Details of the Target

General Information of Target

Target ID LDTP00252
Target Name Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PIK3CD)
Gene Name PIK3CD
Gene ID 5293
Synonyms
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform; PI3-kinase subunit delta; PI3K-delta; PI3Kdelta; PtdIns-3-kinase subunit delta; EC 2.7.1.137; EC 2.7.1.153; Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit delta; PtdIns-3-kinase subunit p110-delta; p110delta
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MPPGVDCPMEFWTKEENQSVVVDFLLPTGVYLNFPVSRNANLSTIKQLLWHRAQYEPLFH
MLSGPEAYVFTCINQTAEQQELEDEQRRLCDVQPFLPVLRLVAREGDRVKKLINSQISLL
IGKGLHEFDSLCDPEVNDFRAKMCQFCEEAAARRQQLGWEAWLQYSFPLQLEPSAQTWGP
GTLRLPNRALLVNVKFEGSEESFTFQVSTKDVPLALMACALRKKATVFRQPLVEQPEDYT
LQVNGRHEYLYGSYPLCQFQYICSCLHSGLTPHLTMVHSSSILAMRDEQSNPAPQVQKPR
AKPPPIPAKKPSSVSLWSLEQPFRIELIQGSKVNADERMKLVVQAGLFHGNEMLCKTVSS
SEVSVCSEPVWKQRLEFDINICDLPRMARLCFALYAVIEKAKKARSTKKKSKKADCPIAW
ANLMLFDYKDQLKTGERCLYMWPSVPDEKGELLNPTGTVRSNPNTDSAAALLICLPEVAP
HPVYYPALEKILELGRHSECVHVTEEEQLQLREILERRGSGELYEHEKDLVWKLRHEVQE
HFPEALARLLLVTKWNKHEDVAQMLYLLCSWPELPVLSALELLDFSFPDCHVGSFAIKSL
RKLTDDELFQYLLQLVQVLKYESYLDCELTKFLLDRALANRKIGHFLFWHLRSEMHVPSV
ALRFGLILEAYCRGSTHHMKVLMKQGEALSKLKALNDFVKLSSQKTPKPQTKELMHLCMR
QEAYLEALSHLQSPLDPSTLLAEVCVEQCTFMDSKMKPLWIMYSNEEAGSGGSVGIIFKN
GDDLRQDMLTLQMIQLMDVLWKQEGLDLRMTPYGCLPTGDRTGLIEVVLRSDTIANIQLN
KSNMAATAAFNKDALLNWLKSKNPGEALDRAIEEFTLSCAGYCVATYVLGIGDRHSDNIM
IRESGQLFHIDFGHFLGNFKTKFGINRERVPFILTYDFVHVIQQGKTNNSEKFERFRGYC
ERAYTILRRHGLLFLHLFALMRAAGLPELSCSKDIQYLKDSLALGKTEEEALKHFRVKFN
EALRESWKTKVNWLAHNVSKDNRQ
Target Type
Successful
Target Bioclass
Enzyme
Family
PI3/PI4-kinase family
Subcellular location
Cytoplasm
Function
Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol (PI) and its phosphorylated derivatives at position 3 of the inositol ring to produce 3-phosphoinositides. Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Mediates immune responses. Plays a role in B-cell development, proliferation, migration, and function. Required for B-cell receptor (BCR) signaling. Mediates B-cell proliferation response to anti-IgM, anti-CD40 and IL4 stimulation. Promotes cytokine production in response to TLR4 and TLR9. Required for antibody class switch mediated by TLR9. Involved in the antigen presentation function of B-cells. Involved in B-cell chemotaxis in response to CXCL13 and sphingosine 1-phosphate (S1P). Required for proliferation, signaling and cytokine production of naive, effector and memory T-cells. Required for T-cell receptor (TCR) signaling. Mediates TCR signaling events at the immune synapse. Activation by TCR leads to antigen-dependent memory T-cell migration and retention to antigenic tissues. Together with PIK3CG participates in T-cell development. Contributes to T-helper cell expansion and differentiation. Required for T-cell migration mediated by homing receptors SELL/CD62L, CCR7 and S1PR1 and antigen dependent recruitment of T-cells. Together with PIK3CG is involved in natural killer (NK) cell development and migration towards the sites of inflammation. Participates in NK cell receptor activation. Plays a role in NK cell maturation and cytokine production. Together with PIK3CG is involved in neutrophil chemotaxis and extravasation. Together with PIK3CG participates in neutrophil respiratory burst. Plays important roles in mast-cell development and mast cell mediated allergic response. Involved in stem cell factor (SCF)-mediated proliferation, adhesion and migration. Required for allergen-IgE-induced degranulation and cytokine release. The lipid kinase activity is required for its biological function. Isoform 2 may be involved in stabilizing total RAS levels, resulting in increased ERK phosphorylation and increased PI3K activity.
TTD ID
T67849
Uniprot ID
O00329
DrugMap ID
TTK5FVJ
Ensemble ID
ENST00000377346.9
HGNC ID
HGNC:8977
ChEMBL ID
CHEMBL3130

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HEC1 SNV: p.S764N DBIA    Probe Info 
HEC1B SNV: p.S764N .
HT115 SNV: p.L725I; p.E1021K .
Ishikawa (Heraklio) 02 ER Deletion: p.N464TfsTer83 .
JURKAT SNV: p.A396T .
MDAMB453 SNV: p.G4E .
MEWO SNV: p.P186S DBIA    Probe Info 
MOLT4 SNV: p.A388T; p.S738N IA-alkyne    Probe Info 
NCIH1993 SNV: p.E320D; p.E320Ter .
PEO1 SNV: p.C132Y .
REH SNV: p.E1021K DBIA    Probe Info 
SNU1 SNV: p.P294H DBIA    Probe Info 
TE8 SNV: p.M683I .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 9 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
BTD
 Probe Info  		C991(0.56)  LDD2140  [1]
Johansson_61
 Probe Info  		_(6.74)  LDD1485  [2]
AHL-Pu-1
 Probe Info  		C474(3.29)  LDD0170  [3]
DBIA
 Probe Info  		C991(6.96)  LDD0209  [4]
4-Iodoacetamidophenylacetylene
 Probe Info  		C991(0.00); C219(0.00); C132(0.00); C90(0.00)  LDD0038  [5]
IA-alkyne
 Probe Info  		C438(0.00); C219(0.00); C132(0.00); C90(0.00)  LDD0036  [5]
Lodoacetamide azide
 Probe Info  		C438(0.00); C219(0.00); C132(0.00); C90(0.00)  LDD0037  [5]
NAIA_4
 Probe Info  		C90(0.00); C474(0.00)  LDD2226  [6]
KY-26
 Probe Info  		N.A.  LDD0301  [7]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
VE-P
 Probe Info  		N.A.  LDD0396  [8]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0025  4SU-RNA DM93 C474(3.29)  LDD0170  [3]
 LDCM0026  4SU-RNA+native RNA DM93 C219(4.97)  LDD0171  [3]
 LDCM0214  AC1 PaTu 8988t C90(1.69)  LDD1093  [9]
 LDCM0215  AC10 PaTu 8988t C144(0.62); C147(0.62); C90(1.16)  LDD1094  [9]
 LDCM0216  AC100 PaTu 8988t C144(1.04); C147(1.04); C219(0.98); C90(0.99)  LDD1095  [9]
 LDCM0217  AC101 PaTu 8988t C144(0.97); C147(0.97); C219(0.94); C90(1.06)  LDD1096  [9]
 LDCM0218  AC102 PaTu 8988t C144(0.81); C147(0.81); C219(0.90); C90(1.22)  LDD1097  [9]
 LDCM0219  AC103 PaTu 8988t C144(0.91); C147(0.91); C219(1.06); C90(1.30)  LDD1098  [9]
 LDCM0220  AC104 PaTu 8988t C144(1.54); C147(1.54); C219(0.81); C90(1.04)  LDD1099  [9]
 LDCM0221  AC105 PaTu 8988t C144(1.02); C147(1.02); C219(0.72); C90(0.97)  LDD1100  [9]
 LDCM0222  AC106 PaTu 8988t C144(0.81); C147(0.81); C219(0.83); C90(1.14)  LDD1101  [9]
 LDCM0223  AC107 PaTu 8988t C144(0.84); C147(0.84); C219(1.09); C90(0.91)  LDD1102  [9]
 LDCM0224  AC108 PaTu 8988t C144(0.81); C147(0.81); C219(0.88); C90(1.12)  LDD1103  [9]
 LDCM0225  AC109 PaTu 8988t C144(0.78); C147(0.78); C219(0.96); C90(1.20)  LDD1104  [9]
 LDCM0226  AC11 PaTu 8988t C144(0.67); C147(0.67); C90(1.09)  LDD1105  [9]
 LDCM0227  AC110 PaTu 8988t C144(0.72); C147(0.72); C219(1.16); C90(1.22)  LDD1106  [9]
 LDCM0228  AC111 PaTu 8988t C144(0.74); C147(0.74); C219(0.55); C90(1.21)  LDD1107  [9]
 LDCM0229  AC112 PaTu 8988t C144(0.79); C147(0.79); C219(0.75); C90(1.14)  LDD1108  [9]
 LDCM0230  AC113 PaTu 8988t C144(1.35); C147(1.35); C90(1.00)  LDD1109  [9]
 LDCM0231  AC114 PaTu 8988t C144(0.85); C147(0.85); C90(1.04)  LDD1110  [9]
 LDCM0232  AC115 PaTu 8988t C144(1.10); C147(1.10); C90(1.17)  LDD1111  [9]
 LDCM0233  AC116 PaTu 8988t C144(1.28); C147(1.28); C90(1.06)  LDD1112  [9]
 LDCM0234  AC117 PaTu 8988t C144(1.27); C147(1.27); C90(1.07)  LDD1113  [9]
 LDCM0235  AC118 PaTu 8988t C144(0.84); C147(0.84); C90(1.04)  LDD1114  [9]
 LDCM0236  AC119 PaTu 8988t C144(1.11); C147(1.11); C90(1.03)  LDD1115  [9]
 LDCM0237  AC12 PaTu 8988t C144(0.71); C147(0.71); C90(1.14)  LDD1116  [9]
 LDCM0238  AC120 PaTu 8988t C144(1.33); C147(1.33); C90(0.92)  LDD1117  [9]
 LDCM0239  AC121 PaTu 8988t C144(0.93); C147(0.93); C90(1.14)  LDD1118  [9]
 LDCM0240  AC122 PaTu 8988t C144(1.02); C147(1.02); C90(0.94)  LDD1119  [9]
 LDCM0241  AC123 PaTu 8988t C144(1.21); C147(1.21); C90(0.97)  LDD1120  [9]
 LDCM0242  AC124 PaTu 8988t C144(0.97); C147(0.97); C90(1.05)  LDD1121  [9]
 LDCM0243  AC125 PaTu 8988t C144(0.85); C147(0.85); C90(1.22)  LDD1122  [9]
 LDCM0244  AC126 PaTu 8988t C144(1.01); C147(1.01); C90(0.98)  LDD1123  [9]
 LDCM0245  AC127 PaTu 8988t C144(1.16); C147(1.16); C90(0.98)  LDD1124  [9]
 LDCM0246  AC128 PaTu 8988t C144(0.93); C147(0.93); C90(1.03)  LDD1125  [9]
 LDCM0247  AC129 PaTu 8988t C144(0.72); C147(0.72); C90(1.21)  LDD1126  [9]
 LDCM0249  AC130 PaTu 8988t C144(0.80); C147(0.80); C90(1.00)  LDD1128  [9]
 LDCM0250  AC131 PaTu 8988t C144(0.96); C147(0.96); C90(1.04)  LDD1129  [9]
 LDCM0251  AC132 PaTu 8988t C144(0.79); C147(0.79); C90(1.22)  LDD1130  [9]
 LDCM0252  AC133 PaTu 8988t C144(0.87); C147(0.87); C90(1.12)  LDD1131  [9]
 LDCM0253  AC134 PaTu 8988t C144(0.90); C147(0.90); C90(1.06)  LDD1132  [9]
 LDCM0254  AC135 PaTu 8988t C144(0.85); C147(0.85); C90(1.12)  LDD1133  [9]
 LDCM0255  AC136 PaTu 8988t C144(0.91); C147(0.91); C90(1.26)  LDD1134  [9]
 LDCM0256  AC137 PaTu 8988t C144(0.83); C147(0.83); C90(1.03)  LDD1135  [9]
 LDCM0257  AC138 PaTu 8988t C144(0.84); C147(0.84); C90(1.11)  LDD1136  [9]
 LDCM0258  AC139 PaTu 8988t C144(1.12); C147(1.12); C90(1.10)  LDD1137  [9]
 LDCM0259  AC14 PaTu 8988t C144(0.67); C147(0.67); C90(0.81)  LDD1138  [9]
 LDCM0260  AC140 PaTu 8988t C144(1.19); C147(1.19); C90(1.10)  LDD1139  [9]
 LDCM0261  AC141 PaTu 8988t C144(0.94); C147(0.94); C90(1.22)  LDD1140  [9]
 LDCM0262  AC142 PaTu 8988t C144(0.87); C147(0.87); C90(1.11)  LDD1141  [9]
 LDCM0263  AC143 PaTu 8988t C144(0.74); C147(0.74); C219(0.89)  LDD1142  [9]
 LDCM0264  AC144 PaTu 8988t C144(0.73); C147(0.73); C219(0.85)  LDD1143  [9]
 LDCM0265  AC145 PaTu 8988t C144(0.80); C147(0.80); C219(1.07)  LDD1144  [9]
 LDCM0266  AC146 PaTu 8988t C144(0.55); C147(0.55); C219(1.04)  LDD1145  [9]
 LDCM0267  AC147 PaTu 8988t C144(0.71); C147(0.71); C219(1.00)  LDD1146  [9]
 LDCM0268  AC148 PaTu 8988t C144(0.65); C147(0.65); C219(1.12)  LDD1147  [9]
 LDCM0269  AC149 PaTu 8988t C144(0.67); C147(0.67); C219(1.19)  LDD1148  [9]
 LDCM0270  AC15 PaTu 8988t C144(0.65); C147(0.65); C90(0.96)  LDD1149  [9]
 LDCM0271  AC150 PaTu 8988t C144(0.53); C147(0.53); C219(1.23)  LDD1150  [9]
 LDCM0272  AC151 PaTu 8988t C144(0.58); C147(0.58); C219(1.57)  LDD1151  [9]
 LDCM0273  AC152 PaTu 8988t C144(0.64); C147(0.64); C219(1.07)  LDD1152  [9]
 LDCM0274  AC153 PaTu 8988t C144(0.52); C147(0.52); C219(1.27)  LDD1153  [9]
 LDCM0621  AC154 PaTu 8988t C144(0.58); C147(0.58); C219(1.51)  LDD2166  [9]
 LDCM0622  AC155 PaTu 8988t C144(0.58); C147(0.58); C219(1.17)  LDD2167  [9]
 LDCM0623  AC156 PaTu 8988t C144(0.62); C147(0.62); C219(1.17)  LDD2168  [9]
 LDCM0624  AC157 PaTu 8988t C144(0.56); C147(0.56); C219(1.46)  LDD2169  [9]
 LDCM0276  AC17 PaTu 8988t C219(0.82); C90(0.80)  LDD1155  [9]
 LDCM0277  AC18 PaTu 8988t C219(0.86); C90(1.00)  LDD1156  [9]
 LDCM0278  AC19 PaTu 8988t C219(1.00); C90(0.88)  LDD1157  [9]
 LDCM0279  AC2 PaTu 8988t C90(1.41)  LDD1158  [9]
 LDCM0280  AC20 PaTu 8988t C219(0.75); C90(1.00)  LDD1159  [9]
 LDCM0281  AC21 PaTu 8988t C219(0.76); C90(0.86)  LDD1160  [9]
 LDCM0282  AC22 PaTu 8988t C219(0.96); C90(1.03)  LDD1161  [9]
 LDCM0283  AC23 PaTu 8988t C219(0.96); C90(1.27)  LDD1162  [9]
 LDCM0284  AC24 PaTu 8988t C219(0.92); C90(1.03)  LDD1163  [9]
 LDCM0285  AC25 PaTu 8988t C144(0.91); C147(0.91); C219(0.88); C90(0.98)  LDD1164  [9]
 LDCM0286  AC26 PaTu 8988t C144(0.87); C147(0.87); C219(0.91); C90(1.04)  LDD1165  [9]
 LDCM0287  AC27 PaTu 8988t C144(0.95); C147(0.95); C219(1.16); C90(1.06)  LDD1166  [9]
 LDCM0288  AC28 PaTu 8988t C144(0.88); C147(0.88); C219(1.15); C90(1.07)  LDD1167  [9]
 LDCM0289  AC29 PaTu 8988t C144(0.76); C147(0.76); C219(1.06); C90(1.02)  LDD1168  [9]
 LDCM0290  AC3 PaTu 8988t C90(1.26)  LDD1169  [9]
 LDCM0291  AC30 PaTu 8988t C144(1.26); C147(1.26); C219(1.07); C90(1.02)  LDD1170  [9]
 LDCM0292  AC31 PaTu 8988t C144(0.87); C147(0.87); C219(0.92); C90(0.89)  LDD1171  [9]
 LDCM0293  AC32 PaTu 8988t C144(0.79); C147(0.79); C219(0.91); C90(0.93)  LDD1172  [9]
 LDCM0294  AC33 PaTu 8988t C144(0.75); C147(0.75); C219(1.23); C90(0.97)  LDD1173  [9]
 LDCM0295  AC34 PaTu 8988t C144(0.68); C147(0.68); C219(0.91); C90(1.26)  LDD1174  [9]
 LDCM0296  AC35 PaTu 8988t C144(1.37); C147(1.37); C90(1.06)  LDD1175  [9]
 LDCM0297  AC36 PaTu 8988t C144(1.10); C147(1.10); C90(1.20)  LDD1176  [9]
 LDCM0298  AC37 PaTu 8988t C144(0.83); C147(0.83); C90(1.23)  LDD1177  [9]
 LDCM0299  AC38 PaTu 8988t C144(0.88); C147(0.88); C90(1.34)  LDD1178  [9]
 LDCM0300  AC39 PaTu 8988t C144(1.09); C147(1.09); C90(1.24)  LDD1179  [9]
 LDCM0301  AC4 PaTu 8988t C90(1.09)  LDD1180  [9]
 LDCM0302  AC40 PaTu 8988t C144(0.75); C147(0.75); C90(1.46)  LDD1181  [9]
 LDCM0303  AC41 PaTu 8988t C144(0.89); C147(0.89); C90(1.18)  LDD1182  [9]
 LDCM0304  AC42 PaTu 8988t C144(0.71); C147(0.71); C90(1.30)  LDD1183  [9]
 LDCM0305  AC43 PaTu 8988t C144(1.03); C147(1.03); C90(1.27)  LDD1184  [9]
 LDCM0306  AC44 PaTu 8988t C144(0.71); C147(0.71); C90(1.36)  LDD1185  [9]
 LDCM0307  AC45 PaTu 8988t C144(0.73); C147(0.73); C90(1.27)  LDD1186  [9]
 LDCM0308  AC46 PaTu 8988t C219(1.08)  LDD1187  [9]
 LDCM0309  AC47 PaTu 8988t C219(1.12)  LDD1188  [9]
 LDCM0310  AC48 PaTu 8988t C219(1.19)  LDD1189  [9]
 LDCM0311  AC49 PaTu 8988t C219(1.04)  LDD1190  [9]
 LDCM0312  AC5 PaTu 8988t C90(1.55)  LDD1191  [9]
 LDCM0313  AC50 PaTu 8988t C219(1.00)  LDD1192  [9]
 LDCM0314  AC51 PaTu 8988t C219(0.94)  LDD1193  [9]
 LDCM0315  AC52 PaTu 8988t C219(1.09)  LDD1194  [9]
 LDCM0316  AC53 PaTu 8988t C219(1.11)  LDD1195  [9]
 LDCM0317  AC54 PaTu 8988t C219(1.35)  LDD1196  [9]
 LDCM0318  AC55 PaTu 8988t C219(0.97)  LDD1197  [9]
 LDCM0319  AC56 PaTu 8988t C219(1.24)  LDD1198  [9]
 LDCM0320  AC57 PaTu 8988t C90(1.25)  LDD1199  [9]
 LDCM0321  AC58 PaTu 8988t C90(1.25)  LDD1200  [9]
 LDCM0322  AC59 PaTu 8988t C90(1.13)  LDD1201  [9]
 LDCM0323  AC6 PaTu 8988t C144(1.08); C147(1.08); C90(0.94)  LDD1202  [9]
 LDCM0324  AC60 PaTu 8988t C90(1.36)  LDD1203  [9]
 LDCM0325  AC61 PaTu 8988t C90(1.23)  LDD1204  [9]
 LDCM0326  AC62 PaTu 8988t C90(1.17)  LDD1205  [9]
 LDCM0327  AC63 PaTu 8988t C90(1.22)  LDD1206  [9]
 LDCM0328  AC64 PaTu 8988t C90(1.15)  LDD1207  [9]
 LDCM0329  AC65 PaTu 8988t C90(1.05)  LDD1208  [9]
 LDCM0330  AC66 PaTu 8988t C90(1.20)  LDD1209  [9]
 LDCM0331  AC67 PaTu 8988t C90(1.16)  LDD1210  [9]
 LDCM0332  AC68 PaTu 8988t C144(1.00); C147(1.00); C219(1.00); C90(0.81)  LDD1211  [9]
 LDCM0333  AC69 PaTu 8988t C144(0.89); C147(0.89); C219(0.89); C90(1.13)  LDD1212  [9]
 LDCM0334  AC7 PaTu 8988t C144(1.23); C147(1.23); C90(0.98)  LDD1213  [9]
 LDCM0335  AC70 PaTu 8988t C144(0.92); C147(0.92); C219(1.10); C90(0.98)  LDD1214  [9]
 LDCM0336  AC71 PaTu 8988t C144(1.15); C147(1.15); C219(1.27); C90(1.16)  LDD1215  [9]
 LDCM0337  AC72 PaTu 8988t C144(1.07); C147(1.07); C219(1.03); C90(0.95)  LDD1216  [9]
 LDCM0338  AC73 PaTu 8988t C144(1.14); C147(1.14); C219(1.30); C90(0.84)  LDD1217  [9]
 LDCM0339  AC74 PaTu 8988t C144(0.91); C147(0.91); C219(1.12); C90(1.12)  LDD1218  [9]
 LDCM0340  AC75 PaTu 8988t C144(1.14); C147(1.14); C219(1.05); C90(1.12)  LDD1219  [9]
 LDCM0341  AC76 PaTu 8988t C144(0.98); C147(0.98); C219(1.23); C90(1.00)  LDD1220  [9]
 LDCM0342  AC77 PaTu 8988t C144(1.07); C147(1.07); C219(1.22); C90(1.00)  LDD1221  [9]
 LDCM0343  AC78 PaTu 8988t C144(0.91); C147(0.91); C219(1.04); C90(1.01)  LDD1222  [9]
 LDCM0344  AC79 PaTu 8988t C144(1.05); C147(1.05); C219(1.16); C90(1.16)  LDD1223  [9]
 LDCM0345  AC8 PaTu 8988t C144(0.83); C147(0.83); C90(0.90)  LDD1224  [9]
 LDCM0346  AC80 PaTu 8988t C144(0.84); C147(0.84); C219(1.14); C90(0.94)  LDD1225  [9]
 LDCM0347  AC81 PaTu 8988t C144(0.96); C147(0.96); C219(1.46); C90(0.93)  LDD1226  [9]
 LDCM0348  AC82 PaTu 8988t C144(0.83); C147(0.83); C219(1.27); C90(1.20)  LDD1227  [9]
 LDCM0349  AC83 PaTu 8988t C219(0.97); C90(0.98)  LDD1228  [9]
 LDCM0350  AC84 PaTu 8988t C219(1.11); C90(0.90)  LDD1229  [9]
 LDCM0351  AC85 PaTu 8988t C219(0.89); C90(0.86)  LDD1230  [9]
 LDCM0352  AC86 PaTu 8988t C219(0.89); C90(1.08)  LDD1231  [9]
 LDCM0353  AC87 PaTu 8988t C219(1.04); C90(0.94)  LDD1232  [9]
 LDCM0354  AC88 PaTu 8988t C219(1.12); C90(0.99)  LDD1233  [9]
 LDCM0355  AC89 PaTu 8988t C219(0.99); C90(1.16)  LDD1234  [9]
 LDCM0357  AC90 PaTu 8988t C219(1.45); C90(0.96)  LDD1236  [9]
 LDCM0358  AC91 PaTu 8988t C219(0.94); C90(0.94)  LDD1237  [9]
 LDCM0359  AC92 PaTu 8988t C219(0.81); C90(1.03)  LDD1238  [9]
 LDCM0360  AC93 PaTu 8988t C219(0.95); C90(0.84)  LDD1239  [9]
 LDCM0361  AC94 PaTu 8988t C219(1.14); C90(0.99)  LDD1240  [9]
 LDCM0362  AC95 PaTu 8988t C219(0.83); C90(1.04)  LDD1241  [9]
 LDCM0363  AC96 PaTu 8988t C219(1.18); C90(0.91)  LDD1242  [9]
 LDCM0364  AC97 PaTu 8988t C219(0.92); C90(0.94)  LDD1243  [9]
 LDCM0365  AC98 PaTu 8988t C144(0.75); C147(0.75); C219(0.98); C90(1.12)  LDD1244  [9]
 LDCM0366  AC99 PaTu 8988t C144(0.73); C147(0.73); C219(0.75); C90(1.07)  LDD1245  [9]
 LDCM0248  AKOS034007472 PaTu 8988t C144(0.59); C147(0.59); C90(0.90)  LDD1127  [9]
 LDCM0356  AKOS034007680 PaTu 8988t C144(0.79); C147(0.79); C90(1.46)  LDD1235  [9]
 LDCM0275  AKOS034007705 PaTu 8988t C144(0.64); C147(0.64); C90(1.28)  LDD1154  [9]
 LDCM0367  CL1 PaTu 8988t C219(0.87)  LDD1246  [9]
 LDCM0368  CL10 PaTu 8988t C219(1.06)  LDD1247  [9]
 LDCM0369  CL100 PaTu 8988t C90(1.23)  LDD1248  [9]
 LDCM0370  CL101 PaTu 8988t C144(0.95); C147(0.95); C90(1.33)  LDD1249  [9]
 LDCM0371  CL102 PaTu 8988t C144(0.85); C147(0.85); C90(1.07)  LDD1250  [9]
 LDCM0372  CL103 PaTu 8988t C144(0.75); C147(0.75); C90(1.26)  LDD1251  [9]
 LDCM0373  CL104 PaTu 8988t C144(0.81); C147(0.81); C90(1.06)  LDD1252  [9]
 LDCM0374  CL105 PaTu 8988t C219(0.69); C90(0.92)  LDD1253  [9]
 LDCM0375  CL106 PaTu 8988t C219(0.88); C90(0.99)  LDD1254  [9]
 LDCM0376  CL107 PaTu 8988t C219(0.95); C90(0.78)  LDD1255  [9]
 LDCM0377  CL108 PaTu 8988t C219(1.00); C90(0.88)  LDD1256  [9]
 LDCM0378  CL109 PaTu 8988t C219(0.96); C90(1.10)  LDD1257  [9]
 LDCM0379  CL11 PaTu 8988t C219(1.07)  LDD1258  [9]
 LDCM0380  CL110 PaTu 8988t C219(0.97); C90(1.08)  LDD1259  [9]
 LDCM0381  CL111 PaTu 8988t C219(1.01); C90(1.40)  LDD1260  [9]
 LDCM0382  CL112 PaTu 8988t C144(0.82); C147(0.82); C219(0.95); C90(0.91)  LDD1261  [9]
 LDCM0383  CL113 PaTu 8988t C144(0.94); C147(0.94); C219(1.05); C90(0.94)  LDD1262  [9]
 LDCM0384  CL114 PaTu 8988t C144(1.04); C147(1.04); C219(1.12); C90(0.99)  LDD1263  [9]
 LDCM0385  CL115 PaTu 8988t C144(0.87); C147(0.87); C219(1.12); C90(0.92)  LDD1264  [9]
 LDCM0386  CL116 PaTu 8988t C144(0.92); C147(0.92); C219(1.16); C90(0.98)  LDD1265  [9]
 LDCM0387  CL117 PaTu 8988t C144(1.10); C147(1.10); C90(1.08)  LDD1266  [9]
 LDCM0388  CL118 PaTu 8988t C144(0.64); C147(0.64); C90(1.02)  LDD1267  [9]
 LDCM0389  CL119 PaTu 8988t C144(0.84); C147(0.84); C90(1.31)  LDD1268  [9]
 LDCM0390  CL12 PaTu 8988t C219(0.82)  LDD1269  [9]
 LDCM0391  CL120 PaTu 8988t C144(1.23); C147(1.23); C90(1.34)  LDD1270  [9]
 LDCM0392  CL121 PaTu 8988t C219(1.00)  LDD1271  [9]
 LDCM0393  CL122 PaTu 8988t C219(1.12)  LDD1272  [9]
 LDCM0394  CL123 PaTu 8988t C219(1.11)  LDD1273  [9]
 LDCM0395  CL124 PaTu 8988t C219(1.08)  LDD1274  [9]
 LDCM0396  CL125 PaTu 8988t C90(1.19)  LDD1275  [9]
 LDCM0397  CL126 PaTu 8988t C90(1.11)  LDD1276  [9]
 LDCM0398  CL127 PaTu 8988t C90(1.24)  LDD1277  [9]
 LDCM0399  CL128 PaTu 8988t C90(1.15)  LDD1278  [9]
 LDCM0400  CL13 PaTu 8988t C219(1.24)  LDD1279  [9]
 LDCM0401  CL14 PaTu 8988t C219(1.31)  LDD1280  [9]
 LDCM0402  CL15 PaTu 8988t C219(0.89)  LDD1281  [9]
 LDCM0403  CL16 PaTu 8988t C144(0.90); C147(0.90)  LDD1282  [9]
 LDCM0404  CL17 PaTu 8988t C144(0.73); C147(0.73)  LDD1283  [9]
 LDCM0405  CL18 PaTu 8988t C144(0.72); C147(0.72)  LDD1284  [9]
 LDCM0406  CL19 PaTu 8988t C144(0.71); C147(0.71)  LDD1285  [9]
 LDCM0407  CL2 PaTu 8988t C219(0.98)  LDD1286  [9]
 LDCM0408  CL20 PaTu 8988t C144(0.74); C147(0.74)  LDD1287  [9]
 LDCM0409  CL21 PaTu 8988t C144(0.77); C147(0.77)  LDD1288  [9]
 LDCM0410  CL22 PaTu 8988t C144(0.71); C147(0.71)  LDD1289  [9]
 LDCM0411  CL23 PaTu 8988t C144(0.77); C147(0.77)  LDD1290  [9]
 LDCM0412  CL24 PaTu 8988t C144(0.77); C147(0.77)  LDD1291  [9]
 LDCM0413  CL25 PaTu 8988t C144(0.84); C147(0.84)  LDD1292  [9]
 LDCM0414  CL26 PaTu 8988t C144(0.78); C147(0.78)  LDD1293  [9]
 LDCM0415  CL27 PaTu 8988t C144(0.76); C147(0.76)  LDD1294  [9]
 LDCM0416  CL28 PaTu 8988t C144(0.83); C147(0.83)  LDD1295  [9]
 LDCM0417  CL29 PaTu 8988t C144(0.86); C147(0.86)  LDD1296  [9]
 LDCM0418  CL3 PaTu 8988t C219(0.94)  LDD1297  [9]
 LDCM0419  CL30 PaTu 8988t C144(0.71); C147(0.71)  LDD1298  [9]
 LDCM0420  CL31 PaTu 8988t C144(0.88); C147(0.88); C219(1.08)  LDD1299  [9]
 LDCM0421  CL32 PaTu 8988t C144(1.07); C147(1.07); C219(1.11)  LDD1300  [9]
 LDCM0422  CL33 PaTu 8988t C144(0.86); C147(0.86); C219(1.27)  LDD1301  [9]
 LDCM0423  CL34 PaTu 8988t C144(0.77); C147(0.77); C219(1.08)  LDD1302  [9]
 LDCM0424  CL35 PaTu 8988t C144(0.78); C147(0.78); C219(1.06)  LDD1303  [9]
 LDCM0425  CL36 PaTu 8988t C144(0.80); C147(0.80); C219(0.55)  LDD1304  [9]
 LDCM0426  CL37 PaTu 8988t C144(0.86); C147(0.86); C219(1.01)  LDD1305  [9]
 LDCM0428  CL39 PaTu 8988t C144(0.87); C147(0.87); C219(1.20)  LDD1307  [9]
 LDCM0429  CL4 PaTu 8988t C219(0.74)  LDD1308  [9]
 LDCM0430  CL40 PaTu 8988t C144(0.80); C147(0.80); C219(1.04)  LDD1309  [9]
 LDCM0431  CL41 PaTu 8988t C144(0.77); C147(0.77); C219(1.24)  LDD1310  [9]
 LDCM0432  CL42 PaTu 8988t C144(0.76); C147(0.76); C219(1.18)  LDD1311  [9]
 LDCM0433  CL43 PaTu 8988t C144(0.89); C147(0.89); C219(1.24)  LDD1312  [9]
 LDCM0434  CL44 PaTu 8988t C144(0.72); C147(0.72); C219(1.39)  LDD1313  [9]
 LDCM0435  CL45 PaTu 8988t C144(0.71); C147(0.71); C219(1.31)  LDD1314  [9]
 LDCM0440  CL5 PaTu 8988t C219(1.14)  LDD1319  [9]
 LDCM0451  CL6 PaTu 8988t C219(1.11)  LDD1330  [9]
 LDCM0453  CL61 PaTu 8988t C219(1.00); C90(0.97)  LDD1332  [9]
 LDCM0454  CL62 PaTu 8988t C219(0.86); C90(1.27)  LDD1333  [9]
 LDCM0455  CL63 PaTu 8988t C219(0.78); C90(1.41)  LDD1334  [9]
 LDCM0456  CL64 PaTu 8988t C219(0.95); C90(1.20)  LDD1335  [9]
 LDCM0457  CL65 PaTu 8988t C219(1.14); C90(1.53)  LDD1336  [9]
 LDCM0458  CL66 PaTu 8988t C219(0.88); C90(1.65)  LDD1337  [9]
 LDCM0459  CL67 PaTu 8988t C219(1.27); C90(1.24)  LDD1338  [9]
 LDCM0460  CL68 PaTu 8988t C219(1.15); C90(1.36)  LDD1339  [9]
 LDCM0461  CL69 PaTu 8988t C219(1.25); C90(1.91)  LDD1340  [9]
 LDCM0462  CL7 PaTu 8988t C219(1.42)  LDD1341  [9]
 LDCM0463  CL70 PaTu 8988t C219(1.17); C90(1.38)  LDD1342  [9]
 LDCM0464  CL71 PaTu 8988t C219(0.81); C90(1.22)  LDD1343  [9]
 LDCM0465  CL72 PaTu 8988t C219(0.70); C90(1.32)  LDD1344  [9]
 LDCM0466  CL73 PaTu 8988t C219(1.09); C90(1.91)  LDD1345  [9]
 LDCM0467  CL74 PaTu 8988t C219(0.83); C90(1.46)  LDD1346  [9]
 LDCM0469  CL76 PaTu 8988t C144(0.66); C147(0.66); C219(0.99)  LDD1348  [9]
 LDCM0470  CL77 PaTu 8988t C144(0.90); C147(0.90); C219(1.19)  LDD1349  [9]
 LDCM0471  CL78 PaTu 8988t C144(0.87); C147(0.87); C219(1.42)  LDD1350  [9]
 LDCM0472  CL79 PaTu 8988t C144(0.80); C147(0.80); C219(1.54)  LDD1351  [9]
 LDCM0473  CL8 PaTu 8988t C219(1.10)  LDD1352  [9]
 LDCM0474  CL80 PaTu 8988t C144(0.61); C147(0.61); C219(1.23)  LDD1353  [9]
 LDCM0475  CL81 PaTu 8988t C144(0.69); C147(0.69); C219(1.40)  LDD1354  [9]
 LDCM0476  CL82 PaTu 8988t C144(0.67); C147(0.67); C219(1.10)  LDD1355  [9]
 LDCM0477  CL83 PaTu 8988t C144(0.90); C147(0.90); C219(1.29)  LDD1356  [9]
 LDCM0478  CL84 PaTu 8988t C144(0.70); C147(0.70); C219(1.05)  LDD1357  [9]
 LDCM0479  CL85 PaTu 8988t C144(0.85); C147(0.85); C219(1.48)  LDD1358  [9]
 LDCM0480  CL86 PaTu 8988t C144(0.70); C147(0.70); C219(1.67)  LDD1359  [9]
 LDCM0481  CL87 PaTu 8988t C144(0.65); C147(0.65); C219(1.54)  LDD1360  [9]
 LDCM0482  CL88 PaTu 8988t C144(0.67); C147(0.67); C219(1.35)  LDD1361  [9]
 LDCM0483  CL89 PaTu 8988t C144(0.68); C147(0.68); C219(1.23)  LDD1362  [9]
 LDCM0484  CL9 PaTu 8988t C219(1.08)  LDD1363  [9]
 LDCM0485  CL90 PaTu 8988t C144(0.76); C147(0.76); C219(1.40)  LDD1364  [9]
 LDCM0486  CL91 PaTu 8988t C90(1.44)  LDD1365  [9]
 LDCM0487  CL92 PaTu 8988t C90(1.41)  LDD1366  [9]
 LDCM0488  CL93 PaTu 8988t C90(1.17)  LDD1367  [9]
 LDCM0489  CL94 PaTu 8988t C90(1.42)  LDD1368  [9]
 LDCM0490  CL95 PaTu 8988t C90(1.51)  LDD1369  [9]
 LDCM0491  CL96 PaTu 8988t C90(1.48)  LDD1370  [9]
 LDCM0492  CL97 PaTu 8988t C90(1.24)  LDD1371  [9]
 LDCM0493  CL98 PaTu 8988t C90(1.57)  LDD1372  [9]
 LDCM0494  CL99 PaTu 8988t C90(1.24)  LDD1373  [9]
 LDCM0495  E2913 HEK-293T C90(1.01)  LDD1698  [10]
 LDCM0625  F8 Ramos C90(1.23); C219(0.73); C366(1.47)  LDD2187  [11]
 LDCM0572  Fragment10 Ramos C90(0.87); C219(0.68); C366(0.67)  LDD2189  [11]
 LDCM0573  Fragment11 Ramos C90(0.17); C219(20.00); C366(1.91)  LDD2190  [11]
 LDCM0574  Fragment12 Ramos C90(0.90); C219(0.65); C366(0.51)  LDD2191  [11]
 LDCM0575  Fragment13 Ramos C90(1.01); C219(0.86); C366(0.99)  LDD2192  [11]
 LDCM0576  Fragment14 Ramos C90(0.69); C219(1.77)  LDD2193  [11]
 LDCM0579  Fragment20 Ramos C90(0.60); C219(0.70); C366(0.56)  LDD2194  [11]
 LDCM0580  Fragment21 Ramos C90(0.94); C219(0.55)  LDD2195  [11]
 LDCM0582  Fragment23 Ramos C90(1.01); C219(0.73)  LDD2196  [11]
 LDCM0578  Fragment27 Ramos C90(0.83); C219(0.66); C366(0.95)  LDD2197  [11]
 LDCM0586  Fragment28 Ramos C90(0.80); C219(0.50); C366(0.63)  LDD2198  [11]
 LDCM0588  Fragment30 Ramos C90(0.95); C219(0.95); C366(0.77)  LDD2199  [11]
 LDCM0589  Fragment31 Ramos C90(0.87); C219(0.90); C366(0.75)  LDD2200  [11]
 LDCM0590  Fragment32 Ramos C90(1.53); C219(0.50); C366(0.61)  LDD2201  [11]
 LDCM0468  Fragment33 PaTu 8988t C219(0.91); C90(1.68)  LDD1347  [9]
 LDCM0596  Fragment38 Ramos C90(0.59); C219(0.44); C366(0.45)  LDD2203  [11]
 LDCM0566  Fragment4 Ramos C90(1.42); C219(1.09)  LDD2184  [11]
 LDCM0427  Fragment51 PaTu 8988t C144(0.76); C147(0.76); C219(1.09)  LDD1306  [9]
 LDCM0610  Fragment52 Ramos C90(0.82); C219(0.58); C366(1.06)  LDD2204  [11]
 LDCM0614  Fragment56 Ramos C90(0.89); C219(1.80)  LDD2205  [11]
 LDCM0569  Fragment7 Jurkat _(6.74)  LDD1485  [2]
 LDCM0571  Fragment9 Ramos C90(0.66); C219(0.84); C366(0.63)  LDD2188  [11]
 LDCM0022  KB02 Ramos C90(1.10); C219(0.91); C366(0.65)  LDD2182  [11]
 LDCM0023  KB03 Jurkat C991(6.96)  LDD0209  [4]
 LDCM0024  KB05 MKN-1 C219(4.71); C474(0.69); C366(1.25)  LDD3331  [12]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C991(0.56)  LDD2140  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
GTPase HRas (HRAS) Ras family P01112
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) PI3K p85 subunit family P27986
Phosphatidylinositol 3-kinase regulatory subunit gamma (PIK3R3) PI3K p85 subunit family Q92569

The Drug(s) Related To This Target

Approved
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bay 80-6946 Small molecular drug D0S5LD
Caffeine Small molecular drug DB00201
Duvelisib Small molecular drug DB11952
Fostamatinib Small molecular drug DB12010
Idelalisib Small molecular drug D0J5VR
Ipi-145 Small molecular drug D0RU0O
Copanlisib . DB12483
Umbralisib . D0O8SJ
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Buparlisib Small molecular drug D01QSO
Phase 2
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Incb40093 Small molecular drug D07CWH
Leniolisib Small molecular drug DGO2C1
Pa-799 Small molecular drug D05CBJ
Parsaclisib Small molecular drug DP1SE6
Incb50465 . D07RHP
Rp6530 . D0LG7X
Phase 1
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bgb-10188 Small molecular drug DA02DE
Hmpl-689 Small molecular drug DDE3Z4
Amg 319 . D03FOP
Gs-9820 . D03IJO
Gs-9901 . D0U5PT
Me-401 . D08WLY
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Xl-499 . D08TAB
Investigative
Click To Hide/Show 8 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ethyl 1-[(1h-benzimidazol-2(3h)One-5-yl)Sulfonyl]-1h-pyrrole-2-carboxylate Small molecular drug D0W1ST
Etp-46321 Small molecular drug DOR1I0
Ic87114 Small molecular drug D00ZIK
Ic980033 Small molecular drug D0O2HL
Ly-292223 Small molecular drug D07APP
Tg100-115 Small molecular drug DB05552
2-((9h-purin-6-ylthio)Methyl)-5-chloro-3-(2-methoxyphenyl)Quinazolin-4(3h)-one . DB06831
Xl765 . DB05241
Patented
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pyrrolo[2,3-d]Pyrimidine Derivative 28 Small molecular drug D00GTY
Discontinued
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Wortmannin Small molecular drug D0P1JI

References

1 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
2 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.
3 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
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 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
7 Direct Target Site Identification of a Sulfonyl-Triazole Covalent Kinase Probe by LC-MS Chemical Proteomics. Anal Chem. 2021 Sep 7;93(35):11946-11955. doi: 10.1021/acs.analchem.1c01591. Epub 2021 Aug 25.
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.
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Mass spectrometry data entry: PXD044402
11 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
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Mass spectrometry data entry: PXD047840