General Information of Target

Target ID LDTP05433
Target Name Protein kinase C theta type (PRKCQ)
Gene Name PRKCQ
Gene ID 5588
Synonyms
PRKCT; Protein kinase C theta type; EC 2.7.11.13; nPKC-theta
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSPFLRIGLSNFDCGSCQSCQGEAVNPYCAVLVKEYVESENGQMYIQKKPTMYPPWDSTF
DAHINKGRVMQIIVKGKNVDLISETTVELYSLAERCRKNNGKTEIWLELKPQGRMLMNAR
YFLEMSDTKDMNEFETEGFFALHQRRGAIKQAKVHHVKCHEFTATFFPQPTFCSVCHEFV
WGLNKQGYQCRQCNAAIHKKCIDKVIAKCTGSAINSRETMFHKERFKIDMPHRFKVYNYK
SPTFCEHCGTLLWGLARQGLKCDACGMNVHHRCQTKVANLCGINQKLMAEALAMIESTQQ
ARCLRDTEQIFREGPVEIGLPCSIKNEARPPCLPTPGKREPQGISWESPLDEVDKMCHLP
EPELNKERPSLQIKLKIEDFILHKMLGKGSFGKVFLAEFKKTNQFFAIKALKKDVVLMDD
DVECTMVEKRVLSLAWEHPFLTHMFCTFQTKENLFFVMEYLNGGDLMYHIQSCHKFDLSR
ATFYAAEIILGLQFLHSKGIVYRDLKLDNILLDKDGHIKIADFGMCKENMLGDAKTNTFC
GTPDYIAPEILLGQKYNHSVDWWSFGVLLYEMLIGQSPFHGQDEEELFHSIRMDNPFYPR
WLEKEAKDLLVKLFVREPEKRLGVRGDIRQHPLFREINWEELERKEIDPPFRPKVKSPFD
CSNFDKEFLNEKPRLSFADRALINSMDQNMFRNFSFMNPGMERLIS
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Protein kinase superfamily, AGC Ser/Thr protein kinase family, PKC subfamily
Subcellular location
Cytoplasm
Function
Calcium-independent, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that mediates non-redundant functions in T-cell receptor (TCR) signaling, including T-cells activation, proliferation, differentiation and survival, by mediating activation of multiple transcription factors such as NF-kappa-B, JUN, NFATC1 and NFATC2. In TCR-CD3/CD28-co-stimulated T-cells, is required for the activation of NF-kappa-B and JUN, which in turn are essential for IL2 production, and participates in the calcium-dependent NFATC1 and NFATC2 transactivation. Mediates the activation of the canonical NF-kappa-B pathway (NFKB1) by direct phosphorylation of CARD11 on several serine residues, inducing CARD11 association with lipid rafts and recruitment of the BCL10-MALT1 complex, which then activates IKK complex, resulting in nuclear translocation and activation of NFKB1. May also play an indirect role in activation of the non-canonical NF-kappa-B (NFKB2) pathway. In the signaling pathway leading to JUN activation, acts by phosphorylating the mediator STK39/SPAK and may not act through MAP kinases signaling. Plays a critical role in TCR/CD28-induced NFATC1 and NFATC2 transactivation by participating in the regulation of reduced inositol 1,4,5-trisphosphate generation and intracellular calcium mobilization. After costimulation of T-cells through CD28 can phosphorylate CBLB and is required for the ubiquitination and subsequent degradation of CBLB, which is a prerequisite for the activation of TCR. During T-cells differentiation, plays an important role in the development of T-helper 2 (Th2) cells following immune and inflammatory responses, and, in the development of inflammatory autoimmune diseases, is necessary for the activation of IL17-producing Th17 cells. May play a minor role in Th1 response. Upon TCR stimulation, mediates T-cell protective survival signal by phosphorylating BAD, thus protecting T-cells from BAD-induced apoptosis, and by up-regulating BCL-X(L)/BCL2L1 levels through NF-kappa-B and JUN pathways. In platelets, regulates signal transduction downstream of the ITGA2B, CD36/GP4, F2R/PAR1 and F2RL3/PAR4 receptors, playing a positive role in 'outside-in' signaling and granule secretion signal transduction. May relay signals from the activated ITGA2B receptor by regulating the uncoupling of WASP and WIPF1, thereby permitting the regulation of actin filament nucleation and branching activity of the Arp2/3 complex. May mediate inhibitory effects of free fatty acids on insulin signaling by phosphorylating IRS1, which in turn blocks IRS1 tyrosine phosphorylation and downstream activation of the PI3K/AKT pathway. Phosphorylates MSN (moesin) in the presence of phosphatidylglycerol or phosphatidylinositol. Phosphorylates PDPK1 at 'Ser-504' and 'Ser-532' and negatively regulates its ability to phosphorylate PKB/AKT1. Phosphorylates CCDC88A/GIV and inhibits its guanine nucleotide exchange factor activity.
TTD ID
T23995
Uniprot ID
Q04759
DrugMap ID
TT8QL1J
Ensemble ID
ENST00000263125.10
HGNC ID
HGNC:9410
ChEMBL ID
CHEMBL3920

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AU565 SNV: p.P341L; p.E352K DBIA    Probe Info 
HCT15 SNV: p.S685I DBIA    Probe Info 
LNCaP clone FGC SNV: p.E313Ter DBIA    Probe Info 
MEWO SNV: p.G211E DBIA    Probe Info 
MFE319 SNV: p.K451R DBIA    Probe Info 
NCIH1048 SNV: p.A278D DBIA    Probe Info 
PF382 SNV: p.R592C DBIA    Probe Info 
SHP77 SNV: p.V180F .
SUPT1 SNV: p.G463R; p.R592H DBIA    Probe Info 
WM793 SNV: p.A93D DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 12 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
THZ1-DTB
 Probe Info 
C661(2.76)  LDD0460  [1]
BTD
 Probe Info 
C281(1.87)  LDD1700  [2]
Johansson_61
 Probe Info 
_(20.00)  LDD1485  [3]
DBIA
 Probe Info 
C661(5.22)  LDD0209  [4]
4-Iodoacetamidophenylacetylene
 Probe Info 
C209(0.00); C322(0.00); C357(0.00); C661(0.00)  LDD0038  [5]
IA-alkyne
 Probe Info 
C245(0.00); C248(0.00); C209(0.00); C322(0.00)  LDD0036  [5]
Lodoacetamide azide
 Probe Info 
C322(0.00); C540(0.00); C281(0.00); C209(0.00)  LDD0037  [5]
Compound 10
 Probe Info 
N.A.  LDD2216  [6]
Compound 11
 Probe Info 
N.A.  LDD2213  [6]
IPM
 Probe Info 
C661(0.00); C322(0.00); C526(0.00)  LDD2156  [7]
YN-1
 Probe Info 
N.A.  LDD0446  [8]
NAIA_5
 Probe Info 
C526(0.00); C193(0.00)  LDD2223  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C193(0.98)  LDD2130  [2]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C281(0.95)  LDD2117  [2]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C281(1.30)  LDD2152  [2]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C193(0.61)  LDD2132  [2]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C193(0.98)  LDD2131  [2]
 LDCM0214  AC1 HEK-293T C322(1.05)  LDD0812  [10]
 LDCM0215  AC10 HEK-293T C322(1.18); C661(0.68)  LDD0813  [10]
 LDCM0216  AC100 HEK-293T C322(1.18)  LDD0814  [10]
 LDCM0217  AC101 HEK-293T C322(1.05)  LDD0815  [10]
 LDCM0218  AC102 HEK-293T C322(1.13)  LDD0816  [10]
 LDCM0219  AC103 HEK-293T C322(1.30)  LDD0817  [10]
 LDCM0220  AC104 HEK-293T C322(1.23)  LDD0818  [10]
 LDCM0221  AC105 HEK-293T C322(0.96)  LDD0819  [10]
 LDCM0222  AC106 HEK-293T C322(0.74)  LDD0820  [10]
 LDCM0223  AC107 HEK-293T C322(1.09)  LDD0821  [10]
 LDCM0224  AC108 HEK-293T C322(0.88)  LDD0822  [10]
 LDCM0225  AC109 HEK-293T C322(0.94)  LDD0823  [10]
 LDCM0226  AC11 HEK-293T C322(1.19); C661(0.87)  LDD0824  [10]
 LDCM0227  AC110 HEK-293T C322(1.61)  LDD0825  [10]
 LDCM0228  AC111 HEK-293T C322(1.94)  LDD0826  [10]
 LDCM0229  AC112 HEK-293T C322(1.88)  LDD0827  [10]
 LDCM0230  AC113 PaTu 8988t C661(0.86)  LDD1109  [10]
 LDCM0231  AC114 PaTu 8988t C661(0.78)  LDD1110  [10]
 LDCM0232  AC115 PaTu 8988t C661(1.30)  LDD1111  [10]
 LDCM0233  AC116 PaTu 8988t C661(1.27)  LDD1112  [10]
 LDCM0234  AC117 PaTu 8988t C661(1.22)  LDD1113  [10]
 LDCM0235  AC118 PaTu 8988t C661(0.81)  LDD1114  [10]
 LDCM0236  AC119 PaTu 8988t C661(0.84)  LDD1115  [10]
 LDCM0237  AC12 HEK-293T C322(1.22); C661(0.65)  LDD0835  [10]
 LDCM0238  AC120 PaTu 8988t C661(0.75)  LDD1117  [10]
 LDCM0239  AC121 PaTu 8988t C661(0.80)  LDD1118  [10]
 LDCM0240  AC122 PaTu 8988t C661(0.71)  LDD1119  [10]
 LDCM0241  AC123 PaTu 8988t C661(0.77)  LDD1120  [10]
 LDCM0242  AC124 PaTu 8988t C661(0.93)  LDD1121  [10]
 LDCM0243  AC125 PaTu 8988t C661(1.00)  LDD1122  [10]
 LDCM0244  AC126 PaTu 8988t C661(0.82)  LDD1123  [10]
 LDCM0245  AC127 PaTu 8988t C661(0.78)  LDD1124  [10]
 LDCM0246  AC128 HEK-293T C322(0.95)  LDD0844  [10]
 LDCM0247  AC129 HEK-293T C322(1.34)  LDD0845  [10]
 LDCM0249  AC130 HEK-293T C322(1.27)  LDD0847  [10]
 LDCM0250  AC131 HEK-293T C322(1.04)  LDD0848  [10]
 LDCM0251  AC132 HEK-293T C322(1.15)  LDD0849  [10]
 LDCM0252  AC133 HEK-293T C322(1.34)  LDD0850  [10]
 LDCM0253  AC134 HEK-293T C322(1.43)  LDD0851  [10]
 LDCM0254  AC135 HEK-293T C322(1.23)  LDD0852  [10]
 LDCM0255  AC136 HEK-293T C322(1.39)  LDD0853  [10]
 LDCM0256  AC137 HEK-293T C322(1.95)  LDD0854  [10]
 LDCM0257  AC138 HEK-293T C322(2.22)  LDD0855  [10]
 LDCM0258  AC139 HEK-293T C322(1.76)  LDD0856  [10]
 LDCM0259  AC14 HEK-293T C322(1.17); C661(0.81)  LDD0857  [10]
 LDCM0260  AC140 HEK-293T C322(1.41)  LDD0858  [10]
 LDCM0261  AC141 HEK-293T C322(1.83)  LDD0859  [10]
 LDCM0262  AC142 HEK-293T C322(1.55)  LDD0860  [10]
 LDCM0263  AC143 HEK-293T C322(1.18); C661(1.02)  LDD0861  [10]
 LDCM0264  AC144 HEK-293T C322(2.12); C661(0.84)  LDD0862  [10]
 LDCM0265  AC145 HEK-293T C322(1.87); C661(0.74)  LDD0863  [10]
 LDCM0266  AC146 HEK-293T C322(2.41); C661(0.61)  LDD0864  [10]
 LDCM0267  AC147 HEK-293T C322(1.64); C661(0.74)  LDD0865  [10]
 LDCM0268  AC148 HEK-293T C322(1.49); C661(1.00)  LDD0866  [10]
 LDCM0269  AC149 HEK-293T C322(1.14); C661(0.84)  LDD0867  [10]
 LDCM0270  AC15 HEK-293T C322(1.45); C661(0.73)  LDD0868  [10]
 LDCM0271  AC150 HEK-293T C322(1.66); C661(0.96)  LDD0869  [10]
 LDCM0272  AC151 HEK-293T C322(1.54); C661(1.06)  LDD0870  [10]
 LDCM0273  AC152 HEK-293T C322(1.52); C661(0.88)  LDD0871  [10]
 LDCM0274  AC153 HEK-293T C322(1.49); C661(0.87)  LDD0872  [10]
 LDCM0621  AC154 HEK-293T C322(1.19); C661(0.96)  LDD2162  [10]
 LDCM0622  AC155 HEK-293T C322(1.49); C661(0.84)  LDD2163  [10]
 LDCM0623  AC156 HEK-293T C322(1.82); C661(0.78)  LDD2164  [10]
 LDCM0624  AC157 HEK-293T C322(2.02); C661(0.76)  LDD2165  [10]
 LDCM0276  AC17 HEK-293T C322(1.54)  LDD0874  [10]
 LDCM0277  AC18 HEK-293T C322(1.22)  LDD0875  [10]
 LDCM0278  AC19 HEK-293T C322(1.15)  LDD0876  [10]
 LDCM0279  AC2 HEK-293T C322(1.25)  LDD0877  [10]
 LDCM0280  AC20 HEK-293T C322(1.41)  LDD0878  [10]
 LDCM0281  AC21 HEK-293T C322(1.28)  LDD0879  [10]
 LDCM0282  AC22 HEK-293T C322(1.42)  LDD0880  [10]
 LDCM0283  AC23 HEK-293T C322(1.64)  LDD0881  [10]
 LDCM0284  AC24 HEK-293T C322(1.25)  LDD0882  [10]
 LDCM0285  AC25 PaTu 8988t C661(1.04)  LDD1164  [10]
 LDCM0286  AC26 PaTu 8988t C661(1.25)  LDD1165  [10]
 LDCM0287  AC27 PaTu 8988t C661(1.49)  LDD1166  [10]
 LDCM0288  AC28 PaTu 8988t C661(1.52)  LDD1167  [10]
 LDCM0289  AC29 PaTu 8988t C661(1.15)  LDD1168  [10]
 LDCM0290  AC3 HEK-293T C322(1.13)  LDD0888  [10]
 LDCM0291  AC30 PaTu 8988t C661(1.37)  LDD1170  [10]
 LDCM0292  AC31 PaTu 8988t C661(1.39)  LDD1171  [10]
 LDCM0293  AC32 PaTu 8988t C661(1.45)  LDD1172  [10]
 LDCM0294  AC33 PaTu 8988t C661(1.45)  LDD1173  [10]
 LDCM0295  AC34 PaTu 8988t C661(1.62)  LDD1174  [10]
 LDCM0296  AC35 HEK-293T C322(0.74)  LDD0894  [10]
 LDCM0297  AC36 HEK-293T C322(0.91)  LDD0895  [10]
 LDCM0298  AC37 HEK-293T C322(0.93)  LDD0896  [10]
 LDCM0299  AC38 HEK-293T C322(0.93)  LDD0897  [10]
 LDCM0300  AC39 HEK-293T C322(0.83)  LDD0898  [10]
 LDCM0301  AC4 HEK-293T C322(1.00)  LDD0899  [10]
 LDCM0302  AC40 HEK-293T C322(0.94)  LDD0900  [10]
 LDCM0303  AC41 HEK-293T C322(0.92)  LDD0901  [10]
 LDCM0304  AC42 HEK-293T C322(1.06)  LDD0902  [10]
 LDCM0305  AC43 HEK-293T C322(0.99)  LDD0903  [10]
 LDCM0306  AC44 HEK-293T C322(0.98)  LDD0904  [10]
 LDCM0307  AC45 HEK-293T C322(0.98)  LDD0905  [10]
 LDCM0308  AC46 HEK-293T C322(1.01)  LDD0906  [10]
 LDCM0309  AC47 HEK-293T C322(1.08)  LDD0907  [10]
 LDCM0310  AC48 HEK-293T C322(1.07)  LDD0908  [10]
 LDCM0311  AC49 HEK-293T C322(1.15)  LDD0909  [10]
 LDCM0312  AC5 HEK-293T C322(1.04)  LDD0910  [10]
 LDCM0313  AC50 HEK-293T C322(1.20)  LDD0911  [10]
 LDCM0314  AC51 HEK-293T C322(1.23)  LDD0912  [10]
 LDCM0315  AC52 HEK-293T C322(1.27)  LDD0913  [10]
 LDCM0316  AC53 HEK-293T C322(1.40)  LDD0914  [10]
 LDCM0317  AC54 HEK-293T C322(1.31)  LDD0915  [10]
 LDCM0318  AC55 HEK-293T C322(1.15)  LDD0916  [10]
 LDCM0319  AC56 HEK-293T C322(1.34)  LDD0917  [10]
 LDCM0320  AC57 HEK-293T C281(0.88); C661(0.95); C357(0.89)  LDD1559  [11]
 LDCM0321  AC58 HEK-293T C281(0.99); C661(0.98); C193(0.99)  LDD1560  [11]
 LDCM0322  AC59 HEK-293T C281(0.94); C661(1.00)  LDD1561  [11]
 LDCM0323  AC6 HEK-293T C322(1.16); C661(1.13)  LDD0921  [10]
 LDCM0324  AC60 HEK-293T C281(0.99); C661(1.39); C322(1.07)  LDD1563  [11]
 LDCM0325  AC61 HEK-293T C281(0.94); C193(1.08)  LDD1564  [11]
 LDCM0326  AC62 HEK-293T C281(0.98); C193(0.99); C322(1.02); C540(1.02)  LDD1565  [11]
 LDCM0327  AC63 HEK-293T C281(1.01); C193(0.97)  LDD1566  [11]
 LDCM0328  AC64 HEK-293T C281(0.98); C322(0.90)  LDD1567  [11]
 LDCM0332  AC68 HEK-293T C661(1.17)  LDD0930  [10]
 LDCM0333  AC69 HEK-293T C661(0.89)  LDD0931  [10]
 LDCM0334  AC7 HEK-293T C322(1.19); C661(1.35)  LDD0932  [10]
 LDCM0335  AC70 HEK-293T C661(1.20)  LDD0933  [10]
 LDCM0336  AC71 HEK-293T C661(0.77)  LDD0934  [10]
 LDCM0337  AC72 HEK-293T C661(0.88)  LDD0935  [10]
 LDCM0338  AC73 HEK-293T C661(1.21)  LDD0936  [10]
 LDCM0339  AC74 HEK-293T C661(0.93)  LDD0937  [10]
 LDCM0340  AC75 HEK-293T C661(0.72)  LDD0938  [10]
 LDCM0341  AC76 HEK-293T C661(1.00)  LDD0939  [10]
 LDCM0342  AC77 HEK-293T C661(0.90)  LDD0940  [10]
 LDCM0343  AC78 HEK-293T C661(0.82)  LDD0941  [10]
 LDCM0344  AC79 HEK-293T C661(0.83)  LDD0942  [10]
 LDCM0345  AC8 HEK-293T C322(1.49); C661(0.67)  LDD0943  [10]
 LDCM0346  AC80 HEK-293T C661(0.80)  LDD0944  [10]
 LDCM0347  AC81 HEK-293T C661(0.82)  LDD0945  [10]
 LDCM0348  AC82 HEK-293T C661(0.81)  LDD0946  [10]
 LDCM0349  AC83 PaTu 8988t C661(0.84)  LDD1228  [10]
 LDCM0350  AC84 PaTu 8988t C661(0.73)  LDD1229  [10]
 LDCM0351  AC85 PaTu 8988t C661(0.77)  LDD1230  [10]
 LDCM0352  AC86 PaTu 8988t C661(1.12)  LDD1231  [10]
 LDCM0353  AC87 PaTu 8988t C661(0.84)  LDD1232  [10]
 LDCM0354  AC88 PaTu 8988t C661(0.92)  LDD1233  [10]
 LDCM0355  AC89 PaTu 8988t C661(0.96)  LDD1234  [10]
 LDCM0357  AC90 PaTu 8988t C661(1.20)  LDD1236  [10]
 LDCM0358  AC91 PaTu 8988t C661(0.90)  LDD1237  [10]
 LDCM0359  AC92 PaTu 8988t C661(0.98)  LDD1238  [10]
 LDCM0360  AC93 PaTu 8988t C661(0.76)  LDD1239  [10]
 LDCM0361  AC94 PaTu 8988t C661(0.80)  LDD1240  [10]
 LDCM0362  AC95 PaTu 8988t C661(1.03)  LDD1241  [10]
 LDCM0363  AC96 PaTu 8988t C661(0.91)  LDD1242  [10]
 LDCM0364  AC97 PaTu 8988t C661(0.80)  LDD1243  [10]
 LDCM0365  AC98 HEK-293T C322(0.87)  LDD0963  [10]
 LDCM0366  AC99 HEK-293T C322(0.85)  LDD0964  [10]
 LDCM0248  AKOS034007472 HEK-293T C322(1.15); C661(1.15)  LDD0846  [10]
 LDCM0356  AKOS034007680 HEK-293T C322(1.55); C661(0.77)  LDD0954  [10]
 LDCM0275  AKOS034007705 HEK-293T C322(1.34); C661(0.73)  LDD0873  [10]
 LDCM0498  BS-3668 MDA-MB-231 C193(0.84)  LDD2091  [2]
 LDCM0367  CL1 HEK-293T C281(0.99); C446(0.97)  LDD1571  [11]
 LDCM0368  CL10 HEK-293T C281(0.89); C193(1.01); C322(1.19); C540(0.99)  LDD1572  [11]
 LDCM0369  CL100 HEK-293T C322(1.37)  LDD0967  [10]
 LDCM0370  CL101 HEK-293T C322(1.60); C661(0.67)  LDD0968  [10]
 LDCM0371  CL102 HEK-293T C322(1.75); C661(0.92)  LDD0969  [10]
 LDCM0372  CL103 HEK-293T C322(1.37); C661(0.66)  LDD0970  [10]
 LDCM0373  CL104 HEK-293T C322(1.44); C661(0.80)  LDD0971  [10]
 LDCM0374  CL105 HEK-293T C322(1.13)  LDD0972  [10]
 LDCM0375  CL106 HEK-293T C322(1.29)  LDD0973  [10]
 LDCM0376  CL107 HEK-293T C322(1.08)  LDD0974  [10]
 LDCM0377  CL108 HEK-293T C322(1.26)  LDD0975  [10]
 LDCM0378  CL109 HEK-293T C322(1.17)  LDD0976  [10]
 LDCM0379  CL11 HEK-293T C281(0.91); C193(1.03)  LDD1583  [11]
 LDCM0380  CL110 HEK-293T C322(1.43)  LDD0978  [10]
 LDCM0381  CL111 HEK-293T C322(1.21)  LDD0979  [10]
 LDCM0382  CL112 PaTu 8988t C661(1.11)  LDD1261  [10]
 LDCM0383  CL113 PaTu 8988t C661(1.23)  LDD1262  [10]
 LDCM0384  CL114 PaTu 8988t C661(1.27)  LDD1263  [10]
 LDCM0385  CL115 PaTu 8988t C661(1.19)  LDD1264  [10]
 LDCM0386  CL116 PaTu 8988t C661(1.28)  LDD1265  [10]
 LDCM0387  CL117 HEK-293T C322(0.88)  LDD0985  [10]
 LDCM0388  CL118 HEK-293T C322(0.80)  LDD0986  [10]
 LDCM0389  CL119 HEK-293T C322(1.05)  LDD0987  [10]
 LDCM0390  CL12 HEK-293T C281(0.96); C322(1.15)  LDD1594  [11]
 LDCM0391  CL120 HEK-293T C322(0.94)  LDD0989  [10]
 LDCM0392  CL121 HEK-293T C322(1.33)  LDD0990  [10]
 LDCM0393  CL122 HEK-293T C322(1.23)  LDD0991  [10]
 LDCM0394  CL123 HEK-293T C322(1.10)  LDD0992  [10]
 LDCM0395  CL124 HEK-293T C322(1.21)  LDD0993  [10]
 LDCM0396  CL125 HEK-293T C281(1.04); C446(0.89)  LDD1600  [11]
 LDCM0397  CL126 HEK-293T C281(0.95); C661(1.04)  LDD1601  [11]
 LDCM0398  CL127 HEK-293T C281(0.96); C357(0.79)  LDD1602  [11]
 LDCM0399  CL128 HEK-293T C281(0.94); C661(1.05); C357(0.88)  LDD1603  [11]
 LDCM0400  CL13 HEK-293T C281(1.06); C446(0.94)  LDD1604  [11]
 LDCM0401  CL14 HEK-293T C281(1.01); C661(1.28)  LDD1605  [11]
 LDCM0402  CL15 HEK-293T C281(0.74); C357(0.96)  LDD1606  [11]
 LDCM0403  CL16 HEK-293T C322(1.12)  LDD1001  [10]
 LDCM0404  CL17 HEK-293T C322(1.07)  LDD1002  [10]
 LDCM0405  CL18 HEK-293T C322(1.13)  LDD1003  [10]
 LDCM0406  CL19 HEK-293T C322(1.18)  LDD1004  [10]
 LDCM0407  CL2 HEK-293T C281(1.04); C661(1.39)  LDD1611  [11]
 LDCM0408  CL20 HEK-293T C322(1.15)  LDD1006  [10]
 LDCM0409  CL21 HEK-293T C322(1.17)  LDD1007  [10]
 LDCM0410  CL22 HEK-293T C322(1.17)  LDD1008  [10]
 LDCM0411  CL23 HEK-293T C322(0.92)  LDD1009  [10]
 LDCM0412  CL24 HEK-293T C322(0.96)  LDD1010  [10]
 LDCM0413  CL25 HEK-293T C322(1.21)  LDD1011  [10]
 LDCM0414  CL26 HEK-293T C322(1.00)  LDD1012  [10]
 LDCM0415  CL27 HEK-293T C322(1.03)  LDD1013  [10]
 LDCM0416  CL28 HEK-293T C322(0.99)  LDD1014  [10]
 LDCM0417  CL29 HEK-293T C322(1.02)  LDD1015  [10]
 LDCM0418  CL3 HEK-293T C281(0.91); C357(0.86)  LDD1622  [11]
 LDCM0419  CL30 HEK-293T C322(1.27)  LDD1017  [10]
 LDCM0420  CL31 HEK-293T C322(1.44)  LDD1018  [10]
 LDCM0421  CL32 HEK-293T C322(1.27)  LDD1019  [10]
 LDCM0422  CL33 HEK-293T C322(2.06)  LDD1020  [10]
 LDCM0423  CL34 HEK-293T C322(1.38)  LDD1021  [10]
 LDCM0424  CL35 HEK-293T C322(1.36)  LDD1022  [10]
 LDCM0425  CL36 HEK-293T C322(1.33)  LDD1023  [10]
 LDCM0426  CL37 HEK-293T C322(1.42)  LDD1024  [10]
 LDCM0428  CL39 HEK-293T C322(2.26)  LDD1026  [10]
 LDCM0429  CL4 HEK-293T C281(0.92); C661(0.99); C357(0.88)  LDD1633  [11]
 LDCM0430  CL40 HEK-293T C322(1.40)  LDD1028  [10]
 LDCM0431  CL41 HEK-293T C322(2.02)  LDD1029  [10]
 LDCM0432  CL42 HEK-293T C322(1.81)  LDD1030  [10]
 LDCM0433  CL43 HEK-293T C322(1.94)  LDD1031  [10]
 LDCM0434  CL44 HEK-293T C322(1.41)  LDD1032  [10]
 LDCM0435  CL45 HEK-293T C322(1.89)  LDD1033  [10]
 LDCM0436  CL46 HEK-293T C661(0.99)  LDD1034  [10]
 LDCM0437  CL47 HEK-293T C661(0.82)  LDD1035  [10]
 LDCM0438  CL48 HEK-293T C661(1.06)  LDD1036  [10]
 LDCM0439  CL49 HEK-293T C661(0.81)  LDD1037  [10]
 LDCM0440  CL5 HEK-293T C281(0.84); C661(1.13); C357(0.94)  LDD1644  [11]
 LDCM0441  CL50 HEK-293T C661(0.84)  LDD1039  [10]
 LDCM0442  CL51 HEK-293T C661(0.97)  LDD1040  [10]
 LDCM0443  CL52 HEK-293T C661(0.91)  LDD1041  [10]
 LDCM0444  CL53 HEK-293T C661(0.93)  LDD1042  [10]
 LDCM0445  CL54 HEK-293T C661(0.81)  LDD1043  [10]
 LDCM0446  CL55 HEK-293T C661(0.77)  LDD1044  [10]
 LDCM0447  CL56 HEK-293T C661(0.92)  LDD1045  [10]
 LDCM0448  CL57 HEK-293T C661(0.91)  LDD1046  [10]
 LDCM0449  CL58 HEK-293T C661(0.98)  LDD1047  [10]
 LDCM0450  CL59 HEK-293T C661(0.87)  LDD1048  [10]
 LDCM0451  CL6 HEK-293T C281(0.91); C661(1.03); C193(1.11)  LDD1654  [11]
 LDCM0452  CL60 HEK-293T C661(1.10)  LDD1050  [10]
 LDCM0453  CL61 HEK-293T C322(1.24)  LDD1051  [10]
 LDCM0454  CL62 HEK-293T C322(1.33)  LDD1052  [10]
 LDCM0455  CL63 HEK-293T C322(1.53)  LDD1053  [10]
 LDCM0456  CL64 HEK-293T C322(1.33)  LDD1054  [10]
 LDCM0457  CL65 HEK-293T C322(1.35)  LDD1055  [10]
 LDCM0458  CL66 HEK-293T C322(1.37)  LDD1056  [10]
 LDCM0459  CL67 HEK-293T C322(1.22)  LDD1057  [10]
 LDCM0460  CL68 HEK-293T C322(1.31)  LDD1058  [10]
 LDCM0461  CL69 HEK-293T C322(1.19)  LDD1059  [10]
 LDCM0462  CL7 HEK-293T C281(0.92); C661(1.12)  LDD1665  [11]
 LDCM0463  CL70 HEK-293T C322(1.10)  LDD1061  [10]
 LDCM0464  CL71 HEK-293T C322(1.23)  LDD1062  [10]
 LDCM0465  CL72 HEK-293T C322(1.09)  LDD1063  [10]
 LDCM0466  CL73 HEK-293T C322(1.25)  LDD1064  [10]
 LDCM0467  CL74 HEK-293T C322(2.09)  LDD1065  [10]
 LDCM0469  CL76 HEK-293T C322(0.97); C661(1.02)  LDD1067  [10]
 LDCM0470  CL77 HEK-293T C322(1.02); C661(0.96)  LDD1068  [10]
 LDCM0471  CL78 HEK-293T C322(0.84); C661(0.85)  LDD1069  [10]
 LDCM0472  CL79 HEK-293T C322(0.96); C661(0.99)  LDD1070  [10]
 LDCM0473  CL8 HEK-293T C281(0.80); C661(1.23); C322(1.20)  LDD1676  [11]
 LDCM0474  CL80 HEK-293T C322(0.92); C661(1.09)  LDD1072  [10]
 LDCM0475  CL81 HEK-293T C322(1.01); C661(0.99)  LDD1073  [10]
 LDCM0476  CL82 HEK-293T C322(1.11); C661(0.88)  LDD1074  [10]
 LDCM0477  CL83 HEK-293T C322(1.15); C661(0.86)  LDD1075  [10]
 LDCM0478  CL84 HEK-293T C322(1.02); C661(1.02)  LDD1076  [10]
 LDCM0479  CL85 HEK-293T C322(0.84); C661(0.98)  LDD1077  [10]
 LDCM0480  CL86 HEK-293T C322(0.73); C661(1.12)  LDD1078  [10]
 LDCM0481  CL87 HEK-293T C322(0.87); C661(1.14)  LDD1079  [10]
 LDCM0482  CL88 HEK-293T C322(0.99); C661(1.04)  LDD1080  [10]
 LDCM0483  CL89 HEK-293T C322(0.93); C661(0.97)  LDD1081  [10]
 LDCM0484  CL9 HEK-293T C281(0.91); C193(1.18)  LDD1687  [11]
 LDCM0485  CL90 HEK-293T C322(1.30); C661(0.90)  LDD1083  [10]
 LDCM0486  CL91 HEK-293T C322(1.06)  LDD1084  [10]
 LDCM0487  CL92 HEK-293T C322(1.21)  LDD1085  [10]
 LDCM0488  CL93 HEK-293T C322(1.27)  LDD1086  [10]
 LDCM0489  CL94 HEK-293T C322(1.60)  LDD1087  [10]
 LDCM0490  CL95 HEK-293T C322(2.04)  LDD1088  [10]
 LDCM0491  CL96 HEK-293T C322(1.34)  LDD1089  [10]
 LDCM0492  CL97 HEK-293T C322(1.17)  LDD1090  [10]
 LDCM0493  CL98 HEK-293T C322(1.23)  LDD1091  [10]
 LDCM0494  CL99 HEK-293T C322(1.23)  LDD1092  [10]
 LDCM0198  Dimethyl Fumarate(DMF) T cell C14, C17, C20(5.11)  LDD0526  [12]
 LDCM0495  E2913 HEK-293T C281(1.07); C357(0.96)  LDD1698  [11]
 LDCM0468  Fragment33 HEK-293T C322(1.78)  LDD1066  [10]
 LDCM0427  Fragment51 HEK-293T C322(1.48)  LDD1025  [10]
 LDCM0569  Fragment7 Jurkat _(20.00)  LDD1485  [3]
 LDCM0022  KB02 HEK-293T C281(1.00); C661(1.02)  LDD1492  [11]
 LDCM0023  KB03 Jurkat C661(5.22)  LDD0209  [4]
 LDCM0024  KB05 HMCB C281(1.13)  LDD3312  [13]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C193(0.69)  LDD2121  [2]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C193(0.91)  LDD2089  [2]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C281(1.05)  LDD2093  [2]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C281(0.92)  LDD2099  [2]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C281(0.72)  LDD2101  [2]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C281(1.00); C193(1.03)  LDD2107  [2]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C281(0.53)  LDD2109  [2]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C281(0.95); C193(0.80)  LDD2111  [2]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C281(0.74); C193(1.18)  LDD2123  [2]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C281(0.90); C193(0.97); C526(1.42)  LDD2127  [2]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C281(1.13)  LDD2129  [2]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C281(1.25)  LDD2135  [2]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C281(1.09)  LDD2136  [2]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C281(0.76)  LDD2137  [2]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C281(1.87)  LDD1700  [2]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C281(0.61)  LDD2140  [2]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C281(2.49)  LDD2144  [2]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C281(0.91)  LDD2146  [2]
 LDCM0021  THZ1 HeLa S3 C661(2.76)  LDD0460  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein kinase C zeta type (PRKCZ) AGC Ser/Thr protein kinase family Q05513
Mitogen-activated protein kinase kinase kinase kinase 3 (MAP4K3) STE Ser/Thr protein kinase family Q8IVH8
Tyrosine-protein kinase Fyn (FYN) Tyr protein kinase family P06241
Tyrosine-protein kinase Lck (LCK) Tyr protein kinase family P06239
Tyrosine-protein kinase BTK (BTK) Tyr protein kinase family Q06187
Glutaredoxin-3 (GLRX3) . O76003
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Heat shock factor protein 1 (HSF1) HSF family Q00613

The Drug(s) Related To This Target

Approved
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dequalinium Small molecular drug DB04209
Fostamatinib Small molecular drug DB12010
Tamoxifen Small molecular drug DB00675
Benzoyl Peroxide . DB09096
Investigative
Click To Hide/Show 14 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Isis 109351 Antisense drug D00NQN
Isis 109352 Antisense drug D00PYD
Isis 109353 Antisense drug D00XRM
Isis 109354 Antisense drug D0TT6X
Isis 109355 Antisense drug D05QWZ
4-(1h-indol-5-ylamino)-5-styrylnicotinonitrile Small molecular drug D0U9YY
4-(1h-indol-5-yloxy)-5-styrylnicotinonitrile Small molecular drug D0S7UD
4-(1h-indol-6-ylamino)-5-styrylnicotinonitrile Small molecular drug D08HCY
4-(3h-indol-4-ylamino)-5-styrylnicotinonitrile Small molecular drug D0W1FM
8-octyl-benzolactam-v9 Small molecular drug D04AXH
Dexfosfoserine Small molecular drug DB04522
Phosphonothreonine Small molecular drug DB02482
Prostratin Small molecular drug D04JNZ
Staurosporine Small molecular drug DB02010

References

1 A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification. J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.
2 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
3 Proteome-wide covalent ligand discovery in native biological systems. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15.
4 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
5 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
6 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
7 Benchmarking Cleavable Biotin Tags for Peptide-Centric Chemoproteomics. J Proteome Res. 2022 May 6;21(5):1349-1358. doi: 10.1021/acs.jproteome.2c00174. Epub 2022 Apr 25.
Mass spectrometry data entry: PXD031019
8 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.
9 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
10 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.
11 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
12 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.
13 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840