Details of the Target

General Information of Target

Target ID LDTP10958
Target Name Sigma non-opioid intracellular receptor 1 (SIGMAR1)
Gene Name SIGMAR1
Gene ID 10280
Synonyms
OPRS1; SRBP; Sigma non-opioid intracellular receptor 1; Aging-associated gene 8 protein; SR31747-binding protein; SR-BP; Sigma 1-type opioid receptor; SIG-1R; Sigma1-receptor; Sigma1R; hSigmaR1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSTGLRYKSKLATPEDKQDIDKQYVGFATLPNQVHRKSVKKGFDFTLMVAGESGLGKSTL
VHSLFLTDLYKDRKLLSAEERISQTVEILKHTVDIEEKGVKLKLTIVDTPGFGDAVNNTE
CWKPITDYVDQQFEQYFRDESGLNRKNIQDNRVHCCLYFISPFGHGLRPVDVGFMKALHE
KVNIVPLIAKADCLVPSEIRKLKERIREEIDKFGIHVYQFPECDSDEDEDFKQQDRELKE
SAPFAVIGSNTVVEAKGQRVRGRLYPWGIVEVENQAHCDFVKLRNMLIRTHMHDLKDVTC
DVHYENYRAHCIQQMTSKLTQDSRMESPIPILPLPTPDAETEKLIRMKDEELRRMQEMLQ
RMKQQMQDQ
Target Type
Successful
Target Bioclass
Transporter and channel
Family
ERG2 family
Subcellular location
Nucleus inner membrane
Function
Functions in lipid transport from the endoplasmic reticulum and is involved in a wide array of cellular functions probably through regulation of the biogenesis of lipid microdomains at the plasma membrane. Involved in the regulation of different receptors it plays a role in BDNF signaling and EGF signaling. Also regulates ion channels like the potassium channel and could modulate neurotransmitter release. Plays a role in calcium signaling through modulation together with ANK2 of the ITP3R-dependent calcium efflux at the endoplasmic reticulum. Plays a role in several other cell functions including proliferation, survival and death. Originally identified for its ability to bind various psychoactive drugs it is involved in learning processes, memory and mood alteration. Necessary for proper mitochondrial axonal transport in motor neurons, in particular the retrograde movement of mitochondria. Plays a role in protecting cells against oxidative stress-induced cell death via its interaction with RNF112.
TTD ID
T46360
Uniprot ID
Q99720
DrugMap ID
TTTPE1L
Ensemble ID
ENST00000277010.9
HGNC ID
HGNC:8157
ChEMBL ID
CHEMBL287

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
JURKAT SNV: p.A86V .
OCIAML2 SNV: p.W11L .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Jackson_1
 Probe Info  		2.46  LDD0120  [1]
PAL-AfBPP Probe
Click To Hide/Show 171 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C001
 Probe Info  		6.45  LDD1711  [2]
C004
 Probe Info  		16.22  LDD1714  [2]
C006
 Probe Info  		17.75  LDD1715  [2]
C007
 Probe Info  		10.41  LDD1716  [2]
C008
 Probe Info  		5.78  LDD1717  [2]
C010
 Probe Info  		9.58  LDD1719  [2]
C022
 Probe Info  		23.92  LDD1728  [2]
C024
 Probe Info  		11.00  LDD1730  [2]
C040
 Probe Info  		24.59  LDD1740  [2]
C041
 Probe Info  		20.53  LDD1741  [2]
C045
 Probe Info  		5.06  LDD1744  [2]
C051
 Probe Info  		4.96  LDD1749  [2]
C052
 Probe Info  		6.23  LDD1750  [2]
C055
 Probe Info  		39.12  LDD1752  [2]
C058
 Probe Info  		4.92  LDD1755  [2]
C063
 Probe Info  		15.35  LDD1760  [2]
C064
 Probe Info  		10.85  LDD1761  [2]
C067
 Probe Info  		18.51  LDD1763  [2]
C070
 Probe Info  		37.53  LDD1766  [2]
C071
 Probe Info  		10.70  LDD1767  [2]
C072
 Probe Info  		18.38  LDD1768  [2]
C073
 Probe Info  		7.78  LDD1769  [2]
C075
 Probe Info  		8.06  LDD1770  [2]
C082
 Probe Info  		5.58  LDD1774  [2]
C085
 Probe Info  		15.03  LDD1777  [2]
C088
 Probe Info  		5.74  LDD1780  [2]
C092
 Probe Info  		32.90  LDD1783  [2]
C094
 Probe Info  		67.65  LDD1785  [2]
C100
 Probe Info  		8.46  LDD1789  [2]
C102
 Probe Info  		9.32  LDD1790  [2]
C106
 Probe Info  		23.92  LDD1793  [2]
C107
 Probe Info  		35.02  LDD1794  [2]
C108
 Probe Info  		21.11  LDD1795  [2]
C112
 Probe Info  		30.70  LDD1799  [2]
C113
 Probe Info  		5.94  LDD1800  [2]
C117
 Probe Info  		5.66  LDD1804  [2]
C130
 Probe Info  		16.11  LDD1812  [2]
C134
 Probe Info  		22.16  LDD1816  [2]
C135
 Probe Info  		18.77  LDD1817  [2]
C138
 Probe Info  		31.34  LDD1820  [2]
C140
 Probe Info  		24.93  LDD1822  [2]
C141
 Probe Info  		65.34  LDD1823  [2]
C143
 Probe Info  		70.52  LDD1825  [2]
C145
 Probe Info  		25.63  LDD1827  [2]
C147
 Probe Info  		24.08  LDD1829  [2]
C152
 Probe Info  		7.41  LDD1833  [2]
C153
 Probe Info  		55.72  LDD1834  [2]
C156
 Probe Info  		22.94  LDD1836  [2]
C157
 Probe Info  		5.31  LDD1837  [2]
C159
 Probe Info  		8.40  LDD1839  [2]
C160
 Probe Info  		51.27  LDD1840  [2]
C161
 Probe Info  		55.33  LDD1841  [2]
C163
 Probe Info  		11.24  LDD1843  [2]
C165
 Probe Info  		12.38  LDD1845  [2]
C166
 Probe Info  		9.71  LDD1846  [2]
C167
 Probe Info  		10.06  LDD1847  [2]
C169
 Probe Info  		29.65  LDD1849  [2]
C171
 Probe Info  		6.59  LDD1851  [2]
C174
 Probe Info  		5.31  LDD1854  [2]
C176
 Probe Info  		8.34  LDD1855  [2]
C177
 Probe Info  		53.45  LDD1856  [2]
C180
 Probe Info  		15.03  LDD1859  [2]
C183
 Probe Info  		23.26  LDD1861  [2]
C185
 Probe Info  		21.26  LDD1863  [2]
C187
 Probe Info  		30.06  LDD1865  [2]
C194
 Probe Info  		32.90  LDD1870  [2]
C199
 Probe Info  		22.16  LDD1875  [2]
C200
 Probe Info  		14.03  LDD1876  [2]
C201
 Probe Info  		58.08  LDD1877  [2]
C206
 Probe Info  		37.27  LDD1881  [2]
C215
 Probe Info  		7.89  LDD1889  [2]
C217
 Probe Info  		5.90  LDD1891  [2]
C218
 Probe Info  		18.90  LDD1892  [2]
C219
 Probe Info  		10.13  LDD1893  [2]
C220
 Probe Info  		11.96  LDD1894  [2]
C221
 Probe Info  		5.43  LDD1895  [2]
C225
 Probe Info  		18.38  LDD1898  [2]
C228
 Probe Info  		27.28  LDD1901  [2]
C229
 Probe Info  		28.05  LDD1902  [2]
C230
 Probe Info  		9.58  LDD1903  [2]
C231
 Probe Info  		20.25  LDD1904  [2]
C232
 Probe Info  		41.93  LDD1905  [2]
C233
 Probe Info  		36.25  LDD1906  [2]
C234
 Probe Info  		6.73  LDD1907  [2]
C235
 Probe Info  		96.34  LDD1908  [2]
C237
 Probe Info  		7.36  LDD1910  [2]
C240
 Probe Info  		25.11  LDD1913  [2]
C242
 Probe Info  		12.64  LDD1915  [2]
C243
 Probe Info  		36.76  LDD1916  [2]
C244
 Probe Info  		29.65  LDD1917  [2]
C245
 Probe Info  		11.63  LDD1918  [2]
C246
 Probe Info  		13.74  LDD1919  [2]
C252
 Probe Info  		9.51  LDD1925  [2]
C253
 Probe Info  		6.73  LDD1926  [2]
C255
 Probe Info  		6.68  LDD1928  [2]
C258
 Probe Info  		7.67  LDD1931  [2]
C266
 Probe Info  		10.63  LDD1937  [2]
C272
 Probe Info  		5.21  LDD1942  [2]
C273
 Probe Info  		12.64  LDD1943  [2]
C276
 Probe Info  		11.96  LDD1946  [2]
C277
 Probe Info  		24.93  LDD1947  [2]
C278
 Probe Info  		60.97  LDD1948  [2]
C280
 Probe Info  		15.03  LDD1950  [2]
C286
 Probe Info  		5.24  LDD1956  [2]
C287
 Probe Info  		15.14  LDD1957  [2]
C288
 Probe Info  		14.93  LDD1958  [2]
C289
 Probe Info  		38.85  LDD1959  [2]
C290
 Probe Info  		24.25  LDD1960  [2]
C293
 Probe Info  		27.86  LDD1963  [2]
C297
 Probe Info  		5.03  LDD1967  [2]
C299
 Probe Info  		16.11  LDD1968  [2]
C305
 Probe Info  		20.25  LDD1974  [2]
C307
 Probe Info  		11.88  LDD1975  [2]
C310
 Probe Info  		9.51  LDD1977  [2]
C316
 Probe Info  		5.82  LDD1982  [2]
C317
 Probe Info  		6.50  LDD1983  [2]
C327
 Probe Info  		5.54  LDD1991  [2]
C339
 Probe Info  		26.35  LDD2002  [2]
C343
 Probe Info  		23.92  LDD2005  [2]
C348
 Probe Info  		22.32  LDD2009  [2]
C349
 Probe Info  		62.25  LDD2010  [2]
C350
 Probe Info  		99.73  LDD2011  [2]
C351
 Probe Info  		11.88  LDD2012  [2]
C352
 Probe Info  		9.38  LDD2013  [2]
C354
 Probe Info  		13.27  LDD2015  [2]
C355
 Probe Info  		78.79  LDD2016  [2]
C356
 Probe Info  		34.54  LDD2017  [2]
C357
 Probe Info  		18.51  LDD2018  [2]
C360
 Probe Info  		12.30  LDD2021  [2]
C361
 Probe Info  		20.68  LDD2022  [2]
C362
 Probe Info  		28.25  LDD2023  [2]
C366
 Probe Info  		9.71  LDD2027  [2]
C367
 Probe Info  		5.35  LDD2028  [2]
C370
 Probe Info  		18.38  LDD2031  [2]
C371
 Probe Info  		13.36  LDD2032  [2]
C373
 Probe Info  		12.82  LDD2033  [2]
C374
 Probe Info  		12.30  LDD2034  [2]
C375
 Probe Info  		13.36  LDD2035  [2]
C376
 Probe Info  		30.48  LDD2036  [2]
C378
 Probe Info  		7.16  LDD2037  [2]
C380
 Probe Info  		19.29  LDD2039  [2]
C381
 Probe Info  		6.15  LDD2040  [2]
C382
 Probe Info  		25.46  LDD2041  [2]
C383
 Probe Info  		14.72  LDD2042  [2]
C384
 Probe Info  		4.99  LDD2043  [2]
C386
 Probe Info  		26.35  LDD2045  [2]
C389
 Probe Info  		9.00  LDD2048  [2]
C390
 Probe Info  		99.73  LDD2049  [2]
C391
 Probe Info  		18.64  LDD2050  [2]
C393
 Probe Info  		15.14  LDD2052  [2]
C396
 Probe Info  		8.69  LDD2055  [2]
C399
 Probe Info  		11.55  LDD2058  [2]
C403
 Probe Info  		20.53  LDD2061  [2]
C405
 Probe Info  		12.91  LDD2063  [2]
C407
 Probe Info  		15.35  LDD2064  [2]
C419
 Probe Info  		65.80  LDD2074  [2]
C420
 Probe Info  		64.89  LDD2075  [2]
C422
 Probe Info  		14.22  LDD2077  [2]
C424
 Probe Info  		9.45  LDD2079  [2]
C425
 Probe Info  		8.88  LDD2080  [2]
C426
 Probe Info  		14.03  LDD2081  [2]
C429
 Probe Info  		21.26  LDD2084  [2]
C431
 Probe Info  		13.83  LDD2086  [2]
C432
 Probe Info  		6.19  LDD2087  [2]
C433
 Probe Info  		6.11  LDD2088  [2]
FFF probe13
 Probe Info  		17.48  LDD0475  [3]
FFF probe14
 Probe Info  		20.00  LDD0477  [3]
FFF probe2
 Probe Info  		12.46  LDD0463  [3]
FFF probe3
 Probe Info  		16.96  LDD0464  [3]
A-DA
 Probe Info  		2.08  LDD0145  [4]
OEA-DA
 Probe Info  		6.78  LDD0046  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0070  Cisar_cp37 MDA-MB-231 2.46  LDD0120  [1]
 LDCM0084  Ro 48-8071 A-549 2.08  LDD0145  [4]

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
cAMP-dependent protein kinase catalytic subunit alpha (PRKACA) AGC Ser/Thr protein kinase family P17612
TGF-beta receptor type-2 (TGFBR2) TKL Ser/Thr protein kinase family P37173
Other
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Serpin H1 (SERPINH1) Serpin family P50454

The Drug(s) Related To This Target

Approved
Click To Hide/Show 16 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Amitriptyline Small molecular drug DB00321
Cocaine Small molecular drug DB00907
Dextromethorphan Small molecular drug D09OBB
Fenfluramine Small molecular drug DB00574
Haloperidol Small molecular drug DB00502
Hydrocodone Small molecular drug DB00956
Naltrexone Small molecular drug DB00704
Nortriptyline Small molecular drug DB00540
Pentazocine Small molecular drug DB00652
Pimavanserin Small molecular drug DB05316
Prasterone Small molecular drug DB01708
Remoxipride Small molecular drug DB00409
Sertraline Small molecular drug DB01104
Dextromethorphan Polistirex . D00KFB
Noscapine . DB06174
Pentoxyverine . DB11186
Phase 3
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Adx N05 . D0GW6K
Avp-786 . D0Z6IB
Cm-2395 . D0X6XH
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Igmesine Small molecular drug D0N5LJ
Opc-14523 Small molecular drug D0R8GR
Phase 1
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ssr-125047 Small molecular drug D0Q7QY
Anavex 2-73 . D09AOO
Sa-5845 . D0G9SH
Ssr-125329a . D0T6ES
Preclinical
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cutamesine Small molecular drug D00KVE
Anavex 1-41 . D0T0UC
Anavex 1007 . D0M6OW
Investigative
Click To Hide/Show 13 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(+)-sk&f10047 Small molecular drug D0IZ1X
(Rs)-ppcc Small molecular drug D07LVT
1,3-ditolylguanidine Small molecular drug D02WJT
2-(1h-indol-3-yl)-n,N-dimethylethanamine Small molecular drug D03DLZ
Bd-1047 Small molecular drug D09CGH
Captodiame Small molecular drug DB09014
Dimemorfan Small molecular drug D09AUU
[3h]Pentazocine Small molecular drug D0G4KB
C-10068 . D0F1WD
Cm-156 . D0J9VK
Cns-1169 . D0A3XA
Mc-113 . D0G5RT
Mc-116 . D05BLG
Patented
Click To Hide/Show 27 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1,2,4-triazole Derivative 3 Small molecular drug D0MD6P
1,2,4-triazole Derivative 4 Small molecular drug D08RUG
Aryl Alkanolamine Derivative 1 Small molecular drug D0E9CK
Aryl Alkanolamine Derivative 2 Small molecular drug D07XVQ
Benzamide Derivative 10 Small molecular drug D05YFF
Benzamide Derivative 11 Small molecular drug D0W3TS
Benzamide Derivative 7 Small molecular drug D0RS2J
Benzamide Derivative 8 Small molecular drug D0H2SE
Benzamide Derivative 9 Small molecular drug D03MKY
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
Phenylpropylamine Derivative 1 Small molecular drug D0G4GT
Phenylpropylamine Derivative 2 Small molecular drug D0L0CD
Phenylpropylamine Derivative 3 Small molecular drug D0C1YW
Phenylpropylamine Derivative 4 Small molecular drug D0A0DV
Phenylpropylamine Derivative 5 Small molecular drug D0G7GN
Piperazine Derivative 7 Small molecular drug D0J9SL
Piperidine Derivative 4 Small molecular drug D0X5FS
Piperidine Derivative 5 Small molecular drug D0X9RA
Piperidine Derivative 6 Small molecular drug D0T5SO
Pmid28051882-compound-xiv Small molecular drug D0EO9Z
Pmid30185082-compound-57 Small molecular drug D0DW1D
Pmid30185082-compound-64 Small molecular drug D0SG9W
Pyrazole Derivative 86 Small molecular drug D04PCA
Discontinued
Click To Hide/Show 22 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ah-9700 Small molecular drug D0T8BP
Bms-181100 Small molecular drug D01YOC
Dimethyltryptamine Small molecular drug DB01488
Dup-734 Small molecular drug D0Z4QV
E-5842 Small molecular drug D00IRU
E-6276 Small molecular drug D0B7BX
Fh-510 Small molecular drug D0Z5HB
Gevotroline Small molecular drug D0L7BV
Kb-5492 Small molecular drug D0L4PY
Ms-377 Small molecular drug D09OTG
Ne-100 Small molecular drug D09DRG
Npc-16377 Small molecular drug D0B1PD
Panamesine Small molecular drug D00EZE
Phencyclidine Small molecular drug DB03575
Pre-084 Small molecular drug D01KIU
Rimcazole Small molecular drug D0M9GE
Sr-31742a Small molecular drug D0MK2C
Cns-1307 . D0U7VO
Hydrocodex . D0Q7OA
Lu-29252 . D0T8HU
Ne-033 . D0L1YS
Oxycodex . D02JNX

References

1 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.
2 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
3 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.
4 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.
5 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