Details of the Target

General Information of Target

Target ID LDTP01664
Target Name Serine/threonine-protein kinase OSR1 (OXSR1)
Gene Name OXSR1
Gene ID 9943
Synonyms
KIAA1101; OSR1; Serine/threonine-protein kinase OSR1; EC 2.7.11.1; Oxidative stress-responsive 1 protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSEDSSALPWSINRDDYELQEVIGSGATAVVQAAYCAPKKEKVAIKRINLEKCQTSMDEL
LKEIQAMSQCHHPNIVSYYTSFVVKDELWLVMKLLSGGSVLDIIKHIVAKGEHKSGVLDE
STIATILREVLEGLEYLHKNGQIHRDVKAGNILLGEDGSVQIADFGVSAFLATGGDITRN
KVRKTFVGTPCWMAPEVMEQVRGYDFKADIWSFGITAIELATGAAPYHKYPPMKVLMLTL
QNDPPSLETGVQDKEMLKKYGKSFRKMISLCLQKDPEKRPTAAELLRHKFFQKAKNKEFL
QEKTLQRAPTISERAKKVRRVPGSSGRLHKTEDGGWEWSDDEFDEESEEGKAAISQLRSP
RVKESISNSELFPTTDPVGTLLQVPEQISAHLPQPAGQIATQPTQVSLPPTAEPAKTAQA
LSSGSGSQETKIPISLVLRLRNSKKELNDIRFEFTPGRDTAEGVSQELISAGLVDGRDLV
IVAANLQKIVEEPQSNRSVTFKLASGVEGSDIPDDGKLIGFAQLSIS
Target Type
Literature-reported
Target Bioclass
Enzyme
Family
Protein kinase superfamily, STE Ser/Thr protein kinase family, STE20 subfamily
Subcellular location
Cytoplasm
Function
Effector serine/threonine-protein kinase component of the WNK-SPAK/OSR1 kinase cascade, which is involved in various processes, such as ion transport, response to hypertonic stress and blood pressure. Specifically recognizes and binds proteins with a RFXV motif. Acts downstream of WNK kinases (WNK1, WNK2, WNK3 or WNK4): following activation by WNK kinases, catalyzes phosphorylation of ion cotransporters, such as SLC12A1/NKCC2, SLC12A2/NKCC1, SLC12A3/NCC, SLC12A5/KCC2 or SLC12A6/KCC3, regulating their activity. Mediates regulatory volume increase in response to hyperosmotic stress by catalyzing phosphorylation of ion cotransporters SLC12A1/NKCC2, SLC12A2/NKCC1 and SLC12A6/KCC3 downstream of WNK1 and WNK3 kinases. Phosphorylation of Na-K-Cl cotransporters SLC12A2/NKCC1 and SLC12A2/NKCC1 promote their activation and ion influx; simultaneously, phosphorylation of K-Cl cotransporters SLC12A5/KCC2 and SLC12A6/KCC3 inhibit their activity, blocking ion efflux. Acts as a regulator of NaCl reabsorption in the distal nephron by mediating phosphorylation and activation of the thiazide-sensitive Na-Cl cotransporter SLC12A3/NCC in distal convoluted tubule cells of kidney downstream of WNK4. Also acts as a regulator of angiogenesis in endothelial cells downstream of WNK1. Acts as an activator of inward rectifier potassium channels KCNJ2/Kir2.1 and KCNJ4/Kir2.3 downstream of WNK1: recognizes and binds the RXFXV/I variant motif on KCNJ2/Kir2.1 and KCNJ4/Kir2.3 and regulates their localization to the cell membrane without mediating their phosphorylation. Phosphorylates RELL1, RELL2 and RELT. Phosphorylates PAK1. Phosphorylates PLSCR1 in the presence of RELT.
TTD ID
T08198
Uniprot ID
O95747
DrugMap ID
TT7ZY03
Ensemble ID
ENST00000311806.8
HGNC ID
HGNC:8508
ChEMBL ID
CHEMBL1163104

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 17 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
TH211
 Probe Info  		Y227(6.28)  LDD0260  [2]
YN-1
 Probe Info  		100.00  LDD0444  [3]
STPyne
 Probe Info  		K266(9.43); K289(3.39); K295(4.30); K303(3.90)  LDD0277  [4]
IPM
 Probe Info  		C53(0.00); C271(0.00)  LDD0241  [5]
BTD
 Probe Info  		C53(1.04)  LDD2089  [6]
EA-probe
 Probe Info  		C191(0.88)  LDD2210  [7]
DBIA
 Probe Info  		C271(1.26)  LDD0080  [8]
5E-2FA
 Probe Info  		N.A.  LDD2235  [9]
ATP probe
 Probe Info  		K52(0.00); K266(0.00); K184(0.00)  LDD0199  [10]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [11]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [11]
Lodoacetamide azide
 Probe Info  		C53(0.00); C271(0.00); C191(0.00)  LDD0037  [11]
ENE
 Probe Info  		N.A.  LDD0006  [12]
Acrolein
 Probe Info  		C191(0.00); H138(0.00)  LDD0217  [13]
W1
 Probe Info  		C191(0.00); C271(0.00)  LDD0236  [5]
NAIA_5
 Probe Info  		C53(0.00); C191(0.00); C36(0.00)  LDD2223  [14]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C296
 Probe Info  		14.32  LDD1966  [15]
C407
 Probe Info  		10.85  LDD2064  [15]
STS-2
 Probe Info  		N.A.  LDD0138  [16]
Probe 12
 Probe Info  		N.A.  LDD0420  [17]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C53(1.22); C271(1.27)  LDD2117  [6]
 LDCM0214  AC1 HCT 116 C271(0.78)  LDD0531  [8]
 LDCM0215  AC10 HCT 116 C271(0.89)  LDD0532  [8]
 LDCM0216  AC100 HCT 116 C271(0.34)  LDD0533  [8]
 LDCM0217  AC101 HCT 116 C271(0.38)  LDD0534  [8]
 LDCM0218  AC102 HCT 116 C271(0.32)  LDD0535  [8]
 LDCM0219  AC103 HCT 116 C271(0.26)  LDD0536  [8]
 LDCM0220  AC104 HCT 116 C271(0.25)  LDD0537  [8]
 LDCM0221  AC105 HCT 116 C271(0.26)  LDD0538  [8]
 LDCM0222  AC106 HCT 116 C271(0.25)  LDD0539  [8]
 LDCM0223  AC107 HCT 116 C271(0.53)  LDD0540  [8]
 LDCM0224  AC108 HCT 116 C271(0.70)  LDD0541  [8]
 LDCM0225  AC109 HCT 116 C271(0.68)  LDD0542  [8]
 LDCM0226  AC11 HCT 116 C271(0.74)  LDD0543  [8]
 LDCM0227  AC110 HCT 116 C271(0.63)  LDD0544  [8]
 LDCM0228  AC111 HCT 116 C271(0.58)  LDD0545  [8]
 LDCM0229  AC112 HCT 116 C271(0.59)  LDD0546  [8]
 LDCM0230  AC113 HEK-293T C271(1.01)  LDD0828  [8]
 LDCM0231  AC114 HEK-293T C271(1.11)  LDD0829  [8]
 LDCM0232  AC115 HEK-293T C271(1.15)  LDD0830  [8]
 LDCM0233  AC116 HEK-293T C271(1.32)  LDD0831  [8]
 LDCM0234  AC117 HEK-293T C271(0.94)  LDD0832  [8]
 LDCM0235  AC118 HEK-293T C271(1.47)  LDD0833  [8]
 LDCM0236  AC119 HEK-293T C271(0.99)  LDD0834  [8]
 LDCM0237  AC12 HCT 116 C271(0.83)  LDD0554  [8]
 LDCM0238  AC120 HEK-293T C271(1.01)  LDD0836  [8]
 LDCM0239  AC121 HEK-293T C271(0.93)  LDD0837  [8]
 LDCM0240  AC122 HEK-293T C271(0.93)  LDD0838  [8]
 LDCM0241  AC123 HEK-293T C271(1.00)  LDD0839  [8]
 LDCM0242  AC124 HEK-293T C271(0.98)  LDD0840  [8]
 LDCM0243  AC125 HEK-293T C271(0.99)  LDD0841  [8]
 LDCM0244  AC126 HEK-293T C271(1.04)  LDD0842  [8]
 LDCM0245  AC127 HEK-293T C271(1.15)  LDD0843  [8]
 LDCM0246  AC128 HCT 116 C271(1.13)  LDD0563  [8]
 LDCM0247  AC129 HCT 116 C271(1.26)  LDD0564  [8]
 LDCM0249  AC130 HCT 116 C271(0.96)  LDD0566  [8]
 LDCM0250  AC131 HCT 116 C271(1.07)  LDD0567  [8]
 LDCM0251  AC132 HCT 116 C271(1.19)  LDD0568  [8]
 LDCM0252  AC133 HCT 116 C271(0.97)  LDD0569  [8]
 LDCM0253  AC134 HCT 116 C271(0.99)  LDD0570  [8]
 LDCM0254  AC135 HCT 116 C271(0.97)  LDD0571  [8]
 LDCM0255  AC136 HCT 116 C271(1.04)  LDD0572  [8]
 LDCM0256  AC137 HCT 116 C271(1.06)  LDD0573  [8]
 LDCM0257  AC138 HCT 116 C271(1.07)  LDD0574  [8]
 LDCM0258  AC139 HCT 116 C271(0.99)  LDD0575  [8]
 LDCM0259  AC14 HCT 116 C271(0.80)  LDD0576  [8]
 LDCM0260  AC140 HCT 116 C271(0.97)  LDD0577  [8]
 LDCM0261  AC141 HCT 116 C271(0.95)  LDD0578  [8]
 LDCM0262  AC142 HCT 116 C271(1.17)  LDD0579  [8]
 LDCM0263  AC143 HEK-293T C271(1.18)  LDD0861  [8]
 LDCM0264  AC144 HEK-293T C271(1.08)  LDD0862  [8]
 LDCM0265  AC145 HEK-293T C271(1.01)  LDD0863  [8]
 LDCM0266  AC146 HEK-293T C271(1.07)  LDD0864  [8]
 LDCM0267  AC147 HEK-293T C271(2.14)  LDD0865  [8]
 LDCM0268  AC148 HEK-293T C271(1.32)  LDD0866  [8]
 LDCM0269  AC149 HEK-293T C271(1.32)  LDD0867  [8]
 LDCM0270  AC15 HCT 116 C271(0.81)  LDD0587  [8]
 LDCM0271  AC150 HEK-293T C271(1.25)  LDD0869  [8]
 LDCM0272  AC151 HEK-293T C271(1.03)  LDD0870  [8]
 LDCM0273  AC152 HEK-293T C271(1.31)  LDD0871  [8]
 LDCM0274  AC153 HEK-293T C271(1.31)  LDD0872  [8]
 LDCM0621  AC154 HEK-293T C271(1.47)  LDD2162  [8]
 LDCM0622  AC155 HEK-293T C271(1.16)  LDD2163  [8]
 LDCM0623  AC156 HEK-293T C271(1.08)  LDD2164  [8]
 LDCM0624  AC157 HEK-293T C271(1.54)  LDD2165  [8]
 LDCM0276  AC17 HCT 116 C271(0.91)  LDD0593  [8]
 LDCM0277  AC18 HCT 116 C271(0.80)  LDD0594  [8]
 LDCM0278  AC19 HCT 116 C271(0.86)  LDD0595  [8]
 LDCM0279  AC2 HCT 116 C271(0.83)  LDD0596  [8]
 LDCM0280  AC20 HCT 116 C271(0.95)  LDD0597  [8]
 LDCM0281  AC21 HCT 116 C271(0.90)  LDD0598  [8]
 LDCM0282  AC22 HCT 116 C271(1.01)  LDD0599  [8]
 LDCM0283  AC23 HCT 116 C271(0.96)  LDD0600  [8]
 LDCM0284  AC24 HCT 116 C271(1.03)  LDD0601  [8]
 LDCM0285  AC25 HCT 116 C271(0.83)  LDD0602  [8]
 LDCM0286  AC26 HCT 116 C271(0.74)  LDD0603  [8]
 LDCM0287  AC27 HCT 116 C271(0.80)  LDD0604  [8]
 LDCM0288  AC28 HCT 116 C271(0.81)  LDD0605  [8]
 LDCM0289  AC29 HCT 116 C271(0.79)  LDD0606  [8]
 LDCM0290  AC3 HCT 116 C271(0.84)  LDD0607  [8]
 LDCM0291  AC30 HCT 116 C271(0.83)  LDD0608  [8]
 LDCM0292  AC31 HCT 116 C271(0.75)  LDD0609  [8]
 LDCM0293  AC32 HCT 116 C271(0.64)  LDD0610  [8]
 LDCM0294  AC33 HCT 116 C271(0.72)  LDD0611  [8]
 LDCM0295  AC34 HCT 116 C271(0.72)  LDD0612  [8]
 LDCM0296  AC35 HCT 116 C271(1.10)  LDD0613  [8]
 LDCM0297  AC36 HCT 116 C271(1.03)  LDD0614  [8]
 LDCM0298  AC37 HCT 116 C271(1.04)  LDD0615  [8]
 LDCM0299  AC38 HCT 116 C271(1.05)  LDD0616  [8]
 LDCM0300  AC39 HCT 116 C271(1.01)  LDD0617  [8]
 LDCM0301  AC4 HCT 116 C271(0.76)  LDD0618  [8]
 LDCM0302  AC40 HCT 116 C271(1.04)  LDD0619  [8]
 LDCM0303  AC41 HCT 116 C271(0.97)  LDD0620  [8]
 LDCM0304  AC42 HCT 116 C271(0.98)  LDD0621  [8]
 LDCM0305  AC43 HCT 116 C271(1.06)  LDD0622  [8]
 LDCM0306  AC44 HCT 116 C271(1.03)  LDD0623  [8]
 LDCM0307  AC45 HCT 116 C271(1.00)  LDD0624  [8]
 LDCM0308  AC46 HCT 116 C271(1.01)  LDD0625  [8]
 LDCM0309  AC47 HCT 116 C271(1.00)  LDD0626  [8]
 LDCM0310  AC48 HCT 116 C271(1.03)  LDD0627  [8]
 LDCM0311  AC49 HCT 116 C271(1.14)  LDD0628  [8]
 LDCM0312  AC5 HCT 116 C271(0.78)  LDD0629  [8]
 LDCM0313  AC50 HCT 116 C271(1.11)  LDD0630  [8]
 LDCM0314  AC51 HCT 116 C271(1.28)  LDD0631  [8]
 LDCM0315  AC52 HCT 116 C271(0.99)  LDD0632  [8]
 LDCM0316  AC53 HCT 116 C271(1.03)  LDD0633  [8]
 LDCM0317  AC54 HCT 116 C271(1.11)  LDD0634  [8]
 LDCM0318  AC55 HCT 116 C271(1.12)  LDD0635  [8]
 LDCM0319  AC56 HCT 116 C271(1.34)  LDD0636  [8]
 LDCM0320  AC57 HCT 116 C271(0.72)  LDD0637  [8]
 LDCM0321  AC58 HCT 116 C271(0.68)  LDD0638  [8]
 LDCM0322  AC59 HCT 116 C271(0.77)  LDD0639  [8]
 LDCM0323  AC6 HCT 116 C271(0.96)  LDD0640  [8]
 LDCM0324  AC60 HCT 116 C271(0.81)  LDD0641  [8]
 LDCM0325  AC61 HCT 116 C271(0.72)  LDD0642  [8]
 LDCM0326  AC62 HCT 116 C271(0.83)  LDD0643  [8]
 LDCM0327  AC63 HCT 116 C271(0.68)  LDD0644  [8]
 LDCM0328  AC64 HCT 116 C271(0.88)  LDD0645  [8]
 LDCM0329  AC65 HCT 116 C271(0.85)  LDD0646  [8]
 LDCM0330  AC66 HCT 116 C271(0.84)  LDD0647  [8]
 LDCM0331  AC67 HCT 116 C271(0.89)  LDD0648  [8]
 LDCM0332  AC68 HCT 116 C271(0.99)  LDD0649  [8]
 LDCM0333  AC69 HCT 116 C271(1.06)  LDD0650  [8]
 LDCM0334  AC7 HCT 116 C271(0.89)  LDD0651  [8]
 LDCM0335  AC70 HCT 116 C271(0.94)  LDD0652  [8]
 LDCM0336  AC71 HCT 116 C271(1.04)  LDD0653  [8]
 LDCM0337  AC72 HCT 116 C271(0.98)  LDD0654  [8]
 LDCM0338  AC73 HCT 116 C271(1.13)  LDD0655  [8]
 LDCM0339  AC74 HCT 116 C271(1.11)  LDD0656  [8]
 LDCM0340  AC75 HCT 116 C271(1.20)  LDD0657  [8]
 LDCM0341  AC76 HCT 116 C271(1.02)  LDD0658  [8]
 LDCM0342  AC77 HCT 116 C271(1.00)  LDD0659  [8]
 LDCM0343  AC78 HCT 116 C271(1.05)  LDD0660  [8]
 LDCM0344  AC79 HCT 116 C271(0.97)  LDD0661  [8]
 LDCM0345  AC8 HCT 116 C271(0.86)  LDD0662  [8]
 LDCM0346  AC80 HCT 116 C271(0.99)  LDD0663  [8]
 LDCM0347  AC81 HCT 116 C271(1.00)  LDD0664  [8]
 LDCM0348  AC82 HCT 116 C271(1.12)  LDD0665  [8]
 LDCM0349  AC83 HCT 116 C271(0.76)  LDD0666  [8]
 LDCM0350  AC84 HCT 116 C271(0.77)  LDD0667  [8]
 LDCM0351  AC85 HCT 116 C271(0.77)  LDD0668  [8]
 LDCM0352  AC86 HCT 116 C271(0.78)  LDD0669  [8]
 LDCM0353  AC87 HCT 116 C271(0.90)  LDD0670  [8]
 LDCM0354  AC88 HCT 116 C271(0.87)  LDD0671  [8]
 LDCM0355  AC89 HCT 116 C271(0.69)  LDD0672  [8]
 LDCM0357  AC90 HCT 116 C271(1.27)  LDD0674  [8]
 LDCM0358  AC91 HCT 116 C271(0.77)  LDD0675  [8]
 LDCM0359  AC92 HCT 116 C271(0.74)  LDD0676  [8]
 LDCM0360  AC93 HCT 116 C271(0.75)  LDD0677  [8]
 LDCM0361  AC94 HCT 116 C271(0.74)  LDD0678  [8]
 LDCM0362  AC95 HCT 116 C271(0.68)  LDD0679  [8]
 LDCM0363  AC96 HCT 116 C271(0.69)  LDD0680  [8]
 LDCM0364  AC97 HCT 116 C271(0.62)  LDD0681  [8]
 LDCM0365  AC98 HCT 116 C271(0.34)  LDD0682  [8]
 LDCM0366  AC99 HCT 116 C271(0.46)  LDD0683  [8]
 LDCM0248  AKOS034007472 HCT 116 C271(0.88)  LDD0565  [8]
 LDCM0356  AKOS034007680 HCT 116 C271(0.90)  LDD0673  [8]
 LDCM0275  AKOS034007705 HCT 116 C271(0.96)  LDD0592  [8]
 LDCM0156  Aniline NCI-H1299 11.89  LDD0403  [1]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [13]
 LDCM0367  CL1 HCT 116 C271(0.97)  LDD0684  [8]
 LDCM0368  CL10 HCT 116 C271(1.15)  LDD0685  [8]
 LDCM0369  CL100 HCT 116 C271(0.80)  LDD0686  [8]
 LDCM0370  CL101 HCT 116 C271(0.78)  LDD0687  [8]
 LDCM0371  CL102 HCT 116 C271(0.93)  LDD0688  [8]
 LDCM0372  CL103 HCT 116 C271(0.79)  LDD0689  [8]
 LDCM0373  CL104 HCT 116 C271(0.91)  LDD0690  [8]
 LDCM0374  CL105 HCT 116 C271(0.78)  LDD0691  [8]
 LDCM0375  CL106 HCT 116 C271(0.86)  LDD0692  [8]
 LDCM0376  CL107 HCT 116 C271(0.74)  LDD0693  [8]
 LDCM0377  CL108 HCT 116 C271(0.73)  LDD0694  [8]
 LDCM0378  CL109 HCT 116 C271(0.80)  LDD0695  [8]
 LDCM0379  CL11 HCT 116 C271(1.13)  LDD0696  [8]
 LDCM0380  CL110 HCT 116 C271(0.74)  LDD0697  [8]
 LDCM0381  CL111 HCT 116 C271(0.87)  LDD0698  [8]
 LDCM0382  CL112 HCT 116 C271(0.95)  LDD0699  [8]
 LDCM0383  CL113 HCT 116 C271(0.69)  LDD0700  [8]
 LDCM0384  CL114 HCT 116 C271(0.81)  LDD0701  [8]
 LDCM0385  CL115 HCT 116 C271(0.77)  LDD0702  [8]
 LDCM0386  CL116 HCT 116 C271(0.70)  LDD0703  [8]
 LDCM0387  CL117 HCT 116 C271(1.22)  LDD0704  [8]
 LDCM0388  CL118 HCT 116 C271(0.94)  LDD0705  [8]
 LDCM0389  CL119 HCT 116 C271(1.04)  LDD0706  [8]
 LDCM0390  CL12 HCT 116 C271(1.38)  LDD0707  [8]
 LDCM0391  CL120 HCT 116 C271(1.03)  LDD0708  [8]
 LDCM0392  CL121 HCT 116 C271(1.04)  LDD0709  [8]
 LDCM0393  CL122 HCT 116 C271(1.02)  LDD0710  [8]
 LDCM0394  CL123 HCT 116 C271(1.01)  LDD0711  [8]
 LDCM0395  CL124 HCT 116 C271(1.06)  LDD0712  [8]
 LDCM0396  CL125 HCT 116 C271(0.96)  LDD0713  [8]
 LDCM0397  CL126 HCT 116 C271(0.82)  LDD0714  [8]
 LDCM0398  CL127 HCT 116 C271(0.88)  LDD0715  [8]
 LDCM0399  CL128 HCT 116 C271(0.72)  LDD0716  [8]
 LDCM0400  CL13 HCT 116 C271(1.02)  LDD0717  [8]
 LDCM0401  CL14 HCT 116 C271(1.01)  LDD0718  [8]
 LDCM0402  CL15 HCT 116 C271(0.91)  LDD0719  [8]
 LDCM0403  CL16 HCT 116 C271(0.92)  LDD0720  [8]
 LDCM0404  CL17 HCT 116 C271(0.73)  LDD0721  [8]
 LDCM0405  CL18 HCT 116 C271(0.65)  LDD0722  [8]
 LDCM0406  CL19 HCT 116 C271(0.71)  LDD0723  [8]
 LDCM0407  CL2 HCT 116 C271(1.10)  LDD0724  [8]
 LDCM0408  CL20 HCT 116 C271(0.68)  LDD0725  [8]
 LDCM0409  CL21 HCT 116 C271(0.72)  LDD0726  [8]
 LDCM0410  CL22 HCT 116 C271(1.02)  LDD0727  [8]
 LDCM0411  CL23 HCT 116 C271(0.64)  LDD0728  [8]
 LDCM0412  CL24 HCT 116 C271(0.76)  LDD0729  [8]
 LDCM0413  CL25 HCT 116 C271(0.71)  LDD0730  [8]
 LDCM0414  CL26 HCT 116 C271(0.74)  LDD0731  [8]
 LDCM0415  CL27 HCT 116 C271(0.64)  LDD0732  [8]
 LDCM0416  CL28 HCT 116 C271(0.69)  LDD0733  [8]
 LDCM0417  CL29 HCT 116 C271(0.71)  LDD0734  [8]
 LDCM0418  CL3 HCT 116 C271(0.97)  LDD0735  [8]
 LDCM0419  CL30 HCT 116 C271(0.76)  LDD0736  [8]
 LDCM0420  CL31 HCT 116 C271(0.84)  LDD0737  [8]
 LDCM0421  CL32 HCT 116 C271(0.84)  LDD0738  [8]
 LDCM0422  CL33 HCT 116 C271(0.79)  LDD0739  [8]
 LDCM0423  CL34 HCT 116 C271(0.85)  LDD0740  [8]
 LDCM0424  CL35 HCT 116 C271(0.90)  LDD0741  [8]
 LDCM0425  CL36 HCT 116 C271(0.81)  LDD0742  [8]
 LDCM0426  CL37 HCT 116 C271(0.85)  LDD0743  [8]
 LDCM0428  CL39 HCT 116 C271(0.90)  LDD0745  [8]
 LDCM0429  CL4 HCT 116 C271(0.92)  LDD0746  [8]
 LDCM0430  CL40 HCT 116 C271(0.84)  LDD0747  [8]
 LDCM0431  CL41 HCT 116 C271(0.82)  LDD0748  [8]
 LDCM0432  CL42 HCT 116 C271(1.11)  LDD0749  [8]
 LDCM0433  CL43 HCT 116 C271(0.97)  LDD0750  [8]
 LDCM0434  CL44 HCT 116 C271(0.86)  LDD0751  [8]
 LDCM0435  CL45 HCT 116 C271(0.97)  LDD0752  [8]
 LDCM0436  CL46 HCT 116 C271(1.00)  LDD0753  [8]
 LDCM0437  CL47 HCT 116 C271(0.95)  LDD0754  [8]
 LDCM0438  CL48 HCT 116 C271(0.87)  LDD0755  [8]
 LDCM0439  CL49 HCT 116 C271(1.20)  LDD0756  [8]
 LDCM0440  CL5 HCT 116 C271(0.98)  LDD0757  [8]
 LDCM0441  CL50 HCT 116 C271(1.02)  LDD0758  [8]
 LDCM0442  CL51 HCT 116 C271(1.12)  LDD0759  [8]
 LDCM0443  CL52 HCT 116 C271(1.13)  LDD0760  [8]
 LDCM0444  CL53 HCT 116 C271(0.90)  LDD0761  [8]
 LDCM0445  CL54 HCT 116 C271(1.04)  LDD0762  [8]
 LDCM0446  CL55 HCT 116 C271(1.21)  LDD0763  [8]
 LDCM0447  CL56 HCT 116 C271(0.95)  LDD0764  [8]
 LDCM0448  CL57 HCT 116 C271(0.96)  LDD0765  [8]
 LDCM0449  CL58 HCT 116 C271(0.99)  LDD0766  [8]
 LDCM0450  CL59 HCT 116 C271(0.90)  LDD0767  [8]
 LDCM0451  CL6 HCT 116 C271(0.94)  LDD0768  [8]
 LDCM0452  CL60 HCT 116 C271(0.91)  LDD0769  [8]
 LDCM0453  CL61 HCT 116 C271(0.94)  LDD0770  [8]
 LDCM0454  CL62 HCT 116 C271(0.94)  LDD0771  [8]
 LDCM0455  CL63 HCT 116 C271(0.91)  LDD0772  [8]
 LDCM0456  CL64 HCT 116 C271(0.89)  LDD0773  [8]
 LDCM0457  CL65 HCT 116 C271(1.21)  LDD0774  [8]
 LDCM0458  CL66 HCT 116 C271(1.06)  LDD0775  [8]
 LDCM0459  CL67 HCT 116 C271(1.12)  LDD0776  [8]
 LDCM0460  CL68 HCT 116 C271(1.04)  LDD0777  [8]
 LDCM0461  CL69 HCT 116 C271(0.92)  LDD0778  [8]
 LDCM0462  CL7 HCT 116 C271(1.13)  LDD0779  [8]
 LDCM0463  CL70 HCT 116 C271(1.05)  LDD0780  [8]
 LDCM0464  CL71 HCT 116 C271(1.18)  LDD0781  [8]
 LDCM0465  CL72 HCT 116 C271(1.07)  LDD0782  [8]
 LDCM0466  CL73 HCT 116 C271(0.92)  LDD0783  [8]
 LDCM0467  CL74 HCT 116 C271(1.12)  LDD0784  [8]
 LDCM0469  CL76 HCT 116 C271(0.80)  LDD0786  [8]
 LDCM0470  CL77 HCT 116 C271(0.81)  LDD0787  [8]
 LDCM0471  CL78 HCT 116 C271(0.83)  LDD0788  [8]
 LDCM0472  CL79 HCT 116 C271(0.79)  LDD0789  [8]
 LDCM0473  CL8 HCT 116 C271(0.89)  LDD0790  [8]
 LDCM0474  CL80 HCT 116 C271(0.78)  LDD0791  [8]
 LDCM0475  CL81 HCT 116 C271(0.75)  LDD0792  [8]
 LDCM0476  CL82 HCT 116 C271(0.85)  LDD0793  [8]
 LDCM0477  CL83 HCT 116 C271(0.81)  LDD0794  [8]
 LDCM0478  CL84 HCT 116 C271(0.86)  LDD0795  [8]
 LDCM0479  CL85 HCT 116 C271(0.74)  LDD0796  [8]
 LDCM0480  CL86 HCT 116 C271(0.82)  LDD0797  [8]
 LDCM0481  CL87 HCT 116 C271(0.76)  LDD0798  [8]
 LDCM0482  CL88 HCT 116 C271(0.84)  LDD0799  [8]
 LDCM0483  CL89 HCT 116 C271(1.08)  LDD0800  [8]
 LDCM0484  CL9 HCT 116 C271(0.95)  LDD0801  [8]
 LDCM0485  CL90 HCT 116 C271(1.03)  LDD0802  [8]
 LDCM0486  CL91 HCT 116 C271(0.85)  LDD0803  [8]
 LDCM0487  CL92 HCT 116 C271(0.92)  LDD0804  [8]
 LDCM0488  CL93 HCT 116 C271(0.89)  LDD0805  [8]
 LDCM0489  CL94 HCT 116 C271(0.72)  LDD0806  [8]
 LDCM0490  CL95 HCT 116 C271(0.77)  LDD0807  [8]
 LDCM0491  CL96 HCT 116 C271(0.81)  LDD0808  [8]
 LDCM0492  CL97 HCT 116 C271(0.73)  LDD0809  [8]
 LDCM0493  CL98 HCT 116 C271(0.76)  LDD0810  [8]
 LDCM0494  CL99 HCT 116 C271(0.80)  LDD0811  [8]
 LDCM0165  Compound 9 HL-60 N.A.  LDD0420  [17]
 LDCM0634  CY-0357 Hep-G2 C53(0.95)  LDD2228  [14]
 LDCM0495  E2913 HEK-293T C271(0.96); C70(1.23)  LDD1698  [18]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C271(4.05)  LDD1702  [6]
 LDCM0175  Ethacrynic acid HeLa C191(0.88)  LDD2210  [7]
 LDCM0468  Fragment33 HCT 116 C271(0.90)  LDD0785  [8]
 LDCM0427  Fragment51 HCT 116 C271(1.05)  LDD0744  [8]
 LDCM0015  HNE MDA-MB-231 C191(1.11)  LDD0346  [19]
 LDCM0107  IAA HeLa N.A.  LDD0221  [13]
 LDCM0022  KB02 HCT 116 C271(1.26)  LDD0080  [8]
 LDCM0023  KB03 HCT 116 C271(1.41)  LDD0081  [8]
 LDCM0024  KB05 HCT 116 C271(1.90)  LDD0082  [8]
 LDCM0109  NEM HeLa N.A.  LDD0223  [13]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C53(1.04)  LDD2089  [6]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C271(0.94)  LDD2101  [6]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C53(0.86)  LDD2109  [6]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C271(0.58)  LDD2115  [6]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C53(0.81)  LDD2125  [6]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C271(1.42)  LDD2127  [6]
 LDCM0540  Nucleophilic fragment 35 MDA-MB-231 C271(0.73)  LDD2133  [6]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C271(1.59)  LDD2135  [6]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C271(1.20)  LDD2136  [6]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C271(0.89)  LDD2137  [6]
 LDCM0627  NUDT7-COV-1 HEK-293T C191(0.79); C191(0.52)  LDD2206  [20]
 LDCM0628  OTUB2-COV-1 HEK-293T C191(0.76); C191(0.53)  LDD2207  [20]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Serine/threonine-protein kinase WNK1 (WNK1) Ser/Thr protein kinase family Q9H4A3
Serine/threonine-protein kinase WNK4 (WNK4) Ser/Thr protein kinase family Q96J92
Serine/threonine-protein kinase OSR1 (OXSR1) STE Ser/Thr protein kinase family O95747
Serine/threonine-protein kinase LMTK1 (AATK) Tyr protein kinase family Q6ZMQ8
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Solute carrier family 12 member 2 (SLC12A2) SLC12A transporter family P55011
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Calcium-binding protein 39 (CAB39) Mo25 family Q9Y376
RELT-like protein 2 (RELL2) RELT family Q8NC24

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
Fostamatinib Small molecular drug DB12010
Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid24793884c74 Small molecular drug D0RJ8J

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 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.
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 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.
6 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
7 Chemoproteomic Profiling Reveals Ethacrynic Acid Targets Adenine Nucleotide Translocases to Impair Mitochondrial Function. Mol Pharm. 2018 Jun 4;15(6):2413-2422. doi: 10.1021/acs.molpharmaceut.8b00250. Epub 2018 May 15.
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 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.
11 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
12 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
13 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.
14 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
15 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
16 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.
17 A Photoaffinity Displacement Assay and Probes to Study the Cyclin-Dependent Kinase Family. Angew Chem Int Ed Engl. 2019 Nov 25;58(48):17322-17327. doi: 10.1002/anie.201906321. Epub 2019 Oct 31.
18 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
19 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
20 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.