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PsychedeliaDokholyan Laboratory
TargetSigma receptors

Sigma 1

σ1 and σ2 binding sites.

Measurements
51
Compounds
23
Binding constants
35
Median pX
6.26

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

SGMR1_HUMANSIGMAR1Homo sapiens

Sigma non-opioid intracellular receptor 1

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 alteration16472803,9341151. 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)

Quoted from UniProt’s FUNCTION annotation for Q99720 (reviewed). The superscript numbers are UniProt’s own PubMed citations, kept in the sentence and in order, each linking to the paper it names.

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
HSPA50.9920.1130.0000.992
CYP51A10.9850.9540.0000.660
ERG280.9830.9540.0000.615
SQLE0.9740.9540.0000.418
KCNH60.9440.0000.0000.944
TMEM970.9430.0000.0000.937
ITPR10.9380.0000.0000.937
ITPR30.9340.2920.0000.910
KCNA40.9170.0910.0000.913
MSMO10.8930.7820.1390.340

Where it sits in the cell

UniProt, curated 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

Expression by cell type

Single cell type RNA, the 4 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Extravillous trophoblasts111.9 nCPM
  • Hepatocytes108.2 nCPM
  • Esophageal basal cells96.4 nCPM
  • Migrating cytotrophoblasts84 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • liver167.8 nTPM

III · Ranking

Compounds by strongest binding constant

One bar per compound: its strongest Ki or Kd at this target, expressed as pX. Compounds measured here only by a functional assay do not appear — they are in the table below.

  1. 01Dextromethorphan8.00
  2. 02DALT7.00
  3. 03Ibogaine6.60
  4. 045-MeO-DALT6.52
  5. 05DPT6.40
  6. 061-(2-naphthyl)piperazine6.26
  7. 07para-chlorophenylpiperazine5.94
  8. 08TFMPP5.87
  9. 09DiPT5.75
  10. 10Rimonabant5.36
  11. 11Mitragynine5.35
  12. 12DMT5.28
  13. 13meta-chlorophenylpiperazine5.21

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Equilibrium binding constants 35

Ki and Kd — a concentration at equilibrium. Directly comparable across rows at the same target.

TargetClassTypeValue (nM)pXOrganismAssay
Sigma 1Sigma receptorsKi10.008.00Cavia porcellusCHEMBL4775642
Sigma 1Sigma receptorsKi63.007.20Cavia porcellusCHEMBL4775632
Sigma 1Sigma receptorsKi1007.00Homo sapiensCHEMBL3756496
Sigma 1Sigma receptorsKi1017.00RATPMID 29499272
Sigma 1Sigma receptorsKi2506.60Cavia porcellusCHEMBL915240
Sigma 1Sigma receptorsKi3016.52RATPMID 29499272
Sigma 1Sigma receptorsKi3026.52Homo sapiensCHEMBL3756496
Sigma 1Sigma receptorsKi3486.46Homo sapiensCHEMBL808203
Sigma 1Sigma receptorsKi3976.40HUMANPMID 20126400
Sigma 1Sigma receptorsKi3986.40Cavia porcellusCHEMBL2395634
Sigma 1Sigma receptorsKi4006.40Cavia porcellusCHEMBL2395634
Sigma 1Sigma receptorsKi5506.26Homo sapiensCHEMBL803922
Sigma 1Sigma receptorsKi1,1505.94Homo sapiensCHEMBL803922
Sigma 1Sigma receptorsKi1,3405.87Homo sapiensCHEMBL803922
Sigma 1Sigma receptorsKi1,7985.75HUMANPMID 20126400
Sigma 1Sigma receptorsKi4,3505.36RATPDSP
Sigma 1Sigma receptorsKi4,4715.35RATPDSP
Sigma 1Sigma receptorsKi5,0705.29Rattus norvegicusCHEMBL807413
Sigma 1Sigma receptorsKi5,2095.28HUMANPMID 20126400
Sigma 1Sigma receptorsKi5,8395.23HUMANPMID 20126400
Sigma 1Sigma receptorsKi6,1505.21Homo sapiensCHEMBL803922
Sigma 1Sigma receptorsKi8,5545.07Homo sapiensCHEMBL3238652
Sigma 1Sigma receptorsKi15,0004.82Cavia porcellusCHEMBL1780499
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3756496
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL3756496
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXRattus norvegicusCHEMBL3106940
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL808204
Sigma 1Sigma receptorsKi— no normalized value— value does not convert to pXHomo sapiensCHEMBL803926

Functional readouts 13

IC₅₀, EC₅₀, AC₅₀ and potency. Assay-dependent, and not interchangeable with a binding constant.

TargetClassTypeValue (nM)pXOrganismAssay
Sigma 1Sigma receptorsIC5015.207.82Cavia porcellusCHEMBL946010
Sigma 1Sigma receptorsIC502326.63Cavia porcellusCHEMBL946009
Sigma 1Sigma receptorsIC502406.62Rattus norvegicusCHEMBL808179
Sigma 1Sigma receptorsIC509126.04Homo sapiensCHEMBL805753
Sigma 1Sigma receptorsIC501,1005.96Homo sapiensCHEMBL846627
Sigma 1Sigma receptorsIC502,0605.69Homo sapiensCHEMBL846484
Sigma 1Sigma receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110
Sigma 1Sigma receptorsIC50— no normalized value— value does not convert to pXHomo sapiensCHEMBL1909110

Other measurements 3

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Sigma 1Sigma receptorsActivity— no normalized value— value does not convert to pXRattus norvegicusCHEMBL916724
Sigma 1Sigma receptorsInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL4687651
Sigma 1Sigma receptorsRatio Ki— no normalized value— value does not convert to pXCavia porcellusCHEMBL4775643
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