGLKPSCAKEVKSCKGRCFERTFGNC
RCDAACVELGNCCLDYQETCIEPEHIWTCNKFRCGEKRLTRSLCACSDDCKDKGDCCINY
SSVCQGEKSWVEEPCESINEPQCPAGFETPPTLLFSLDGFRAEYLHTWGGLLPVISKLKK
CGTYTKNMRPVYPTKTFPNHYSIVTGLYPESHGIIDNKMYDPKMNASFSLKSKEKFNPEW
YKGEPIWVTAKYQGLKSGTFFWPGSDVEINGIFPDIYKMYNGSVPFEERILAVLQWLQLP
KDERPHFYTLYLEEPDSSGHSYGPVSSEVIKALQRVDGMVGMLMDGLKELNLHRCLNLIL
ISDHGMEQGSCKKYIYLNKYLGDVKNIKVIYGPAARLRPSDVPDKYYSFNYEGIARNLSC
REPNQHFKPYLKHFLPKRLHFAKSDRIEPLTFYLDPQWQLALNPSERKYCGSGFHGSDNV
FSNMQALFVGYGPGFKHGIEADTFENIEVYNLMCDLLNLTPAPNNGTHGSLNHLLKNPVY
TPKHPKEVHPLVQCPFTRNPRDNLGCSCNPSILPIEDFQTQFNLTVAEEKIIKHETLPYG
RPRVLQKENTICLLSQHQFMSGYSQDILMPLWTSYTVDRNDSFSTEDFSNCLYQDFRIPL
SPVHKCSFYKNNTKVSYGFLSPPQLNKNSSGIYSEALLTTNIVPMYQSFQVIWRYFHDTL
LRKYAEERNGVNVVSGPVFDFDYDGRCDSLENLRQKRRVIRNQEILIPTHFFIVLTSCKD
TSQTPLHCENLDTLAFILPHRTDNSESCVHGKHDSSWVEELLMLHRARITDVEHITGLSF
YQQRKEPVSDILKLKTHLPTFSQED
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Nucleotide pyrophosphatase/phosphodiesterase family
Subcellular location
Secreted; Cell membrane
Function
Nucleotide pyrophosphatase that generates diphosphate (PPi) and functions in bone mineralization and soft tissue calcification by regulating pyrophosphate levels. PPi inhibits bone mineralization and soft tissue calcification by binding to nascent hydroxyapatite crystals, thereby preventing further growth of these crystals. Preferentially hydrolyzes ATP, but can also hydrolyze other nucleoside 5' triphosphates such as GTP, CTP and UTP to their corresponding monophosphates with release of pyrophosphate, as well as diadenosine polyphosphates, and also 3',5'-cAMP to AMP. May also be involved in the regulation of the availability of nucleotide sugars in the endoplasmic reticulum and Golgi, and the regulation of purinergic signaling. Inhibits ectopic joint calcification and maintains articular chondrocytes by repressing hedgehog signaling; it is however unclear whether hedgehog inhibition is direct or indirect. Appears to modulate insulin sensitivity and function. Also involved in melanogenesis. Also able to hydrolyze 2',3'-cGAMP (cyclic GMP-AMP), a second messenger that activates TMEM173/STING and triggers type-I interferon production. 2',3'-cGAMP degradation takes place in the lumen or extracellular space, and not in the cytosol where it is produced; the role of 2',3'-cGAMP hydrolysis is therefore unclear. Not able to hydrolyze the 2',3'-cGAMP linkage isomer 3'-3'-cGAMP.
TTD ID
T63194
Uniprot ID
P22413
DrugMap ID
TTZTIWS
Ensemble ID
ENST00000647893.1
HGNC ID
HGNC:3356
ChEMBL ID
CHEMBL5925

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 14 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info 
100.00  LDD0444  [1]
STPyne
 Probe Info 
K653(4.47)  LDD0277  [2]
IPM
 Probe Info 
C807(0.00); C6(0.00); C868(0.00)  LDD0241  [3]
OPA-S-S-alkyne
 Probe Info 
K448(0.53); K465(1.52); K503(1.89)  LDD3494  [4]
Probe 1
 Probe Info 
Y803(2.80)  LDD3495  [5]
DBIA
 Probe Info 
C6(1.55)  LDD0080  [6]
5E-2FA
 Probe Info 
N.A.  LDD2235  [7]
ATP probe
 Probe Info 
K278(0.00); K283(0.00); K653(0.00)  LDD0199  [8]
m-APA
 Probe Info 
H847(0.00); H894(0.00)  LDD2231  [7]
IA-alkyne
 Probe Info 
C868(0.00); C838(0.00); C848(0.00); C614(0.00)  LDD0165  [9]
NAIA_5
 Probe Info 
N.A.  LDD2224  [10]
ENE
 Probe Info 
N.A.  LDD0006  [11]
SF
 Probe Info 
N.A.  LDD0028  [12]
Phosphinate-6
 Probe Info 
N.A.  LDD0018  [13]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C027
 Probe Info 
11.31  LDD1733  [14]
C158
 Probe Info 
58.49  LDD1838  [14]
C364
 Probe Info 
17.15  LDD2025  [14]
Alk-rapa
 Probe Info 
4.30  LDD0213  [15]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0215  AC10 HEK-293T C6(1.06)  LDD0813  [6]
 LDCM0216  AC100 HEK-293T C6(0.83)  LDD0814  [6]
 LDCM0217  AC101 HEK-293T C6(0.82)  LDD0815  [6]
 LDCM0218  AC102 HEK-293T C6(1.27)  LDD0816  [6]
 LDCM0219  AC103 HEK-293T C6(0.61)  LDD0817  [6]
 LDCM0220  AC104 HEK-293T C6(1.19)  LDD0818  [6]
 LDCM0221  AC105 HEK-293T C6(0.82)  LDD0819  [6]
 LDCM0222  AC106 HEK-293T C6(0.98)  LDD0820  [6]
 LDCM0223  AC107 HEK-293T C6(0.94)  LDD0821  [6]
 LDCM0224  AC108 HEK-293T C6(1.17)  LDD0822  [6]
 LDCM0225  AC109 HEK-293T C6(0.90)  LDD0823  [6]
 LDCM0226  AC11 HEK-293T C6(0.94)  LDD0824  [6]
 LDCM0227  AC110 HEK-293T C6(0.86)  LDD0825  [6]
 LDCM0228  AC111 HEK-293T C6(0.84)  LDD0826  [6]
 LDCM0229  AC112 HEK-293T C6(0.96)  LDD0827  [6]
 LDCM0237  AC12 HEK-293T C6(0.82)  LDD0835  [6]
 LDCM0259  AC14 HEK-293T C6(0.87)  LDD0857  [6]
 LDCM0263  AC143 HEK-293T C6(0.74)  LDD0861  [6]
 LDCM0264  AC144 HEK-293T C6(0.76)  LDD0862  [6]
 LDCM0265  AC145 HEK-293T C6(0.97)  LDD0863  [6]
 LDCM0266  AC146 HEK-293T C6(0.89)  LDD0864  [6]
 LDCM0267  AC147 HEK-293T C6(0.65)  LDD0865  [6]
 LDCM0268  AC148 HEK-293T C6(0.74)  LDD0866  [6]
 LDCM0269  AC149 HEK-293T C6(0.59)  LDD0867  [6]
 LDCM0270  AC15 HEK-293T C6(0.94)  LDD0868  [6]
 LDCM0271  AC150 HEK-293T C6(0.77)  LDD0869  [6]
 LDCM0272  AC151 HEK-293T C6(0.75)  LDD0870  [6]
 LDCM0273  AC152 HEK-293T C6(0.70)  LDD0871  [6]
 LDCM0274  AC153 HEK-293T C6(0.53)  LDD0872  [6]
 LDCM0621  AC154 HEK-293T C6(0.60)  LDD2162  [6]
 LDCM0622  AC155 HEK-293T C6(0.57)  LDD2163  [6]
 LDCM0623  AC156 HEK-293T C6(0.74)  LDD2164  [6]
 LDCM0624  AC157 HEK-293T C6(0.59)  LDD2165  [6]
 LDCM0276  AC17 HEK-293T C6(1.87)  LDD0874  [6]
 LDCM0277  AC18 HEK-293T C6(1.69)  LDD0875  [6]
 LDCM0278  AC19 HEK-293T C6(1.42)  LDD0876  [6]
 LDCM0280  AC20 HEK-293T C6(1.06)  LDD0878  [6]
 LDCM0281  AC21 HEK-293T C6(1.18)  LDD0879  [6]
 LDCM0282  AC22 HEK-293T C6(0.90)  LDD0880  [6]
 LDCM0283  AC23 HEK-293T C6(1.19)  LDD0881  [6]
 LDCM0284  AC24 HEK-293T C6(1.35)  LDD0882  [6]
 LDCM0285  AC25 HEK-293T C6(0.55)  LDD0883  [6]
 LDCM0286  AC26 HEK-293T C6(1.80)  LDD0884  [6]
 LDCM0287  AC27 HEK-293T C6(1.19)  LDD0885  [6]
 LDCM0288  AC28 HEK-293T C6(0.73)  LDD0886  [6]
 LDCM0289  AC29 HEK-293T C6(0.68)  LDD0887  [6]
 LDCM0291  AC30 HEK-293T C6(0.97)  LDD0889  [6]
 LDCM0292  AC31 HEK-293T C6(0.67)  LDD0890  [6]
 LDCM0293  AC32 HEK-293T C6(0.97)  LDD0891  [6]
 LDCM0294  AC33 HEK-293T C6(0.86)  LDD0892  [6]
 LDCM0295  AC34 HEK-293T C6(0.78)  LDD0893  [6]
 LDCM0297  AC36 HEK-293T C807(1.07)  LDD1536  [16]
 LDCM0298  AC37 HEK-293T C807(1.13)  LDD1537  [16]
 LDCM0299  AC38 HEK-293T C807(0.77)  LDD1538  [16]
 LDCM0300  AC39 HEK-293T C807(1.09)  LDD1539  [16]
 LDCM0301  AC4 HEK-293T C807(0.84)  LDD1540  [16]
 LDCM0302  AC40 HEK-293T C807(0.93); C431(0.70)  LDD1541  [16]
 LDCM0306  AC44 HEK-293T C807(1.09)  LDD1545  [16]
 LDCM0307  AC45 HEK-293T C807(1.10)  LDD1546  [16]
 LDCM0308  AC46 HEK-293T C6(0.89)  LDD0906  [6]
 LDCM0309  AC47 HEK-293T C6(0.73)  LDD0907  [6]
 LDCM0310  AC48 HEK-293T C6(1.69)  LDD0908  [6]
 LDCM0311  AC49 HEK-293T C6(1.21)  LDD0909  [6]
 LDCM0312  AC5 HEK-293T C807(1.06)  LDD1551  [16]
 LDCM0313  AC50 HEK-293T C6(0.92)  LDD0911  [6]
 LDCM0314  AC51 HEK-293T C6(1.09)  LDD0912  [6]
 LDCM0315  AC52 HEK-293T C6(1.45)  LDD0913  [6]
 LDCM0316  AC53 HEK-293T C6(0.99)  LDD0914  [6]
 LDCM0317  AC54 HEK-293T C6(0.98)  LDD0915  [6]
 LDCM0318  AC55 HEK-293T C6(1.46)  LDD0916  [6]
 LDCM0319  AC56 HEK-293T C6(0.97)  LDD0917  [6]
 LDCM0323  AC6 HEK-293T C6(0.86)  LDD0921  [6]
 LDCM0324  AC60 HEK-293T C807(0.93)  LDD1563  [16]
 LDCM0325  AC61 HEK-293T C807(1.08)  LDD1564  [16]
 LDCM0326  AC62 HEK-293T C807(0.78)  LDD1565  [16]
 LDCM0327  AC63 HEK-293T C807(0.92)  LDD1566  [16]
 LDCM0328  AC64 HEK-293T C807(1.01); C431(0.83)  LDD1567  [16]
 LDCM0332  AC68 HEK-293T C6(1.20)  LDD0930  [6]
 LDCM0333  AC69 HEK-293T C6(1.30)  LDD0931  [6]
 LDCM0334  AC7 HEK-293T C6(0.81)  LDD0932  [6]
 LDCM0335  AC70 HEK-293T C6(1.02)  LDD0933  [6]
 LDCM0336  AC71 HEK-293T C6(0.93)  LDD0934  [6]
 LDCM0337  AC72 HEK-293T C6(1.07)  LDD0935  [6]
 LDCM0338  AC73 HEK-293T C6(0.83)  LDD0936  [6]
 LDCM0339  AC74 HEK-293T C6(0.74)  LDD0937  [6]
 LDCM0340  AC75 HEK-293T C6(0.87)  LDD0938  [6]
 LDCM0341  AC76 HEK-293T C6(1.16)  LDD0939  [6]
 LDCM0342  AC77 HEK-293T C6(1.63)  LDD0940  [6]
 LDCM0343  AC78 HEK-293T C6(1.42)  LDD0941  [6]
 LDCM0344  AC79 HEK-293T C6(1.32)  LDD0942  [6]
 LDCM0345  AC8 HEK-293T C6(0.69)  LDD0943  [6]
 LDCM0346  AC80 HEK-293T C6(1.07)  LDD0944  [6]
 LDCM0347  AC81 HEK-293T C6(1.30)  LDD0945  [6]
 LDCM0348  AC82 HEK-293T C6(2.14)  LDD0946  [6]
 LDCM0365  AC98 HEK-293T C6(1.03)  LDD0963  [6]
 LDCM0366  AC99 HEK-293T C6(0.86)  LDD0964  [6]
 LDCM0248  AKOS034007472 HEK-293T C6(0.82)  LDD0846  [6]
 LDCM0356  AKOS034007680 HEK-293T C6(0.95)  LDD0954  [6]
 LDCM0275  AKOS034007705 HEK-293T C6(0.99)  LDD0873  [6]
 LDCM0020  ARS-1620 HCC44 C6(0.80)  LDD2171  [6]
 LDCM0367  CL1 HEK-293T C6(1.17)  LDD0965  [6]
 LDCM0368  CL10 HEK-293T C6(1.20)  LDD0966  [6]
 LDCM0369  CL100 HEK-293T C6(0.94)  LDD1573  [16]
 LDCM0370  CL101 HEK-293T C6(0.75)  LDD0968  [6]
 LDCM0371  CL102 HEK-293T C6(0.95)  LDD0969  [6]
 LDCM0372  CL103 HEK-293T C6(0.69)  LDD0970  [6]
 LDCM0373  CL104 HEK-293T C6(0.81)  LDD0971  [6]
 LDCM0374  CL105 HEK-293T C6(0.93)  LDD0972  [6]
 LDCM0375  CL106 HEK-293T C6(1.24)  LDD0973  [6]
 LDCM0376  CL107 HEK-293T C6(1.33)  LDD0974  [6]
 LDCM0377  CL108 HEK-293T C6(1.24)  LDD0975  [6]
 LDCM0378  CL109 HEK-293T C6(2.02)  LDD0976  [6]
 LDCM0379  CL11 HEK-293T C6(1.23)  LDD0977  [6]
 LDCM0380  CL110 HEK-293T C6(1.03)  LDD0978  [6]
 LDCM0381  CL111 HEK-293T C6(1.09)  LDD0979  [6]
 LDCM0382  CL112 HEK-293T C6(0.79)  LDD0980  [6]
 LDCM0383  CL113 HEK-293T C6(0.95)  LDD0981  [6]
 LDCM0384  CL114 HEK-293T C6(0.73)  LDD0982  [6]
 LDCM0385  CL115 HEK-293T C6(1.16)  LDD0983  [6]
 LDCM0386  CL116 HEK-293T C6(1.13)  LDD0984  [6]
 LDCM0387  CL117 HEK-293T C807(1.19)  LDD1591  [16]
 LDCM0388  CL118 HEK-293T C6(1.03)  LDD1592  [16]
 LDCM0390  CL12 HEK-293T C6(1.40)  LDD0988  [6]
 LDCM0391  CL120 HEK-293T C6(0.98)  LDD1595  [16]
 LDCM0392  CL121 HEK-293T C6(0.96)  LDD0990  [6]
 LDCM0393  CL122 HEK-293T C6(1.11)  LDD0991  [6]
 LDCM0394  CL123 HEK-293T C6(1.08)  LDD0992  [6]
 LDCM0395  CL124 HEK-293T C6(1.14)  LDD0993  [6]
 LDCM0396  CL125 HEK-293T C807(1.18)  LDD1600  [16]
 LDCM0397  CL126 HEK-293T C6(0.91)  LDD1601  [16]
 LDCM0399  CL128 HEK-293T C6(0.97)  LDD1603  [16]
 LDCM0400  CL13 HEK-293T C6(1.10)  LDD0998  [6]
 LDCM0401  CL14 HEK-293T C6(1.29)  LDD0999  [6]
 LDCM0402  CL15 HEK-293T C6(1.33)  LDD1000  [6]
 LDCM0403  CL16 HEK-293T C6(1.37)  LDD1001  [6]
 LDCM0404  CL17 HEK-293T C6(0.97)  LDD1002  [6]
 LDCM0405  CL18 HEK-293T C6(1.30)  LDD1003  [6]
 LDCM0406  CL19 HEK-293T C6(1.04)  LDD1004  [6]
 LDCM0407  CL2 HEK-293T C6(1.51)  LDD1005  [6]
 LDCM0408  CL20 HEK-293T C6(1.05)  LDD1006  [6]
 LDCM0409  CL21 HEK-293T C6(1.60)  LDD1007  [6]
 LDCM0410  CL22 HEK-293T C6(1.08)  LDD1008  [6]
 LDCM0411  CL23 HEK-293T C6(0.73)  LDD1009  [6]
 LDCM0412  CL24 HEK-293T C6(0.95)  LDD1010  [6]
 LDCM0413  CL25 HEK-293T C6(0.92)  LDD1011  [6]
 LDCM0414  CL26 HEK-293T C6(0.63)  LDD1012  [6]
 LDCM0415  CL27 HEK-293T C6(1.07)  LDD1013  [6]
 LDCM0416  CL28 HEK-293T C6(0.78)  LDD1014  [6]
 LDCM0417  CL29 HEK-293T C6(1.07)  LDD1015  [6]
 LDCM0418  CL3 HEK-293T C6(1.33)  LDD1016  [6]
 LDCM0419  CL30 HEK-293T C6(0.89)  LDD1017  [6]
 LDCM0420  CL31 HEK-293T C6(1.33)  LDD1018  [6]
 LDCM0421  CL32 HEK-293T C6(1.62)  LDD1019  [6]
 LDCM0422  CL33 HEK-293T C6(2.99)  LDD1020  [6]
 LDCM0423  CL34 HEK-293T C6(1.24)  LDD1021  [6]
 LDCM0424  CL35 HEK-293T C6(1.41)  LDD1022  [6]
 LDCM0425  CL36 HEK-293T C6(1.42)  LDD1023  [6]
 LDCM0426  CL37 HEK-293T C6(1.40)  LDD1024  [6]
 LDCM0428  CL39 HEK-293T C6(1.73)  LDD1026  [6]
 LDCM0429  CL4 HEK-293T C6(1.40)  LDD1027  [6]
 LDCM0430  CL40 HEK-293T C6(0.97)  LDD1028  [6]
 LDCM0431  CL41 HEK-293T C6(1.31)  LDD1029  [6]
 LDCM0432  CL42 HEK-293T C6(1.15)  LDD1030  [6]
 LDCM0433  CL43 HEK-293T C6(1.29)  LDD1031  [6]
 LDCM0434  CL44 HEK-293T C6(1.27)  LDD1032  [6]
 LDCM0435  CL45 HEK-293T C6(1.12)  LDD1033  [6]
 LDCM0436  CL46 HEK-293T C6(0.64)  LDD1034  [6]
 LDCM0437  CL47 HEK-293T C6(0.65)  LDD1035  [6]
 LDCM0438  CL48 HEK-293T C6(2.31)  LDD1036  [6]
 LDCM0439  CL49 HEK-293T C6(0.85)  LDD1037  [6]
 LDCM0440  CL5 HEK-293T C6(1.49)  LDD1038  [6]
 LDCM0441  CL50 HEK-293T C6(0.89)  LDD1039  [6]
 LDCM0442  CL51 HEK-293T C6(0.93)  LDD1040  [6]
 LDCM0443  CL52 HEK-293T C6(0.59)  LDD1041  [6]
 LDCM0444  CL53 HEK-293T C6(0.88)  LDD1042  [6]
 LDCM0445  CL54 HEK-293T C6(0.85)  LDD1043  [6]
 LDCM0446  CL55 HEK-293T C6(0.45)  LDD1044  [6]
 LDCM0447  CL56 HEK-293T C6(0.65)  LDD1045  [6]
 LDCM0448  CL57 HEK-293T C6(1.03)  LDD1046  [6]
 LDCM0449  CL58 HEK-293T C6(0.88)  LDD1047  [6]
 LDCM0450  CL59 HEK-293T C6(0.75)  LDD1048  [6]
 LDCM0451  CL6 HEK-293T C6(1.43)  LDD1049  [6]
 LDCM0452  CL60 HEK-293T C6(0.61)  LDD1050  [6]
 LDCM0453  CL61 HEK-293T C6(1.08)  LDD1051  [6]
 LDCM0454  CL62 HEK-293T C6(0.69)  LDD1052  [6]
 LDCM0455  CL63 HEK-293T C6(0.53)  LDD1053  [6]
 LDCM0456  CL64 HEK-293T C6(1.47)  LDD1054  [6]
 LDCM0457  CL65 HEK-293T C6(0.88)  LDD1055  [6]
 LDCM0458  CL66 HEK-293T C6(0.54)  LDD1056  [6]
 LDCM0459  CL67 HEK-293T C6(0.97)  LDD1057  [6]
 LDCM0460  CL68 HEK-293T C6(0.79)  LDD1058  [6]
 LDCM0461  CL69 HEK-293T C6(0.54)  LDD1059  [6]
 LDCM0462  CL7 HEK-293T C6(1.14)  LDD1060  [6]
 LDCM0463  CL70 HEK-293T C6(0.87)  LDD1061  [6]
 LDCM0464  CL71 HEK-293T C6(0.67)  LDD1062  [6]
 LDCM0465  CL72 HEK-293T C6(0.66)  LDD1063  [6]
 LDCM0466  CL73 HEK-293T C6(0.88)  LDD1064  [6]
 LDCM0467  CL74 HEK-293T C6(0.47)  LDD1065  [6]
 LDCM0469  CL76 HEK-293T C6(0.89)  LDD1067  [6]
 LDCM0470  CL77 HEK-293T C6(1.11)  LDD1068  [6]
 LDCM0471  CL78 HEK-293T C6(0.78)  LDD1069  [6]
 LDCM0472  CL79 HEK-293T C6(1.02)  LDD1070  [6]
 LDCM0473  CL8 HEK-293T C807(0.73)  LDD1676  [16]
 LDCM0474  CL80 HEK-293T C6(0.95)  LDD1072  [6]
 LDCM0475  CL81 HEK-293T C6(1.06)  LDD1073  [6]
 LDCM0476  CL82 HEK-293T C6(0.64)  LDD1074  [6]
 LDCM0477  CL83 HEK-293T C6(0.61)  LDD1075  [6]
 LDCM0478  CL84 HEK-293T C6(1.01)  LDD1076  [6]
 LDCM0479  CL85 HEK-293T C6(0.83)  LDD1077  [6]
 LDCM0480  CL86 HEK-293T C6(0.91)  LDD1078  [6]
 LDCM0481  CL87 HEK-293T C6(1.01)  LDD1079  [6]
 LDCM0482  CL88 HEK-293T C6(1.09)  LDD1080  [6]
 LDCM0483  CL89 HEK-293T C6(0.90)  LDD1081  [6]
 LDCM0484  CL9 HEK-293T C807(1.00)  LDD1687  [16]
 LDCM0485  CL90 HEK-293T C6(0.87)  LDD1083  [6]
 LDCM0487  CL92 HEK-293T C807(0.91)  LDD1690  [16]
 LDCM0488  CL93 HEK-293T C807(1.10)  LDD1691  [16]
 LDCM0489  CL94 HEK-293T C807(0.90)  LDD1692  [16]
 LDCM0490  CL95 HEK-293T C807(0.93)  LDD1693  [16]
 LDCM0491  CL96 HEK-293T C807(1.04); C431(0.72)  LDD1694  [16]
 LDCM0492  CL97 HEK-293T C807(0.96)  LDD1695  [16]
 LDCM0493  CL98 HEK-293T C6(1.00)  LDD1696  [16]
 LDCM0468  Fragment33 HEK-293T C6(0.78)  LDD1066  [6]
 LDCM0427  Fragment51 HEK-293T C6(1.72)  LDD1025  [6]
 LDCM0022  KB02 HCT 116 C6(1.55)  LDD0080  [6]
 LDCM0023  KB03 HCT 116 C6(1.19)  LDD0081  [6]
 LDCM0024  KB05 HCT 116 C6(1.46)  LDD0082  [6]
 LDCM0090  Rapamycin JHH-7 4.30  LDD0213  [15]
 LDCM0021  THZ1 HCT 116 C6(0.80)  LDD2173  [6]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Polyethylene Glycol 400 . DB11077
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Taribavirin . DB06408

References

1 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.
2 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
3 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.
4 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
5 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.
6 Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries. Nat Biotechnol. 2021 May;39(5):630-641. doi: 10.1038/s41587-020-00778-3. Epub 2021 Jan 4.
7 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
8 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.
9 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
10 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
11 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
12 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
13 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
14 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
15 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.
16 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