Details of the Target

General Information of Target

Target ID LDTP03408
Target Name Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1)
Gene Name PIK3R1
Gene ID 5295
Synonyms
GRB1; Phosphatidylinositol 3-kinase regulatory subunit alpha; PI3-kinase regulatory subunit alpha; PI3K regulatory subunit alpha; PtdIns-3-kinase regulatory subunit alpha; Phosphatidylinositol 3-kinase 85 kDa regulatory subunit alpha; PI3-kinase subunit p85-alpha; PtdIns-3-kinase regulatory subunit p85-alpha
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSAEGYQYRALYDYKKEREEDIDLHLGDILTVNKGSLVALGFSDGQEARPEEIGWLNGYN
ETTGERGDFPGTYVEYIGRKKISPPTPKPRPPRPLPVAPGSSKTEADVEQQALTLPDLAE
QFAPPDIAPPLLIKLVEAIEKKGLECSTLYRTQSSSNLAELRQLLDCDTPSVDLEMIDVH
VLADAFKRYLLDLPNPVIPAAVYSEMISLAPEVQSSEEYIQLLKKLIRSPSIPHQYWLTL
QYLLKHFFKLSQTSSKNLLNARVLSEIFSPMLFRFSAASSDNTENLIKVIEILISTEWNE
RQPAPALPPKPPKPTTVANNGMNNNMSLQDAEWYWGDISREEVNEKLRDTADGTFLVRDA
STKMHGDYTLTLRKGGNNKLIKIFHRDGKYGFSDPLTFSSVVELINHYRNESLAQYNPKL
DVKLLYPVSKYQQDQVVKEDNIEAVGKKLHEYNTQFQEKSREYDRLYEEYTRTSQEIQMK
RTAIEAFNETIKIFEEQCQTQERYSKEYIEKFKREGNEKEIQRIMHNYDKLKSRISEIID
SRRRLEEDLKKQAAEYREIDKRMNSIKPDLIQLRKTRDQYLMWLTQKGVRQKKLNEWLGN
ENTEDQYSLVEDDEDLPHHDEKTWNVGSSNRNKAENLLRGKRDGTFLVRESSKQGCYACS
VVVDGEVKHCVINKTATGYGFAEPYNLYSSLKELVLHYQHTSLVQHNDSLNVTLAYPVYA
QQRR
Target Bioclass
Other
Family
PI3K p85 subunit family
Function
Binds to activated (phosphorylated) protein-Tyr kinases, through its SH2 domain, and acts as an adapter, mediating the association of the p110 catalytic unit to the plasma membrane. Necessary for the insulin-stimulated increase in glucose uptake and glycogen synthesis in insulin-sensitive tissues. Plays an important role in signaling in response to FGFR1, FGFR2, FGFR3, FGFR4, KITLG/SCF, KIT, PDGFRA and PDGFRB. Likewise, plays a role in ITGB2 signaling. Modulates the cellular response to ER stress by promoting nuclear translocation of XBP1 isoform 2 in a ER stress- and/or insulin-dependent manner during metabolic overloading in the liver and hence plays a role in glucose tolerance improvement.
Uniprot ID
P27986
Ensemble ID
ENST00000320694.13
HGNC ID
HGNC:8979
ChEMBL ID
CHEMBL2506

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA Deletion: p.R557_K561delinsQ DBIA    Probe Info 
DAOY Deletion: p.L380del DBIA    Probe Info 
EFO27 Deletion: p.D643WfsTer10 .
GAMG Insertion: p.Y463_D464insELHEYNTQFQEKSREY .
HCT15 SNV: p.P312L .
HS578T Insertion: p.N453_T453insN DBIA    Probe Info 
Ishikawa (Heraklio) 02 ER SNV: p.L570P DBIA    Probe Info 
KMCH1 SNV: p.L132I .
KNS81FD Deletion: p.K448_L449delinsI .
LNCaP clone FGC SNV: p.R639Ter DBIA    Probe Info 
MDAMB436 SNV: p.Y73Ter .
MFE319 Deletion: p.L347del
Insertion: p.I82NfsTer24		 DBIA    Probe Info 
OVK18 Deletion: p.F456_Q457del
Insertion: p.T371NfsTer8		 DBIA    Probe Info 
OVTOKO Deletion: p.V436_H450del
Insertion: p.N453dup		 DBIA    Probe Info 
REH SNV: p.G376E DBIA    Probe Info 
RL952 SNV: p.R386G; p.R639Ter DBIA    Probe Info 
WM115 SNV: p.R642Ter .

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
STPyne
 Probe Info  		K530(10.00)  LDD0277  [1]
Probe 1
 Probe Info  		Y73(14.22); Y467(28.22)  LDD3495  [2]
DBIA
 Probe Info  		C146(2.34)  LDD3310  [3]
HHS-475
 Probe Info  		Y452(2.01)  LDD0264  [4]
Acrolein
 Probe Info  		N.A.  LDD0222  [5]
4-Iodoacetamidophenylacetylene
 Probe Info  		C146(0.00); C498(0.00); C167(0.00)  LDD0038  [6]
IA-alkyne
 Probe Info  		C146(0.00); C498(0.00)  LDD0036  [6]
IPIAA_L
 Probe Info  		N.A.  LDD0031  [7]
Lodoacetamide azide
 Probe Info  		C498(0.00); C146(0.00); C167(0.00)  LDD0037  [6]
NAIA_5
 Probe Info  		N.A.  LDD2224  [8]
WYneN
 Probe Info  		N.A.  LDD0021  [9]
IPM
 Probe Info  		N.A.  LDD2156  [10]
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  [11]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C146(1.03); C498(0.99); C167(0.90)  LDD1507  [12]
 LDCM0215  AC10 HEK-293T C146(0.98); C498(0.95); C167(1.13)  LDD1508  [12]
 LDCM0226  AC11 HEK-293T C146(0.99); C498(1.12); C167(1.10)  LDD1509  [12]
 LDCM0237  AC12 HEK-293T C146(0.97); C498(0.93)  LDD1510  [12]
 LDCM0259  AC14 HEK-293T C146(1.03); C498(1.02); C167(1.10)  LDD1512  [12]
 LDCM0270  AC15 HEK-293T C146(1.03); C498(1.02); C167(1.09)  LDD1513  [12]
 LDCM0276  AC17 HEK-293T C146(0.93); C498(0.84); C167(1.03)  LDD1515  [12]
 LDCM0277  AC18 HEK-293T C146(1.09); C498(0.75); C167(1.00)  LDD1516  [12]
 LDCM0278  AC19 HEK-293T C146(0.89); C498(0.90); C167(0.95)  LDD1517  [12]
 LDCM0279  AC2 HEK-293T C146(0.97); C498(1.02); C167(1.00)  LDD1518  [12]
 LDCM0280  AC20 HEK-293T C146(0.96); C498(1.14)  LDD1519  [12]
 LDCM0281  AC21 HEK-293T C146(1.01); C167(1.03)  LDD1520  [12]
 LDCM0282  AC22 HEK-293T C146(0.95); C498(0.92); C167(1.06)  LDD1521  [12]
 LDCM0283  AC23 HEK-293T C146(0.96); C498(0.96); C167(1.23)  LDD1522  [12]
 LDCM0284  AC24 HEK-293T C146(0.98); C498(1.06); C167(0.90)  LDD1523  [12]
 LDCM0285  AC25 HEK-293T C146(0.97); C498(1.03); C167(1.04)  LDD1524  [12]
 LDCM0286  AC26 HEK-293T C146(1.00); C498(0.87); C167(0.92)  LDD1525  [12]
 LDCM0287  AC27 HEK-293T C146(0.96); C498(0.93); C167(0.98)  LDD1526  [12]
 LDCM0288  AC28 HEK-293T C146(0.99); C498(1.05)  LDD1527  [12]
 LDCM0289  AC29 HEK-293T C146(0.99); C167(1.14)  LDD1528  [12]
 LDCM0290  AC3 HEK-293T C146(1.01); C498(0.94); C167(1.04)  LDD1529  [12]
 LDCM0291  AC30 HEK-293T C146(0.95); C498(1.09); C167(1.20)  LDD1530  [12]
 LDCM0292  AC31 HEK-293T C146(1.01); C498(1.06); C167(1.08)  LDD1531  [12]
 LDCM0293  AC32 HEK-293T C146(1.70); C498(1.00); C167(1.11)  LDD1532  [12]
 LDCM0294  AC33 HEK-293T C146(1.02); C498(0.79); C167(0.89)  LDD1533  [12]
 LDCM0295  AC34 HEK-293T C146(0.94); C498(0.80); C167(1.14)  LDD1534  [12]
 LDCM0296  AC35 HEK-293T C146(1.00); C498(1.03); C167(1.07)  LDD1535  [12]
 LDCM0297  AC36 HEK-293T C146(0.98); C498(1.04)  LDD1536  [12]
 LDCM0298  AC37 HEK-293T C146(1.02); C167(1.04)  LDD1537  [12]
 LDCM0299  AC38 HEK-293T C146(1.00); C498(1.13); C167(1.10)  LDD1538  [12]
 LDCM0300  AC39 HEK-293T C146(1.06); C498(0.90); C167(0.96)  LDD1539  [12]
 LDCM0301  AC4 HEK-293T C146(0.93); C498(1.04)  LDD1540  [12]
 LDCM0302  AC40 HEK-293T C146(1.07); C498(0.94); C167(1.18)  LDD1541  [12]
 LDCM0303  AC41 HEK-293T C146(1.05); C498(0.87); C167(1.02)  LDD1542  [12]
 LDCM0304  AC42 HEK-293T C146(0.97); C498(0.81); C167(1.14)  LDD1543  [12]
 LDCM0305  AC43 HEK-293T C146(1.01); C498(1.12); C167(0.98)  LDD1544  [12]
 LDCM0306  AC44 HEK-293T C146(0.96); C498(1.29)  LDD1545  [12]
 LDCM0307  AC45 HEK-293T C146(1.14); C167(1.08)  LDD1546  [12]
 LDCM0308  AC46 HEK-293T C146(0.99); C498(1.09); C167(1.03)  LDD1547  [12]
 LDCM0309  AC47 HEK-293T C146(0.98); C498(0.94); C167(1.27)  LDD1548  [12]
 LDCM0310  AC48 HEK-293T C146(1.03); C498(1.02); C167(1.14)  LDD1549  [12]
 LDCM0311  AC49 HEK-293T C146(1.02); C498(0.82); C167(0.99)  LDD1550  [12]
 LDCM0312  AC5 HEK-293T C146(1.00); C167(1.08)  LDD1551  [12]
 LDCM0313  AC50 HEK-293T C146(1.03); C498(0.83); C167(1.12)  LDD1552  [12]
 LDCM0314  AC51 HEK-293T C146(1.03); C498(1.17); C167(0.98)  LDD1553  [12]
 LDCM0315  AC52 HEK-293T C146(0.99); C498(1.13)  LDD1554  [12]
 LDCM0316  AC53 HEK-293T C146(1.00); C167(1.10)  LDD1555  [12]
 LDCM0317  AC54 HEK-293T C146(0.98); C498(1.01); C167(1.14)  LDD1556  [12]
 LDCM0318  AC55 HEK-293T C146(1.04); C498(1.03); C167(1.01)  LDD1557  [12]
 LDCM0319  AC56 HEK-293T C146(1.03); C498(0.93); C167(1.29)  LDD1558  [12]
 LDCM0320  AC57 HEK-293T C146(1.04); C498(1.22); C167(1.01)  LDD1559  [12]
 LDCM0321  AC58 HEK-293T C146(1.02); C498(0.88); C167(1.17)  LDD1560  [12]
 LDCM0322  AC59 HEK-293T C146(0.96); C498(1.00); C167(0.99)  LDD1561  [12]
 LDCM0323  AC6 HEK-293T C146(1.01); C498(0.99); C167(1.12)  LDD1562  [12]
 LDCM0324  AC60 HEK-293T C146(0.91); C498(1.05)  LDD1563  [12]
 LDCM0325  AC61 HEK-293T C146(1.00); C167(1.04)  LDD1564  [12]
 LDCM0326  AC62 HEK-293T C146(0.97); C498(0.98); C167(1.17)  LDD1565  [12]
 LDCM0327  AC63 HEK-293T C146(1.10); C498(1.04); C167(1.07)  LDD1566  [12]
 LDCM0328  AC64 HEK-293T C146(1.02); C498(0.95); C167(1.08)  LDD1567  [12]
 LDCM0334  AC7 HEK-293T C146(1.05); C498(0.94); C167(0.99)  LDD1568  [12]
 LDCM0345  AC8 HEK-293T C146(0.94); C498(0.92); C167(0.98)  LDD1569  [12]
 LDCM0248  AKOS034007472 HEK-293T C146(1.02); C167(1.05)  LDD1511  [12]
 LDCM0356  AKOS034007680 HEK-293T C146(0.99); C498(0.85); C167(0.96)  LDD1570  [12]
 LDCM0275  AKOS034007705 HEK-293T C146(0.99); C498(0.97); C167(1.19)  LDD1514  [12]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [5]
 LDCM0367  CL1 HEK-293T C146(0.95); C498(1.02); C167(0.95)  LDD1571  [12]
 LDCM0368  CL10 HEK-293T C146(0.89); C498(1.14); C167(1.29)  LDD1572  [12]
 LDCM0369  CL100 HEK-293T C146(0.95); C498(0.87); C167(0.89)  LDD1573  [12]
 LDCM0370  CL101 HEK-293T C146(1.02); C498(1.00); C167(0.88)  LDD1574  [12]
 LDCM0371  CL102 HEK-293T C146(0.92); C498(0.83); C167(1.00)  LDD1575  [12]
 LDCM0372  CL103 HEK-293T C146(1.00); C498(1.05); C167(1.25)  LDD1576  [12]
 LDCM0373  CL104 HEK-293T C146(0.95); C498(0.98); C167(1.03)  LDD1577  [12]
 LDCM0374  CL105 HEK-293T C146(0.94); C498(1.02); C167(0.96)  LDD1578  [12]
 LDCM0375  CL106 HEK-293T C146(0.99); C498(0.87); C167(0.93)  LDD1579  [12]
 LDCM0376  CL107 HEK-293T C146(0.98); C498(1.09); C167(1.11)  LDD1580  [12]
 LDCM0377  CL108 HEK-293T C146(0.85); C498(0.84); C167(1.01)  LDD1581  [12]
 LDCM0378  CL109 HEK-293T C146(0.93); C498(0.97); C167(0.88)  LDD1582  [12]
 LDCM0379  CL11 HEK-293T C146(1.00); C498(1.05); C167(1.22)  LDD1583  [12]
 LDCM0380  CL110 HEK-293T C146(0.92); C498(0.91); C167(0.92)  LDD1584  [12]
 LDCM0381  CL111 HEK-293T C146(1.00); C498(0.90); C167(1.18)  LDD1585  [12]
 LDCM0382  CL112 HEK-293T C146(0.90); C498(0.99); C167(0.94)  LDD1586  [12]
 LDCM0383  CL113 HEK-293T C146(1.01); C498(1.06); C167(0.99)  LDD1587  [12]
 LDCM0384  CL114 HEK-293T C146(0.95); C498(0.92); C167(0.88)  LDD1588  [12]
 LDCM0385  CL115 HEK-293T C146(1.03); C498(0.98); C167(1.22)  LDD1589  [12]
 LDCM0386  CL116 HEK-293T C146(0.84); C498(0.83); C167(0.98)  LDD1590  [12]
 LDCM0387  CL117 HEK-293T C146(1.02); C498(0.94); C167(0.82)  LDD1591  [12]
 LDCM0388  CL118 HEK-293T C146(0.93); C498(1.09); C167(1.03)  LDD1592  [12]
 LDCM0389  CL119 HEK-293T C146(1.01); C498(0.99); C167(1.12)  LDD1593  [12]
 LDCM0390  CL12 HEK-293T C146(1.12); C498(1.22); C167(1.22)  LDD1594  [12]
 LDCM0391  CL120 HEK-293T C146(0.91); C498(1.01); C167(0.97)  LDD1595  [12]
 LDCM0392  CL121 HEK-293T C146(1.02); C498(0.99); C167(0.96)  LDD1596  [12]
 LDCM0393  CL122 HEK-293T C146(0.96); C498(1.01); C167(0.96)  LDD1597  [12]
 LDCM0394  CL123 HEK-293T C146(0.90); C498(1.04); C167(1.03)  LDD1598  [12]
 LDCM0395  CL124 HEK-293T C146(0.90); C498(0.99); C167(0.99)  LDD1599  [12]
 LDCM0396  CL125 HEK-293T C146(0.99); C498(0.91); C167(1.09)  LDD1600  [12]
 LDCM0397  CL126 HEK-293T C146(1.04); C498(1.06); C167(1.00)  LDD1601  [12]
 LDCM0398  CL127 HEK-293T C146(1.00); C498(1.01); C167(1.35)  LDD1602  [12]
 LDCM0399  CL128 HEK-293T C146(0.93); C498(0.97); C167(1.04)  LDD1603  [12]
 LDCM0400  CL13 HEK-293T C146(1.06); C498(1.02); C167(0.99)  LDD1604  [12]
 LDCM0401  CL14 HEK-293T C146(1.05); C498(1.11); C167(0.98)  LDD1605  [12]
 LDCM0402  CL15 HEK-293T C146(0.91); C498(0.98); C167(1.26)  LDD1606  [12]
 LDCM0403  CL16 HEK-293T C146(0.90); C498(1.02); C167(1.05)  LDD1607  [12]
 LDCM0404  CL17 HEK-293T C146(0.91); C498(0.77); C167(1.07)  LDD1608  [12]
 LDCM0405  CL18 HEK-293T C146(1.05); C498(0.92); C167(1.22)  LDD1609  [12]
 LDCM0406  CL19 HEK-293T C146(1.03); C498(1.11); C167(1.10)  LDD1610  [12]
 LDCM0407  CL2 HEK-293T C146(1.02); C498(1.04); C167(1.05)  LDD1611  [12]
 LDCM0408  CL20 HEK-293T C146(0.91); C498(1.19)  LDD1612  [12]
 LDCM0409  CL21 HEK-293T C146(1.00); C167(0.97)  LDD1613  [12]
 LDCM0410  CL22 HEK-293T C146(0.98); C498(1.40); C167(1.57)  LDD1614  [12]
 LDCM0411  CL23 HEK-293T C146(1.09); C498(1.21); C167(1.37)  LDD1615  [12]
 LDCM0412  CL24 HEK-293T C146(1.13); C498(1.29); C167(1.34)  LDD1616  [12]
 LDCM0413  CL25 HEK-293T C146(0.99); C498(0.97); C167(0.90)  LDD1617  [12]
 LDCM0414  CL26 HEK-293T C146(0.93); C498(0.92); C167(0.93)  LDD1618  [12]
 LDCM0415  CL27 HEK-293T C146(0.96); C498(1.11); C167(1.57)  LDD1619  [12]
 LDCM0416  CL28 HEK-293T C146(0.87); C498(0.99); C167(1.06)  LDD1620  [12]
 LDCM0417  CL29 HEK-293T C146(0.95); C498(1.22); C167(1.00)  LDD1621  [12]
 LDCM0418  CL3 HEK-293T C146(1.00); C498(0.92); C167(1.18)  LDD1622  [12]
 LDCM0419  CL30 HEK-293T C146(1.07); C498(0.96); C167(1.05)  LDD1623  [12]
 LDCM0420  CL31 HEK-293T C146(1.14); C498(1.06); C167(1.04)  LDD1624  [12]
 LDCM0421  CL32 HEK-293T C146(0.99); C498(1.02)  LDD1625  [12]
 LDCM0422  CL33 HEK-293T C146(0.89); C167(0.85)  LDD1626  [12]
 LDCM0423  CL34 HEK-293T C146(0.98); C498(1.30); C167(1.28)  LDD1627  [12]
 LDCM0424  CL35 HEK-293T C146(1.09); C498(1.18); C167(1.35)  LDD1628  [12]
 LDCM0425  CL36 HEK-293T C146(0.98); C498(1.31); C167(1.21)  LDD1629  [12]
 LDCM0426  CL37 HEK-293T C146(0.96); C498(1.05); C167(1.01)  LDD1630  [12]
 LDCM0428  CL39 HEK-293T C146(1.00); C498(0.99); C167(1.21)  LDD1632  [12]
 LDCM0429  CL4 HEK-293T C146(0.87); C498(0.92); C167(1.03)  LDD1633  [12]
 LDCM0430  CL40 HEK-293T C146(0.87); C498(1.23); C167(1.07)  LDD1634  [12]
 LDCM0431  CL41 HEK-293T C146(0.94); C498(0.94); C167(0.86)  LDD1635  [12]
 LDCM0432  CL42 HEK-293T C146(1.08); C498(0.94); C167(1.31)  LDD1636  [12]
 LDCM0433  CL43 HEK-293T C146(1.11); C498(1.24); C167(1.24)  LDD1637  [12]
 LDCM0434  CL44 HEK-293T C146(1.09); C498(1.02)  LDD1638  [12]
 LDCM0435  CL45 HEK-293T C146(0.99); C167(1.06)  LDD1639  [12]
 LDCM0436  CL46 HEK-293T C146(1.06); C498(1.21); C167(1.14)  LDD1640  [12]
 LDCM0437  CL47 HEK-293T C146(1.05); C498(0.93); C167(1.14)  LDD1641  [12]
 LDCM0438  CL48 HEK-293T C146(1.02); C498(1.26); C167(1.07)  LDD1642  [12]
 LDCM0439  CL49 HEK-293T C146(0.96); C498(0.94); C167(0.86)  LDD1643  [12]
 LDCM0440  CL5 HEK-293T C146(1.04); C498(0.90); C167(1.18)  LDD1644  [12]
 LDCM0441  CL50 HEK-293T C146(1.03); C498(1.02); C167(0.98)  LDD1645  [12]
 LDCM0443  CL52 HEK-293T C146(0.86); C498(1.09); C167(1.15)  LDD1646  [12]
 LDCM0444  CL53 HEK-293T C146(0.91); C498(0.91); C167(0.95)  LDD1647  [12]
 LDCM0445  CL54 HEK-293T C146(0.91); C498(0.90); C167(1.16)  LDD1648  [12]
 LDCM0446  CL55 HEK-293T C146(1.03); C498(1.29); C167(1.14)  LDD1649  [12]
 LDCM0447  CL56 HEK-293T C146(1.00); C498(0.98)  LDD1650  [12]
 LDCM0448  CL57 HEK-293T C146(0.98); C167(1.08)  LDD1651  [12]
 LDCM0449  CL58 HEK-293T C146(1.07); C498(1.37); C167(1.48)  LDD1652  [12]
 LDCM0450  CL59 HEK-293T C146(1.08); C498(1.14); C167(1.33)  LDD1653  [12]
 LDCM0451  CL6 HEK-293T C146(0.92); C498(0.93); C167(1.03)  LDD1654  [12]
 LDCM0452  CL60 HEK-293T C146(1.06); C498(1.36); C167(1.12)  LDD1655  [12]
 LDCM0453  CL61 HEK-293T C146(1.00); C498(0.90); C167(1.04)  LDD1656  [12]
 LDCM0454  CL62 HEK-293T C146(1.00); C498(0.99); C167(1.04)  LDD1657  [12]
 LDCM0455  CL63 HEK-293T C146(1.04); C498(1.15); C167(1.33)  LDD1658  [12]
 LDCM0456  CL64 HEK-293T C146(0.87); C498(0.95); C167(0.86)  LDD1659  [12]
 LDCM0457  CL65 HEK-293T C146(1.04); C498(0.75); C167(1.06)  LDD1660  [12]
 LDCM0458  CL66 HEK-293T C146(1.02); C498(0.80); C167(1.20)  LDD1661  [12]
 LDCM0459  CL67 HEK-293T C146(1.08); C498(1.01); C167(1.09)  LDD1662  [12]
 LDCM0460  CL68 HEK-293T C146(0.95); C498(1.13)  LDD1663  [12]
 LDCM0461  CL69 HEK-293T C146(1.00); C167(1.06)  LDD1664  [12]
 LDCM0462  CL7 HEK-293T C146(0.98); C498(1.00); C167(1.04)  LDD1665  [12]
 LDCM0463  CL70 HEK-293T C146(1.05); C498(1.28); C167(1.05)  LDD1666  [12]
 LDCM0464  CL71 HEK-293T C146(1.08); C498(1.04); C167(1.20)  LDD1667  [12]
 LDCM0465  CL72 HEK-293T C146(1.10); C498(1.22); C167(1.08)  LDD1668  [12]
 LDCM0466  CL73 HEK-293T C146(1.01); C498(0.92); C167(1.14)  LDD1669  [12]
 LDCM0467  CL74 HEK-293T C146(0.97); C498(0.97); C167(0.93)  LDD1670  [12]
 LDCM0469  CL76 HEK-293T C146(0.90); C498(0.84); C167(0.97)  LDD1672  [12]
 LDCM0470  CL77 HEK-293T C146(0.97); C498(0.86); C167(1.03)  LDD1673  [12]
 LDCM0471  CL78 HEK-293T C146(1.05); C498(0.82); C167(1.23)  LDD1674  [12]
 LDCM0472  CL79 HEK-293T C146(0.99); C498(1.05); C167(1.14)  LDD1675  [12]
 LDCM0473  CL8 HEK-293T C146(0.83); C498(0.76)  LDD1676  [12]
 LDCM0474  CL80 HEK-293T C146(1.12); C498(1.04)  LDD1677  [12]
 LDCM0475  CL81 HEK-293T C146(1.09); C167(1.11)  LDD1678  [12]
 LDCM0476  CL82 HEK-293T C146(0.89); C498(1.22); C167(1.00)  LDD1679  [12]
 LDCM0477  CL83 HEK-293T C146(1.05); C498(1.00); C167(1.13)  LDD1680  [12]
 LDCM0478  CL84 HEK-293T C146(0.99); C498(1.12); C167(1.06)  LDD1681  [12]
 LDCM0479  CL85 HEK-293T C146(0.93); C498(0.93); C167(0.94)  LDD1682  [12]
 LDCM0480  CL86 HEK-293T C146(0.99); C498(1.14); C167(0.90)  LDD1683  [12]
 LDCM0481  CL87 HEK-293T C146(1.01); C498(1.01); C167(1.15)  LDD1684  [12]
 LDCM0482  CL88 HEK-293T C146(0.96); C498(0.97); C167(1.14)  LDD1685  [12]
 LDCM0483  CL89 HEK-293T C146(1.06); C498(0.88); C167(1.02)  LDD1686  [12]
 LDCM0484  CL9 HEK-293T C146(1.01); C167(1.06)  LDD1687  [12]
 LDCM0485  CL90 HEK-293T C146(0.89); C498(0.80); C167(0.97)  LDD1688  [12]
 LDCM0486  CL91 HEK-293T C146(1.08); C498(1.12); C167(1.32)  LDD1689  [12]
 LDCM0487  CL92 HEK-293T C146(0.92); C498(0.90)  LDD1690  [12]
 LDCM0488  CL93 HEK-293T C146(0.99); C167(1.00)  LDD1691  [12]
 LDCM0489  CL94 HEK-293T C146(0.98); C498(1.23); C167(1.14)  LDD1692  [12]
 LDCM0490  CL95 HEK-293T C146(1.06); C498(0.90); C167(1.10)  LDD1693  [12]
 LDCM0491  CL96 HEK-293T C146(0.99); C498(0.97); C167(1.26)  LDD1694  [12]
 LDCM0492  CL97 HEK-293T C146(0.98); C498(1.05); C167(0.90)  LDD1695  [12]
 LDCM0493  CL98 HEK-293T C146(0.97); C498(0.91); C167(0.94)  LDD1696  [12]
 LDCM0494  CL99 HEK-293T C146(1.00); C498(0.95); C167(1.10)  LDD1697  [12]
 LDCM0495  E2913 HEK-293T C146(1.23); C498(1.12); C167(1.50)  LDD1698  [12]
 LDCM0625  F8 Ramos C146(1.49)  LDD2187  [13]
 LDCM0572  Fragment10 Ramos C146(1.62)  LDD2189  [13]
 LDCM0573  Fragment11 Ramos C146(0.32)  LDD2190  [13]
 LDCM0574  Fragment12 Ramos C146(1.19)  LDD2191  [13]
 LDCM0575  Fragment13 Ramos C146(1.14)  LDD2192  [13]
 LDCM0576  Fragment14 Ramos C146(0.79)  LDD2193  [13]
 LDCM0579  Fragment20 Ramos C146(0.91)  LDD2194  [13]
 LDCM0580  Fragment21 Ramos C146(1.31)  LDD2195  [13]
 LDCM0582  Fragment23 Ramos C146(1.53)  LDD2196  [13]
 LDCM0578  Fragment27 Ramos C146(1.20)  LDD2197  [13]
 LDCM0586  Fragment28 Ramos C146(0.81)  LDD2198  [13]
 LDCM0588  Fragment30 Ramos C146(1.27)  LDD2199  [13]
 LDCM0589  Fragment31 Ramos C146(1.30)  LDD2200  [13]
 LDCM0590  Fragment32 Ramos C146(1.37)  LDD2201  [13]
 LDCM0468  Fragment33 HEK-293T C146(1.04); C498(1.03); C167(1.25)  LDD1671  [12]
 LDCM0596  Fragment38 Ramos C146(1.17)  LDD2203  [13]
 LDCM0566  Fragment4 Ramos C146(1.11)  LDD2184  [13]
 LDCM0427  Fragment51 HEK-293T C146(0.90); C498(0.99); C167(0.96)  LDD1631  [12]
 LDCM0610  Fragment52 Ramos C146(1.93)  LDD2204  [13]
 LDCM0614  Fragment56 Ramos C146(1.59)  LDD2205  [13]
 LDCM0569  Fragment7 Ramos C146(1.01)  LDD2186  [13]
 LDCM0571  Fragment9 Ramos C146(1.18)  LDD2188  [13]
 LDCM0116  HHS-0101 DM93 Y452(2.01)  LDD0264  [4]
 LDCM0117  HHS-0201 DM93 Y452(3.79)  LDD0265  [4]
 LDCM0118  HHS-0301 DM93 Y452(1.48)  LDD0266  [4]
 LDCM0119  HHS-0401 DM93 Y452(0.81)  LDD0267  [4]
 LDCM0120  HHS-0701 DM93 Y452(0.74)  LDD0268  [4]
 LDCM0022  KB02 HEK-293T C498(1.05); C146(0.92); C167(0.90)  LDD1492  [12]
 LDCM0023  KB03 HEK-293T C498(1.05); C146(1.03); C167(0.98)  LDD1497  [12]
 LDCM0024  KB05 COLO792 C146(2.34)  LDD3310  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 41 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
N-alpha-acetyltransferase 10 (NAA10) Acetyltransferase family P41227
Dopamine beta-hydroxylase (DBH) Copper type II ascorbate-dependent monooxygenase family P09172
Palmitoyltransferase ZDHHC17 (ZDHHC17) DHHC palmitoyltransferase family Q8IUH5
Presenilin-2 (PSEN2) Peptidase A22A family P49810
Caspase-7 (CASP7) Peptidase C14A family P55210
Tryptase alpha/beta-1 (TPSAB1) Peptidase S1 family Q15661
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PIK3CA) PI3/PI4-kinase family P42336
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (PIK3CB) PI3/PI4-kinase family P42338
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (PIK3CD) PI3/PI4-kinase family O00329
cAMP-dependent protein kinase catalytic subunit alpha (PRKACA) AGC Ser/Thr protein kinase family P17612
Ribosomal protein S6 kinase alpha-3 (RPS6KA3) AGC Ser/Thr protein kinase family P51812
Calcium/calmodulin-dependent protein kinase type II subunit alpha (CAMK2A) CAMK Ser/Thr protein kinase family Q9UQM7
Serine/threonine-protein kinase SIK2 (SIK2) CAMK Ser/Thr protein kinase family Q9H0K1
Cyclin-dependent kinase 1 (CDK1) CMGC Ser/Thr protein kinase family P06493
Mitogen-activated protein kinase 8 (MAPK8) CMGC Ser/Thr protein kinase family P45983
Mitogen-activated protein kinase kinase kinase kinase 1 (MAP4K1) STE Ser/Thr protein kinase family Q92918
Hepatocyte growth factor receptor (MET) Tyr protein kinase family P08581
Tyrosine-protein kinase ABL2 (ABL2) Tyr protein kinase family P42684
Tyrosine-protein kinase receptor UFO (AXL) Tyr protein kinase family P30530
Mast/stem cell growth factor receptor Kit (KIT) Tyr protein kinase family P10721
Platelet-derived growth factor receptor beta (PDGFRB) Tyr protein kinase family P09619
Receptor-type tyrosine-protein kinase FLT3 (FLT3) Tyr protein kinase family P36888
Vascular endothelial growth factor receptor 1 (FLT1) Tyr protein kinase family P17948
Epidermal growth factor receptor (EGFR) Tyr protein kinase family P00533
Receptor tyrosine-protein kinase erbB-2 (ERBB2) Tyr protein kinase family P04626
Receptor tyrosine-protein kinase erbB-3 (ERBB3) Tyr protein kinase family P21860
Fibroblast growth factor receptor 1 (FGFR1) Tyr protein kinase family P11362
High affinity nerve growth factor receptor (NTRK1) Tyr protein kinase family P04629
Insulin receptor (INSR) Tyr protein kinase family P06213
Insulin-like growth factor 1 receptor (IGF1R) Tyr protein kinase family P08069
Proto-oncogene tyrosine-protein kinase Src (SRC) Tyr protein kinase family P12931
Tyrosine-protein kinase Blk (BLK) Tyr protein kinase family P51451
Tyrosine-protein kinase Lyn (LYN) Tyr protein kinase family P07948
Tyrosine-protein kinase TXK (TXK) Tyr protein kinase family P42681
NAD-dependent protein deacetylase sirtuin-1 (SIRT1) Sirtuin family Q96EB6
GTPase NRas (NRAS) Ras family P01111
Ras-related C3 botulinum toxin substrate 1 (RAC1) Rho family P63000
Transthyretin (TTR) Transthyretin family P02766
Ubiquitin-conjugating enzyme E2 G2 (UBE2G2) Ubiquitin-conjugating enzyme family P60604
E3 ubiquitin-protein ligase CBL (CBL) . P22681
E3 ubiquitin-protein ligase CHIP (STUB1) . Q9UNE7
Transporter and channel
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Cytochrome c oxidase subunit 5A, mitochondrial (COX5A) Cytochrome c oxidase subunit 5A family P20674
Huntingtin (HTT) Huntingtin family P42858
Integrin beta-1 (ITGB1) Integrin beta chain family P05556
Toll-like receptor 3 (TLR3) Toll-like receptor family O15455
Toll/interleukin-1 receptor domain-containing adapter protein (TIRAP) . P58753
Wolframin (WFS1) . O76024
Transcription factor
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein c-Fos (FOS) BZIP family P01100
Transcription factor Jun (JUN) BZIP family P05412
Mothers against decapentaplegic homolog 3 (SMAD3) Dwarfin/SMAD family P84022
ETS domain-containing protein Elk-3 (ELK3) ETS family P41970
Retinoic acid receptor RXR-alpha (RXRA) Nuclear hormone receptor family P19793
Androgen receptor (AR) Nuclear hormone receptor family P10275
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Somatostatin receptor type 2 (SSTR2) G-protein coupled receptor 1 family P30874
Immunoglobulin
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Cytotoxic T-lymphocyte protein 4 (CTLA4) . P16410
T-cell-specific surface glycoprotein CD28 (CD28) . P10747
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tumor necrosis factor ligand superfamily member 6 (FASLG) Tumor necrosis factor family P48023
Other
Click To Hide/Show 27 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein AATF (AATF) AATF family Q9NY61
Abl interactor 1 (ABI1) ABI family Q8IZP0
Chromatin assembly factor 1 subunit A (CHAF1A) CHAF1A family Q13111
Adapter molecule crk (CRK) CRK family P46108
Large ribosomal subunit protein eL13 (RPL13) Eukaryotic ribosomal protein eL13 family P26373
GRB2-associated-binding protein 1 (GAB1) GAB family Q13480
Growth factor receptor-bound protein 2 (GRB2) GRB2/sem-5/DRK family P62993
Growth factor receptor-bound protein 10 (GRB10) GRB7/10/14 family Q13322
Ganglioside-induced differentiation-associated protein 1 (GDAP1) GST superfamily Q8TB36
Glial fibrillary acidic protein (GFAP) Intermediate filament family P14136
Negative elongation factor B (NELFB) NELF-B family Q8WX92
Alpha-2-macroglobulin (A2M) Protease inhibitor I39 (alpha-2-macroglobulin) family P01023
Disks large-associated protein 4 (DLGAP4) SAPAP family Q9Y2H0
SH3 and multiple ankyrin repeat domains protein 2 (SHANK2) SHANK family Q9UPX8
Syndecan-2 (SDC2) Syndecan proteoglycan family P34741
Targeting protein for Xklp2 (TPX2) TPX2 family Q9ULW0
Amyloid-beta A4 precursor protein-binding family B member 3 (APBB3) . O95704
C-Maf-inducing protein (CMIP) . Q8IY22
Guanine nucleotide exchange factor VAV3 (VAV3) . Q9UKW4
Inducible T-cell costimulator (ICOS) . Q9Y6W8
Insulin receptor substrate 1 (IRS1) . P35568
Insulin receptor substrate 2 (IRS2) . Q9Y4H2
Linker for activation of T-cells family member 1 (LAT) . O43561
Numb-like protein (NUMBL) . Q9Y6R0
Rap guanine nucleotide exchange factor 1 (RAPGEF1) . Q13905
SH2 domain-containing protein 2A (SH2D2A) . Q9NP31
Son of sevenless homolog 1 (SOS1) . Q07889

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Enzastaurin Small molecular drug DB06486
Sf1126 Small molecular drug DB05210
Wortmannin Small molecular drug DB08059

References

1 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
2 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
3 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
4 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
5 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
6 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
7 SP3-Enabled Rapid and High Coverage Chemoproteomic Identification of Cell-State-Dependent Redox-Sensitive Cysteines. Mol Cell Proteomics. 2022 Apr;21(4):100218. doi: 10.1016/j.mcpro.2022.100218. Epub 2022 Feb 25.
Mass spectrometry data entry: PXD029500 , PXD031647
8 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
9 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
10 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
11 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.
12 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
13 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