Details of the Target

General Information of Target

Target ID LDTP08950
Target Name ADP-ribosylation factor GTPase-activating protein 1 (ARFGAP1)
Gene Name ARFGAP1
Gene ID 55738
Synonyms
ARF1GAP; ADP-ribosylation factor GTPase-activating protein 1; ARF GAP 1; ADP-ribosylation factor 1 GTPase-activating protein; ARF1 GAP; ARF1-directed GTPase-activating protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASPRTRKVLKEVRVQDENNVCFECGAFNPQWVSVTYGIWICLECSGRHRGLGVHLSFVR
SVTMDKWKDIELEKMKAGGNAKFREFLESQEDYDPCWSLQEKYNSRAAALFRDKVVALAE
GREWSLESSPAQNWTPPQPRTLPSMVHRVSGQPQSVTASSDKAFEDWLNDDLGSYQGAQG
NRYVGFGNTPPPQKKEDDFLNNAMSSLYSGWSSFTTGASRFASAAKEGATKFGSQASQKA
SELGHSLNENVLKPAQEKVKEGKIFDDVSSGVSQLASKVQGVGSKGWRDVTTFFSGKAEG
PLDSPSEGHSYQNSGLDHFQNSNIDQSFWETFGSAEPTKTRKSPSSDSWTCADTSTERRS
SDSWEVWGSASTNRNSNSDGGEGGEGTKKAVPPAVPTDDGWDNQNW
Target Bioclass
Other
Subcellular location
Cytoplasm
Function
GTPase-activating protein (GAP) for the ADP ribosylation factor 1 (ARF1). Involved in membrane trafficking and /or vesicle transport. Promotes hydrolysis of the ARF1-bound GTP and thus, is required for the dissociation of coat proteins from Golgi-derived membranes and vesicles, a prerequisite for vesicle's fusion with target compartment. Probably regulates ARF1-mediated transport via its interaction with the KDELR proteins and TMED2. Overexpression induces the redistribution of the entire Golgi complex to the endoplasmic reticulum, as when ARF1 is deactivated. Its activity is stimulated by phosphoinosides and inhibited by phosphatidylcholine.
Uniprot ID
Q8N6T3
Ensemble ID
ENST00000353546.7
HGNC ID
HGNC:15852

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT116 SNV: p.A276V .
RKO SNV: p.A27T .
SKMEL2 Deletion: p.S295RfsTer30 DBIA    Probe Info 
SUPT1 SNV: p.R182H; p.G386C DBIA    Probe Info 
TGBC1TKB SNV: p.L99S DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 28 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
CY-1
 Probe Info  		100.00  LDD0243  [2]
TH211
 Probe Info  		Y183(8.08)  LDD0260  [3]
STPyne
 Probe Info  		K11(5.38); K114(10.00); K226(5.84); K231(1.43)  LDD0277  [4]
ONAyne
 Probe Info  		K226(5.56)  LDD0275  [4]
Probe 1
 Probe Info  		Y175(6.36); Y183(13.50)  LDD3495  [5]
DBIA
 Probe Info  		C96(0.72)  LDD3314  [6]
BTD
 Probe Info  		C351(0.89)  LDD2091  [7]
Jackson_1
 Probe Info  		20.00  LDD0121  [8]
AHL-Pu-1
 Probe Info  		C96(2.60); C351(2.54)  LDD0168  [9]
HHS-475
 Probe Info  		Y183(0.81); Y311(1.22); Y175(1.68)  LDD0264  [10]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [11]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [11]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [11]
NAIA_4
 Probe Info  		C96(0.00); C351(0.00)  LDD2226  [12]
TFBX
 Probe Info  		N.A.  LDD0027  [13]
WYneN
 Probe Info  		N.A.  LDD0021  [14]
DA-P3
 Probe Info  		N.A.  LDD0178  [15]
Compound 10
 Probe Info  		N.A.  LDD2216  [16]
Compound 11
 Probe Info  		N.A.  LDD2213  [16]
IPM
 Probe Info  		N.A.  LDD0005  [14]
NHS
 Probe Info  		N.A.  LDD0010  [14]
Phosphinate-6
 Probe Info  		C96(0.00); C351(0.00)  LDD0018  [17]
Acrolein
 Probe Info  		C351(0.00); C96(0.00)  LDD0217  [18]
Methacrolein
 Probe Info  		N.A.  LDD0218  [18]
W1
 Probe Info  		C96(0.00); C351(0.00)  LDD0236  [19]
AOyne
 Probe Info  		11.50  LDD0443  [20]
NAIA_5
 Probe Info  		C96(0.00); C351(0.00)  LDD2223  [12]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C187
 Probe Info  		18.51  LDD1865  [21]
C191
 Probe Info  		14.62  LDD1868  [21]
C193
 Probe Info  		6.23  LDD1869  [21]
A-DA
 Probe Info  		14.31  LDD0143  [22]
Alk-rapa
 Probe Info  		4.02  LDD0213  [23]

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 C351(1.19)  LDD2130  [7]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C351(0.72)  LDD2132  [7]
 LDCM0025  4SU-RNA HEK-293T C96(2.60); C351(2.54)  LDD0168  [9]
 LDCM0026  4SU-RNA+native RNA HEK-293T C351(5.56)  LDD0169  [9]
 LDCM0214  AC1 HEK-293T C351(1.05); C96(1.09)  LDD1507  [24]
 LDCM0215  AC10 HEK-293T C351(0.92); C96(0.88)  LDD1508  [24]
 LDCM0226  AC11 HEK-293T C351(1.10); C96(0.99)  LDD1509  [24]
 LDCM0237  AC12 HEK-293T C351(1.07); C96(0.99)  LDD1510  [24]
 LDCM0259  AC14 HEK-293T C351(1.02); C96(0.92)  LDD1512  [24]
 LDCM0270  AC15 HEK-293T C351(1.01); C96(0.92)  LDD1513  [24]
 LDCM0276  AC17 HEK-293T C351(1.01); C96(0.98)  LDD1515  [24]
 LDCM0277  AC18 HEK-293T C351(1.00); C96(0.92)  LDD1516  [24]
 LDCM0278  AC19 HEK-293T C351(1.15); C96(1.03)  LDD1517  [24]
 LDCM0279  AC2 HEK-293T C351(1.12); C96(0.98)  LDD1518  [24]
 LDCM0280  AC20 HEK-293T C351(1.04); C96(0.99)  LDD1519  [24]
 LDCM0281  AC21 HEK-293T C351(1.06); C96(1.00)  LDD1520  [24]
 LDCM0282  AC22 HEK-293T C351(1.03); C96(0.91)  LDD1521  [24]
 LDCM0283  AC23 HEK-293T C351(1.01); C96(1.09)  LDD1522  [24]
 LDCM0284  AC24 HEK-293T C351(0.97); C96(0.94)  LDD1523  [24]
 LDCM0285  AC25 HEK-293T C351(1.02); C96(1.00)  LDD1524  [24]
 LDCM0286  AC26 HEK-293T C351(0.97); C96(0.87)  LDD1525  [24]
 LDCM0287  AC27 HEK-293T C351(1.14); C96(1.05)  LDD1526  [24]
 LDCM0288  AC28 HEK-293T C351(0.96); C96(0.93)  LDD1527  [24]
 LDCM0289  AC29 HEK-293T C351(1.19); C96(0.96)  LDD1528  [24]
 LDCM0290  AC3 HEK-293T C351(1.13); C96(1.11)  LDD1529  [24]
 LDCM0291  AC30 HEK-293T C351(1.10); C96(1.04)  LDD1530  [24]
 LDCM0292  AC31 HEK-293T C351(1.04); C96(0.98)  LDD1531  [24]
 LDCM0293  AC32 HEK-293T C351(0.92); C96(0.95)  LDD1532  [24]
 LDCM0294  AC33 HEK-293T C351(1.09); C96(0.95)  LDD1533  [24]
 LDCM0295  AC34 HEK-293T C351(1.08); C96(0.92)  LDD1534  [24]
 LDCM0296  AC35 HEK-293T C351(1.12); C96(1.12)  LDD1535  [24]
 LDCM0297  AC36 HEK-293T C351(1.07); C96(0.99)  LDD1536  [24]
 LDCM0298  AC37 HEK-293T C351(1.18); C96(1.00)  LDD1537  [24]
 LDCM0299  AC38 HEK-293T C351(1.13); C96(0.86)  LDD1538  [24]
 LDCM0300  AC39 HEK-293T C351(1.07); C96(0.98)  LDD1539  [24]
 LDCM0301  AC4 HEK-293T C351(1.07); C96(1.01)  LDD1540  [24]
 LDCM0302  AC40 HEK-293T C351(0.94); C96(0.84)  LDD1541  [24]
 LDCM0303  AC41 HEK-293T C351(1.05); C96(0.99)  LDD1542  [24]
 LDCM0304  AC42 HEK-293T C351(1.01); C96(0.88)  LDD1543  [24]
 LDCM0305  AC43 HEK-293T C351(1.04); C96(1.05)  LDD1544  [24]
 LDCM0306  AC44 HEK-293T C351(1.07); C96(0.95)  LDD1545  [24]
 LDCM0307  AC45 HEK-293T C351(1.13); C96(0.95)  LDD1546  [24]
 LDCM0308  AC46 HEK-293T C351(0.98); C96(0.92)  LDD1547  [24]
 LDCM0309  AC47 HEK-293T C351(0.99); C96(0.96)  LDD1548  [24]
 LDCM0310  AC48 HEK-293T C351(0.93); C96(0.94)  LDD1549  [24]
 LDCM0311  AC49 HEK-293T C351(1.18); C96(0.99)  LDD1550  [24]
 LDCM0312  AC5 HEK-293T C351(0.98); C96(0.97)  LDD1551  [24]
 LDCM0313  AC50 HEK-293T C351(0.97); C96(0.89)  LDD1552  [24]
 LDCM0314  AC51 HEK-293T C351(1.07); C96(1.04)  LDD1553  [24]
 LDCM0315  AC52 HEK-293T C351(1.07); C96(0.91)  LDD1554  [24]
 LDCM0316  AC53 HEK-293T C351(1.14); C96(0.99)  LDD1555  [24]
 LDCM0317  AC54 HEK-293T C351(1.06); C96(0.95)  LDD1556  [24]
 LDCM0318  AC55 HEK-293T C351(0.98); C96(0.97)  LDD1557  [24]
 LDCM0319  AC56 HEK-293T C351(1.04); C96(0.93)  LDD1558  [24]
 LDCM0320  AC57 HEK-293T C351(1.16); C96(0.99)  LDD1559  [24]
 LDCM0321  AC58 HEK-293T C351(1.01); C96(0.95)  LDD1560  [24]
 LDCM0322  AC59 HEK-293T C351(1.03); C96(1.09)  LDD1561  [24]
 LDCM0323  AC6 HEK-293T C351(1.02); C96(0.95)  LDD1562  [24]
 LDCM0324  AC60 HEK-293T C351(1.11); C96(1.12)  LDD1563  [24]
 LDCM0325  AC61 HEK-293T C351(1.09); C96(0.94)  LDD1564  [24]
 LDCM0326  AC62 HEK-293T C351(1.35); C96(0.92)  LDD1565  [24]
 LDCM0327  AC63 HEK-293T C351(1.03); C96(0.95)  LDD1566  [24]
 LDCM0328  AC64 HEK-293T C351(0.93); C96(1.06)  LDD1567  [24]
 LDCM0334  AC7 HEK-293T C351(1.01); C96(1.01)  LDD1568  [24]
 LDCM0345  AC8 HEK-293T C351(0.93); C96(0.91)  LDD1569  [24]
 LDCM0248  AKOS034007472 HEK-293T C351(1.16); C96(0.98)  LDD1511  [24]
 LDCM0356  AKOS034007680 HEK-293T C351(1.09); C96(0.97)  LDD1570  [24]
 LDCM0275  AKOS034007705 HEK-293T C351(0.90); C96(0.94)  LDD1514  [24]
 LDCM0156  Aniline NCI-H1299 12.29  LDD0403  [1]
 LDCM0083  Avasimibe A-549 14.31  LDD0143  [22]
 LDCM0498  BS-3668 MDA-MB-231 C351(0.89)  LDD2091  [7]
 LDCM0630  CCW28-3 231MFP C96(1.64)  LDD2214  [25]
 LDCM0108  Chloroacetamide HeLa C351(0.00); C96(0.00)  LDD0222  [18]
 LDCM0071  Cisar_cp14 MDA-MB-231 20.00  LDD0121  [8]
 LDCM0632  CL-Sc Hep-G2 C351(1.08); C351(0.74); C351(0.64)  LDD2227  [12]
 LDCM0367  CL1 HEK-293T C351(1.05); C96(0.83)  LDD1571  [24]
 LDCM0368  CL10 HEK-293T C351(0.88); C96(0.77)  LDD1572  [24]
 LDCM0369  CL100 HEK-293T C351(0.98); C96(1.00)  LDD1573  [24]
 LDCM0370  CL101 HEK-293T C351(1.05); C96(0.80)  LDD1574  [24]
 LDCM0371  CL102 HEK-293T C351(0.99); C96(0.95)  LDD1575  [24]
 LDCM0372  CL103 HEK-293T C351(1.08); C96(1.04)  LDD1576  [24]
 LDCM0373  CL104 HEK-293T C351(0.93); C96(0.98)  LDD1577  [24]
 LDCM0374  CL105 HEK-293T C351(1.01); C96(0.85)  LDD1578  [24]
 LDCM0375  CL106 HEK-293T C351(1.05); C96(1.20)  LDD1579  [24]
 LDCM0376  CL107 HEK-293T C351(0.96); C96(1.05)  LDD1580  [24]
 LDCM0377  CL108 HEK-293T C351(0.98); C96(0.96)  LDD1581  [24]
 LDCM0378  CL109 HEK-293T C351(0.90); C96(0.90)  LDD1582  [24]
 LDCM0379  CL11 HEK-293T C351(1.13); C96(1.18)  LDD1583  [24]
 LDCM0380  CL110 HEK-293T C351(0.98); C96(1.11)  LDD1584  [24]
 LDCM0381  CL111 HEK-293T C351(0.96); C96(0.91)  LDD1585  [24]
 LDCM0382  CL112 HEK-293T C351(1.00); C96(0.93)  LDD1586  [24]
 LDCM0383  CL113 HEK-293T C351(1.04); C96(0.79)  LDD1587  [24]
 LDCM0384  CL114 HEK-293T C351(1.00); C96(0.88)  LDD1588  [24]
 LDCM0385  CL115 HEK-293T C351(0.99); C96(0.88)  LDD1589  [24]
 LDCM0386  CL116 HEK-293T C351(0.98); C96(0.97)  LDD1590  [24]
 LDCM0387  CL117 HEK-293T C351(0.96); C96(0.74)  LDD1591  [24]
 LDCM0388  CL118 HEK-293T C351(1.10); C96(0.98)  LDD1592  [24]
 LDCM0389  CL119 HEK-293T C351(0.98); C96(0.95)  LDD1593  [24]
 LDCM0390  CL12 HEK-293T C351(0.79); C96(1.00)  LDD1594  [24]
 LDCM0391  CL120 HEK-293T C351(0.91); C96(1.04)  LDD1595  [24]
 LDCM0392  CL121 HEK-293T C351(0.96); C96(0.96)  LDD1596  [24]
 LDCM0393  CL122 HEK-293T C351(0.98); C96(1.16)  LDD1597  [24]
 LDCM0394  CL123 HEK-293T C351(1.11); C96(0.84)  LDD1598  [24]
 LDCM0395  CL124 HEK-293T C351(0.99); C96(0.90)  LDD1599  [24]
 LDCM0396  CL125 HEK-293T C351(1.02); C96(0.77)  LDD1600  [24]
 LDCM0397  CL126 HEK-293T C351(1.06); C96(0.94)  LDD1601  [24]
 LDCM0398  CL127 HEK-293T C351(0.98); C96(0.99)  LDD1602  [24]
 LDCM0399  CL128 HEK-293T C351(0.96); C96(0.90)  LDD1603  [24]
 LDCM0400  CL13 HEK-293T C351(1.02); C96(0.83)  LDD1604  [24]
 LDCM0401  CL14 HEK-293T C351(1.15); C96(1.14)  LDD1605  [24]
 LDCM0402  CL15 HEK-293T C351(1.11); C96(0.90)  LDD1606  [24]
 LDCM0403  CL16 HEK-293T C351(0.96); C96(0.90)  LDD1607  [24]
 LDCM0404  CL17 HEK-293T C351(1.18); C96(0.90)  LDD1608  [24]
 LDCM0405  CL18 HEK-293T C351(1.07); C96(0.82)  LDD1609  [24]
 LDCM0406  CL19 HEK-293T C351(1.11); C96(0.93)  LDD1610  [24]
 LDCM0407  CL2 HEK-293T C351(1.07); C96(1.24)  LDD1611  [24]
 LDCM0408  CL20 HEK-293T C351(1.14); C96(0.63)  LDD1612  [24]
 LDCM0409  CL21 HEK-293T C351(0.92); C96(0.99)  LDD1613  [24]
 LDCM0410  CL22 HEK-293T C351(0.84); C96(0.92)  LDD1614  [24]
 LDCM0411  CL23 HEK-293T C351(1.20); C96(1.21)  LDD1615  [24]
 LDCM0412  CL24 HEK-293T C351(0.83); C96(0.93)  LDD1616  [24]
 LDCM0413  CL25 HEK-293T C351(0.84); C96(0.88)  LDD1617  [24]
 LDCM0414  CL26 HEK-293T C351(1.21); C96(1.02)  LDD1618  [24]
 LDCM0415  CL27 HEK-293T C351(1.08); C96(0.96)  LDD1619  [24]
 LDCM0416  CL28 HEK-293T C351(0.90); C96(0.92)  LDD1620  [24]
 LDCM0417  CL29 HEK-293T C351(1.09); C96(1.07)  LDD1621  [24]
 LDCM0418  CL3 HEK-293T C351(1.10); C96(0.94)  LDD1622  [24]
 LDCM0419  CL30 HEK-293T C351(1.00); C96(0.89)  LDD1623  [24]
 LDCM0420  CL31 HEK-293T C351(1.16); C96(0.87)  LDD1624  [24]
 LDCM0421  CL32 HEK-293T C351(1.15); C96(0.68)  LDD1625  [24]
 LDCM0422  CL33 HEK-293T C351(0.89); C96(0.90)  LDD1626  [24]
 LDCM0423  CL34 HEK-293T C351(0.82); C96(0.86)  LDD1627  [24]
 LDCM0424  CL35 HEK-293T C351(1.13); C96(1.22)  LDD1628  [24]
 LDCM0425  CL36 HEK-293T C351(0.74); C96(0.87)  LDD1629  [24]
 LDCM0426  CL37 HEK-293T C351(1.11); C96(0.79)  LDD1630  [24]
 LDCM0428  CL39 HEK-293T C351(1.11); C96(0.96)  LDD1632  [24]
 LDCM0429  CL4 HEK-293T C351(1.03); C96(0.94)  LDD1633  [24]
 LDCM0430  CL40 HEK-293T C351(0.91); C96(1.03)  LDD1634  [24]
 LDCM0431  CL41 HEK-293T C351(1.14); C96(0.90)  LDD1635  [24]
 LDCM0432  CL42 HEK-293T C351(1.04); C96(0.87)  LDD1636  [24]
 LDCM0433  CL43 HEK-293T C351(1.05); C96(0.92)  LDD1637  [24]
 LDCM0434  CL44 HEK-293T C351(1.21); C96(0.76)  LDD1638  [24]
 LDCM0435  CL45 HEK-293T C351(1.12); C96(1.07)  LDD1639  [24]
 LDCM0436  CL46 HEK-293T C351(0.93); C96(0.88)  LDD1640  [24]
 LDCM0437  CL47 HEK-293T C351(1.02); C96(1.12)  LDD1641  [24]
 LDCM0438  CL48 HEK-293T C351(0.68); C96(0.89)  LDD1642  [24]
 LDCM0439  CL49 HEK-293T C351(0.95); C96(0.71)  LDD1643  [24]
 LDCM0440  CL5 HEK-293T C351(1.09); C96(1.01)  LDD1644  [24]
 LDCM0441  CL50 HEK-293T C351(1.08); C96(0.86)  LDD1645  [24]
 LDCM0443  CL52 HEK-293T C351(0.95); C96(1.01)  LDD1646  [24]
 LDCM0444  CL53 HEK-293T C351(1.26); C96(0.96)  LDD1647  [24]
 LDCM0445  CL54 HEK-293T C351(1.01); C96(0.75)  LDD1648  [24]
 LDCM0446  CL55 HEK-293T C351(1.05); C96(1.05)  LDD1649  [24]
 LDCM0447  CL56 HEK-293T C351(1.13); C96(0.69)  LDD1650  [24]
 LDCM0448  CL57 HEK-293T C351(1.04); C96(1.05)  LDD1651  [24]
 LDCM0449  CL58 HEK-293T C351(0.81); C96(0.89)  LDD1652  [24]
 LDCM0450  CL59 HEK-293T C351(1.12); C96(1.20)  LDD1653  [24]
 LDCM0451  CL6 HEK-293T C351(0.97); C96(0.81)  LDD1654  [24]
 LDCM0452  CL60 HEK-293T C351(0.75); C96(0.80)  LDD1655  [24]
 LDCM0453  CL61 HEK-293T C351(1.00); C96(0.84)  LDD1656  [24]
 LDCM0454  CL62 HEK-293T C351(1.00); C96(0.94)  LDD1657  [24]
 LDCM0455  CL63 HEK-293T C351(1.12); C96(0.88)  LDD1658  [24]
 LDCM0456  CL64 HEK-293T C351(1.07); C96(0.87)  LDD1659  [24]
 LDCM0457  CL65 HEK-293T C351(1.08); C96(1.06)  LDD1660  [24]
 LDCM0458  CL66 HEK-293T C351(1.03); C96(0.86)  LDD1661  [24]
 LDCM0459  CL67 HEK-293T C351(1.11); C96(0.94)  LDD1662  [24]
 LDCM0460  CL68 HEK-293T C351(1.09); C96(0.69)  LDD1663  [24]
 LDCM0461  CL69 HEK-293T C351(1.04); C96(1.08)  LDD1664  [24]
 LDCM0462  CL7 HEK-293T C351(1.16); C96(0.97)  LDD1665  [24]
 LDCM0463  CL70 HEK-293T C351(0.80); C96(0.95)  LDD1666  [24]
 LDCM0464  CL71 HEK-293T C351(1.03); C96(1.16)  LDD1667  [24]
 LDCM0465  CL72 HEK-293T C351(0.85); C96(0.89)  LDD1668  [24]
 LDCM0466  CL73 HEK-293T C351(0.89); C96(0.72)  LDD1669  [24]
 LDCM0467  CL74 HEK-293T C351(1.16); C96(1.06)  LDD1670  [24]
 LDCM0469  CL76 HEK-293T C351(0.96); C96(0.93)  LDD1672  [24]
 LDCM0470  CL77 HEK-293T C351(1.18); C96(0.87)  LDD1673  [24]
 LDCM0471  CL78 HEK-293T C351(1.02); C96(0.86)  LDD1674  [24]
 LDCM0472  CL79 HEK-293T C351(1.02); C96(1.03)  LDD1675  [24]
 LDCM0473  CL8 HEK-293T C351(0.95); C96(0.62)  LDD1676  [24]
 LDCM0474  CL80 HEK-293T C351(1.10); C96(0.83)  LDD1677  [24]
 LDCM0475  CL81 HEK-293T C351(1.12); C96(1.05)  LDD1678  [24]
 LDCM0476  CL82 HEK-293T C351(0.95); C96(0.97)  LDD1679  [24]
 LDCM0477  CL83 HEK-293T C351(1.01); C96(1.12)  LDD1680  [24]
 LDCM0478  CL84 HEK-293T C351(0.76); C96(0.92)  LDD1681  [24]
 LDCM0479  CL85 HEK-293T C351(0.96); C96(0.69)  LDD1682  [24]
 LDCM0480  CL86 HEK-293T C351(1.11); C96(0.88)  LDD1683  [24]
 LDCM0481  CL87 HEK-293T C351(1.09); C96(0.94)  LDD1684  [24]
 LDCM0482  CL88 HEK-293T C351(0.90); C96(1.02)  LDD1685  [24]
 LDCM0483  CL89 HEK-293T C351(1.06); C96(0.98)  LDD1686  [24]
 LDCM0484  CL9 HEK-293T C351(0.96); C96(1.06)  LDD1687  [24]
 LDCM0485  CL90 HEK-293T C351(0.99); C96(0.72)  LDD1688  [24]
 LDCM0486  CL91 HEK-293T C351(1.23); C96(1.05)  LDD1689  [24]
 LDCM0487  CL92 HEK-293T C351(0.97); C96(0.83)  LDD1690  [24]
 LDCM0488  CL93 HEK-293T C351(0.97); C96(1.03)  LDD1691  [24]
 LDCM0489  CL94 HEK-293T C351(0.92); C96(0.94)  LDD1692  [24]
 LDCM0490  CL95 HEK-293T C351(1.16); C96(0.90)  LDD1693  [24]
 LDCM0491  CL96 HEK-293T C351(0.79); C96(1.09)  LDD1694  [24]
 LDCM0492  CL97 HEK-293T C351(0.91); C96(0.84)  LDD1695  [24]
 LDCM0493  CL98 HEK-293T C351(1.12); C96(1.09)  LDD1696  [24]
 LDCM0494  CL99 HEK-293T C351(1.09); C96(1.00)  LDD1697  [24]
 LDCM0634  CY-0357 Hep-G2 C351(1.50); C351(0.65)  LDD2228  [12]
 LDCM0028  Dobutamine HEK-293T 9.24  LDD0180  [15]
 LDCM0027  Dopamine HEK-293T 25.77  LDD0179  [15]
 LDCM0495  E2913 HEK-293T C351(1.05); C96(1.05)  LDD1698  [24]
 LDCM0031  Epigallocatechin gallate HEK-293T 20.17  LDD0183  [15]
 LDCM0625  F8 Ramos C351(1.66)  LDD2187  [26]
 LDCM0572  Fragment10 Ramos C351(2.27)  LDD2189  [26]
 LDCM0573  Fragment11 Ramos C351(0.60); C96(1.06)  LDD2190  [26]
 LDCM0574  Fragment12 Ramos C351(0.85)  LDD2191  [26]
 LDCM0575  Fragment13 Ramos C351(1.17)  LDD2192  [26]
 LDCM0576  Fragment14 Ramos C351(0.93); C96(0.86)  LDD2193  [26]
 LDCM0579  Fragment20 Ramos C351(1.17)  LDD2194  [26]
 LDCM0580  Fragment21 Ramos C351(0.81)  LDD2195  [26]
 LDCM0582  Fragment23 Ramos C351(1.73)  LDD2196  [26]
 LDCM0578  Fragment27 Ramos C351(1.29)  LDD2197  [26]
 LDCM0586  Fragment28 Ramos C351(0.97); C96(1.24)  LDD2198  [26]
 LDCM0588  Fragment30 Ramos C351(1.51)  LDD2199  [26]
 LDCM0589  Fragment31 Ramos C351(1.22)  LDD2200  [26]
 LDCM0590  Fragment32 Ramos C351(2.00)  LDD2201  [26]
 LDCM0468  Fragment33 HEK-293T C351(1.07); C96(0.88)  LDD1671  [24]
 LDCM0596  Fragment38 Ramos C351(1.61)  LDD2203  [26]
 LDCM0566  Fragment4 Ramos C351(0.79); C96(0.60)  LDD2184  [26]
 LDCM0427  Fragment51 HEK-293T C351(1.02); C96(1.13)  LDD1631  [24]
 LDCM0610  Fragment52 Ramos C351(1.18)  LDD2204  [26]
 LDCM0614  Fragment56 Ramos C351(1.26)  LDD2205  [26]
 LDCM0569  Fragment7 Ramos C351(0.90); C96(0.62)  LDD2186  [26]
 LDCM0571  Fragment9 Ramos C351(1.27)  LDD2188  [26]
 LDCM0116  HHS-0101 DM93 Y183(0.81); Y311(1.22); Y175(1.68)  LDD0264  [10]
 LDCM0117  HHS-0201 DM93 Y183(0.49); Y311(1.51); Y175(3.66)  LDD0265  [10]
 LDCM0118  HHS-0301 DM93 Y183(0.39)  LDD0266  [10]
 LDCM0119  HHS-0401 DM93 Y183(0.81); Y175(0.89)  LDD0267  [10]
 LDCM0120  HHS-0701 DM93 Y183(0.56); Y175(1.44)  LDD0268  [10]
 LDCM0022  KB02 HEK-293T C96(1.12)  LDD1492  [24]
 LDCM0023  KB03 HEK-293T C96(1.05)  LDD1497  [24]
 LDCM0024  KB05 IGR37 C96(0.72)  LDD3314  [6]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C351(0.94)  LDD2121  [7]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C351(0.68)  LDD2150  [7]
 LDCM0627  NUDT7-COV-1 HEK-293T C351(0.88); C351(0.40)  LDD2206  [27]
 LDCM0032  Oleacein HEK-293T 11.17  LDD0184  [15]
 LDCM0628  OTUB2-COV-1 HEK-293T C351(0.90); C351(0.72)  LDD2207  [27]
 LDCM0131  RA190 MM1.R C96(1.33); C351(1.20)  LDD0304  [28]
 LDCM0090  Rapamycin JHH-7 4.02  LDD0213  [23]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Nitric oxide synthase 3 (NOS3) NOS family P29474
Ubiquitin carboxyl-terminal hydrolase isozyme L1 (UCHL1) Peptidase C12 family P09936
Leucine-rich repeat serine/threonine-protein kinase 2 (LRRK2) TKL Ser/Thr protein kinase family Q5S007
E3 ubiquitin-protein ligase TRIM23 (TRIM23) Arf family P36406
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Alpha-synuclein (SNCA) Synuclein family P37840
Other
Click To Hide/Show 7 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Gamma-aminobutyric acid receptor-associated protein-like 2 (GABARAPL2) ATG8 family P60520
Ataxin-1 (ATXN1) ATXN1 family P54253
Progranulin (GRN) Granulin family P28799
Glial fibrillary acidic protein (GFAP) Intermediate filament family P14136
Keratin-associated protein 10-9 (KRTAP10-9) KRTAP type 10 family P60411
Keratin-associated protein 3-2 (KRTAP3-2) KRTAP type 3 family Q9BYR7
Keratin-associated protein 9-2 (KRTAP9-2) KRTAP type 9 family Q9BYQ4

References

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2 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
3 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
4 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
5 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.
6 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
7 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
8 Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide. J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
9 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
10 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.
11 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
12 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
13 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
14 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
15 A chemical probe unravels the reactive proteome of health-associated catechols. Chem Sci. 2023 Jul 22;14(32):8635-8643. doi: 10.1039/d3sc00888f. eCollection 2023 Aug 16.
Mass spectrometry data entry: PXD043348
16 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
17 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
18 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.
19 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
20 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.
21 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
22 A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells. Cell. 2015 Jun 18;161(7):1668-80. doi: 10.1016/j.cell.2015.05.045.
23 Rapamycin targets STAT3 and impacts c-Myc to suppress tumor growth. Cell Chem Biol. 2022 Mar 17;29(3):373-385.e6. doi: 10.1016/j.chembiol.2021.10.006. Epub 2021 Oct 26.
24 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
25 Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications. ACS Chem Biol. 2019 Nov 15;14(11):2430-2440. doi: 10.1021/acschembio.8b01083. Epub 2019 May 13.
26 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
27 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
28 Physical and Functional Analysis of the Putative Rpn13 Inhibitor RA190. Cell Chem Biol. 2020 Nov 19;27(11):1371-1382.e6. doi: 10.1016/j.chembiol.2020.08.007. Epub 2020 Aug 27.