Details of the Target

General Information of Target

Target ID LDTP10754
Target Name Pannexin-1 (PANX1)
Gene Name PANX1
Gene ID 24145
Synonyms
MRS1; Pannexin-1; PANX1) [Cleaved into: Caspase-activated pannexin-1; Caspase-activated PANX1)]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MWRVKKLSLSLSPSPQTGKPSMRTPLRELTLQPGALTNSGKRSPACSSLTPSLCKLGLQE
GSNNSSPVDFVNNKRTDLSSEHFSHSSKWLETCQHESDEQPLDPIPQISSTPKTSEEAVD
PLGNYMVKTIVLVPSPLGQQQDMIFEARLDTMAETNSISLNGPLRTDDLVREEVAPCMGD
RFSEVAAVSEKPIFQESPSHLLEESPPNPCSEQLHCSKESLSSRTEAVREDLVPSESNAF
LPSSVLWLSPSTALAADFRVNHVDPEEEIVEHGAMEEREMRFPTHPKESETEDQALVSSV
EDILSTCLTPNLVEMESQEAPGPAVEDVGRILGSDTESWMSPLAWLEKGVNTSVMLENLR
QSLSLPSMLRDAAIGTTPFSTCSVGTWFTPSAPQEKSTNTSQTGLVGTKHSTSETEQLLC
GRPPDLTALSRHDLEDNLLSSLVILEVLSRQLRDWKSQLAVPHPETQDSSTQTDTSHSGI
TNKLQHLKESHEMGQALQQARNVMQSWVLISKELISLLHLSLLHLEEDKTTVSQESRRAE
TLVCCCFDLLKKLRAKLQSLKAEREEARHREEMALRGKDAAEIVLEAFCAHASQRISQLE
QDLASMREFRGLLKDAQTQLVGLHAKQEELVQQTVSLTSTLQQDWRSMQLDYTTWTALLS
RSRQLTEKLTVKSQQALQERDVAIEEKQEVSRVLEQVSAQLEECKGQTEQLELENSRLAT
DLRAQLQILANMDSQLKELQSQHTHCAQDLAMKDELLCQLTQSNEEQAAQWQKEEMALKH
MQAELQQQQAVLAKEVRDLKETLEFADQENQVAHLELGQVECQLKTTLEVLRERSLQCEN
LKDTVENLTAKLASTIADNQEQDLEKTRQYSQKLGLLTEQLQSLTLFLQTKLKEKTEQET
LLLSTACPPTQEHPLPNDRTFLGSILTAVADEEPESTPVPLLGSDKSAFTRVASMVSLQP
AETPGMEESLAEMSIMTTELQSLCSLLQESKEEAIRTLQRKICELQARLQAQEEQHQEVQ
KAKEADIEKLNQALCLRYKNEKELQEVIQQQNEKILEQIDKSGELISLREEVTHLTRSLR
RAETETKVLQEALAGQLDSNCQPMATNWIQEKVWLSQEVDKLRVMFLEMKNEKEKLMIKF
QSHRNILEENLRRSDKELEKLDDIVQHIYKTLLSIPEVVRGCKELQGLLEFLS
Target Bioclass
Transporter and channel
Family
Pannexin family
Subcellular location
Cell membrane
Function
Ion channel involved in a variety of physiological functions such as blood pressure regulation, apoptotic cell clearance and oogenesis. Forms anion-selective channels with relatively low conductance and an order of permeabilities: nitrate>iodide>chlroride>>aspartate=glutamate=gluconate. Can release ATP upon activation through phosphorylation or cleavage at C-terminus. May play a role as a Ca(2+)-leak channel to regulate ER Ca(2+) homeostasis.; [Caspase-activated pannexin-1]: During apoptosis, the C terminal tail is cleaved by caspases, which opens the main pore acting as a large-pore ATP efflux channel with a broad distribution, which allows the regulated release of molecules and ions smaller than 1 kDa, such as nucleotides ATP and UTP, and selective plasma membrane permeability to attract phagocytes that engulf the dying cells.
Uniprot ID
Q96RD7
Ensemble ID
ENST00000227638.8
HGNC ID
HGNC:8599
ChEMBL ID
CHEMBL3779756

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
A3KAW SNV: p.G380D .
HCT15 SNV: p.G393R .
K562 SNV: p.L139M .
MDAMB231 SNV: p.Q90Ter .
REH Insertion: p.T314HfsTer3 DBIA    Probe Info 
THP1 Deletion: p.V378del .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		11.34  LDD0402  [1]
FBP2
 Probe Info  		2.46  LDD0317  [2]
BTD
 Probe Info  		C136(0.82)  LDD2117  [3]
IPM
 Probe Info  		C136(1.49)  LDD1701  [3]
DBIA
 Probe Info  		C84(0.76)  LDD0593  [4]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [5]
IA-alkyne
 Probe Info  		C170(0.00); C136(0.00)  LDD0036  [5]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [5]
NAIA_4
 Probe Info  		N.A.  LDD2226  [6]
Compound 10
 Probe Info  		N.A.  LDD2216  [7]
AOyne
 Probe Info  		13.50  LDD0443  [8]
PAL-AfBPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C055
 Probe Info  		11.71  LDD1752  [9]
C056
 Probe Info  		16.11  LDD1753  [9]
C063
 Probe Info  		10.13  LDD1760  [9]
C091
 Probe Info  		11.55  LDD1782  [9]
C092
 Probe Info  		19.84  LDD1783  [9]
C094
 Probe Info  		25.63  LDD1785  [9]
C106
 Probe Info  		16.68  LDD1793  [9]
C107
 Probe Info  		5.50  LDD1794  [9]
C112
 Probe Info  		19.29  LDD1799  [9]
C153
 Probe Info  		15.45  LDD1834  [9]
C161
 Probe Info  		9.99  LDD1841  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C136(0.82)  LDD2117  [3]
 LDCM0026  4SU-RNA+native RNA HEK-293T C170(6.19)  LDD0372  [10]
 LDCM0214  AC1 HEK-293T C170(0.98); C136(0.97)  LDD1507  [11]
 LDCM0215  AC10 HEK-293T C136(1.03)  LDD1508  [11]
 LDCM0226  AC11 HEK-293T C170(1.05); C136(0.92)  LDD1509  [11]
 LDCM0237  AC12 HEK-293T C170(0.93); C136(1.00)  LDD1510  [11]
 LDCM0259  AC14 HEK-293T C170(0.98)  LDD1512  [11]
 LDCM0270  AC15 HEK-293T C170(1.18); C136(0.95)  LDD1513  [11]
 LDCM0276  AC17 HCT 116 C84(0.76)  LDD0593  [4]
 LDCM0277  AC18 HCT 116 C84(0.81)  LDD0594  [4]
 LDCM0278  AC19 HCT 116 C84(0.98)  LDD0595  [4]
 LDCM0279  AC2 HEK-293T C136(1.02)  LDD1518  [11]
 LDCM0280  AC20 HCT 116 C84(0.97)  LDD0597  [4]
 LDCM0281  AC21 HCT 116 C84(0.90)  LDD0598  [4]
 LDCM0282  AC22 HCT 116 C84(0.82)  LDD0599  [4]
 LDCM0283  AC23 HCT 116 C84(0.76)  LDD0600  [4]
 LDCM0284  AC24 HCT 116 C84(1.03)  LDD0601  [4]
 LDCM0285  AC25 HEK-293T C170(1.09); C136(0.94)  LDD1524  [11]
 LDCM0286  AC26 HEK-293T C136(0.99)  LDD1525  [11]
 LDCM0287  AC27 HEK-293T C170(1.08); C136(0.98)  LDD1526  [11]
 LDCM0288  AC28 HEK-293T C170(0.88); C136(0.97)  LDD1527  [11]
 LDCM0289  AC29 HEK-293T C170(1.28); C136(0.95)  LDD1528  [11]
 LDCM0290  AC3 HEK-293T C170(0.91); C136(0.94)  LDD1529  [11]
 LDCM0291  AC30 HEK-293T C170(1.05)  LDD1530  [11]
 LDCM0292  AC31 HEK-293T C170(1.21); C136(0.97)  LDD1531  [11]
 LDCM0293  AC32 HEK-293T C170(1.06)  LDD1532  [11]
 LDCM0294  AC33 HEK-293T C170(1.05); C136(1.04)  LDD1533  [11]
 LDCM0295  AC34 HEK-293T C136(1.11)  LDD1534  [11]
 LDCM0296  AC35 HEK-293T C170(1.06); C136(1.07)  LDD1535  [11]
 LDCM0297  AC36 HEK-293T C170(0.93); C136(0.93)  LDD1536  [11]
 LDCM0298  AC37 HEK-293T C170(0.88); C136(0.92)  LDD1537  [11]
 LDCM0299  AC38 HEK-293T C170(0.99)  LDD1538  [11]
 LDCM0300  AC39 HEK-293T C170(0.97); C136(1.01)  LDD1539  [11]
 LDCM0301  AC4 HEK-293T C170(1.00); C136(0.98)  LDD1540  [11]
 LDCM0302  AC40 HEK-293T C170(1.03)  LDD1541  [11]
 LDCM0303  AC41 HEK-293T C170(1.02); C136(1.10)  LDD1542  [11]
 LDCM0304  AC42 HEK-293T C136(0.99)  LDD1543  [11]
 LDCM0305  AC43 HEK-293T C170(1.12); C136(0.93)  LDD1544  [11]
 LDCM0306  AC44 HEK-293T C170(1.07); C136(0.89)  LDD1545  [11]
 LDCM0307  AC45 HEK-293T C170(0.99); C136(0.94)  LDD1546  [11]
 LDCM0308  AC46 HEK-293T C170(1.16)  LDD1547  [11]
 LDCM0309  AC47 HEK-293T C170(0.98); C136(0.94)  LDD1548  [11]
 LDCM0310  AC48 HEK-293T C170(1.12)  LDD1549  [11]
 LDCM0311  AC49 HEK-293T C170(1.04); C136(1.02)  LDD1550  [11]
 LDCM0312  AC5 HEK-293T C170(1.01); C136(0.96)  LDD1551  [11]
 LDCM0313  AC50 HEK-293T C136(1.01)  LDD1552  [11]
 LDCM0314  AC51 HEK-293T C170(1.10); C136(1.02)  LDD1553  [11]
 LDCM0315  AC52 HEK-293T C170(1.00); C136(0.96)  LDD1554  [11]
 LDCM0316  AC53 HEK-293T C170(0.92); C136(0.95)  LDD1555  [11]
 LDCM0317  AC54 HEK-293T C170(1.00)  LDD1556  [11]
 LDCM0318  AC55 HEK-293T C170(1.08); C136(0.97)  LDD1557  [11]
 LDCM0319  AC56 HEK-293T C170(1.01)  LDD1558  [11]
 LDCM0320  AC57 HEK-293T C170(1.03); C136(1.00)  LDD1559  [11]
 LDCM0321  AC58 HEK-293T C136(0.99)  LDD1560  [11]
 LDCM0322  AC59 HEK-293T C170(1.00); C136(1.00)  LDD1561  [11]
 LDCM0323  AC6 HEK-293T C170(1.01)  LDD1562  [11]
 LDCM0324  AC60 HEK-293T C170(1.04); C136(0.99)  LDD1563  [11]
 LDCM0325  AC61 HEK-293T C170(0.89); C136(0.92)  LDD1564  [11]
 LDCM0326  AC62 HEK-293T C170(1.00)  LDD1565  [11]
 LDCM0327  AC63 HEK-293T C170(0.93); C136(0.98)  LDD1566  [11]
 LDCM0328  AC64 HEK-293T C170(0.95)  LDD1567  [11]
 LDCM0332  AC68 HCT 116 C84(0.82)  LDD0649  [4]
 LDCM0333  AC69 HCT 116 C84(0.68)  LDD0650  [4]
 LDCM0334  AC7 HEK-293T C170(1.09); C136(1.00)  LDD1568  [11]
 LDCM0335  AC70 HCT 116 C84(0.70)  LDD0652  [4]
 LDCM0336  AC71 HCT 116 C84(0.92)  LDD0653  [4]
 LDCM0337  AC72 HCT 116 C84(0.84)  LDD0654  [4]
 LDCM0338  AC73 HCT 116 C84(0.59)  LDD0655  [4]
 LDCM0339  AC74 HCT 116 C84(0.45)  LDD0656  [4]
 LDCM0340  AC75 HCT 116 C84(0.61)  LDD0657  [4]
 LDCM0341  AC76 HCT 116 C84(0.72)  LDD0658  [4]
 LDCM0342  AC77 HCT 116 C84(0.71)  LDD0659  [4]
 LDCM0343  AC78 HCT 116 C84(0.72)  LDD0660  [4]
 LDCM0344  AC79 HCT 116 C84(0.90)  LDD0661  [4]
 LDCM0345  AC8 HEK-293T C170(1.00)  LDD1569  [11]
 LDCM0346  AC80 HCT 116 C84(0.68)  LDD0663  [4]
 LDCM0347  AC81 HCT 116 C84(1.10)  LDD0664  [4]
 LDCM0348  AC82 HCT 116 C84(0.34)  LDD0665  [4]
 LDCM0248  AKOS034007472 HEK-293T C170(0.89); C136(0.96)  LDD1511  [11]
 LDCM0356  AKOS034007680 HEK-293T C170(1.12); C136(1.04)  LDD1570  [11]
 LDCM0275  AKOS034007705 HEK-293T C170(1.05)  LDD1514  [11]
 LDCM0367  CL1 HCT 116 C84(1.23)  LDD0684  [4]
 LDCM0368  CL10 HCT 116 C84(0.59)  LDD0685  [4]
 LDCM0369  CL100 HEK-293T C170(0.95)  LDD1573  [11]
 LDCM0370  CL101 HEK-293T C170(0.91); C136(0.93)  LDD1574  [11]
 LDCM0371  CL102 HEK-293T C170(1.01); C136(1.09)  LDD1575  [11]
 LDCM0372  CL103 HEK-293T C170(1.06)  LDD1576  [11]
 LDCM0373  CL104 HEK-293T C170(0.88)  LDD1577  [11]
 LDCM0374  CL105 HCT 116 C84(0.76)  LDD0691  [4]
 LDCM0375  CL106 HCT 116 C84(0.47)  LDD0692  [4]
 LDCM0376  CL107 HCT 116 C84(0.82)  LDD0693  [4]
 LDCM0377  CL108 HCT 116 C84(0.82)  LDD0694  [4]
 LDCM0378  CL109 HCT 116 C84(0.82)  LDD0695  [4]
 LDCM0379  CL11 HCT 116 C84(0.58)  LDD0696  [4]
 LDCM0380  CL110 HCT 116 C84(0.73)  LDD0697  [4]
 LDCM0381  CL111 HCT 116 C84(0.96)  LDD0698  [4]
 LDCM0382  CL112 HEK-293T C170(0.93)  LDD1586  [11]
 LDCM0383  CL113 HEK-293T C170(0.97); C136(1.01)  LDD1587  [11]
 LDCM0384  CL114 HEK-293T C170(1.02); C136(1.00)  LDD1588  [11]
 LDCM0385  CL115 HEK-293T C170(0.93)  LDD1589  [11]
 LDCM0386  CL116 HEK-293T C170(0.95)  LDD1590  [11]
 LDCM0387  CL117 HEK-293T C170(1.00); C136(0.94)  LDD1591  [11]
 LDCM0388  CL118 HEK-293T C170(1.00); C136(0.95)  LDD1592  [11]
 LDCM0389  CL119 HEK-293T C170(0.94)  LDD1593  [11]
 LDCM0390  CL12 HCT 116 C84(0.79)  LDD0707  [4]
 LDCM0391  CL120 HEK-293T C170(0.92)  LDD1595  [11]
 LDCM0392  CL121 HEK-293T C170(0.88); C136(1.03)  LDD1596  [11]
 LDCM0393  CL122 HEK-293T C170(0.86); C136(1.08)  LDD1597  [11]
 LDCM0394  CL123 HEK-293T C170(0.92)  LDD1598  [11]
 LDCM0395  CL124 HEK-293T C170(0.86)  LDD1599  [11]
 LDCM0396  CL125 HEK-293T C170(0.79); C136(1.01)  LDD1600  [11]
 LDCM0397  CL126 HEK-293T C170(0.87); C136(0.99)  LDD1601  [11]
 LDCM0398  CL127 HEK-293T C170(0.87)  LDD1602  [11]
 LDCM0399  CL128 HEK-293T C170(0.87)  LDD1603  [11]
 LDCM0400  CL13 HCT 116 C84(0.60)  LDD0717  [4]
 LDCM0401  CL14 HCT 116 C84(1.03)  LDD0718  [4]
 LDCM0402  CL15 HCT 116 C84(0.37)  LDD0719  [4]
 LDCM0403  CL16 HCT 116 C84(0.86)  LDD0720  [4]
 LDCM0404  CL17 HCT 116 C84(0.62)  LDD0721  [4]
 LDCM0405  CL18 HCT 116 C84(0.45)  LDD0722  [4]
 LDCM0406  CL19 HCT 116 C84(0.48)  LDD0723  [4]
 LDCM0407  CL2 HCT 116 C84(1.36)  LDD0724  [4]
 LDCM0408  CL20 HCT 116 C84(0.54)  LDD0725  [4]
 LDCM0409  CL21 HCT 116 C84(0.45)  LDD0726  [4]
 LDCM0410  CL22 HCT 116 C84(0.35)  LDD0727  [4]
 LDCM0411  CL23 HCT 116 C84(0.64)  LDD0728  [4]
 LDCM0412  CL24 HCT 116 C84(0.53)  LDD0729  [4]
 LDCM0413  CL25 HCT 116 C84(0.53)  LDD0730  [4]
 LDCM0414  CL26 HCT 116 C84(0.62)  LDD0731  [4]
 LDCM0415  CL27 HCT 116 C84(0.72)  LDD0732  [4]
 LDCM0416  CL28 HCT 116 C84(0.49)  LDD0733  [4]
 LDCM0417  CL29 HCT 116 C84(0.47)  LDD0734  [4]
 LDCM0418  CL3 HCT 116 C84(1.01)  LDD0735  [4]
 LDCM0419  CL30 HCT 116 C84(0.68)  LDD0736  [4]
 LDCM0420  CL31 HCT 116 C84(0.78)  LDD0737  [4]
 LDCM0421  CL32 HCT 116 C84(0.62)  LDD0738  [4]
 LDCM0422  CL33 HCT 116 C84(0.72)  LDD0739  [4]
 LDCM0423  CL34 HCT 116 C84(0.47)  LDD0740  [4]
 LDCM0424  CL35 HCT 116 C84(0.60)  LDD0741  [4]
 LDCM0425  CL36 HCT 116 C84(0.70)  LDD0742  [4]
 LDCM0426  CL37 HCT 116 C84(0.72)  LDD0743  [4]
 LDCM0428  CL39 HCT 116 C84(0.66)  LDD0745  [4]
 LDCM0429  CL4 HCT 116 C84(1.00)  LDD0746  [4]
 LDCM0430  CL40 HCT 116 C84(0.63)  LDD0747  [4]
 LDCM0431  CL41 HCT 116 C84(1.01)  LDD0748  [4]
 LDCM0432  CL42 HCT 116 C84(0.43)  LDD0749  [4]
 LDCM0433  CL43 HCT 116 C84(0.59)  LDD0750  [4]
 LDCM0434  CL44 HCT 116 C84(0.43)  LDD0751  [4]
 LDCM0435  CL45 HCT 116 C84(0.40)  LDD0752  [4]
 LDCM0436  CL46 HEK-293T C170(0.99)  LDD1640  [11]
 LDCM0437  CL47 HEK-293T C170(1.21); C136(0.83)  LDD1641  [11]
 LDCM0438  CL48 HEK-293T C170(0.93)  LDD1642  [11]
 LDCM0439  CL49 HEK-293T C170(0.93); C136(1.01)  LDD1643  [11]
 LDCM0440  CL5 HCT 116 C84(0.86)  LDD0757  [4]
 LDCM0441  CL50 HEK-293T C170(1.00); C136(1.05)  LDD1645  [11]
 LDCM0443  CL52 HEK-293T C170(0.97)  LDD1646  [11]
 LDCM0444  CL53 HEK-293T C170(1.01); C136(1.03)  LDD1647  [11]
 LDCM0445  CL54 HEK-293T C136(1.19)  LDD1648  [11]
 LDCM0446  CL55 HEK-293T C170(1.11); C136(0.83)  LDD1649  [11]
 LDCM0447  CL56 HEK-293T C170(0.78); C136(0.88)  LDD1650  [11]
 LDCM0448  CL57 HEK-293T C170(1.20); C136(0.89)  LDD1651  [11]
 LDCM0449  CL58 HEK-293T C170(0.96)  LDD1652  [11]
 LDCM0450  CL59 HEK-293T C170(1.05); C136(0.94)  LDD1653  [11]
 LDCM0451  CL6 HCT 116 C84(0.65)  LDD0768  [4]
 LDCM0452  CL60 HEK-293T C170(1.11)  LDD1655  [11]
 LDCM0453  CL61 HEK-293T C170(0.91); C136(0.98)  LDD1656  [11]
 LDCM0454  CL62 HEK-293T C170(1.00); C136(0.95)  LDD1657  [11]
 LDCM0455  CL63 HEK-293T C170(0.83)  LDD1658  [11]
 LDCM0456  CL64 HEK-293T C170(0.95)  LDD1659  [11]
 LDCM0457  CL65 HEK-293T C170(1.04); C136(0.97)  LDD1660  [11]
 LDCM0458  CL66 HEK-293T C136(1.00)  LDD1661  [11]
 LDCM0459  CL67 HEK-293T C170(1.04); C136(0.86)  LDD1662  [11]
 LDCM0460  CL68 HEK-293T C170(0.90); C136(0.91)  LDD1663  [11]
 LDCM0461  CL69 HEK-293T C170(0.91); C136(0.98)  LDD1664  [11]
 LDCM0462  CL7 HCT 116 C84(0.73)  LDD0779  [4]
 LDCM0463  CL70 HEK-293T C170(1.07)  LDD1666  [11]
 LDCM0464  CL71 HEK-293T C170(1.01); C136(0.94)  LDD1667  [11]
 LDCM0465  CL72 HEK-293T C170(1.19)  LDD1668  [11]
 LDCM0466  CL73 HEK-293T C170(0.87); C136(0.97)  LDD1669  [11]
 LDCM0467  CL74 HEK-293T C170(1.03); C136(0.91)  LDD1670  [11]
 LDCM0469  CL76 HCT 116 C84(0.62)  LDD0786  [4]
 LDCM0470  CL77 HCT 116 C84(0.69)  LDD0787  [4]
 LDCM0471  CL78 HCT 116 C84(0.77)  LDD0788  [4]
 LDCM0472  CL79 HCT 116 C84(0.93)  LDD0789  [4]
 LDCM0473  CL8 HCT 116 C84(0.70)  LDD0790  [4]
 LDCM0474  CL80 HCT 116 C84(0.49)  LDD0791  [4]
 LDCM0475  CL81 HCT 116 C84(0.82)  LDD0792  [4]
 LDCM0476  CL82 HCT 116 C84(0.76)  LDD0793  [4]
 LDCM0477  CL83 HCT 116 C84(0.58)  LDD0794  [4]
 LDCM0478  CL84 HCT 116 C84(0.54)  LDD0795  [4]
 LDCM0479  CL85 HCT 116 C84(0.81)  LDD0796  [4]
 LDCM0480  CL86 HCT 116 C84(0.70)  LDD0797  [4]
 LDCM0481  CL87 HCT 116 C84(0.87)  LDD0798  [4]
 LDCM0482  CL88 HCT 116 C84(0.68)  LDD0799  [4]
 LDCM0483  CL89 HCT 116 C84(0.45)  LDD0800  [4]
 LDCM0484  CL9 HCT 116 C84(1.04)  LDD0801  [4]
 LDCM0485  CL90 HCT 116 C84(0.84)  LDD0802  [4]
 LDCM0486  CL91 HEK-293T C170(0.83); C136(0.76)  LDD1689  [11]
 LDCM0487  CL92 HEK-293T C170(1.02); C136(1.04)  LDD1690  [11]
 LDCM0488  CL93 HEK-293T C170(1.01); C136(1.10)  LDD1691  [11]
 LDCM0489  CL94 HEK-293T C170(0.98)  LDD1692  [11]
 LDCM0490  CL95 HEK-293T C170(1.10); C136(1.11)  LDD1693  [11]
 LDCM0491  CL96 HEK-293T C170(0.84)  LDD1694  [11]
 LDCM0492  CL97 HEK-293T C170(0.98); C136(1.15)  LDD1695  [11]
 LDCM0493  CL98 HEK-293T C170(0.87); C136(1.21)  LDD1696  [11]
 LDCM0494  CL99 HEK-293T C170(1.03)  LDD1697  [11]
 LDCM0495  E2913 HEK-293T C170(0.87)  LDD1698  [11]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C136(0.76)  LDD1702  [3]
 LDCM0468  Fragment33 HEK-293T C170(0.87)  LDD1671  [11]
 LDCM0427  Fragment51 HCT 116 C84(0.62)  LDD0744  [4]
 LDCM0022  KB02 HEK-293T C136(0.97); C170(1.02)  LDD1492  [11]
 LDCM0023  KB03 HEK-293T C136(0.90); C170(0.99)  LDD1497  [11]
 LDCM0024  KB05 G361 C136(1.42)  LDD3311  [12]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Squalene synthase (FDFT1) Phytoene/squalene synthase family P37268
Fatty acid hydroxylase domain-containing protein 2 (FAXDC2) Sterol desaturase family Q96IV6
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Sodium-coupled neutral amino acid transporter 7 (SLC38A7) Amino acid/polyamine transporter 2 family Q9NVC3
Apolipoprotein A-II (APOA2) Apolipoprotein A2 family P02652
Bcl-2-like protein 2 (BCL2L2) Bcl-2 family Q92843
Aquaporin-2 (AQP2) MIP/aquaporin (TC 1.A.8) family P41181
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Tumor necrosis factor (TNF) Tumor necrosis factor family P01375
Other
Click To Hide/Show 5 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Apolipoprotein L2 (APOL2) Apolipoprotein L family Q9BQE5
Vesicle-associated membrane protein 5 (VAMP5) Synaptobrevin family O95183
Transmembrane protein 229B (TMEM229B) TMEM229 family Q8NBD8
Complement factor H-related protein 5 (CFHR5) . Q9BXR6
WAP four-disulfide core domain protein 2 (WFDC2) . Q14508

The Drug(s) Related To This Target

Approved
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Probenecid Small molecular drug DB01032

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580
3 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
4 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.
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 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
8 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
9 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
10 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
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 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