General Information of Target

Target ID LDTP03772
Target Name Basigin (BSG)
Gene Name BSG
Gene ID 682
Synonyms
Basigin; 5F7; Collagenase stimulatory factor; Extracellular matrix metalloproteinase inducer; EMMPRIN; Hepatoma-associated antigen; HAb18G; Leukocyte activation antigen M6; OK blood group antigen; Tumor cell-derived collagenase stimulatory factor; TCSF; CD antigen CD147
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAAALFVLLGFALLGTHGASGAAGFVQAPLSQQRWVGGSVELHCEAVGSPVPEIQWWFEG
QGPNDTCSQLWDGARLDRVHIHATYHQHAASTISIDTLVEEDTGTYECRASNDPDRNHLT
RAPRVKWVRAQAVVLVLEPGTVFTTVEDLGSKILLTCSLNDSATEVTGHRWLKGGVVLKE
DALPGQKTEFKVDSDDQWGEYSCVFLPEPMGTANIQLHGPPRVKAVKSSEHINEGETAML
VCKSESVPPVTDWAWYKITDSEDKALMNGSESRFFVSSSQGRSELHIENLNMEADPGQYR
CNGTSSKGSDQAIITLRVRSHLAALWPFLGIVAEVLVLVTIIFIYEKRRKPEDVLDDDDA
GSAPLKSSGQHQNDKGKNVRQRNSS
Target Type
Clinical trial
Target Bioclass
Immunoglobulin
Subcellular location
Melanosome; Cell membrane
Function
[Isoform 1]: Essential for normal retinal maturation and development. Acts as a retinal cell surface receptor for NXNL1 and plays an important role in NXNL1-mediated survival of retinal cone photoreceptors. In association with glucose transporter SLC16A1/GLUT1 and NXNL1, promotes retinal cone survival by enhancing aerobic glycolysis and accelerating the entry of glucose into photoreceptors. May act as a potent stimulator of IL6 secretion in multiple cell lines that include monocytes.; [Isoform 1]: (Microbial infection) Erythrocyte receptor for P.falciparum RH5 which is essential for erythrocyte invasion by the merozoite stage of P.falciparum isolates 3D7 and Dd2.; [Isoform 2]: Signaling receptor for cyclophilins, essential for PPIA/CYPA and PPIB/CYPB-dependent signaling related to chemotaxis and adhesion of immune cells. Plays an important role in targeting monocarboxylate transporters SLC16A1/GLUT1, SLC16A11 and SLC16A12 to the plasma membrane. Acts as a coreceptor for vascular endothelial growth factor receptor 2 (KDR/VEGFR2) in endothelial cells enhancing its VEGFA-mediated activation and downstream signaling. Promotes angiogenesis through EPAS1/HIF2A-mediated up-regulation of VEGFA (isoform VEGF-165 and VEGF-121) and KDR/VEGFR2 in endothelial cells. Plays a key role in regulating tumor growth, invasion, metastasis and neoangiogenesis by stimulating the production and release of extracellular matrix metalloproteinases and KDR/VEGFR2 by both tumor cells and stromal cells (fibroblasts and endothelial cells).; [Isoform 2]: (Microbial infection) Erythrocyte receptor for P.falciparum RH5 which is essential for erythrocyte invasion by the merozoite stage of P.falciparum isolates 3D7, Dd2, 7G8 and HB3. Binding of P.falciparum RH5 results in BSG dimerization which triggers an increase in intracellular Ca(2+) in the erythrocyte. This essential step leads to a rearrangement of the erythrocyte cytoskeleton required for the merozoite invasion.; [Isoform 2]: (Microbial infection) Can facilitate human SARS coronavirus (SARS-CoV-1) infection via its interaction with virus-associated PPIA/CYPA.; [Isoform 2]: (Microbial infection) Can facilitate HIV-1 infection via its interaction with virus-associated PPIA/CYPA.; [Isoform 2]: (Microbial infection) First described as a receptor for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), it is not required for SARS-CoV-2 infection.; [Isoform 2]: (Microbial infection) Acts as a receptor for measles virus.; [Isoform 2]: (Microbial infection) Promotes entry of pentamer-expressing human cytomegalovirus (HCMV) into epithelial and endothelial cells.
TTD ID
T35040
Uniprot ID
P35613
DrugMap ID
TTG21IS
Ensemble ID
ENST00000333511.9
HGNC ID
HGNC:1116
ChEMBL ID
CHEMBL3580492

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAL51 SNV: p.G369W DBIA    Probe Info 
HCT15 SNV: p.D359G .
KYSE410 SNV: p.G269S .
MEWO SNV: p.P207S .
MOLT4 SNV: p.S320N IA-alkyne    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 27 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
HDSF-alk
 Probe Info 
1.87  LDD0197  [2]
P8
 Probe Info 
10.00  LDD0451  [3]
FBPP2
 Probe Info 
35.79  LDD0318  [4]
FBP2
 Probe Info 
5.11  LDD0323  [4]
STPyne
 Probe Info 
K179(10.00); K375(8.68)  LDD0277  [5]
ONAyne
 Probe Info 
N.A.  LDD0273  [5]
IPM
 Probe Info 
N.A.  LDD0241  [6]
OPA-S-S-alkyne
 Probe Info 
K264(2.59)  LDD3494  [7]
P11
 Probe Info 
15.98  LDD0201  [8]
DBIA
 Probe Info 
C62(1.28)  LDD3310  [9]
5E-2FA
 Probe Info 
H286(0.00); H231(0.00); H371(0.00)  LDD2235  [10]
ATP probe
 Probe Info 
K179(0.00); K227(0.00); K375(0.00); K377(0.00)  LDD0199  [11]
m-APA
 Probe Info 
H286(0.00); H231(0.00); H371(0.00); H218(0.00)  LDD2231  [10]
4-Iodoacetamidophenylacetylene
 Probe Info 
C242(0.00); C203(0.00)  LDD0038  [12]
IA-alkyne
 Probe Info 
C203(0.00); C242(0.00)  LDD0032  [13]
Lodoacetamide azide
 Probe Info 
C242(0.00); C203(0.00)  LDD0037  [12]
ATP probe
 Probe Info 
N.A.  LDD0035  [14]
BTD
 Probe Info 
N.A.  LDD0004  [15]
NHS
 Probe Info 
K375(0.00); K187(0.00); K179(0.00)  LDD0010  [15]
PPMS
 Probe Info 
N.A.  LDD0008  [15]
VSF
 Probe Info 
N.A.  LDD0007  [15]
Ox-W18
 Probe Info 
N.A.  LDD2175  [16]
Acrolein
 Probe Info 
C242(0.00); H231(0.00); H286(0.00)  LDD0217  [17]
Crotonaldehyde
 Probe Info 
C242(0.00); H231(0.00)  LDD0219  [17]
Methacrolein
 Probe Info 
N.A.  LDD0218  [17]
AOyne
 Probe Info 
4.70  LDD0443  [18]
NAIA_5
 Probe Info 
N.A.  LDD2223  [19]
PAL-AfBPP Probe
Click To Hide/Show 75 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C003
 Probe Info 
15.35  LDD1713  [20]
C004
 Probe Info 
5.58  LDD1714  [20]
C022
 Probe Info 
10.20  LDD1728  [20]
C040
 Probe Info 
9.71  LDD1740  [20]
C052
 Probe Info 
4.92  LDD1750  [20]
C055
 Probe Info 
15.56  LDD1752  [20]
C056
 Probe Info 
25.99  LDD1753  [20]
C063
 Probe Info 
12.21  LDD1760  [20]
C070
 Probe Info 
10.85  LDD1766  [20]
C091
 Probe Info 
13.45  LDD1782  [20]
C092
 Probe Info 
18.38  LDD1783  [20]
C094
 Probe Info 
31.12  LDD1785  [20]
C106
 Probe Info 
32.22  LDD1793  [20]
C107
 Probe Info 
8.34  LDD1794  [20]
C108
 Probe Info 
9.25  LDD1795  [20]
C112
 Probe Info 
26.72  LDD1799  [20]
C134
 Probe Info 
26.54  LDD1816  [20]
C143
 Probe Info 
18.13  LDD1825  [20]
C153
 Probe Info 
25.63  LDD1834  [20]
C158
 Probe Info 
10.13  LDD1838  [20]
C160
 Probe Info 
6.96  LDD1840  [20]
C161
 Probe Info 
10.06  LDD1841  [20]
C169
 Probe Info 
21.11  LDD1849  [20]
C178
 Probe Info 
14.62  LDD1857  [20]
C194
 Probe Info 
8.51  LDD1870  [20]
C201
 Probe Info 
31.34  LDD1877  [20]
C218
 Probe Info 
14.52  LDD1892  [20]
C219
 Probe Info 
5.21  LDD1893  [20]
C220
 Probe Info 
22.32  LDD1894  [20]
C228
 Probe Info 
16.91  LDD1901  [20]
C231
 Probe Info 
20.53  LDD1904  [20]
C234
 Probe Info 
8.28  LDD1907  [20]
C235
 Probe Info 
16.91  LDD1908  [20]
C243
 Probe Info 
12.91  LDD1916  [20]
C246
 Probe Info 
18.13  LDD1919  [20]
C277
 Probe Info 
7.78  LDD1947  [20]
C287
 Probe Info 
9.25  LDD1957  [20]
C299
 Probe Info 
12.30  LDD1968  [20]
C305
 Probe Info 
9.58  LDD1974  [20]
C310
 Probe Info 
12.04  LDD1977  [20]
C314
 Probe Info 
15.35  LDD1981  [20]
C338
 Probe Info 
13.27  LDD2001  [20]
C339
 Probe Info 
8.28  LDD2002  [20]
C343
 Probe Info 
16.11  LDD2005  [20]
C347
 Probe Info 
4.99  LDD2008  [20]
C348
 Probe Info 
13.36  LDD2009  [20]
C350
 Probe Info 
57.28  LDD2011  [20]
C354
 Probe Info 
8.40  LDD2015  [20]
C362
 Probe Info 
36.76  LDD2023  [20]
C364
 Probe Info 
15.03  LDD2025  [20]
C373
 Probe Info 
9.99  LDD2033  [20]
C376
 Probe Info 
9.19  LDD2036  [20]
C388
 Probe Info 
48.84  LDD2047  [20]
C390
 Probe Info 
41.93  LDD2049  [20]
C391
 Probe Info 
13.36  LDD2050  [20]
C407
 Probe Info 
11.55  LDD2064  [20]
C413
 Probe Info 
12.38  LDD2069  [20]
C419
 Probe Info 
8.28  LDD2074  [20]
C426
 Probe Info 
14.83  LDD2081  [20]
C431
 Probe Info 
15.78  LDD2086  [20]
FFF probe11
 Probe Info 
20.00  LDD0471  [21]
FFF probe12
 Probe Info 
7.88  LDD0473  [21]
FFF probe13
 Probe Info 
20.00  LDD0475  [21]
FFF probe14
 Probe Info 
20.00  LDD0477  [21]
FFF probe15
 Probe Info 
5.55  LDD0478  [21]
FFF probe2
 Probe Info 
16.45  LDD0463  [21]
FFF probe3
 Probe Info 
20.00  LDD0464  [21]
FFF probe4
 Probe Info 
12.31  LDD0466  [21]
FFF probe9
 Probe Info 
20.00  LDD0470  [21]
JN0003
 Probe Info 
17.46  LDD0469  [21]
STS-2
 Probe Info 
1.14  LDD0138  [22]
VE-P
 Probe Info 
N.A.  LDD0396  [23]
A-DA
 Probe Info 
2.40  LDD0144  [24]
Diazir
 Probe Info 
N.A.  LDD0011  [15]
LD-F
 Probe Info 
E293(0.00); E288(0.00)  LDD0015  [25]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C242(1.06)  LDD2142  [26]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C242(1.02)  LDD2112  [26]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C242(1.05)  LDD2130  [26]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C242(1.22)  LDD2117  [26]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C242(1.80)  LDD2152  [26]
 LDCM0510  3-(4-(Hydroxydiphenylmethyl)piperidin-1-yl)-3-oxopropanenitrile MDA-MB-231 C242(0.90)  LDD2103  [26]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C242(0.84)  LDD2132  [26]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C242(0.95)  LDD2131  [26]
 LDCM0214  AC1 HEK-293T C301(1.26); C242(1.07)  LDD1507  [27]
 LDCM0215  AC10 HEK-293T C301(1.27); C242(1.00)  LDD1508  [27]
 LDCM0226  AC11 HEK-293T C301(1.22); C242(1.00)  LDD1509  [27]
 LDCM0237  AC12 HEK-293T C301(1.05); C242(1.18)  LDD1510  [27]
 LDCM0259  AC14 HEK-293T C301(1.20); C242(1.08)  LDD1512  [27]
 LDCM0270  AC15 HEK-293T C301(1.19); C242(0.94)  LDD1513  [27]
 LDCM0276  AC17 HEK-293T C301(1.28); C242(1.03)  LDD1515  [27]
 LDCM0277  AC18 HEK-293T C301(1.14); C242(1.01)  LDD1516  [27]
 LDCM0278  AC19 HEK-293T C301(1.53); C242(1.16)  LDD1517  [27]
 LDCM0279  AC2 HEK-293T C301(1.07); C242(1.02)  LDD1518  [27]
 LDCM0280  AC20 HEK-293T C301(1.06); C242(1.16)  LDD1519  [27]
 LDCM0281  AC21 HEK-293T C301(1.07); C242(0.99)  LDD1520  [27]
 LDCM0282  AC22 HEK-293T C301(1.12); C242(1.06)  LDD1521  [27]
 LDCM0283  AC23 HEK-293T C301(1.05); C242(0.98)  LDD1522  [27]
 LDCM0284  AC24 HEK-293T C301(0.88); C242(1.01)  LDD1523  [27]
 LDCM0285  AC25 HEK-293T C301(1.25); C242(1.09)  LDD1524  [27]
 LDCM0286  AC26 HEK-293T C301(1.16); C242(0.96)  LDD1525  [27]
 LDCM0287  AC27 HEK-293T C301(1.13); C242(1.00)  LDD1526  [27]
 LDCM0288  AC28 HEK-293T C301(1.03); C242(1.24)  LDD1527  [27]
 LDCM0289  AC29 HEK-293T C301(1.10); C242(1.04)  LDD1528  [27]
 LDCM0290  AC3 HEK-293T C301(1.19); C242(0.97)  LDD1529  [27]
 LDCM0291  AC30 HEK-293T C301(1.11); C242(0.99)  LDD1530  [27]
 LDCM0292  AC31 HEK-293T C301(1.02); C242(0.94)  LDD1531  [27]
 LDCM0293  AC32 HEK-293T C301(0.99); C242(0.99)  LDD1532  [27]
 LDCM0294  AC33 HEK-293T C301(1.44); C242(1.14)  LDD1533  [27]
 LDCM0295  AC34 HEK-293T C301(1.15); C242(1.00)  LDD1534  [27]
 LDCM0296  AC35 HEK-293T C301(1.33); C242(1.05)  LDD1535  [27]
 LDCM0297  AC36 HEK-293T C301(1.02); C242(1.51)  LDD1536  [27]
 LDCM0298  AC37 HEK-293T C301(1.00); C242(1.00)  LDD1537  [27]
 LDCM0299  AC38 HEK-293T C301(1.25); C242(0.99)  LDD1538  [27]
 LDCM0300  AC39 HEK-293T C301(1.27); C242(0.96)  LDD1539  [27]
 LDCM0301  AC4 HEK-293T C301(1.11); C242(1.06)  LDD1540  [27]
 LDCM0302  AC40 HEK-293T C301(1.13); C242(1.08)  LDD1541  [27]
 LDCM0303  AC41 HEK-293T C301(1.39); C242(1.07)  LDD1542  [27]
 LDCM0304  AC42 HEK-293T C301(1.26); C242(1.08)  LDD1543  [27]
 LDCM0305  AC43 HEK-293T C301(1.26); C242(1.04)  LDD1544  [27]
 LDCM0306  AC44 HEK-293T C301(1.07); C242(1.07)  LDD1545  [27]
 LDCM0307  AC45 HEK-293T C301(1.17); C242(1.10)  LDD1546  [27]
 LDCM0308  AC46 HEK-293T C301(1.21); C242(0.97)  LDD1547  [27]
 LDCM0309  AC47 HEK-293T C301(1.31); C242(1.01)  LDD1548  [27]
 LDCM0310  AC48 HEK-293T C301(1.06); C242(1.03)  LDD1549  [27]
 LDCM0311  AC49 HEK-293T C301(1.49); C242(1.01)  LDD1550  [27]
 LDCM0312  AC5 HEK-293T C301(1.05); C242(1.02)  LDD1551  [27]
 LDCM0313  AC50 HEK-293T C301(1.25); C242(1.04)  LDD1552  [27]
 LDCM0314  AC51 HEK-293T C301(1.19); C242(0.92)  LDD1553  [27]
 LDCM0315  AC52 HEK-293T C301(1.10); C242(1.07)  LDD1554  [27]
 LDCM0316  AC53 HEK-293T C301(1.08); C242(0.98)  LDD1555  [27]
 LDCM0317  AC54 HEK-293T C301(1.33); C242(0.97)  LDD1556  [27]
 LDCM0318  AC55 HEK-293T C301(1.30); C242(0.98)  LDD1557  [27]
 LDCM0319  AC56 HEK-293T C301(1.09); C242(0.94)  LDD1558  [27]
 LDCM0320  AC57 HEK-293T C301(1.38); C242(1.05)  LDD1559  [27]
 LDCM0321  AC58 HEK-293T C301(1.12); C242(0.94)  LDD1560  [27]
 LDCM0322  AC59 HEK-293T C301(1.16); C242(0.93)  LDD1561  [27]
 LDCM0323  AC6 HEK-293T C301(1.22); C242(0.99)  LDD1562  [27]
 LDCM0324  AC60 HEK-293T C301(1.03); C242(1.24)  LDD1563  [27]
 LDCM0325  AC61 HEK-293T C301(1.15); C242(1.04)  LDD1564  [27]
 LDCM0326  AC62 HEK-293T C301(1.24); C242(0.97)  LDD1565  [27]
 LDCM0327  AC63 HEK-293T C301(1.11); C242(1.06)  LDD1566  [27]
 LDCM0328  AC64 HEK-293T C301(1.04); C242(0.96)  LDD1567  [27]
 LDCM0334  AC7 HEK-293T C301(1.03); C242(0.89)  LDD1568  [27]
 LDCM0345  AC8 HEK-293T C301(1.12); C242(1.08)  LDD1569  [27]
 LDCM0545  Acetamide MDA-MB-231 C242(0.68)  LDD2138  [26]
 LDCM0520  AKOS000195272 MDA-MB-231 C242(0.87)  LDD2113  [26]
 LDCM0248  AKOS034007472 HEK-293T C301(1.06); C242(0.96)  LDD1511  [27]
 LDCM0356  AKOS034007680 HEK-293T C301(1.28); C242(1.11)  LDD1570  [27]
 LDCM0275  AKOS034007705 HEK-293T C301(1.16); C242(1.00)  LDD1514  [27]
 LDCM0498  BS-3668 MDA-MB-231 C242(0.80)  LDD2091  [26]
 LDCM0088  C45 HEK-293T 15.98  LDD0201  [8]
 LDCM0108  Chloroacetamide HeLa C242(0.00); C203(0.00); H231(0.00); H286(0.00)  LDD0222  [17]
 LDCM0367  CL1 HEK-293T C301(0.96); C242(1.02)  LDD1571  [27]
 LDCM0368  CL10 HEK-293T C301(1.57); C242(1.34)  LDD1572  [27]
 LDCM0369  CL100 HEK-293T C301(1.24); C242(1.07)  LDD1573  [27]
 LDCM0370  CL101 HEK-293T C301(1.23); C242(1.06)  LDD1574  [27]
 LDCM0371  CL102 HEK-293T C301(1.34); C242(1.05)  LDD1575  [27]
 LDCM0372  CL103 HEK-293T C301(1.31); C242(0.98)  LDD1576  [27]
 LDCM0373  CL104 HEK-293T C301(1.24); C242(0.97)  LDD1577  [27]
 LDCM0374  CL105 HEK-293T C301(1.17); C242(0.98)  LDD1578  [27]
 LDCM0375  CL106 HEK-293T C301(1.21); C242(1.01)  LDD1579  [27]
 LDCM0376  CL107 HEK-293T C301(1.21); C242(0.98)  LDD1580  [27]
 LDCM0377  CL108 HEK-293T C301(1.33); C242(0.98)  LDD1581  [27]
 LDCM0378  CL109 HEK-293T C301(1.16); C242(1.03)  LDD1582  [27]
 LDCM0379  CL11 HEK-293T C301(1.16); C242(1.10)  LDD1583  [27]
 LDCM0380  CL110 HEK-293T C301(1.34); C242(1.11)  LDD1584  [27]
 LDCM0381  CL111 HEK-293T C301(1.18); C242(1.05)  LDD1585  [27]
 LDCM0382  CL112 HEK-293T C301(1.38); C242(1.07)  LDD1586  [27]
 LDCM0383  CL113 HEK-293T C301(1.10); C242(1.09)  LDD1587  [27]
 LDCM0384  CL114 HEK-293T C301(1.50); C242(1.02)  LDD1588  [27]
 LDCM0385  CL115 HEK-293T C301(1.35); C242(1.03)  LDD1589  [27]
 LDCM0386  CL116 HEK-293T C301(1.23); C242(1.08)  LDD1590  [27]
 LDCM0387  CL117 HEK-293T C301(1.15); C242(1.03)  LDD1591  [27]
 LDCM0388  CL118 HEK-293T C301(1.37); C242(1.02)  LDD1592  [27]
 LDCM0389  CL119 HEK-293T C301(1.33); C242(1.02)  LDD1593  [27]
 LDCM0390  CL12 HEK-293T C301(1.15); C242(1.19)  LDD1594  [27]
 LDCM0391  CL120 HEK-293T C301(1.22); C242(1.11)  LDD1595  [27]
 LDCM0392  CL121 HEK-293T C301(1.21); C242(0.99)  LDD1596  [27]
 LDCM0393  CL122 HEK-293T C301(1.33); C242(0.92)  LDD1597  [27]
 LDCM0394  CL123 HEK-293T C301(1.18); C242(0.93)  LDD1598  [27]
 LDCM0395  CL124 HEK-293T C301(1.54); C242(0.94)  LDD1599  [27]
 LDCM0396  CL125 HEK-293T C301(1.24); C242(0.95)  LDD1600  [27]
 LDCM0397  CL126 HEK-293T C301(1.26); C242(0.87)  LDD1601  [27]
 LDCM0398  CL127 HEK-293T C301(1.24); C242(0.92)  LDD1602  [27]
 LDCM0399  CL128 HEK-293T C301(1.22); C242(0.95)  LDD1603  [27]
 LDCM0400  CL13 HEK-293T C301(1.21); C242(1.01)  LDD1604  [27]
 LDCM0401  CL14 HEK-293T C301(1.24); C242(0.95)  LDD1605  [27]
 LDCM0402  CL15 HEK-293T C301(1.23); C242(0.97)  LDD1606  [27]
 LDCM0403  CL16 HEK-293T C301(1.09); C242(1.04)  LDD1607  [27]
 LDCM0404  CL17 HEK-293T C301(1.30); C242(1.12)  LDD1608  [27]
 LDCM0405  CL18 HEK-293T C301(1.17); C242(1.00)  LDD1609  [27]
 LDCM0406  CL19 HEK-293T C301(1.27); C242(0.96)  LDD1610  [27]
 LDCM0407  CL2 HEK-293T C301(1.20); C242(0.97)  LDD1611  [27]
 LDCM0408  CL20 HEK-293T C301(1.18); C242(1.20)  LDD1612  [27]
 LDCM0409  CL21 HEK-293T C301(1.07); C242(1.09)  LDD1613  [27]
 LDCM0410  CL22 HEK-293T C301(1.32); C242(1.06)  LDD1614  [27]
 LDCM0411  CL23 HEK-293T C301(1.08); C242(1.05)  LDD1615  [27]
 LDCM0412  CL24 HEK-293T C301(1.10); C242(1.14)  LDD1616  [27]
 LDCM0413  CL25 HEK-293T C301(1.10); C242(0.99)  LDD1617  [27]
 LDCM0414  CL26 HEK-293T C301(1.10); C242(1.00)  LDD1618  [27]
 LDCM0415  CL27 HEK-293T C301(1.18); C242(1.01)  LDD1619  [27]
 LDCM0416  CL28 HEK-293T C301(1.27); C242(1.01)  LDD1620  [27]
 LDCM0417  CL29 HEK-293T C301(1.27); C242(1.10)  LDD1621  [27]
 LDCM0418  CL3 HEK-293T C301(1.03); C242(1.02)  LDD1622  [27]
 LDCM0419  CL30 HEK-293T C301(1.09); C242(0.96)  LDD1623  [27]
 LDCM0420  CL31 HEK-293T C301(1.23); C242(0.89)  LDD1624  [27]
 LDCM0421  CL32 HEK-293T C301(1.15); C242(1.01)  LDD1625  [27]
 LDCM0422  CL33 HEK-293T C301(1.19); C242(0.96)  LDD1626  [27]
 LDCM0423  CL34 HEK-293T C301(1.13); C242(1.04)  LDD1627  [27]
 LDCM0424  CL35 HEK-293T C301(1.11); C242(0.89)  LDD1628  [27]
 LDCM0425  CL36 HEK-293T C301(1.07); C242(1.13)  LDD1629  [27]
 LDCM0426  CL37 HEK-293T C301(0.94); C242(0.93)  LDD1630  [27]
 LDCM0428  CL39 HEK-293T C301(1.12); C242(1.00)  LDD1632  [27]
 LDCM0429  CL4 HEK-293T C301(1.10); C242(0.95)  LDD1633  [27]
 LDCM0430  CL40 HEK-293T C301(1.03); C242(1.04)  LDD1634  [27]
 LDCM0431  CL41 HEK-293T C301(1.17); C242(1.10)  LDD1635  [27]
 LDCM0432  CL42 HEK-293T C301(1.04); C242(0.85)  LDD1636  [27]
 LDCM0433  CL43 HEK-293T C301(1.01); C242(0.91)  LDD1637  [27]
 LDCM0434  CL44 HEK-293T C301(1.00); C242(1.27)  LDD1638  [27]
 LDCM0435  CL45 HEK-293T C301(1.20); C242(1.03)  LDD1639  [27]
 LDCM0436  CL46 HEK-293T C301(1.17); C242(1.04)  LDD1640  [27]
 LDCM0437  CL47 HEK-293T C301(1.10); C242(1.08)  LDD1641  [27]
 LDCM0438  CL48 HEK-293T C301(0.97); C242(1.03)  LDD1642  [27]
 LDCM0439  CL49 HEK-293T C301(1.21); C242(0.97)  LDD1643  [27]
 LDCM0440  CL5 HEK-293T C301(1.31); C242(1.03)  LDD1644  [27]
 LDCM0441  CL50 HEK-293T C301(1.42); C242(1.11)  LDD1645  [27]
 LDCM0443  CL52 HEK-293T C301(1.16); C242(1.10)  LDD1646  [27]
 LDCM0444  CL53 HEK-293T C301(1.51); C242(1.07)  LDD1647  [27]
 LDCM0445  CL54 HEK-293T C301(1.20); C242(0.85)  LDD1648  [27]
 LDCM0446  CL55 HEK-293T C301(1.33); C242(1.05)  LDD1649  [27]
 LDCM0447  CL56 HEK-293T C301(1.21); C242(0.97)  LDD1650  [27]
 LDCM0448  CL57 HEK-293T C301(1.21); C242(1.19)  LDD1651  [27]
 LDCM0449  CL58 HEK-293T C301(1.45); C242(1.01)  LDD1652  [27]
 LDCM0450  CL59 HEK-293T C301(1.29); C242(1.04)  LDD1653  [27]
 LDCM0451  CL6 HEK-293T C301(1.18); C242(0.86)  LDD1654  [27]
 LDCM0452  CL60 HEK-293T C301(1.05); C242(1.12)  LDD1655  [27]
 LDCM0453  CL61 HEK-293T C301(1.12); C242(1.00)  LDD1656  [27]
 LDCM0454  CL62 HEK-293T C301(1.19); C242(0.98)  LDD1657  [27]
 LDCM0455  CL63 HEK-293T C301(1.16); C242(0.98)  LDD1658  [27]
 LDCM0456  CL64 HEK-293T C301(1.26); C242(1.02)  LDD1659  [27]
 LDCM0457  CL65 HEK-293T C301(1.24); C242(1.17)  LDD1660  [27]
 LDCM0458  CL66 HEK-293T C301(1.15); C242(0.99)  LDD1661  [27]
 LDCM0459  CL67 HEK-293T C301(1.21); C242(0.94)  LDD1662  [27]
 LDCM0460  CL68 HEK-293T C301(1.03); C242(0.99)  LDD1663  [27]
 LDCM0461  CL69 HEK-293T C301(1.10); C242(0.96)  LDD1664  [27]
 LDCM0462  CL7 HEK-293T C301(1.18); C242(0.88)  LDD1665  [27]
 LDCM0463  CL70 HEK-293T C301(1.25); C242(1.10)  LDD1666  [27]
 LDCM0464  CL71 HEK-293T C301(1.26); C242(0.97)  LDD1667  [27]
 LDCM0465  CL72 HEK-293T C301(1.13); C242(1.07)  LDD1668  [27]
 LDCM0466  CL73 HEK-293T C301(1.11); C242(1.01)  LDD1669  [27]
 LDCM0467  CL74 HEK-293T C301(1.12); C242(0.96)  LDD1670  [27]
 LDCM0469  CL76 HEK-293T C301(1.25); C242(1.02)  LDD1672  [27]
 LDCM0470  CL77 HEK-293T C301(1.33); C242(1.01)  LDD1673  [27]
 LDCM0471  CL78 HEK-293T C301(1.17); C242(1.02)  LDD1674  [27]
 LDCM0472  CL79 HEK-293T C301(1.14); C242(0.90)  LDD1675  [27]
 LDCM0473  CL8 HEK-293T C301(1.19); C242(0.99)  LDD1676  [27]
 LDCM0474  CL80 HEK-293T C301(1.01); C242(0.95)  LDD1677  [27]
 LDCM0475  CL81 HEK-293T C301(1.15); C242(0.95)  LDD1678  [27]
 LDCM0476  CL82 HEK-293T C301(1.20); C242(1.01)  LDD1679  [27]
 LDCM0477  CL83 HEK-293T C301(1.13); C242(1.05)  LDD1680  [27]
 LDCM0478  CL84 HEK-293T C301(1.16); C242(0.98)  LDD1681  [27]
 LDCM0479  CL85 HEK-293T C301(1.10); C242(0.98)  LDD1682  [27]
 LDCM0480  CL86 HEK-293T C301(1.28); C242(0.82)  LDD1683  [27]
 LDCM0481  CL87 HEK-293T C301(1.26); C242(0.93)  LDD1684  [27]
 LDCM0482  CL88 HEK-293T C301(1.14); C242(0.89)  LDD1685  [27]
 LDCM0483  CL89 HEK-293T C301(1.36); C242(0.94)  LDD1686  [27]
 LDCM0484  CL9 HEK-293T C301(1.04); C242(1.08)  LDD1687  [27]
 LDCM0485  CL90 HEK-293T C301(1.26); C242(0.84)  LDD1688  [27]
 LDCM0486  CL91 HEK-293T C301(1.25); C242(0.82)  LDD1689  [27]
 LDCM0487  CL92 HEK-293T C301(1.05); C242(0.92)  LDD1690  [27]
 LDCM0488  CL93 HEK-293T C301(1.09); C242(0.98)  LDD1691  [27]
 LDCM0489  CL94 HEK-293T C301(1.31); C242(1.06)  LDD1692  [27]
 LDCM0490  CL95 HEK-293T C301(1.33); C242(1.10)  LDD1693  [27]
 LDCM0491  CL96 HEK-293T C301(1.18); C242(0.88)  LDD1694  [27]
 LDCM0492  CL97 HEK-293T C301(1.12); C242(0.97)  LDD1695  [27]
 LDCM0493  CL98 HEK-293T C301(1.16); C242(1.07)  LDD1696  [27]
 LDCM0494  CL99 HEK-293T C301(1.24); C242(1.02)  LDD1697  [27]
 LDCM0495  E2913 HEK-293T C301(1.25); C242(1.01)  LDD1698  [27]
 LDCM0625  F8 Ramos C242(0.77)  LDD2187  [28]
 LDCM0573  Fragment11 Ramos C242(8.98)  LDD2190  [28]
 LDCM0576  Fragment14 Ramos C242(1.72)  LDD2193  [28]
 LDCM0468  Fragment33 HEK-293T C301(1.21); C242(0.96)  LDD1671  [27]
 LDCM0566  Fragment4 Ramos C242(1.79)  LDD2184  [28]
 LDCM0427  Fragment51 HEK-293T C301(1.04); C242(0.99)  LDD1631  [27]
 LDCM0107  IAA HeLa C242(0.00); H231(0.00); H286(0.00)  LDD0221  [17]
 LDCM0022  KB02 HEK-293T C242(0.99); C301(0.80)  LDD1492  [27]
 LDCM0023  KB03 HEK-293T C242(0.96); C301(1.00)  LDD1497  [27]
 LDCM0024  KB05 COLO792 C62(1.28)  LDD3310  [9]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C242(0.58)  LDD2102  [26]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C242(0.88)  LDD2121  [26]
 LDCM0109  NEM HeLa C242(0.00); H231(0.00); H286(0.00)  LDD0223  [17]
 LDCM0496  Nucleophilic fragment 11a MDA-MB-231 C242(1.02)  LDD2089  [26]
 LDCM0497  Nucleophilic fragment 11b MDA-MB-231 C242(0.99)  LDD2090  [26]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C242(0.93)  LDD2092  [26]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C242(1.41)  LDD2093  [26]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C242(0.85)  LDD2094  [26]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C242(0.81)  LDD2097  [26]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C242(1.11)  LDD2098  [26]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C242(0.88)  LDD2101  [26]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C242(0.86)  LDD2104  [26]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C242(1.07)  LDD2105  [26]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C242(1.19)  LDD2107  [26]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C242(0.86)  LDD2108  [26]
 LDCM0516  Nucleophilic fragment 21a MDA-MB-231 C242(1.17)  LDD2109  [26]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C242(0.65)  LDD2114  [26]
 LDCM0522  Nucleophilic fragment 24a MDA-MB-231 C242(0.41)  LDD2115  [26]
 LDCM0526  Nucleophilic fragment 26a MDA-MB-231 C242(2.37)  LDD2119  [26]
 LDCM0527  Nucleophilic fragment 26b MDA-MB-231 C242(0.94)  LDD2120  [26]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C242(1.21)  LDD2123  [26]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C242(0.97)  LDD2125  [26]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C242(1.21)  LDD2127  [26]
 LDCM0535  Nucleophilic fragment 30b MDA-MB-231 C242(0.98)  LDD2128  [26]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C242(1.50)  LDD2129  [26]
 LDCM0541  Nucleophilic fragment 36 MDA-MB-231 C242(0.60)  LDD2134  [26]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C242(1.25)  LDD2135  [26]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C242(1.86)  LDD2136  [26]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C242(1.05)  LDD2137  [26]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C242(1.38)  LDD1700  [26]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C242(1.20)  LDD2140  [26]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C242(1.31)  LDD2141  [26]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C242(1.13)  LDD2143  [26]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C242(1.54)  LDD2145  [26]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C242(1.23)  LDD2146  [26]
 LDCM0554  Nucleophilic fragment 7a MDA-MB-231 C242(0.63)  LDD2148  [26]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C242(0.64)  LDD2150  [26]
 LDCM0559  Nucleophilic fragment 9b MDA-MB-231 C242(2.33)  LDD2153  [26]
 LDCM0084  Ro 48-8071 A-549 2.40  LDD0144  [24]

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
Peptidyl-prolyl cis-trans isomerase A (PPIA) Cyclophilin-type PPIase family P62937
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Monocarboxylate transporter 11 (SLC16A11) Monocarboxylate porter (TC 2.A.1.13) family Q8NCK7
Monocarboxylate transporter 13 (SLC16A13) Monocarboxylate porter (TC 2.A.1.13) family Q7RTY0
Aquaporin-6 (AQP6) MIP/aquaporin (TC 1.A.8) family Q13520
Other
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein Hook homolog 1 (HOOK1) Hook family Q9UJC3
Nicastrin (NCSTN) Nicastrin family Q92542

The Drug(s) Related To This Target

Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gavilimomab Antibody D03RDQ
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
[131i]-metuximab Antibody D0E5BW

References

1 Labeling Preferences of Diazirines with Protein Biomolecules. J Am Chem Soc. 2021 May 5;143(17):6691-6700. doi: 10.1021/jacs.1c02509. Epub 2021 Apr 20.
Mass spectrometry data entry: PXD025140
2 Fatty Acyl Sulfonyl Fluoride as an Activity-Based Probe for Profiling Fatty Acid-Associated Proteins in Living Cells. Chembiochem. 2022 Feb 16;23(4):e202100628. doi: 10.1002/cbic.202100628. Epub 2021 Dec 30.
3 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
4 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
5 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
6 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.
7 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
8 Discovery of Potent and Selective Inhibitors against Protein-Derived Electrophilic Cofactors. J Am Chem Soc. 2022 Mar 30;144(12):5377-5388. doi: 10.1021/jacs.1c12748. Epub 2022 Mar 2.
9 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
10 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
11 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
12 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
13 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
14 Comparison of Quantitative Mass Spectrometry Platforms for Monitoring Kinase ATP Probe Uptake in Lung Cancer. J Proteome Res. 2018 Jan 5;17(1):63-75. doi: 10.1021/acs.jproteome.7b00329. Epub 2017 Nov 22.
Mass spectrometry data entry: PXD006095 , PXD006096
15 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
16 Oxidative cyclization reagents reveal tryptophan cation- interactions. Nature. 2024 Mar;627(8004):680-687. doi: 10.1038/s41586-024-07140-6. Epub 2024 Mar 6.
Mass spectrometry data entry: PXD001377 , PXD005252
17 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.
18 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.
19 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
20 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
21 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.
22 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
23 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.
24 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.
25 Evaluation of fully-functionalized diazirine tags for chemical proteomic applications. Chem Sci. 2021 May 7;12(22):7839-7847. doi: 10.1039/d1sc01360b.
Mass spectrometry data entry: PXD025652
26 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
27 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
28 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