Details of the Target

General Information of Target

Target ID LDTP04124
Target Name Cytosolic phospholipase A2 (PLA2G4A)
Gene Name PLA2G4A
Gene ID 5321
Synonyms
CPLA2; PLA2G4; Cytosolic phospholipase A2; cPLA2; Phospholipase A2 group IVA) [Includes: Phospholipase A2; EC 3.1.1.4; Phosphatidylcholine 2-acylhydrolase; Lysophospholipase; EC 3.1.1.5)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSFIDPYQHIIVEHQYSHKFTVVVLRATKVTKGAFGDMLDTPDPYVELFISTTPDSRKRT
RHFNNDINPVWNETFEFILDPNQENVLEITLMDANYVMDETLGTATFTVSSMKVGEKKEV
PFIFNQVTEMVLEMSLEVCSCPDLRFSMALCDQEKTFRQQRKEHIRESMKKLLGPKNSEG
LHSARDVPVVAILGSGGGFRAMVGFSGVMKALYESGILDCATYVAGLSGSTWYMSTLYSH
PDFPEKGPEEINEELMKNVSHNPLLLLTPQKVKRYVESLWKKKSSGQPVTFTDIFGMLIG
ETLIHNRMNTTLSSLKEKVNTAQCPLPLFTCLHVKPDVSELMFADWVEFSPYEIGMAKYG
TFMAPDLFGSKFFMGTVVKKYEENPLHFLMGVWGSAFSILFNRVLGVSGSQSRGSTMEEE
LENITTKHIVSNDSSDSDDESHEPKGTENEDAGSDYQSDNQASWIHRMIMALVSDSALFN
TREGRAGKVHNFMLGLNLNTSYPLSPLSDFATQDSFDDDELDAAVADPDEFERIYEPLDV
KSKKIHVVDSGLTFNLPYPLILRPQRGVDLIISFDFSARPSDSSPPFKELLLAEKWAKMN
KLPFPKIDPYVFDREGLKECYVFKPKNPDMEKDCPTIIHFVLANINFRKYRAPGVPRETE
EEKEIADFDIFDDPESPFSTFNFQYPNQAFKRLHDLMHFNTLNNIDVIKEAMVESIEYRR
QNPSRCSVSLSNVEARRFFNKEFLSKPKA
Target Type
Clinical trial
Target Bioclass
Enzyme
Subcellular location
Cytoplasm
Function
Has primarily calcium-dependent phospholipase and lysophospholipase activities, with a major role in membrane lipid remodeling and biosynthesis of lipid mediators of the inflammatory response . Plays an important role in embryo implantation and parturition through its ability to trigger prostanoid production. Preferentially hydrolyzes the ester bond of the fatty acyl group attached at sn-2 position of phospholipids (phospholipase A2 activity) . Selectively hydrolyzes sn-2 arachidonoyl group from membrane phospholipids, providing the precursor for eicosanoid biosynthesis via the cyclooxygenase pathway. In an alternative pathway of eicosanoid biosynthesis, hydrolyzes sn-2 fatty acyl chain of eicosanoid lysophopholipids to release free bioactive eicosanoids. Hydrolyzes the ester bond of the fatty acyl group attached at sn-1 position of phospholipids (phospholipase A1 activity) only if an ether linkage rather than an ester linkage is present at the sn-2 position. This hydrolysis is not stereospecific. Has calcium-independent phospholipase A2 and lysophospholipase activities in the presence of phosphoinositides. Has O-acyltransferase activity. Catalyzes the transfer of fatty acyl chains from phospholipids to a primary hydroxyl group of glycerol (sn-1 or sn-3), potentially contributing to monoacylglycerol synthesis.
TTD ID
T14834
Uniprot ID
P47712
DrugMap ID
TTT1JVS
Ensemble ID
ENST00000367466.4
HGNC ID
HGNC:9035
ChEMBL ID
CHEMBL3816

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 13 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C726(2.24)  LDD0080  [1]
IA-alkyne
 Probe Info  		C726(0.00); C634(0.00); C151(0.00); C620(0.00)  LDD0162  [2]
IPM
 Probe Info  		C620(0.00); C726(0.00)  LDD0025  [3]
JW-RF-010
 Probe Info  		C151(0.00); C726(0.00)  LDD0026  [3]
TFBX
 Probe Info  		N.A.  LDD0027  [3]
WYneN
 Probe Info  		C726(0.00); C151(0.00)  LDD0021  [4]
NPM
 Probe Info  		N.A.  LDD0016  [4]
VSF
 Probe Info  		N.A.  LDD0007  [4]
Acrolein
 Probe Info  		H428(0.00); C151(0.00); H261(0.00); H442(0.00)  LDD0217  [5]
Cinnamaldehyde
 Probe Info  		N.A.  LDD0220  [5]
Crotonaldehyde
 Probe Info  		H428(0.00); C151(0.00); H442(0.00); H182(0.00)  LDD0219  [5]
Methacrolein
 Probe Info  		N.A.  LDD0218  [5]
HHS-482
 Probe Info  		Y359(0.54); Y535(1.92)  LDD2239  [6]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-1
 Probe Info  		N.A.  LDD0136  [7]
STS-2
 Probe Info  		4.38  LDD0138  [7]
VE-P
 Probe Info  		N.A.  LDD0396  [8]
DA-2
 Probe Info  		N.A.  LDD0071  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HCT 116 C726(1.23)  LDD0531  [1]
 LDCM0215  AC10 HCT 116 C726(0.91)  LDD0532  [1]
 LDCM0216  AC100 HEK-293T C726(0.96)  LDD0814  [1]
 LDCM0217  AC101 HEK-293T C726(1.02)  LDD0815  [1]
 LDCM0218  AC102 HEK-293T C726(0.99)  LDD0816  [1]
 LDCM0219  AC103 HEK-293T C726(1.16)  LDD0817  [1]
 LDCM0220  AC104 HEK-293T C726(1.31)  LDD0818  [1]
 LDCM0221  AC105 HEK-293T C726(0.97)  LDD0819  [1]
 LDCM0222  AC106 HEK-293T C726(0.86)  LDD0820  [1]
 LDCM0223  AC107 HEK-293T C726(1.04)  LDD0821  [1]
 LDCM0224  AC108 HEK-293T C726(0.79)  LDD0822  [1]
 LDCM0225  AC109 HEK-293T C726(1.14)  LDD0823  [1]
 LDCM0226  AC11 HCT 116 C726(0.96)  LDD0543  [1]
 LDCM0227  AC110 HEK-293T C726(1.17)  LDD0825  [1]
 LDCM0228  AC111 HEK-293T C726(1.32)  LDD0826  [1]
 LDCM0229  AC112 HEK-293T C726(1.18)  LDD0827  [1]
 LDCM0230  AC113 HCT 116 C726(1.03)  LDD0547  [1]
 LDCM0231  AC114 HCT 116 C726(0.90)  LDD0548  [1]
 LDCM0232  AC115 HCT 116 C726(1.43)  LDD0549  [1]
 LDCM0233  AC116 HCT 116 C726(0.99)  LDD0550  [1]
 LDCM0234  AC117 HCT 116 C726(1.11)  LDD0551  [1]
 LDCM0235  AC118 HCT 116 C726(1.22)  LDD0552  [1]
 LDCM0236  AC119 HCT 116 C726(1.06)  LDD0553  [1]
 LDCM0237  AC12 HCT 116 C726(0.92)  LDD0554  [1]
 LDCM0238  AC120 HCT 116 C726(1.21)  LDD0555  [1]
 LDCM0239  AC121 HCT 116 C726(0.82)  LDD0556  [1]
 LDCM0240  AC122 HCT 116 C726(0.91)  LDD0557  [1]
 LDCM0241  AC123 HCT 116 C726(0.70)  LDD0558  [1]
 LDCM0242  AC124 HCT 116 C726(0.78)  LDD0559  [1]
 LDCM0243  AC125 HCT 116 C726(0.84)  LDD0560  [1]
 LDCM0244  AC126 HCT 116 C726(0.90)  LDD0561  [1]
 LDCM0245  AC127 HCT 116 C726(0.89)  LDD0562  [1]
 LDCM0246  AC128 HEK-293T C726(0.90)  LDD0844  [1]
 LDCM0247  AC129 HEK-293T C726(0.86)  LDD0845  [1]
 LDCM0249  AC130 HEK-293T C726(1.03)  LDD0847  [1]
 LDCM0250  AC131 HEK-293T C726(0.74)  LDD0848  [1]
 LDCM0251  AC132 HEK-293T C726(0.94)  LDD0849  [1]
 LDCM0252  AC133 HEK-293T C726(1.19)  LDD0850  [1]
 LDCM0253  AC134 HEK-293T C726(1.01)  LDD0851  [1]
 LDCM0254  AC135 HEK-293T C726(0.93)  LDD0852  [1]
 LDCM0255  AC136 HEK-293T C726(0.94)  LDD0853  [1]
 LDCM0256  AC137 HEK-293T C726(1.11)  LDD0854  [1]
 LDCM0257  AC138 HEK-293T C726(1.20)  LDD0855  [1]
 LDCM0258  AC139 HEK-293T C726(1.07)  LDD0856  [1]
 LDCM0259  AC14 HCT 116 C726(1.09)  LDD0576  [1]
 LDCM0260  AC140 HEK-293T C726(0.90)  LDD0858  [1]
 LDCM0261  AC141 HEK-293T C726(1.08)  LDD0859  [1]
 LDCM0262  AC142 HEK-293T C726(1.14)  LDD0860  [1]
 LDCM0263  AC143 HCT 116 C726(1.13)  LDD0580  [1]
 LDCM0264  AC144 HCT 116 C726(1.13)  LDD0581  [1]
 LDCM0265  AC145 HCT 116 C726(1.19)  LDD0582  [1]
 LDCM0266  AC146 HCT 116 C726(1.50)  LDD0583  [1]
 LDCM0267  AC147 HCT 116 C726(1.09)  LDD0584  [1]
 LDCM0268  AC148 HCT 116 C726(1.71)  LDD0585  [1]
 LDCM0269  AC149 HCT 116 C726(1.67)  LDD0586  [1]
 LDCM0270  AC15 HCT 116 C726(0.88)  LDD0587  [1]
 LDCM0271  AC150 HCT 116 C726(1.15)  LDD0588  [1]
 LDCM0272  AC151 HCT 116 C726(1.14)  LDD0589  [1]
 LDCM0273  AC152 HCT 116 C726(1.24)  LDD0590  [1]
 LDCM0274  AC153 HCT 116 C726(1.77)  LDD0591  [1]
 LDCM0621  AC154 HCT 116 C726(1.12)  LDD2158  [1]
 LDCM0622  AC155 HCT 116 C726(1.36)  LDD2159  [1]
 LDCM0623  AC156 HCT 116 C726(1.17)  LDD2160  [1]
 LDCM0624  AC157 HCT 116 C726(1.33)  LDD2161  [1]
 LDCM0276  AC17 HCT 116 C726(0.94)  LDD0593  [1]
 LDCM0277  AC18 HCT 116 C726(0.85)  LDD0594  [1]
 LDCM0278  AC19 HCT 116 C726(0.98)  LDD0595  [1]
 LDCM0279  AC2 HCT 116 C726(1.33)  LDD0596  [1]
 LDCM0280  AC20 HCT 116 C726(0.90)  LDD0597  [1]
 LDCM0281  AC21 HCT 116 C726(0.89)  LDD0598  [1]
 LDCM0282  AC22 HCT 116 C726(0.90)  LDD0599  [1]
 LDCM0283  AC23 HCT 116 C726(0.86)  LDD0600  [1]
 LDCM0284  AC24 HCT 116 C726(0.90)  LDD0601  [1]
 LDCM0285  AC25 HCT 116 C726(1.02)  LDD0602  [1]
 LDCM0286  AC26 HCT 116 C726(1.17)  LDD0603  [1]
 LDCM0287  AC27 HCT 116 C726(0.91)  LDD0604  [1]
 LDCM0288  AC28 HCT 116 C726(1.15)  LDD0605  [1]
 LDCM0289  AC29 HCT 116 C726(1.42)  LDD0606  [1]
 LDCM0290  AC3 HCT 116 C726(1.27)  LDD0607  [1]
 LDCM0291  AC30 HCT 116 C726(1.12)  LDD0608  [1]
 LDCM0292  AC31 HCT 116 C726(0.98)  LDD0609  [1]
 LDCM0293  AC32 HCT 116 C726(1.02)  LDD0610  [1]
 LDCM0294  AC33 HCT 116 C726(1.20)  LDD0611  [1]
 LDCM0295  AC34 HCT 116 C726(1.16)  LDD0612  [1]
 LDCM0296  AC35 HCT 116 C726(0.68)  LDD0613  [1]
 LDCM0297  AC36 HCT 116 C726(0.83)  LDD0614  [1]
 LDCM0298  AC37 HCT 116 C726(0.88)  LDD0615  [1]
 LDCM0299  AC38 HCT 116 C726(0.78)  LDD0616  [1]
 LDCM0300  AC39 HCT 116 C726(1.26)  LDD0617  [1]
 LDCM0301  AC4 HCT 116 C726(1.24)  LDD0618  [1]
 LDCM0302  AC40 HCT 116 C726(1.04)  LDD0619  [1]
 LDCM0303  AC41 HCT 116 C726(0.93)  LDD0620  [1]
 LDCM0304  AC42 HCT 116 C726(1.05)  LDD0621  [1]
 LDCM0305  AC43 HCT 116 C726(1.08)  LDD0622  [1]
 LDCM0306  AC44 HCT 116 C726(1.32)  LDD0623  [1]
 LDCM0307  AC45 HCT 116 C726(1.28)  LDD0624  [1]
 LDCM0308  AC46 HCT 116 C726(1.13)  LDD0625  [1]
 LDCM0309  AC47 HCT 116 C726(1.20)  LDD0626  [1]
 LDCM0310  AC48 HCT 116 C726(0.89)  LDD0627  [1]
 LDCM0311  AC49 HCT 116 C726(1.19)  LDD0628  [1]
 LDCM0312  AC5 HCT 116 C726(1.44)  LDD0629  [1]
 LDCM0313  AC50 HCT 116 C726(1.07)  LDD0630  [1]
 LDCM0314  AC51 HCT 116 C726(0.82)  LDD0631  [1]
 LDCM0315  AC52 HCT 116 C726(0.97)  LDD0632  [1]
 LDCM0316  AC53 HCT 116 C726(1.19)  LDD0633  [1]
 LDCM0317  AC54 HCT 116 C726(1.13)  LDD0634  [1]
 LDCM0318  AC55 HCT 116 C726(1.39)  LDD0635  [1]
 LDCM0319  AC56 HCT 116 C726(1.37)  LDD0636  [1]
 LDCM0320  AC57 HCT 116 C726(1.14)  LDD0637  [1]
 LDCM0321  AC58 HCT 116 C726(1.84)  LDD0638  [1]
 LDCM0322  AC59 HCT 116 C726(1.49)  LDD0639  [1]
 LDCM0323  AC6 HCT 116 C726(1.23)  LDD0640  [1]
 LDCM0324  AC60 HCT 116 C726(1.77)  LDD0641  [1]
 LDCM0325  AC61 HCT 116 C726(1.06)  LDD0642  [1]
 LDCM0326  AC62 HCT 116 C726(1.27)  LDD0643  [1]
 LDCM0327  AC63 HCT 116 C726(1.38)  LDD0644  [1]
 LDCM0328  AC64 HCT 116 C726(1.90)  LDD0645  [1]
 LDCM0329  AC65 HCT 116 C726(1.50)  LDD0646  [1]
 LDCM0330  AC66 HCT 116 C726(1.31)  LDD0647  [1]
 LDCM0331  AC67 HCT 116 C726(1.48)  LDD0648  [1]
 LDCM0332  AC68 HCT 116 C726(1.16)  LDD0649  [1]
 LDCM0333  AC69 HCT 116 C726(1.24)  LDD0650  [1]
 LDCM0334  AC7 HCT 116 C726(0.90)  LDD0651  [1]
 LDCM0335  AC70 HCT 116 C726(1.52)  LDD0652  [1]
 LDCM0336  AC71 HCT 116 C726(1.27)  LDD0653  [1]
 LDCM0337  AC72 HCT 116 C726(1.34)  LDD0654  [1]
 LDCM0338  AC73 HCT 116 C726(1.89)  LDD0655  [1]
 LDCM0339  AC74 HCT 116 C726(1.49)  LDD0656  [1]
 LDCM0340  AC75 HCT 116 C726(1.60)  LDD0657  [1]
 LDCM0341  AC76 HCT 116 C726(1.41)  LDD0658  [1]
 LDCM0342  AC77 HCT 116 C726(1.50)  LDD0659  [1]
 LDCM0343  AC78 HCT 116 C726(1.26)  LDD0660  [1]
 LDCM0344  AC79 HCT 116 C726(1.11)  LDD0661  [1]
 LDCM0345  AC8 HCT 116 C726(0.89)  LDD0662  [1]
 LDCM0346  AC80 HCT 116 C726(1.45)  LDD0663  [1]
 LDCM0347  AC81 HCT 116 C726(1.10)  LDD0664  [1]
 LDCM0348  AC82 HCT 116 C726(1.63)  LDD0665  [1]
 LDCM0349  AC83 HCT 116 C726(1.19)  LDD0666  [1]
 LDCM0350  AC84 HCT 116 C726(1.07)  LDD0667  [1]
 LDCM0351  AC85 HCT 116 C726(0.99)  LDD0668  [1]
 LDCM0352  AC86 HCT 116 C726(0.77)  LDD0669  [1]
 LDCM0353  AC87 HCT 116 C726(2.06)  LDD0670  [1]
 LDCM0354  AC88 HCT 116 C726(0.90)  LDD0671  [1]
 LDCM0355  AC89 HCT 116 C726(0.96)  LDD0672  [1]
 LDCM0357  AC90 HCT 116 C726(1.26)  LDD0674  [1]
 LDCM0358  AC91 HCT 116 C726(0.95)  LDD0675  [1]
 LDCM0359  AC92 HCT 116 C726(1.14)  LDD0676  [1]
 LDCM0360  AC93 HCT 116 C726(0.91)  LDD0677  [1]
 LDCM0361  AC94 HCT 116 C726(1.13)  LDD0678  [1]
 LDCM0362  AC95 HCT 116 C726(0.90)  LDD0679  [1]
 LDCM0363  AC96 HCT 116 C726(0.69)  LDD0680  [1]
 LDCM0364  AC97 HCT 116 C726(1.03)  LDD0681  [1]
 LDCM0365  AC98 HEK-293T C726(1.02)  LDD0963  [1]
 LDCM0366  AC99 HEK-293T C726(1.00)  LDD0964  [1]
 LDCM0248  AKOS034007472 HCT 116 C726(0.98)  LDD0565  [1]
 LDCM0356  AKOS034007680 HCT 116 C726(1.52)  LDD0673  [1]
 LDCM0275  AKOS034007705 HCT 116 C726(1.36)  LDD0592  [1]
 LDCM0108  Chloroacetamide HeLa H428(0.00); H694(0.00); C151(0.00); H182(0.00)  LDD0222  [5]
 LDCM0367  CL1 HCT 116 C726(1.12)  LDD0684  [1]
 LDCM0368  CL10 HCT 116 C726(2.02)  LDD0685  [1]
 LDCM0369  CL100 HCT 116 C726(1.17)  LDD0686  [1]
 LDCM0370  CL101 HCT 116 C726(0.85)  LDD0687  [1]
 LDCM0371  CL102 HCT 116 C726(1.32)  LDD0688  [1]
 LDCM0372  CL103 HCT 116 C726(1.42)  LDD0689  [1]
 LDCM0373  CL104 HCT 116 C726(1.34)  LDD0690  [1]
 LDCM0374  CL105 HCT 116 C726(0.90)  LDD0691  [1]
 LDCM0375  CL106 HCT 116 C726(1.14)  LDD0692  [1]
 LDCM0376  CL107 HCT 116 C726(1.07)  LDD0693  [1]
 LDCM0377  CL108 HCT 116 C726(0.91)  LDD0694  [1]
 LDCM0378  CL109 HCT 116 C726(0.97)  LDD0695  [1]
 LDCM0379  CL11 HCT 116 C726(1.02)  LDD0696  [1]
 LDCM0380  CL110 HCT 116 C726(1.06)  LDD0697  [1]
 LDCM0381  CL111 HCT 116 C726(0.95)  LDD0698  [1]
 LDCM0382  CL112 HCT 116 C726(0.85)  LDD0699  [1]
 LDCM0383  CL113 HCT 116 C726(0.92)  LDD0700  [1]
 LDCM0384  CL114 HCT 116 C726(1.33)  LDD0701  [1]
 LDCM0385  CL115 HCT 116 C726(0.93)  LDD0702  [1]
 LDCM0386  CL116 HCT 116 C726(1.11)  LDD0703  [1]
 LDCM0387  CL117 HCT 116 C726(1.33)  LDD0704  [1]
 LDCM0388  CL118 HCT 116 C726(0.80)  LDD0705  [1]
 LDCM0389  CL119 HCT 116 C726(0.95)  LDD0706  [1]
 LDCM0390  CL12 HCT 116 C726(1.74)  LDD0707  [1]
 LDCM0391  CL120 HCT 116 C726(1.11)  LDD0708  [1]
 LDCM0392  CL121 HCT 116 C726(0.65)  LDD0709  [1]
 LDCM0393  CL122 HCT 116 C726(1.16)  LDD0710  [1]
 LDCM0394  CL123 HCT 116 C726(1.17)  LDD0711  [1]
 LDCM0395  CL124 HCT 116 C726(1.61)  LDD0712  [1]
 LDCM0396  CL125 HCT 116 C726(0.79)  LDD0713  [1]
 LDCM0397  CL126 HCT 116 C726(0.90)  LDD0714  [1]
 LDCM0398  CL127 HCT 116 C726(0.75)  LDD0715  [1]
 LDCM0399  CL128 HCT 116 C726(1.89)  LDD0716  [1]
 LDCM0400  CL13 HCT 116 C726(0.95)  LDD0717  [1]
 LDCM0401  CL14 HCT 116 C726(0.90)  LDD0718  [1]
 LDCM0402  CL15 HCT 116 C726(0.88)  LDD0719  [1]
 LDCM0403  CL16 HCT 116 C726(1.10)  LDD0720  [1]
 LDCM0404  CL17 HCT 116 C726(0.76)  LDD0721  [1]
 LDCM0405  CL18 HCT 116 C726(1.34)  LDD0722  [1]
 LDCM0406  CL19 HCT 116 C726(1.35)  LDD0723  [1]
 LDCM0407  CL2 HCT 116 C726(1.14)  LDD0724  [1]
 LDCM0408  CL20 HCT 116 C726(1.41)  LDD0725  [1]
 LDCM0409  CL21 HCT 116 C726(0.80)  LDD0726  [1]
 LDCM0410  CL22 HCT 116 C726(1.49)  LDD0727  [1]
 LDCM0411  CL23 HCT 116 C726(1.31)  LDD0728  [1]
 LDCM0412  CL24 HCT 116 C726(1.35)  LDD0729  [1]
 LDCM0413  CL25 HCT 116 C726(1.15)  LDD0730  [1]
 LDCM0414  CL26 HCT 116 C726(1.09)  LDD0731  [1]
 LDCM0415  CL27 HCT 116 C726(1.97)  LDD0732  [1]
 LDCM0416  CL28 HCT 116 C726(0.85)  LDD0733  [1]
 LDCM0417  CL29 HCT 116 C726(1.55)  LDD0734  [1]
 LDCM0418  CL3 HCT 116 C726(1.55)  LDD0735  [1]
 LDCM0419  CL30 HCT 116 C726(1.17)  LDD0736  [1]
 LDCM0420  CL31 HCT 116 C726(1.21)  LDD0737  [1]
 LDCM0421  CL32 HCT 116 C726(1.02)  LDD0738  [1]
 LDCM0422  CL33 HCT 116 C726(1.25)  LDD0739  [1]
 LDCM0423  CL34 HCT 116 C726(1.00)  LDD0740  [1]
 LDCM0424  CL35 HCT 116 C726(1.40)  LDD0741  [1]
 LDCM0425  CL36 HCT 116 C726(1.22)  LDD0742  [1]
 LDCM0426  CL37 HCT 116 C726(1.27)  LDD0743  [1]
 LDCM0428  CL39 HCT 116 C726(1.39)  LDD0745  [1]
 LDCM0429  CL4 HCT 116 C726(1.48)  LDD0746  [1]
 LDCM0430  CL40 HCT 116 C726(1.45)  LDD0747  [1]
 LDCM0431  CL41 HCT 116 C726(1.17)  LDD0748  [1]
 LDCM0432  CL42 HCT 116 C726(1.09)  LDD0749  [1]
 LDCM0433  CL43 HCT 116 C726(1.15)  LDD0750  [1]
 LDCM0434  CL44 HCT 116 C726(1.09)  LDD0751  [1]
 LDCM0435  CL45 HCT 116 C726(1.23)  LDD0752  [1]
 LDCM0436  CL46 HCT 116 C726(1.13)  LDD0753  [1]
 LDCM0437  CL47 HCT 116 C726(1.22)  LDD0754  [1]
 LDCM0438  CL48 HCT 116 C726(1.12)  LDD0755  [1]
 LDCM0439  CL49 HCT 116 C726(0.90)  LDD0756  [1]
 LDCM0440  CL5 HCT 116 C726(1.19)  LDD0757  [1]
 LDCM0441  CL50 HCT 116 C726(1.59)  LDD0758  [1]
 LDCM0442  CL51 HCT 116 C726(1.02)  LDD0759  [1]
 LDCM0443  CL52 HCT 116 C726(1.10)  LDD0760  [1]
 LDCM0444  CL53 HCT 116 C726(1.03)  LDD0761  [1]
 LDCM0445  CL54 HCT 116 C726(1.00)  LDD0762  [1]
 LDCM0446  CL55 HCT 116 C726(1.07)  LDD0763  [1]
 LDCM0447  CL56 HCT 116 C726(1.22)  LDD0764  [1]
 LDCM0448  CL57 HCT 116 C726(1.14)  LDD0765  [1]
 LDCM0449  CL58 HCT 116 C726(1.11)  LDD0766  [1]
 LDCM0450  CL59 HCT 116 C726(1.42)  LDD0767  [1]
 LDCM0451  CL6 HCT 116 C726(1.24)  LDD0768  [1]
 LDCM0452  CL60 HCT 116 C726(1.47)  LDD0769  [1]
 LDCM0453  CL61 HCT 116 C726(1.25)  LDD0770  [1]
 LDCM0454  CL62 HCT 116 C726(1.12)  LDD0771  [1]
 LDCM0455  CL63 HCT 116 C726(0.97)  LDD0772  [1]
 LDCM0456  CL64 HCT 116 C726(1.25)  LDD0773  [1]
 LDCM0457  CL65 HCT 116 C726(2.36)  LDD0774  [1]
 LDCM0458  CL66 HCT 116 C726(1.67)  LDD0775  [1]
 LDCM0459  CL67 HCT 116 C726(1.18)  LDD0776  [1]
 LDCM0460  CL68 HCT 116 C726(1.68)  LDD0777  [1]
 LDCM0461  CL69 HCT 116 C726(1.18)  LDD0778  [1]
 LDCM0462  CL7 HCT 116 C726(0.94)  LDD0779  [1]
 LDCM0463  CL70 HCT 116 C726(1.04)  LDD0780  [1]
 LDCM0464  CL71 HCT 116 C726(1.25)  LDD0781  [1]
 LDCM0465  CL72 HCT 116 C726(1.27)  LDD0782  [1]
 LDCM0466  CL73 HCT 116 C726(1.87)  LDD0783  [1]
 LDCM0467  CL74 HCT 116 C726(1.47)  LDD0784  [1]
 LDCM0469  CL76 HEK-293T C726(1.02)  LDD1067  [1]
 LDCM0470  CL77 HEK-293T C726(1.04)  LDD1068  [1]
 LDCM0471  CL78 HEK-293T C726(0.88)  LDD1069  [1]
 LDCM0472  CL79 HEK-293T C726(1.01)  LDD1070  [1]
 LDCM0473  CL8 HCT 116 C726(1.44)  LDD0790  [1]
 LDCM0474  CL80 HEK-293T C726(0.98)  LDD1072  [1]
 LDCM0475  CL81 HEK-293T C726(1.01)  LDD1073  [1]
 LDCM0476  CL82 HEK-293T C726(1.08)  LDD1074  [1]
 LDCM0477  CL83 HEK-293T C726(0.93)  LDD1075  [1]
 LDCM0478  CL84 HEK-293T C726(0.90)  LDD1076  [1]
 LDCM0479  CL85 HEK-293T C726(0.97)  LDD1077  [1]
 LDCM0480  CL86 HEK-293T C726(0.94)  LDD1078  [1]
 LDCM0481  CL87 HEK-293T C726(1.06)  LDD1079  [1]
 LDCM0482  CL88 HEK-293T C726(1.10)  LDD1080  [1]
 LDCM0483  CL89 HEK-293T C726(1.18)  LDD1081  [1]
 LDCM0484  CL9 HCT 116 C726(1.05)  LDD0801  [1]
 LDCM0485  CL90 HEK-293T C726(1.17)  LDD1083  [1]
 LDCM0486  CL91 HCT 116 C726(1.25)  LDD0803  [1]
 LDCM0487  CL92 HCT 116 C726(1.25)  LDD0804  [1]
 LDCM0488  CL93 HCT 116 C726(1.20)  LDD0805  [1]
 LDCM0489  CL94 HCT 116 C726(1.58)  LDD0806  [1]
 LDCM0490  CL95 HCT 116 C726(1.43)  LDD0807  [1]
 LDCM0491  CL96 HCT 116 C726(1.41)  LDD0808  [1]
 LDCM0492  CL97 HCT 116 C726(1.13)  LDD0809  [1]
 LDCM0493  CL98 HCT 116 C726(1.72)  LDD0810  [1]
 LDCM0494  CL99 HCT 116 C726(1.51)  LDD0811  [1]
 LDCM0495  E2913 HEK-293T C726(1.06)  LDD1698  [10]
 LDCM0468  Fragment33 HCT 116 C726(1.21)  LDD0785  [1]
 LDCM0427  Fragment51 HCT 116 C726(1.22)  LDD0744  [1]
 LDCM0107  IAA HeLa H428(0.00); H442(0.00); H261(0.00); H182(0.00)  LDD0221  [5]
 LDCM0022  KB02 HCT 116 C726(2.24)  LDD0080  [1]
 LDCM0023  KB03 HCT 116 C726(1.28)  LDD0081  [1]
 LDCM0024  KB05 HCT 116 C726(1.71)  LDD0082  [1]
 LDCM0109  NEM HeLa H428(0.00); H261(0.00); H698(0.00); H694(0.00)  LDD0223  [5]
 LDCM0627  NUDT7-COV-1 HEK-293T C726(0.98)  LDD2206  [11]
 LDCM0628  OTUB2-COV-1 HEK-293T C726(0.72)  LDD2207  [11]
 LDCM0131  RA190 MM1.R C726(0.98)  LDD0304  [12]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aldesleukin BiotechDrug DB00041
Streptokinase Protein/peptide DB00086
Carbamoylcholine Small molecular drug DB00411
Carbenicillin Small molecular drug DB00578
Epirubicin Small molecular drug DB00445
Fluticasone Small molecular drug DB13867
Fluticasone Propionate Small molecular drug DB00588
Orlistat Small molecular drug DB01083
Procaine Small molecular drug DB00721
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Zpl521 . D02XBN
Investigative
Click To Hide/Show 48 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(S)-ethyl 6-(2-oxohexadecanamido)Decanoate Small molecular drug D0B2RW
(S)-methyl 4-(2-oxohexadecanamido)Octanoate Small molecular drug D0K2PI
(S)-tert-butyl 4-(2-oxohexadecanamido)Pentanoate Small molecular drug D0U1YU
(Z)-1,1,1,2,2,3,3-heptafluorohenicos-12-en-4-one Small molecular drug D0D2SE
1,1,1,2,2,3,3,5-octafluoro-8-phenyloctan-4-one Small molecular drug D0P9CN
1,1,1,2,2,3,3-heptafluoro-8-phenyloctan-4-ol Small molecular drug D0UV2N
1,1,1,2,2,4-hexafluoro-7-phenylheptan-3-one Small molecular drug D09ZUX
1,1,1,2,2-pentafluoro-8-phenyl-octan-3-one Small molecular drug D0U2QY
1,1,1,2,2-pentafluoro-9-phenyl-nonan-3-one Small molecular drug D05MUN
1,1,1,3-tetrafluoro-6-phenylhexan-2-one Small molecular drug D05TGU
1,1,1,3-tetrafluoro-7-phenylheptan-2-one Small molecular drug D03FQJ
1,1,1,3-tetrafluoro-heptadecan-2-one Small molecular drug D09CVD
1,1,1-trifluoro-4-(4-hexyloxy-phenyl)-butan-2-one Small molecular drug D08SIJ
1,1,1-trifluoro-5-(4-octylphenoxy)Pentan-2-one Small molecular drug D0F7IW
1,1,1-trifluoro-6-(4-hexyloxy-phenyl)-hexan-2-one Small molecular drug D06XFP
1,1,1-trifluoro-6-(Naphthalen-2-yl)Hexan-2-one Small molecular drug D03DIV
1,1,1-trifluoro-7-phenylheptan-2-one Small molecular drug D08YHD
1,1,1-trifluoroheptadecan-2-one Small molecular drug D0R3AA
1-imidazol-1-yl-3-(4-octylphenoxy)Propan-2-one Small molecular drug D0Y2BD
4-(2-oxohexadecanamido)Butanoic Acid Small molecular drug D03NYE
4-(4-decyloxy-phenyl)-1,1,1-trifluoro-butan-2-one Small molecular drug D0U2GX
6-(4-decyloxy-phenyl)-1,1,1-trifluoro-hexan-2-one Small molecular drug D0F4WJ
Allyl 4-(2-oxohexadecanamido)Butanoate Small molecular drug D0ND4N
Ar-c70484xx Small molecular drug D0W4VM
Arachidonyl Trifluoromethylketone Small molecular drug D0J8TY
Ax-006 Small molecular drug D00GQP
Ax-048 Small molecular drug D05GUD
Darapladib Small molecular drug DB06311
Ecopladib Small molecular drug D0P5UW
Ethyl 2-(2-oxohexadecanamido)Acetate Small molecular drug D0K0HD
Ethyl 4-(2-oxohexadecanamido)Benzoate Small molecular drug D0Q1LD
Methyl 2-(2-oxo-8-phenyloctanamido)Acetate Small molecular drug D0PP8T
Methyl 2-(2-oxohexadecanamido)Acetate Small molecular drug D07QSM
Methyl Arachidonyl Fluorophosphonate Small molecular drug D0V6QA
N-(4-ethoxybutyl)-2-oxohexadecanamide Small molecular drug D01GZV
Niflumic Acid Small molecular drug DB04552
Quinacrine Small molecular drug DB01103
Suramin Small molecular drug DB04786
Tert-butyl 2-(2-oxohexadecanamido)Acetate Small molecular drug D07TCK
Tert-butyl 3-(2-oxo-8-phenyloctanamido)Propanoate Small molecular drug D05TZP
Tert-butyl 3-(2-oxohexadecanamido)Propanoate Small molecular drug D06OXA
Tert-butyl 5-(2-oxohexadecanamido)Pentanoate Small molecular drug D05BTF
Way-196025 Small molecular drug D0F9PM
[3,4''biflavone Small molecular drug D02GTZ
[4',4''-biflavone Small molecular drug D0L6GV
[6,3''biflavone Small molecular drug D07VJT
[6,4''biflavone Small molecular drug D05LWK
1,1,1-trifluoro-8-phenyl-octan-2-one . D0N1CK
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Efipladib Small molecular drug D0E1WY

References

1 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.
2 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
3 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
4 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
5 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.
6 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.
7 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.
8 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
9 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.
10 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
11 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.
12 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.