General Information of Target

Target ID LDTP06945
Target Name Sigma intracellular receptor 2 (TMEM97)
Gene Name TMEM97
Gene ID 27346
Synonyms
MAC30; S2R; Sigma intracellular receptor 2; S2R; Sigma-2 receptor; Sigma2 receptor; Meningioma-associated protein 30; MAC30; Transmembrane protein 97
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MGAPATRRCVEWLLGLYFLSHIPITLFMDLQAVLPRELYPVEFRNLLKWYAKEFKDPLLQ
EPPAWFKSFLFCELVFQLPFFPIATYAFLKGSCKWIRTPAIIYSVHTMTTLIPILSTFLF
EDFSKASGFKGQRPETLHERLTLVSVYAPYLLIPFILLIFMLRSPYYKYEEKRKKK
Target Type
Clinical trial
Target Bioclass
Transporter and channel
Family
TMEM97/sigma-2 receptor family
Subcellular location
Nucleus membrane
Function
Sigma-2 receptor which contributes to ameliorate dysfunctional cellular processes and slow degenerative progression by regulating cell functions including cholesterol biosynthesis/trafficking, membrane trafficking, autophagy, lipid membrane-bound protein trafficking, and receptor stabilization at the cell surface (Probable). Forms a ternary complex with PGRMC1 receptor and low density lipoprotein receptor/LDLR at the plasma membrane, which increases LDLR-mediated LDL cholesterol internalization. Decreases lysosomal sterol transporter NPC1 availability to the cell, probably through NPC1-binding, hence controlling lipid transport, including cholesterol and LBPA, outside of late endosome/lysosome. Binds regio- and stereoselective ligand 20(S)-hydroxycholesterol (20(S)-OHC) which enhances TMEM97-NPC1 interaction and decreases TMEM97-PGRMC1 and TMEM97-TSPO interactions, thereby linking OHC binding to cholesterol homeostasis. Also able to bind cholesterol. Binds histatin 1 (Hst 1)/HN1 salivary peptide at the ER membrane, which is critical for increasing mitochondria-ER contacts and stimulating Hst1 wound healing properties. May alter the activity of some cytochrome P450 proteins. Although shows homologies with sterol isomerases (EXPERA domain), not able to catalyze sterol isomerization (Probable). However, may act as sensors of these molecules (Probable). Acts as a quality control factor in the ER, promoting the proteolytic degradation of nonproductive and extramitochondrial precursor proteins in the ER membrane thus removing them from the ER surface.
TTD ID
T45674
Uniprot ID
Q5BJF2
DrugMap ID
TTIS0R2
Ensemble ID
ENST00000226230.8
HGNC ID
HGNC:28106
ChEMBL ID
CHEMBL4105907

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 14 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info 
100.00  LDD0444  [1]
YN-4
 Probe Info 
100.00  LDD0445  [1]
STPyne
 Probe Info 
K48(7.17)  LDD0277  [2]
OPA-S-S-alkyne
 Probe Info 
K130(3.33)  LDD3494  [3]
FBPP2
 Probe Info 
2.86  LDD0054  [4]
Jackson_1
 Probe Info 
2.04  LDD0120  [5]
HPAP
 Probe Info 
5.03  LDD0062  [6]
Alkyne-RA190
 Probe Info 
9.91  LDD0299  [7]
DBIA
 Probe Info 
C72(0.99)  LDD1507  [8]
ATP probe
 Probe Info 
N.A.  LDD0035  [9]
Acrolein
 Probe Info 
N.A.  LDD0217  [10]
Crotonaldehyde
 Probe Info 
N.A.  LDD0219  [10]
W1
 Probe Info 
E135(0.00); E139(0.00); Q132(0.00); H138(0.00)  LDD0236  [11]
AOyne
 Probe Info 
15.00  LDD0443  [12]
PAL-AfBPP Probe
Click To Hide/Show 146 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C007
 Probe Info 
9.06  LDD1716  [13]
C008
 Probe Info 
9.92  LDD1717  [13]
C010
 Probe Info 
14.03  LDD1719  [13]
C011
 Probe Info 
10.20  LDD1720  [13]
C012
 Probe Info 
5.74  LDD1721  [13]
C018
 Probe Info 
10.78  LDD1726  [13]
C022
 Probe Info 
12.73  LDD1728  [13]
C026
 Probe Info 
12.55  LDD1732  [13]
C040
 Probe Info 
20.82  LDD1740  [13]
C041
 Probe Info 
13.74  LDD1741  [13]
C044
 Probe Info 
8.34  LDD1743  [13]
C049
 Probe Info 
5.43  LDD1747  [13]
C055
 Probe Info 
14.83  LDD1752  [13]
C059
 Probe Info 
6.28  LDD1756  [13]
C060
 Probe Info 
6.32  LDD1757  [13]
C063
 Probe Info 
21.56  LDD1760  [13]
C064
 Probe Info 
12.82  LDD1761  [13]
C065
 Probe Info 
5.98  LDD1762  [13]
C067
 Probe Info 
8.06  LDD1763  [13]
C068
 Probe Info 
5.21  LDD1764  [13]
C070
 Probe Info 
11.55  LDD1766  [13]
C071
 Probe Info 
8.88  LDD1767  [13]
C072
 Probe Info 
12.91  LDD1768  [13]
C075
 Probe Info 
5.03  LDD1770  [13]
C082
 Probe Info 
11.63  LDD1774  [13]
C085
 Probe Info 
8.82  LDD1777  [13]
C087
 Probe Info 
9.99  LDD1779  [13]
C107
 Probe Info 
13.93  LDD1794  [13]
C108
 Probe Info 
8.11  LDD1795  [13]
C110
 Probe Info 
13.00  LDD1797  [13]
C111
 Probe Info 
5.13  LDD1798  [13]
C112
 Probe Info 
20.53  LDD1799  [13]
C130
 Probe Info 
9.38  LDD1812  [13]
C135
 Probe Info 
17.51  LDD1817  [13]
C139
 Probe Info 
13.00  LDD1821  [13]
C140
 Probe Info 
11.00  LDD1822  [13]
C141
 Probe Info 
20.97  LDD1823  [13]
C143
 Probe Info 
27.28  LDD1825  [13]
C145
 Probe Info 
18.77  LDD1827  [13]
C147
 Probe Info 
17.15  LDD1829  [13]
C152
 Probe Info 
5.74  LDD1833  [13]
C156
 Probe Info 
8.28  LDD1836  [13]
C159
 Probe Info 
17.39  LDD1839  [13]
C160
 Probe Info 
22.32  LDD1840  [13]
C161
 Probe Info 
21.11  LDD1841  [13]
C163
 Probe Info 
12.73  LDD1843  [13]
C166
 Probe Info 
8.22  LDD1846  [13]
C169
 Probe Info 
20.53  LDD1849  [13]
C171
 Probe Info 
5.66  LDD1851  [13]
C174
 Probe Info 
9.85  LDD1854  [13]
C176
 Probe Info 
5.43  LDD1855  [13]
C177
 Probe Info 
21.26  LDD1856  [13]
C178
 Probe Info 
15.35  LDD1857  [13]
C182
 Probe Info 
6.82  LDD1860  [13]
C183
 Probe Info 
9.32  LDD1861  [13]
C187
 Probe Info 
22.01  LDD1865  [13]
C193
 Probe Info 
11.71  LDD1869  [13]
C194
 Probe Info 
20.82  LDD1870  [13]
C197
 Probe Info 
8.88  LDD1873  [13]
C198
 Probe Info 
11.55  LDD1874  [13]
C201
 Probe Info 
26.72  LDD1877  [13]
C204
 Probe Info 
6.06  LDD1879  [13]
C205
 Probe Info 
7.52  LDD1880  [13]
C206
 Probe Info 
19.03  LDD1881  [13]
C217
 Probe Info 
10.56  LDD1891  [13]
C218
 Probe Info 
23.26  LDD1892  [13]
C220
 Probe Info 
13.74  LDD1894  [13]
C222
 Probe Info 
8.63  LDD1896  [13]
C225
 Probe Info 
12.21  LDD1898  [13]
C226
 Probe Info 
23.59  LDD1899  [13]
C229
 Probe Info 
12.38  LDD1902  [13]
C231
 Probe Info 
11.63  LDD1904  [13]
C233
 Probe Info 
20.53  LDD1906  [13]
C234
 Probe Info 
7.21  LDD1907  [13]
C235
 Probe Info 
19.97  LDD1908  [13]
C240
 Probe Info 
8.75  LDD1913  [13]
C242
 Probe Info 
5.28  LDD1915  [13]
C243
 Probe Info 
17.75  LDD1916  [13]
C244
 Probe Info 
15.45  LDD1917  [13]
C245
 Probe Info 
13.27  LDD1918  [13]
C246
 Probe Info 
14.12  LDD1919  [13]
C249
 Probe Info 
12.38  LDD1922  [13]
C258
 Probe Info 
8.17  LDD1931  [13]
C260
 Probe Info 
5.86  LDD1932  [13]
C264
 Probe Info 
23.92  LDD1935  [13]
C273
 Probe Info 
10.78  LDD1943  [13]
C280
 Probe Info 
32.45  LDD1950  [13]
C282
 Probe Info 
22.47  LDD1952  [13]
C287
 Probe Info 
14.03  LDD1957  [13]
C288
 Probe Info 
11.39  LDD1958  [13]
C290
 Probe Info 
12.04  LDD1960  [13]
C296
 Probe Info 
18.00  LDD1966  [13]
C297
 Probe Info 
5.10  LDD1967  [13]
C299
 Probe Info 
12.64  LDD1968  [13]
C300
 Probe Info 
4.99  LDD1969  [13]
C301
 Probe Info 
5.24  LDD1970  [13]
C307
 Probe Info 
5.24  LDD1975  [13]
C314
 Probe Info 
26.17  LDD1981  [13]
C322
 Probe Info 
14.72  LDD1988  [13]
C326
 Probe Info 
10.85  LDD1990  [13]
C327
 Probe Info 
6.50  LDD1991  [13]
C328
 Probe Info 
7.16  LDD1992  [13]
C339
 Probe Info 
11.63  LDD2002  [13]
C342
 Probe Info 
10.20  LDD2004  [13]
C346
 Probe Info 
24.59  LDD2007  [13]
C348
 Probe Info 
22.78  LDD2009  [13]
C349
 Probe Info 
22.32  LDD2010  [13]
C350
 Probe Info 
30.91  LDD2011  [13]
C355
 Probe Info 
29.65  LDD2016  [13]
C356
 Probe Info 
18.38  LDD2017  [13]
C357
 Probe Info 
7.78  LDD2018  [13]
C363
 Probe Info 
22.47  LDD2024  [13]
C366
 Probe Info 
15.45  LDD2027  [13]
C373
 Probe Info 
13.45  LDD2033  [13]
C374
 Probe Info 
5.62  LDD2034  [13]
C378
 Probe Info 
7.41  LDD2037  [13]
C380
 Probe Info 
5.78  LDD2039  [13]
C382
 Probe Info 
13.09  LDD2041  [13]
C383
 Probe Info 
18.77  LDD2042  [13]
C385
 Probe Info 
5.70  LDD2044  [13]
C386
 Probe Info 
11.96  LDD2045  [13]
C390
 Probe Info 
27.47  LDD2049  [13]
C391
 Probe Info 
16.80  LDD2050  [13]
C393
 Probe Info 
14.83  LDD2052  [13]
C396
 Probe Info 
5.31  LDD2055  [13]
C399
 Probe Info 
12.82  LDD2058  [13]
C403
 Probe Info 
15.56  LDD2061  [13]
C405
 Probe Info 
9.51  LDD2063  [13]
C407
 Probe Info 
16.68  LDD2064  [13]
C408
 Probe Info 
11.39  LDD2065  [13]
C413
 Probe Info 
20.68  LDD2069  [13]
C419
 Probe Info 
26.35  LDD2074  [13]
C420
 Probe Info 
24.42  LDD2075  [13]
C422
 Probe Info 
14.42  LDD2077  [13]
C423
 Probe Info 
22.47  LDD2078  [13]
C424
 Probe Info 
11.00  LDD2079  [13]
C426
 Probe Info 
32.00  LDD2081  [13]
C428
 Probe Info 
11.00  LDD2083  [13]
FFF probe11
 Probe Info 
16.08  LDD0486  [14]
FFF probe13
 Probe Info 
20.00  LDD0488  [14]
FFF probe14
 Probe Info 
20.00  LDD0477  [14]
FFF probe2
 Probe Info 
20.00  LDD0463  [14]
FFF probe3
 Probe Info 
20.00  LDD0464  [14]
JN0003
 Probe Info 
19.75  LDD0484  [14]
A-DA
 Probe Info 
20.00  LDD0144  [15]
OEA-DA
 Probe Info 
20.00  LDD0046  [16]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0214  AC1 HEK-293T C72(0.99)  LDD1507  [8]
 LDCM0215  AC10 HEK-293T C72(0.83); C93(1.07)  LDD1508  [8]
 LDCM0226  AC11 HEK-293T C72(0.72)  LDD1509  [8]
 LDCM0237  AC12 HEK-293T C72(0.91)  LDD1510  [8]
 LDCM0259  AC14 HEK-293T C72(0.94)  LDD1512  [8]
 LDCM0270  AC15 HEK-293T C72(0.95)  LDD1513  [8]
 LDCM0276  AC17 HEK-293T C72(0.94)  LDD1515  [8]
 LDCM0277  AC18 HEK-293T C72(0.78); C93(0.99)  LDD1516  [8]
 LDCM0278  AC19 HEK-293T C72(0.68)  LDD1517  [8]
 LDCM0279  AC2 HEK-293T C72(0.73); C93(0.93)  LDD1518  [8]
 LDCM0280  AC20 HEK-293T C72(0.92)  LDD1519  [8]
 LDCM0281  AC21 HEK-293T C72(0.79)  LDD1520  [8]
 LDCM0282  AC22 HEK-293T C72(0.96)  LDD1521  [8]
 LDCM0283  AC23 HEK-293T C72(0.99)  LDD1522  [8]
 LDCM0284  AC24 HEK-293T C72(1.03)  LDD1523  [8]
 LDCM0285  AC25 HEK-293T C72(0.93)  LDD1524  [8]
 LDCM0286  AC26 HEK-293T C72(0.68); C93(0.91)  LDD1525  [8]
 LDCM0287  AC27 HEK-293T C72(0.70)  LDD1526  [8]
 LDCM0288  AC28 HEK-293T C72(0.91)  LDD1527  [8]
 LDCM0289  AC29 HEK-293T C72(0.75)  LDD1528  [8]
 LDCM0290  AC3 HEK-293T C72(0.64)  LDD1529  [8]
 LDCM0291  AC30 HEK-293T C72(0.93)  LDD1530  [8]
 LDCM0292  AC31 HEK-293T C72(0.89)  LDD1531  [8]
 LDCM0293  AC32 HEK-293T C72(1.03)  LDD1532  [8]
 LDCM0294  AC33 HEK-293T C72(1.02)  LDD1533  [8]
 LDCM0295  AC34 HEK-293T C72(0.79); C93(1.12)  LDD1534  [8]
 LDCM0296  AC35 HEK-293T C72(0.68)  LDD1535  [8]
 LDCM0297  AC36 HEK-293T C72(0.95)  LDD1536  [8]
 LDCM0298  AC37 HEK-293T C72(0.78)  LDD1537  [8]
 LDCM0299  AC38 HEK-293T C72(1.03)  LDD1538  [8]
 LDCM0300  AC39 HEK-293T C72(0.99)  LDD1539  [8]
 LDCM0301  AC4 HEK-293T C72(0.96)  LDD1540  [8]
 LDCM0302  AC40 HEK-293T C72(1.09)  LDD1541  [8]
 LDCM0303  AC41 HEK-293T C72(0.92)  LDD1542  [8]
 LDCM0304  AC42 HEK-293T C72(0.69); C93(1.04)  LDD1543  [8]
 LDCM0305  AC43 HEK-293T C72(0.68)  LDD1544  [8]
 LDCM0306  AC44 HEK-293T C72(0.94)  LDD1545  [8]
 LDCM0307  AC45 HEK-293T C72(0.80)  LDD1546  [8]
 LDCM0308  AC46 HEK-293T C72(0.99)  LDD1547  [8]
 LDCM0309  AC47 HEK-293T C72(1.02)  LDD1548  [8]
 LDCM0310  AC48 HEK-293T C72(1.01)  LDD1549  [8]
 LDCM0311  AC49 HEK-293T C72(1.02)  LDD1550  [8]
 LDCM0312  AC5 HEK-293T C72(0.80)  LDD1551  [8]
 LDCM0313  AC50 HEK-293T C72(0.80); C93(1.00)  LDD1552  [8]
 LDCM0314  AC51 HEK-293T C72(0.65)  LDD1553  [8]
 LDCM0315  AC52 HEK-293T C72(0.95)  LDD1554  [8]
 LDCM0316  AC53 HEK-293T C72(0.81)  LDD1555  [8]
 LDCM0317  AC54 HEK-293T C72(0.96)  LDD1556  [8]
 LDCM0318  AC55 HEK-293T C72(0.96)  LDD1557  [8]
 LDCM0319  AC56 HEK-293T C72(1.04)  LDD1558  [8]
 LDCM0320  AC57 HEK-293T C72(1.03)  LDD1559  [8]
 LDCM0321  AC58 HEK-293T C72(0.90); C93(0.89)  LDD1560  [8]
 LDCM0322  AC59 HEK-293T C72(0.89)  LDD1561  [8]
 LDCM0323  AC6 HEK-293T C72(0.96)  LDD1562  [8]
 LDCM0324  AC60 HEK-293T C72(1.06)  LDD1563  [8]
 LDCM0325  AC61 HEK-293T C72(0.93)  LDD1564  [8]
 LDCM0326  AC62 HEK-293T C72(0.93)  LDD1565  [8]
 LDCM0327  AC63 HEK-293T C72(1.01)  LDD1566  [8]
 LDCM0328  AC64 HEK-293T C72(0.97)  LDD1567  [8]
 LDCM0334  AC7 HEK-293T C72(0.88)  LDD1568  [8]
 LDCM0345  AC8 HEK-293T C72(1.09)  LDD1569  [8]
 LDCM0248  AKOS034007472 HEK-293T C72(0.72)  LDD1511  [8]
 LDCM0356  AKOS034007680 HEK-293T C72(0.99)  LDD1570  [8]
 LDCM0275  AKOS034007705 HEK-293T C72(1.13)  LDD1514  [8]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [10]
 LDCM0070  Cisar_cp37 MDA-MB-231 2.04  LDD0120  [5]
 LDCM0367  CL1 HEK-293T C72(1.21)  LDD1571  [8]
 LDCM0368  CL10 HEK-293T C72(1.91)  LDD1572  [8]
 LDCM0369  CL100 HEK-293T C72(1.17)  LDD1573  [8]
 LDCM0370  CL101 HEK-293T C72(1.09)  LDD1574  [8]
 LDCM0371  CL102 HEK-293T C72(1.12)  LDD1575  [8]
 LDCM0372  CL103 HEK-293T C72(0.93)  LDD1576  [8]
 LDCM0373  CL104 HEK-293T C72(0.99)  LDD1577  [8]
 LDCM0374  CL105 HEK-293T C72(0.90)  LDD1578  [8]
 LDCM0375  CL106 HEK-293T C72(0.99)  LDD1579  [8]
 LDCM0376  CL107 HEK-293T C72(1.01)  LDD1580  [8]
 LDCM0377  CL108 HEK-293T C72(0.95)  LDD1581  [8]
 LDCM0378  CL109 HEK-293T C72(1.13)  LDD1582  [8]
 LDCM0379  CL11 HEK-293T C72(1.34)  LDD1583  [8]
 LDCM0380  CL110 HEK-293T C72(1.09)  LDD1584  [8]
 LDCM0381  CL111 HEK-293T C72(0.96)  LDD1585  [8]
 LDCM0382  CL112 HEK-293T C72(0.87)  LDD1586  [8]
 LDCM0383  CL113 HEK-293T C72(1.07)  LDD1587  [8]
 LDCM0384  CL114 HEK-293T C72(1.10)  LDD1588  [8]
 LDCM0385  CL115 HEK-293T C72(0.87)  LDD1589  [8]
 LDCM0386  CL116 HEK-293T C72(1.04)  LDD1590  [8]
 LDCM0387  CL117 HEK-293T C72(0.92)  LDD1591  [8]
 LDCM0388  CL118 HEK-293T C72(0.93)  LDD1592  [8]
 LDCM0389  CL119 HEK-293T C72(0.84)  LDD1593  [8]
 LDCM0390  CL12 HEK-293T C72(1.53)  LDD1594  [8]
 LDCM0391  CL120 HEK-293T C72(1.01)  LDD1595  [8]
 LDCM0392  CL121 HEK-293T C72(1.01)  LDD1596  [8]
 LDCM0393  CL122 HEK-293T C72(1.12)  LDD1597  [8]
 LDCM0394  CL123 HEK-293T C72(1.26)  LDD1598  [8]
 LDCM0395  CL124 HEK-293T C72(1.08)  LDD1599  [8]
 LDCM0396  CL125 HEK-293T C72(1.02)  LDD1600  [8]
 LDCM0397  CL126 HEK-293T C72(1.12)  LDD1601  [8]
 LDCM0398  CL127 HEK-293T C72(0.98)  LDD1602  [8]
 LDCM0399  CL128 HEK-293T C72(1.05)  LDD1603  [8]
 LDCM0400  CL13 HEK-293T C72(1.15)  LDD1604  [8]
 LDCM0401  CL14 HEK-293T C72(0.99)  LDD1605  [8]
 LDCM0402  CL15 HEK-293T C72(1.32)  LDD1606  [8]
 LDCM0403  CL16 HEK-293T C72(1.03)  LDD1607  [8]
 LDCM0404  CL17 HEK-293T C72(1.46)  LDD1608  [8]
 LDCM0405  CL18 HEK-293T C72(0.84); C93(1.02)  LDD1609  [8]
 LDCM0406  CL19 HEK-293T C72(0.76)  LDD1610  [8]
 LDCM0407  CL2 HEK-293T C72(1.05)  LDD1611  [8]
 LDCM0408  CL20 HEK-293T C72(1.16)  LDD1612  [8]
 LDCM0409  CL21 HEK-293T C72(1.24)  LDD1613  [8]
 LDCM0410  CL22 HEK-293T C72(1.17)  LDD1614  [8]
 LDCM0411  CL23 HEK-293T C72(1.15)  LDD1615  [8]
 LDCM0412  CL24 HEK-293T C72(1.45)  LDD1616  [8]
 LDCM0413  CL25 HEK-293T C72(1.44)  LDD1617  [8]
 LDCM0414  CL26 HEK-293T C72(0.91)  LDD1618  [8]
 LDCM0415  CL27 HEK-293T C72(0.93)  LDD1619  [8]
 LDCM0416  CL28 HEK-293T C72(1.06)  LDD1620  [8]
 LDCM0417  CL29 HEK-293T C72(1.04)  LDD1621  [8]
 LDCM0418  CL3 HEK-293T C72(1.22)  LDD1622  [8]
 LDCM0419  CL30 HEK-293T C72(0.89); C93(0.90)  LDD1623  [8]
 LDCM0420  CL31 HEK-293T C72(0.71)  LDD1624  [8]
 LDCM0421  CL32 HEK-293T C72(1.03)  LDD1625  [8]
 LDCM0422  CL33 HEK-293T C72(1.67)  LDD1626  [8]
 LDCM0423  CL34 HEK-293T C72(1.20)  LDD1627  [8]
 LDCM0424  CL35 HEK-293T C72(1.15)  LDD1628  [8]
 LDCM0425  CL36 HEK-293T C72(1.48)  LDD1629  [8]
 LDCM0426  CL37 HEK-293T C72(1.42)  LDD1630  [8]
 LDCM0428  CL39 HEK-293T C72(1.11)  LDD1632  [8]
 LDCM0429  CL4 HEK-293T C72(1.16)  LDD1633  [8]
 LDCM0430  CL40 HEK-293T C72(1.00)  LDD1634  [8]
 LDCM0431  CL41 HEK-293T C72(1.12)  LDD1635  [8]
 LDCM0432  CL42 HEK-293T C72(0.80); C93(0.97)  LDD1636  [8]
 LDCM0433  CL43 HEK-293T C72(0.75)  LDD1637  [8]
 LDCM0434  CL44 HEK-293T C72(0.96)  LDD1638  [8]
 LDCM0435  CL45 HEK-293T C72(0.99)  LDD1639  [8]
 LDCM0436  CL46 HEK-293T C72(1.04)  LDD1640  [8]
 LDCM0437  CL47 HEK-293T C72(1.11)  LDD1641  [8]
 LDCM0438  CL48 HEK-293T C72(1.41)  LDD1642  [8]
 LDCM0439  CL49 HEK-293T C72(1.51)  LDD1643  [8]
 LDCM0440  CL5 HEK-293T C72(1.20)  LDD1644  [8]
 LDCM0441  CL50 HEK-293T C72(1.05)  LDD1645  [8]
 LDCM0443  CL52 HEK-293T C72(1.13)  LDD1646  [8]
 LDCM0444  CL53 HEK-293T C72(1.26)  LDD1647  [8]
 LDCM0445  CL54 HEK-293T C72(1.34); C93(3.01)  LDD1648  [8]
 LDCM0446  CL55 HEK-293T C72(0.80)  LDD1649  [8]
 LDCM0447  CL56 HEK-293T C72(1.10)  LDD1650  [8]
 LDCM0448  CL57 HEK-293T C72(1.25)  LDD1651  [8]
 LDCM0449  CL58 HEK-293T C72(1.20)  LDD1652  [8]
 LDCM0450  CL59 HEK-293T C72(1.19)  LDD1653  [8]
 LDCM0451  CL6 HEK-293T C72(1.11); C93(1.66)  LDD1654  [8]
 LDCM0452  CL60 HEK-293T C72(1.52)  LDD1655  [8]
 LDCM0453  CL61 HEK-293T C72(1.12)  LDD1656  [8]
 LDCM0454  CL62 HEK-293T C72(0.88)  LDD1657  [8]
 LDCM0455  CL63 HEK-293T C72(0.91)  LDD1658  [8]
 LDCM0456  CL64 HEK-293T C72(1.21)  LDD1659  [8]
 LDCM0457  CL65 HEK-293T C72(1.04)  LDD1660  [8]
 LDCM0458  CL66 HEK-293T C72(0.80); C93(1.02)  LDD1661  [8]
 LDCM0459  CL67 HEK-293T C72(0.74)  LDD1662  [8]
 LDCM0460  CL68 HEK-293T C72(1.14)  LDD1663  [8]
 LDCM0461  CL69 HEK-293T C72(1.01)  LDD1664  [8]
 LDCM0462  CL7 HEK-293T C72(0.76)  LDD1665  [8]
 LDCM0463  CL70 HEK-293T C72(1.24)  LDD1666  [8]
 LDCM0464  CL71 HEK-293T C72(1.08)  LDD1667  [8]
 LDCM0465  CL72 HEK-293T C72(1.30)  LDD1668  [8]
 LDCM0466  CL73 HEK-293T C72(1.27)  LDD1669  [8]
 LDCM0467  CL74 HEK-293T C72(0.95)  LDD1670  [8]
 LDCM0469  CL76 HEK-293T C72(0.95)  LDD1672  [8]
 LDCM0470  CL77 HEK-293T C72(1.32)  LDD1673  [8]
 LDCM0471  CL78 HEK-293T C72(0.78); C93(0.99)  LDD1674  [8]
 LDCM0472  CL79 HEK-293T C72(0.73)  LDD1675  [8]
 LDCM0473  CL8 HEK-293T C72(4.56)  LDD1676  [8]
 LDCM0474  CL80 HEK-293T C72(1.02)  LDD1677  [8]
 LDCM0475  CL81 HEK-293T C72(0.86)  LDD1678  [8]
 LDCM0476  CL82 HEK-293T C72(1.06)  LDD1679  [8]
 LDCM0477  CL83 HEK-293T C72(1.18)  LDD1680  [8]
 LDCM0478  CL84 HEK-293T C72(1.50)  LDD1681  [8]
 LDCM0479  CL85 HEK-293T C72(1.15)  LDD1682  [8]
 LDCM0480  CL86 HEK-293T C72(1.10)  LDD1683  [8]
 LDCM0481  CL87 HEK-293T C72(1.02)  LDD1684  [8]
 LDCM0482  CL88 HEK-293T C72(1.02)  LDD1685  [8]
 LDCM0483  CL89 HEK-293T C72(1.10)  LDD1686  [8]
 LDCM0484  CL9 HEK-293T C72(1.06)  LDD1687  [8]
 LDCM0485  CL90 HEK-293T C72(1.58); C93(2.58)  LDD1688  [8]
 LDCM0486  CL91 HEK-293T C72(0.81)  LDD1689  [8]
 LDCM0487  CL92 HEK-293T C72(1.25)  LDD1690  [8]
 LDCM0488  CL93 HEK-293T C72(1.19)  LDD1691  [8]
 LDCM0489  CL94 HEK-293T C72(1.10)  LDD1692  [8]
 LDCM0490  CL95 HEK-293T C72(1.63)  LDD1693  [8]
 LDCM0491  CL96 HEK-293T C72(1.55)  LDD1694  [8]
 LDCM0492  CL97 HEK-293T C72(1.26)  LDD1695  [8]
 LDCM0493  CL98 HEK-293T C72(1.04)  LDD1696  [8]
 LDCM0494  CL99 HEK-293T C72(0.91)  LDD1697  [8]
 LDCM0189  Compound 16 HEK-293T 10.00  LDD0492  [14]
 LDCM0185  Compound 17 HEK-293T 9.19  LDD0504  [14]
 LDCM0184  Compound 20 HEK-293T 13.91  LDD0503  [14]
 LDCM0186  Compound 31 HEK-293T 12.12  LDD0506  [14]
 LDCM0187  Compound 32 HEK-293T 45.93  LDD0507  [14]
 LDCM0190  Compound 34 HEK-293T 14.81  LDD0497  [14]
 LDCM0194  Compound 37 HEK-293T 6.51  LDD0498  [14]
 LDCM0495  E2913 HEK-293T C72(0.98)  LDD1698  [8]
 LDCM0468  Fragment33 HEK-293T C72(0.90)  LDD1671  [8]
 LDCM0427  Fragment51 HEK-293T C72(0.96)  LDD1631  [8]
 LDCM0107  IAA HeLa N.A.  LDD0221  [10]
 LDCM0109  NEM HeLa N.A.  LDD0223  [10]
 LDCM0014  Panhematin HEK-293T 5.03  LDD0062  [6]
 LDCM0131  RA190 MM1.R 9.91  LDD0299  [7]
 LDCM0084  Ro 48-8071 A-549 20.00  LDD0144  [15]
 LDCM0008  Tranylcypromine SH-SY5Y 2.86  LDD0054  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
rRNA methyltransferase 1, mitochondrial (MRM1) RNA methyltransferase TrmH family Q6IN84
3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase (EBP) EBP family Q15125
Probable glutathione peroxidase 8 (GPX8) Glutathione peroxidase family Q8TED1
Sphingosine-1-phosphate lyase 1 (SGPL1) Group II decarboxylase family O95470
17-beta-hydroxysteroid dehydrogenase 13 (HSD17B13) Short-chain dehydrogenases/reductases (SDR) family Q7Z5P4
ADP-ribosylation factor-like protein 13B (ARL13B) Arf family Q3SXY8
GTP-binding protein SAR1a (SAR1A) SAR1 family Q9NR31
Peptidyl-prolyl cis-trans isomerase FKBP7 (FKBP7) . Q9Y680
Transporter and channel
Click To Hide/Show 15 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ammonium transporter Rh type C (RHCG) Ammonium transporter family Q9UBD6
Claudin-7 (CLDN7) Claudin family O95471
Gap junction beta-3 protein (GJB3) Connexin family O75712
Receptor expression-enhancing protein 1 (REEP1) DP1 family Q9H902
LHFPL tetraspan subfamily member 5 protein (LHFPL5) LHFP family Q8TAF8
Aquaporin-2 (AQP2) MIP/aquaporin (TC 1.A.8) family P41181
Aquaporin-6 (AQP6) MIP/aquaporin (TC 1.A.8) family Q13520
Leukocyte surface antigen CD53 (CD53) Tetraspanin (TM4SF) family P19397
Transmembrane protein 106C (TMEM106C) TMEM106 family Q9BVX2
Transmembrane protein 14B (TMEM14B) TMEM14 family Q9NUH8
Urea transporter 2 (SLC14A2) Urea transporter family Q15849
Leucine-rich repeat-containing protein 59 (LRRC59) . Q96AG4
Renin receptor (ATP6AP2) . O75787
Thioredoxin-related transmembrane protein 2 (TMX2) . Q9Y320
Transmembrane protein 79 (TMEM79) . Q9BSE2
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Paired-like homeodomain transcription factor LEUTX (LEUTX) Paired homeobox family A8MZ59
GPCR
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Free fatty acid receptor 2 (FFAR2) G-protein coupled receptor 1 family O15552
G-protein coupled receptor 37-like 1 (GPR37L1) G-protein coupled receptor 1 family O60883
Probable G-protein coupled receptor 152 (GPR152) G-protein coupled receptor 1 family Q8TDT2
Immunoglobulin
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Killer cell immunoglobulin-like receptor 2DL3 (KIR2DL3) Immunoglobulin superfamily P43628
Programmed cell death 1 ligand 2 (PDCD1LG2) BTN/MOG family Q9BQ51
V-type immunoglobulin domain-containing suppressor of T-cell activation (VSIR) . Q9H7M9
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Interferon gamma receptor 2 (IFNGR2) Type II cytokine receptor family P38484
Other
Click To Hide/Show 18 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Bcl-2-like protein 13 (BCL2L13) Bcl-2 family Q9BXK5
Calsyntenin-3 (CLSTN3) Calsyntenin family Q9BQT9
Complex I intermediate-associated protein 30, mitochondrial (NDUFAF1) CIA30 family Q9Y375
NADH dehydrogenase 1 alpha subcomplex assembly factor 2 (NDUFAF2) Complex I NDUFA12 subunit family Q8N183
Complexin-4 (CPLX4) Complexin/synaphin family Q7Z7G2
Gap junction beta-5 protein (GJB5) Connexin family O95377
Endoplasmic reticulum-Golgi intermediate compartment protein 3 (ERGIC3) ERGIC family Q9Y282
Protein FAM209A (FAM209A) FAM209 family Q5JX71
Translation initiation factor IF-3, mitochondrial (MTIF3) IF-3 family Q9H2K0
Transmembrane protein 45B (TMEM45B) TMEM45 family Q96B21
Ankyrin repeat, SAM and basic leucine zipper domain-containing protein 1 (ASZ1) . Q8WWH4
Bcl-2-interacting killer (BIK) . Q13323
Cell growth regulator with RING finger domain protein 1 (CGRRF1) . Q99675
FERM domain-containing protein 3 (FRMD3) . A2A2Y4
Lck-interacting transmembrane adapter 1 (LIME1) . Q9H400
PDZK1-interacting protein 1 (PDZK1IP1) . Q13113
Serine-rich single-pass membrane protein 1 (SSMEM1) . Q8WWF3
Transmembrane protein 52B (TMEM52B) . Q4KMG9

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
Min-101 . D0L7TA
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ct1812 . D0FX8N
Preclinical
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Anavex 1007 . D0M6OW
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,3-ditolylguanidine Small molecular drug D02WJT
Sm 21 Small molecular drug D0X7BG
Patented
Click To Hide/Show 52 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aryl Azepine Derivative 1 Small molecular drug D0WE5J
Aryl Azepine Derivative 2 Small molecular drug D0R1QI
Benzamide Derivative 1 Small molecular drug D0M4BI
Benzamide Derivative 10 Small molecular drug D05YFF
Benzamide Derivative 11 Small molecular drug D0W3TS
Benzamide Derivative 2 Small molecular drug D04PDM
Benzamide Derivative 3 Small molecular drug D03DNE
Benzamide Derivative 4 Small molecular drug D0E9CV
Benzamide Derivative 7 Small molecular drug D0RS2J
Benzamide Derivative 8 Small molecular drug D0H2SE
Benzamide Derivative 9 Small molecular drug D03MKY
Bicyclo-heptan-2-amine Derivative 1 Small molecular drug D04OPJ
Bicyclo-heptan-2-amine Derivative 2 Small molecular drug D0PF9X
Bicyclo-heptan-2-amine Derivative 3 Small molecular drug D0FU2M
Bicyclo-heptan-2-amine Derivative 4 Small molecular drug D0Y2NR
Fused Aryl Carbocycle Derivative 1 Small molecular drug D0VE8R
Fused Aryl Carbocycle Derivative 2 Small molecular drug D0LN2J
Fused Aryl Carbocycle Derivative 3 Small molecular drug D0CK6M
Fused Aryl Carbocycle Derivative 4 Small molecular drug D0HY9M
Fused Aryl Carbocycle Derivative 8 Small molecular drug D0K7CD
Fused Aryl Carbocycle Derivative 9 Small molecular drug D0OZ1P
Isoindoline Derivative 1 Small molecular drug D0S3ON
Isoindoline Derivative 2 Small molecular drug D0F8XU
Isoindoline Derivative 3 Small molecular drug D06FNA
Isoindoline Derivative 4 Small molecular drug D0EK3Z
Isoindoline Derivative 5 Small molecular drug D02NPB
N-substituted 9-azabicyclo[3.3.1]Nonan-3alpha-yl-phenylcarbamate Analog 1 Small molecular drug D0V4KJ
N-substituted 9-azabicyclo[3.3.1]Nonan-3alpha-yl-phenylcarbamate Analog 2 Small molecular drug D0FH5K
N-substituted 9-azabicyclo[3.3.1]Nonan-3alpha-yl-phenylcarbamate Analog 3 Small molecular drug D0N6JH
Piperazine Derivative 7 Small molecular drug D0J9SL
Piperazinyl Methyl Quinazolinone Derivative 1 Small molecular drug D0AT9E
Piperazinyl Methyl Quinazolinone Derivative 2 Small molecular drug D01IVR
Piperazinyl Methyl Quinazolinone Derivative 3 Small molecular drug D04WKL
Piperazinyl Norbenzomorphane Compound 1 Small molecular drug D04BSD
Piperazinyl Norbenzomorphane Compound 2 Small molecular drug D0U6OY
Piperazinyl Norbenzomorphane Compound 3 Small molecular drug D0VC0P
Piperazinyl Norbenzomorphane Compound 4 Small molecular drug D0LV1G
Piperidine Derivative 5 Small molecular drug D0X9RA
Piperidine Derivative 6 Small molecular drug D0T5SO
Pmid28051882-compound-figure9 Small molecular drug D0BI1O
Pmid28051882-compound-xi Small molecular drug D06HRI
Pmid28051882-compound-xiv Small molecular drug D0EO9Z
Pmid30185082-compound-14 Small molecular drug D0E3OT
Pmid30185082-compound-27 Small molecular drug D05MST
Pmid30185082-compound-28 Small molecular drug D0A1DV
Pmid30185082-compound-53 Small molecular drug D02ZGY
Pmid30185082-compound-54 Small molecular drug D0DZ5H
Pmid30185082-compound-55 Small molecular drug D0LP3P
Pmid30185082-compound-56 Small molecular drug D0M5LL
Pmid30185082-compound-57 Small molecular drug D0DW1D
Pmid30185082-compound-63 Small molecular drug D0N5JQ
Pmid30185082-compound-64 Small molecular drug D0SG9W

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 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
3 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
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 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.
6 A Chemical Proteomic Map of Heme-Protein Interactions. J Am Chem Soc. 2022 Aug 24;144(33):15013-15019. doi: 10.1021/jacs.2c06104. Epub 2022 Aug 12.
Mass spectrometry data entry: PXD034651
7 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.
8 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
9 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
10 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.
11 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.
12 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.
13 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
14 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.
15 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.
16 Mapping Protein Targets of Bioactive Small Molecules Using Lipid-Based Chemical Proteomics. ACS Chem Biol. 2017 Oct 20;12(10):2671-2681. doi: 10.1021/acschembio.7b00581. Epub 2017 Sep 20.
Mass spectrometry data entry: PXD007570