Details of the Target

General Information of Target

Target ID LDTP03696
Target Name G protein-coupled receptor kinase 5 (GRK5)
Gene Name GRK5
Gene ID 2869
Synonyms
GPRK5; G protein-coupled receptor kinase 5; EC 2.7.11.16; G protein-coupled receptor kinase GRK5
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHISQCEDLRRTIDRDYCSLCDKQ
PIGRLLFRQFCETRPGLECYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFIAQ
VGQDLVSQTEEKLLQKPCKELFSACAQSVHEYLRGEPFHEYLDSMFFDRFLQWKWLERQP
VTKNTFRQYRVLGKGGFGEVCACQVRATGKMYACKRLEKKRIKKRKGESMALNEKQILEK
VNSQFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGNPGFEEERALFYAAEILCGLE
DLHRENTVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVGYMAPEVLNNQ
RYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSIC
KMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDI
EQFSTVKGVNLDHTDDDFYSKFSTGSVSIPWQNEMIETECFKELNVFGPNGTLPPDLNRN
HPPEPPKKGLLQRLFKRQHQNNSKSSPSSKTSFNHHINSNHVSSNSTGSS
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family, GPRK subfamily
Subcellular location
Cytoplasm
Function
Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein-coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70-interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2-mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates internalization of the chemokine receptor. Phosphorylates rhodopsin (RHO) (in vitro) and a non G-protein-coupled receptor, LRP6 during Wnt signaling (in vitro).
TTD ID
T69612
Uniprot ID
P34947
DrugMap ID
TTTCXO0
Ensemble ID
ENST00000392870.3
HGNC ID
HGNC:4544
ChEMBL ID
CHEMBL5678

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
IA-alkyne
 Probe Info  		C138(8.90)  LDD1703  [1]
DBIA
 Probe Info  		C201(0.58); C203(0.58)  LDD0533  [2]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [3]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C201(0.83)  LDD1507  [4]
 LDCM0215  AC10 HEK-293T C203(1.02)  LDD1508  [4]
 LDCM0216  AC100 HCT 116 C201(0.58); C203(0.58)  LDD0533  [2]
 LDCM0217  AC101 HCT 116 C201(0.54); C203(0.54)  LDD0534  [2]
 LDCM0218  AC102 HCT 116 C201(0.42); C203(0.42)  LDD0535  [2]
 LDCM0219  AC103 HCT 116 C201(0.34); C203(0.34)  LDD0536  [2]
 LDCM0220  AC104 HCT 116 C201(0.42); C203(0.42)  LDD0537  [2]
 LDCM0221  AC105 HCT 116 C201(0.32); C203(0.32)  LDD0538  [2]
 LDCM0222  AC106 HCT 116 C201(0.40); C203(0.40)  LDD0539  [2]
 LDCM0223  AC107 HCT 116 C201(0.57); C203(0.56)  LDD0540  [2]
 LDCM0224  AC108 HCT 116 C201(0.29); C203(0.38)  LDD0541  [2]
 LDCM0225  AC109 HCT 116 C201(0.37); C203(0.54)  LDD0542  [2]
 LDCM0226  AC11 HEK-293T C201(1.09); C54(1.00)  LDD1509  [4]
 LDCM0227  AC110 HCT 116 C201(0.43); C203(0.59)  LDD0544  [2]
 LDCM0228  AC111 HCT 116 C201(0.34); C203(0.35)  LDD0545  [2]
 LDCM0229  AC112 HCT 116 C201(0.45); C203(0.47)  LDD0546  [2]
 LDCM0237  AC12 HEK-293T C201(1.11)  LDD1510  [4]
 LDCM0270  AC15 HEK-293T C201(0.96)  LDD1513  [4]
 LDCM0276  AC17 HCT 116 C201(1.13); C203(1.13)  LDD0593  [2]
 LDCM0277  AC18 HCT 116 C201(0.58); C203(0.58)  LDD0594  [2]
 LDCM0278  AC19 HCT 116 C201(1.03); C203(1.03)  LDD0595  [2]
 LDCM0279  AC2 HEK-293T C203(1.00)  LDD1518  [4]
 LDCM0280  AC20 HCT 116 C201(0.88); C203(0.88)  LDD0597  [2]
 LDCM0281  AC21 HCT 116 C201(0.87); C203(0.87)  LDD0598  [2]
 LDCM0282  AC22 HCT 116 C201(1.47); C203(1.47)  LDD0599  [2]
 LDCM0283  AC23 HCT 116 C201(0.89); C203(0.89)  LDD0600  [2]
 LDCM0284  AC24 HCT 116 C201(1.00); C203(1.00)  LDD0601  [2]
 LDCM0285  AC25 HCT 116 C201(0.81); C203(0.81)  LDD0602  [2]
 LDCM0286  AC26 HCT 116 C201(0.67); C203(0.67)  LDD0603  [2]
 LDCM0287  AC27 HCT 116 C201(0.64); C203(0.64)  LDD0604  [2]
 LDCM0288  AC28 HCT 116 C201(0.53); C203(0.53)  LDD0605  [2]
 LDCM0289  AC29 HCT 116 C201(0.90); C203(0.90)  LDD0606  [2]
 LDCM0290  AC3 HEK-293T C201(1.08); C54(0.95)  LDD1529  [4]
 LDCM0291  AC30 HCT 116 C201(0.53); C203(0.53)  LDD0608  [2]
 LDCM0292  AC31 HCT 116 C201(0.87); C203(0.87)  LDD0609  [2]
 LDCM0293  AC32 HCT 116 C201(0.60); C203(0.60)  LDD0610  [2]
 LDCM0294  AC33 HCT 116 C201(0.46); C203(0.46)  LDD0611  [2]
 LDCM0295  AC34 HCT 116 C201(0.44); C203(0.44)  LDD0612  [2]
 LDCM0296  AC35 HCT 116 C201(1.05); C203(1.05)  LDD0613  [2]
 LDCM0297  AC36 HCT 116 C201(20.00); C203(20.00)  LDD0614  [2]
 LDCM0298  AC37 HCT 116 C201(0.99); C203(0.99)  LDD0615  [2]
 LDCM0299  AC38 HCT 116 C201(0.97); C203(0.97)  LDD0616  [2]
 LDCM0300  AC39 HCT 116 C201(1.16); C203(1.16)  LDD0617  [2]
 LDCM0301  AC4 HEK-293T C201(0.97)  LDD1540  [4]
 LDCM0302  AC40 HCT 116 C201(1.20); C203(1.20)  LDD0619  [2]
 LDCM0303  AC41 HCT 116 C201(1.17); C203(1.17)  LDD0620  [2]
 LDCM0304  AC42 HCT 116 C201(0.88); C203(0.88)  LDD0621  [2]
 LDCM0305  AC43 HCT 116 C201(1.17); C203(1.17)  LDD0622  [2]
 LDCM0306  AC44 HCT 116 C201(1.07); C203(1.07)  LDD0623  [2]
 LDCM0307  AC45 HCT 116 C201(0.87); C203(0.87)  LDD0624  [2]
 LDCM0308  AC46 HCT 116 C201(1.18); C203(1.18)  LDD0625  [2]
 LDCM0309  AC47 HCT 116 C201(0.92); C203(0.92)  LDD0626  [2]
 LDCM0310  AC48 HCT 116 C201(1.63); C203(1.63)  LDD0627  [2]
 LDCM0311  AC49 HCT 116 C201(0.92); C203(0.92)  LDD0628  [2]
 LDCM0313  AC50 HCT 116 C201(1.14); C203(1.14)  LDD0630  [2]
 LDCM0314  AC51 HCT 116 C201(1.37); C203(1.37)  LDD0631  [2]
 LDCM0315  AC52 HCT 116 C201(0.95); C203(0.95)  LDD0632  [2]
 LDCM0316  AC53 HCT 116 C201(0.77); C203(0.77)  LDD0633  [2]
 LDCM0317  AC54 HCT 116 C201(0.80); C203(0.80)  LDD0634  [2]
 LDCM0318  AC55 HCT 116 C201(0.96); C203(0.96)  LDD0635  [2]
 LDCM0319  AC56 HCT 116 C201(1.59); C203(1.59)  LDD0636  [2]
 LDCM0320  AC57 HCT 116 C203(0.53); C201(0.77)  LDD0637  [2]
 LDCM0321  AC58 HCT 116 C203(0.46); C201(0.52)  LDD0638  [2]
 LDCM0322  AC59 HCT 116 C203(0.44); C201(0.52)  LDD0639  [2]
 LDCM0324  AC60 HCT 116 C203(0.57); C201(0.66)  LDD0641  [2]
 LDCM0325  AC61 HCT 116 C201(0.52); C203(0.60)  LDD0642  [2]
 LDCM0326  AC62 HCT 116 C203(0.60); C201(0.82)  LDD0643  [2]
 LDCM0327  AC63 HCT 116 C203(0.58); C201(0.65)  LDD0644  [2]
 LDCM0328  AC64 HCT 116 C203(0.52); C201(0.70)  LDD0645  [2]
 LDCM0329  AC65 HCT 116 C203(0.48); C201(0.70)  LDD0646  [2]
 LDCM0330  AC66 HCT 116 C203(0.58); C201(0.72)  LDD0647  [2]
 LDCM0331  AC67 HCT 116 C203(0.48); C201(0.57)  LDD0648  [2]
 LDCM0332  AC68 HCT 116 C201(0.95); C203(0.95)  LDD0649  [2]
 LDCM0333  AC69 HCT 116 C201(0.78); C203(0.78)  LDD0650  [2]
 LDCM0334  AC7 HEK-293T C201(1.08)  LDD1568  [4]
 LDCM0335  AC70 HCT 116 C201(0.96); C203(0.96)  LDD0652  [2]
 LDCM0336  AC71 HCT 116 C201(1.38); C203(1.38)  LDD0653  [2]
 LDCM0337  AC72 HCT 116 C201(0.81); C203(0.81)  LDD0654  [2]
 LDCM0338  AC73 HCT 116 C201(0.87); C203(0.87)  LDD0655  [2]
 LDCM0339  AC74 HCT 116 C201(0.90); C203(0.90)  LDD0656  [2]
 LDCM0340  AC75 HCT 116 C201(0.91); C203(0.91)  LDD0657  [2]
 LDCM0341  AC76 HCT 116 C201(0.71); C203(0.71)  LDD0658  [2]
 LDCM0342  AC77 HCT 116 C201(0.72); C203(0.72)  LDD0659  [2]
 LDCM0343  AC78 HCT 116 C201(1.11); C203(1.11)  LDD0660  [2]
 LDCM0344  AC79 HCT 116 C201(1.03); C203(1.03)  LDD0661  [2]
 LDCM0346  AC80 HCT 116 C201(0.82); C203(0.82)  LDD0663  [2]
 LDCM0347  AC81 HCT 116 C201(1.86); C203(1.86)  LDD0664  [2]
 LDCM0348  AC82 HCT 116 C201(1.06); C203(1.06)  LDD0665  [2]
 LDCM0349  AC83 HCT 116 C201(0.55); C203(0.55)  LDD0666  [2]
 LDCM0350  AC84 HCT 116 C201(0.57); C203(0.57)  LDD0667  [2]
 LDCM0351  AC85 HCT 116 C201(0.66); C203(0.66)  LDD0668  [2]
 LDCM0352  AC86 HCT 116 C201(0.60); C203(0.60)  LDD0669  [2]
 LDCM0353  AC87 HCT 116 C201(0.96); C203(0.96)  LDD0670  [2]
 LDCM0354  AC88 HCT 116 C201(0.72); C203(0.72)  LDD0671  [2]
 LDCM0355  AC89 HCT 116 C201(0.53); C203(0.53)  LDD0672  [2]
 LDCM0357  AC90 HCT 116 C201(1.32); C203(1.32)  LDD0674  [2]
 LDCM0358  AC91 HCT 116 C201(0.46); C203(0.46)  LDD0675  [2]
 LDCM0359  AC92 HCT 116 C201(0.41); C203(0.41)  LDD0676  [2]
 LDCM0360  AC93 HCT 116 C201(0.56); C203(0.56)  LDD0677  [2]
 LDCM0361  AC94 HCT 116 C201(0.69); C203(0.69)  LDD0678  [2]
 LDCM0362  AC95 HCT 116 C201(0.84); C203(0.84)  LDD0679  [2]
 LDCM0363  AC96 HCT 116 C201(0.56); C203(0.56)  LDD0680  [2]
 LDCM0364  AC97 HCT 116 C201(0.46); C203(0.46)  LDD0681  [2]
 LDCM0365  AC98 HCT 116 C201(0.31); C203(0.31)  LDD0682  [2]
 LDCM0366  AC99 HCT 116 C201(1.03); C203(1.03)  LDD0683  [2]
 LDCM0356  AKOS034007680 HEK-293T C201(0.89)  LDD1570  [4]
 LDCM0367  CL1 HCT 116 C201(1.56); C203(1.56)  LDD0684  [2]
 LDCM0368  CL10 HCT 116 C201(0.73); C203(0.73)  LDD0685  [2]
 LDCM0369  CL100 HEK-293T C201(1.11)  LDD1573  [4]
 LDCM0372  CL103 HEK-293T C201(0.94)  LDD1576  [4]
 LDCM0373  CL104 HEK-293T C201(1.12)  LDD1577  [4]
 LDCM0374  CL105 HCT 116 C201(0.77); C203(0.77)  LDD0691  [2]
 LDCM0375  CL106 HCT 116 C201(0.70); C203(0.70)  LDD0692  [2]
 LDCM0376  CL107 HCT 116 C201(0.55); C203(0.55)  LDD0693  [2]
 LDCM0377  CL108 HCT 116 C201(0.65); C203(0.65)  LDD0694  [2]
 LDCM0378  CL109 HCT 116 C201(0.88); C203(0.88)  LDD0695  [2]
 LDCM0379  CL11 HCT 116 C201(0.71); C203(0.71)  LDD0696  [2]
 LDCM0380  CL110 HCT 116 C201(0.87); C203(0.87)  LDD0697  [2]
 LDCM0381  CL111 HCT 116 C201(0.95); C203(0.95)  LDD0698  [2]
 LDCM0382  CL112 HCT 116 C201(0.96); C203(0.96)  LDD0699  [2]
 LDCM0383  CL113 HCT 116 C201(0.60); C203(0.60)  LDD0700  [2]
 LDCM0384  CL114 HCT 116 C201(0.84); C203(0.84)  LDD0701  [2]
 LDCM0385  CL115 HCT 116 C201(0.62); C203(0.62)  LDD0702  [2]
 LDCM0386  CL116 HCT 116 C201(0.68); C203(0.68)  LDD0703  [2]
 LDCM0387  CL117 HCT 116 C201(0.99); C203(0.99)  LDD0704  [2]
 LDCM0388  CL118 HCT 116 C201(0.85); C203(0.85)  LDD0705  [2]
 LDCM0389  CL119 HCT 116 C201(0.87); C203(0.87)  LDD0706  [2]
 LDCM0390  CL12 HCT 116 C201(0.69); C203(0.69)  LDD0707  [2]
 LDCM0391  CL120 HCT 116 C201(0.93); C203(0.93)  LDD0708  [2]
 LDCM0392  CL121 HCT 116 C201(1.77); C203(1.77)  LDD0709  [2]
 LDCM0393  CL122 HCT 116 C201(1.45); C203(1.45)  LDD0710  [2]
 LDCM0394  CL123 HCT 116 C201(1.57); C203(1.57)  LDD0711  [2]
 LDCM0395  CL124 HCT 116 C201(1.09); C203(1.09)  LDD0712  [2]
 LDCM0396  CL125 HCT 116 C203(0.68); C201(0.82)  LDD0713  [2]
 LDCM0397  CL126 HCT 116 C203(0.76); C201(0.84)  LDD0714  [2]
 LDCM0398  CL127 HCT 116 C203(0.64); C201(0.79)  LDD0715  [2]
 LDCM0399  CL128 HCT 116 C203(0.45); C201(0.62)  LDD0716  [2]
 LDCM0400  CL13 HCT 116 C201(0.74); C203(0.74)  LDD0717  [2]
 LDCM0401  CL14 HCT 116 C201(0.88); C203(0.88)  LDD0718  [2]
 LDCM0402  CL15 HCT 116 C201(0.98); C203(0.98)  LDD0719  [2]
 LDCM0403  CL16 HCT 116 C201(0.90); C203(0.90)  LDD0720  [2]
 LDCM0404  CL17 HCT 116 C201(1.70); C203(1.70)  LDD0721  [2]
 LDCM0405  CL18 HCT 116 C201(0.75); C203(0.75)  LDD0722  [2]
 LDCM0406  CL19 HCT 116 C201(0.94); C203(0.94)  LDD0723  [2]
 LDCM0407  CL2 HCT 116 C201(1.34); C203(1.34)  LDD0724  [2]
 LDCM0408  CL20 HCT 116 C201(0.73); C203(0.73)  LDD0725  [2]
 LDCM0409  CL21 HCT 116 C201(0.70); C203(0.70)  LDD0726  [2]
 LDCM0410  CL22 HCT 116 C201(0.70); C203(0.70)  LDD0727  [2]
 LDCM0411  CL23 HCT 116 C201(0.71); C203(0.71)  LDD0728  [2]
 LDCM0412  CL24 HCT 116 C201(0.63); C203(0.63)  LDD0729  [2]
 LDCM0413  CL25 HCT 116 C201(0.62); C203(0.62)  LDD0730  [2]
 LDCM0414  CL26 HCT 116 C201(1.04); C203(1.04)  LDD0731  [2]
 LDCM0415  CL27 HCT 116 C201(0.76); C203(0.76)  LDD0732  [2]
 LDCM0416  CL28 HCT 116 C201(0.73); C203(0.73)  LDD0733  [2]
 LDCM0417  CL29 HCT 116 C201(0.64); C203(0.64)  LDD0734  [2]
 LDCM0418  CL3 HCT 116 C201(0.91); C203(0.91)  LDD0735  [2]
 LDCM0419  CL30 HCT 116 C201(0.95); C203(0.95)  LDD0736  [2]
 LDCM0420  CL31 HCT 116 C201(0.58); C203(0.58)  LDD0737  [2]
 LDCM0421  CL32 HCT 116 C201(0.60); C203(0.60)  LDD0738  [2]
 LDCM0422  CL33 HCT 116 C201(0.62); C203(0.62)  LDD0739  [2]
 LDCM0423  CL34 HCT 116 C201(0.43); C203(0.43)  LDD0740  [2]
 LDCM0424  CL35 HCT 116 C201(0.24); C203(0.24)  LDD0741  [2]
 LDCM0425  CL36 HCT 116 C201(0.35); C203(0.35)  LDD0742  [2]
 LDCM0426  CL37 HCT 116 C201(0.36); C203(0.36)  LDD0743  [2]
 LDCM0428  CL39 HCT 116 C201(0.44); C203(0.44)  LDD0745  [2]
 LDCM0429  CL4 HCT 116 C201(0.96); C203(0.96)  LDD0746  [2]
 LDCM0430  CL40 HCT 116 C201(0.30); C203(0.30)  LDD0747  [2]
 LDCM0431  CL41 HCT 116 C201(0.49); C203(0.49)  LDD0748  [2]
 LDCM0432  CL42 HCT 116 C201(0.36); C203(0.36)  LDD0749  [2]
 LDCM0433  CL43 HCT 116 C201(0.36); C203(0.36)  LDD0750  [2]
 LDCM0434  CL44 HCT 116 C201(0.40); C203(0.40)  LDD0751  [2]
 LDCM0435  CL45 HCT 116 C201(0.54); C203(0.54)  LDD0752  [2]
 LDCM0437  CL47 HEK-293T C201(1.05)  LDD1641  [4]
 LDCM0440  CL5 HCT 116 C201(0.84); C203(0.84)  LDD0757  [2]
 LDCM0443  CL52 HEK-293T C201(1.14)  LDD1646  [4]
 LDCM0444  CL53 HEK-293T C201(0.88)  LDD1647  [4]
 LDCM0445  CL54 HEK-293T C203(0.97)  LDD1648  [4]
 LDCM0446  CL55 HEK-293T C201(1.10); C54(1.22)  LDD1649  [4]
 LDCM0447  CL56 HEK-293T C201(1.16)  LDD1650  [4]
 LDCM0450  CL59 HEK-293T C201(1.02)  LDD1653  [4]
 LDCM0451  CL6 HCT 116 C201(0.94); C203(0.94)  LDD0768  [2]
 LDCM0453  CL61 HCT 116 C201(0.61); C203(0.61)  LDD0770  [2]
 LDCM0454  CL62 HCT 116 C201(0.67); C203(0.67)  LDD0771  [2]
 LDCM0455  CL63 HCT 116 C201(0.67); C203(0.67)  LDD0772  [2]
 LDCM0456  CL64 HCT 116 C201(0.42); C203(0.42)  LDD0773  [2]
 LDCM0457  CL65 HCT 116 C201(0.61); C203(0.61)  LDD0774  [2]
 LDCM0458  CL66 HCT 116 C201(0.42); C203(0.42)  LDD0775  [2]
 LDCM0459  CL67 HCT 116 C201(0.43); C203(0.43)  LDD0776  [2]
 LDCM0460  CL68 HCT 116 C201(0.51); C203(0.51)  LDD0777  [2]
 LDCM0461  CL69 HCT 116 C201(0.85); C203(0.85)  LDD0778  [2]
 LDCM0462  CL7 HCT 116 C201(0.68); C203(0.68)  LDD0779  [2]
 LDCM0463  CL70 HCT 116 C201(0.75); C203(0.75)  LDD0780  [2]
 LDCM0464  CL71 HCT 116 C201(0.56); C203(0.56)  LDD0781  [2]
 LDCM0465  CL72 HCT 116 C201(0.83); C203(0.83)  LDD0782  [2]
 LDCM0466  CL73 HCT 116 C201(0.45); C203(0.45)  LDD0783  [2]
 LDCM0467  CL74 HCT 116 C201(0.44); C203(0.44)  LDD0784  [2]
 LDCM0469  CL76 HEK-293T C201(1.09)  LDD1672  [4]
 LDCM0470  CL77 HEK-293T C201(0.79)  LDD1673  [4]
 LDCM0471  CL78 HEK-293T C203(1.10)  LDD1674  [4]
 LDCM0472  CL79 HEK-293T C201(1.09); C54(1.01)  LDD1675  [4]
 LDCM0473  CL8 HCT 116 C201(0.77); C203(0.77)  LDD0790  [2]
 LDCM0474  CL80 HEK-293T C201(1.03)  LDD1677  [4]
 LDCM0477  CL83 HEK-293T C201(0.96)  LDD1680  [4]
 LDCM0481  CL87 HEK-293T C201(1.06)  LDD1684  [4]
 LDCM0482  CL88 HEK-293T C201(1.26)  LDD1685  [4]
 LDCM0483  CL89 HEK-293T C201(0.92)  LDD1686  [4]
 LDCM0484  CL9 HCT 116 C201(0.77); C203(0.77)  LDD0801  [2]
 LDCM0485  CL90 HEK-293T C203(0.98)  LDD1688  [4]
 LDCM0486  CL91 HEK-293T C201(1.07); C54(0.95)  LDD1689  [4]
 LDCM0487  CL92 HEK-293T C201(1.06)  LDD1690  [4]
 LDCM0490  CL95 HEK-293T C201(1.00)  LDD1693  [4]
 LDCM0494  CL99 HEK-293T C201(0.93)  LDD1697  [4]
 LDCM0495  E2913 HEK-293T C201(0.88)  LDD1698  [4]
 LDCM0468  Fragment33 HCT 116 C201(0.57); C203(0.57)  LDD0785  [2]
 LDCM0427  Fragment51 HCT 116 C201(0.37); C203(0.37)  LDD0744  [2]
 LDCM0022  KB02 T cell C138(8.90)  LDD1703  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
NF-kappa-B inhibitor alpha (NFKBIA) NF-kappa-B inhibitor family P25963

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid24210504c1o Small molecular drug D04CUA
Patented
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bdbm50173323 Small molecular drug D00YYO
Bdbm50173327 Small molecular drug D0U5IW
Bdbm50173330 Small molecular drug D05PTF

References

1 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
2 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.
3 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
4 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