General Information of the Protein
Protein ID
PT01509
Protein Name
Sigma non-opioid intracellular receptor 1
Secondarily
Protein Name
Aging-associated gene 8 protein
SR31747-binding protein
Sigma 1-type opioid receptor
Gene Name
SIGMAR1
Secondarily
Gene Name
OPRS1
SRBP
AAG8
Sequence
MQWAVGRRWAWAALLLAVAAVLTQVVWLWLGTQSFVFQREEIAQLARQYAGLDHELAFSRLIVELRRLHPGHVLPDEELQWVFVNAGGWMGAMCLLHASLSEYVLLFGTALGSRGHSGRYWAEISDTIISGTFHQWREGTTKSEVFYPGETVVHGPGEATAVEWGPNTWMVEYGRGVIPSTLAFALADTVFSTQDFLTLFYTLRSYARGLRLELTTYLFGQDP
    Show/Hide
Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
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 (PubMed:16472803, PubMed:9341151). 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 (By similarity).
    Show/Hide
Uniprot ID
Primary ID:
Q99720

Secondarily ID:
D3DRM7
O00673
O00725
Q0Z9W6
Q153Z1
Q2TSD1
Q53GN2
Q7Z653
Q8N7H3
Q9NYX0
    Show/Hide
Ensembl ID
ENSG00000147955
HGNC ID
HGNC:8157
Subcellular Location
Nucleus inner membrane
Nucleus outer membrane
Nucleus envelope
Cytoplasmic vesicle
Endoplasmic reticulum membrane
Membrane
Lipid droplet
Cell junction
Cell membrane
Cell projection
Growth cone
Postsynaptic density membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0094482
1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine
   Show/Hide
C23H32N2O2
 1
1
Ki = 3.162 nM
   TI
   LI
   LO
   TS
CP0760989
rac-trans-N-(2-(4-(3,4-dichlorobenzyl)piperazin-1-yl)ethyl)-2-phenylcyclopropanecarboxamide
   Show/Hide
C23H27Cl2N3O
 1
1
Ki = 10 nM
   TI
   LI
   LO
   TS
CP0692351
rac-trans-N-(2-(4-benzylpiperazin-1-yl)ethyl)-2-phenylcyclopropanecarboxamide
   Show/Hide
C23H29N3O
 1
1
Ki = 15.85 nM
   TI
   LI
   LO
   TS
CP0676996
rac-trans-N-(3-(4-(2-chloro-6-fluorobenzyl)piperazin-1-yl)propyl)-2-phenylcyclopropanecarboxamide
   Show/Hide
C24H29ClFN3O
 1
1
Ki = 25.12 nM
   TI
   LI
   LO
   TS
CP0960915
rac-trans-N-(2-(4-(2-chloro-6-fluorobenzyl)piperazin-1-yl)ethyl)-2-phenylcyclopropanecarboxamide
   Show/Hide
C23H27ClFN3O
 1
1
Ki = 25.12 nM
   TI
   LI
   LO
   TS
CP0677014
rac-trans-N-(2-(diisopropylamino)ethyl)-2-phenylcyclopropanecarboxamide
   Show/Hide
C18H28N2O
 1
1
Ki = 63.1 nM
   TI
   LI
   LO
   TS
CP0841776
rac-trans-2-phenyl-N-(2-(pyrrolidin-1-yl)ethyl)cyclopropanecarboxamide
   Show/Hide
C16H22N2O
 1
1
Ki = 63.1 nM
   TI
   LI
   LO
   TS
CP0676975
rac-trans-(4-((cyclohexylmethylamino)methyl)piperidin-1-yl)((1S,2S)-2-(4-fluorophenyl)cyclopropyl)methanone
   Show/Hide
C23H33FN2O
 1
1
Ki = 79.43 nM
   TI
   LI
   LO
   TS
CP0762178
rac-trans-1,4'-bipiperidin-1'-yl(2-phenylcyclopropyl)methanone
   Show/Hide
C20H28N2O
 1
1
Ki = 79.43 nM
   TI
   LI
   LO
   TS
CP0962255
rac-trans-1,4'-bipiperidin-1'-yl(2-(4-fluorophenyl)cyclopropyl)methanone
   Show/Hide
C20H27FN2O
 1
1
Ki = 100 nM
   TI
   LI
   LO
   TS
CP0720404
rac-trans-N-(2-(diethylamino)ethyl)-2-phenylcyclopropanecarboxamide
   Show/Hide
C16H24N2O
 1
1
Ki = 125.89 nM
   TI
   LI
   LO
   TS
CP0123791
3-Allyl-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[d]azocin-8-ol
   Show/Hide
C17H23NO
 1
1
Ki = 158.49 nM
   TI
   LI
   LO
   TS
CP0947426
(rac-trans-2-phenylcyclopropyl)(4-(pyrrolidin-1-yl)piperidin-1-yl)methanone
   Show/Hide
C19H26N2O
 1
1
Ki = 199.53 nM
   TI
   LI
   LO
   TS
CP0947425
rac-trans-N-(3-(dimethylamino)-2,2-dimethylpropyl)-2-phenylcyclopropanecarboxamide
   Show/Hide
C17H26N2O
 1
1
Ki = 398.11 nM
   TI
   LI
   LO
   TS
CP0690688
rac-trans-N-(2-(4-(2-chloro-6-fluorobenzoyl)piperazin-1-yl)ethyl)-2-phenylcyclopropanecarboxamide
   Show/Hide
C23H25ClFN3O2
 1
1
Ki = 630.96 nM
   TI
   LI
   LO
   TS
CP0887288
(rac-trans-2-phenylcyclopropyl)(4-phenylpiperazin-1-yl)methanone
   Show/Hide
C20H22N2O
 1
1
Ki = 1258.93 nM
   TI
   LI
   LO
   TS
CP0924094
rac-trans-2-phenyl-N-(4-(piperidin-1-yl)cyclohexyl)cyclopropanecarboxamide
   Show/Hide
C21H30N2O
 1
1
Ki = 1258.93 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0008601
4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one;propionate(HCl)
   Show/Hide
C21H23ClFNO2
 13
1 IC50 = 5.64 nM
2 IC50 = 213.8 nM
3 Ki = 0.2 nM
4 Ki = 0.44 nM
5 Ki = 1.1 nM
6 Ki = 1.9 nM
7 Ki = 2.2 nM
8 Ki = 2.5 nM
9 Ki = 3.7 nM
10 Ki = 5 nM
11 Ki = 6.3 nM
12 Ki = 6.4 nM
13 Ki = 16 nM
CP0073233
(+)-(6R,11S)-6,11-dimethyl-3-(3-methyl-but-2-enyl)-1,2,3,4,5,6-hexahydro-2,6-methano-benzo[d]azocin-8-ol
   Show/Hide
C19H27NO
 3
1 Ki = 1.7 nM
2 Ki = 3.1 nM
3 Ki = 4.4 nM
CP0076802
1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydro-naphthalen-1-yl)-propyl]-piperazine
   Show/Hide
C24H38N2O
 2
1 Ki = 1.995 nM
2 Ki = 13.6 nM
CP0013421
CAS_97-39-2
   Show/Hide
C15H17N3
 6
1 Ki = 15 nM
2 Ki = 21 nM
3 Ki = 27.4 nM
4 Ki = 41 nM
5 Ki = 69 nM
6 Ki = 89 nM
CP0141502
4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine
   Show/Hide
C20H23N3O2
 1
1 Ki = 17 nM
Clinical Information about the Protein
Target 1 ( Opioid receptor sigma 1 (OPRS1) )
Target Type Successful Target
Disease 6 Target-related Diseases  6
1 Cough [ICD-11: MD12]
2 Mood disorder [ICD-11: 6A60-6E23]
3 Schizophrenia [ICD-11: 6A20]
4 Psychotic disorder [ICD-11: 6A20-6A25]
5 Major depressive disorder [ICD-11: 6A70.3]
6 Aging skin [ICD-11: EE40]
Approved Drug(s) 1 Approved Drug  1
1 Dextromethorphan Approved
Cough
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 OPC-14523 Phase 2
Mood disorder
2 SSR-125047 Phase 1
Schizophrenia
Discontinued Drug(s) 8 Discontinued Drugs  8
1 BMS-181100 Discontinued in Phase 3
Psychotic disorder
2 Panamesine Discontinued in Phase 2
Psychotic disorder
3 DUP-734 Discontinued in Phase 1
Psychotic disorder
4 Gevotroline Discontinued in Phase 1
Psychotic disorder
5 E-6276 Terminated
Schizophrenia
6 NE-100 Terminated
Schizophrenia
7 PRE-084 Terminated
Aging skin
8 Rimcazole Terminated
Schizophrenia
Preclinical Drug(s) 1 Preclinical Drug  1
1 Cutamesine Preclinical
Major depressive disorder
Target 2 ( HUMAN opioid receptor sigma 1 (OPRS1) )
Target Type Unknown Type Target
Disease 2 Target-related Diseases  2
1 Schizophrenia [ICD-11: 6A20]
2 Coronavirus Disease 2019 (COVID-19) [ICD-11: 1D6Y]
Investigative Drug(s) 4 Investigative Drugs  4
1 Haloperidol Approved
Schizophrenia
2 E-52862 Investigative
Coronavirus Disease 2019 (COVID-19)
3 PB28 Investigative
Coronavirus Disease 2019 (COVID-19)
4 PD-144418 Investigative
Coronavirus Disease 2019 (COVID-19)