General Information of the Protein
Protein ID
PT01505
Protein Name
Somatostatin receptor type 2
Secondarily
Protein Name
SRIF-1
Gene Name
SSTR2
Sequence
MDMADEPLNGSHTWLSIPFDLNGSVVSTNTSNQTEPYYDLTSNAVLTFIYFVVCIIGLCGNTLVIYVILRYAKMKTITNIYILNLAIADELFMLGLPFLAMQVALVHWPFGKAICRVVMTVDGINQFTSIFCLTVMSIDRYLAVVHPIKSAKWRRPRTAKMITMAVWGVSLLVILPIMIYAGLRSNQWGRSSCTINWPGESGAWYTGFIIYTFILGFLVPLTIICLCYLFIIIKVKSSGIRVGSSKRKKSEKKVTRMVSIVVAVFIFCWLPFYIFNVSSVSMAISPTPALKGMFDFVVVLTYANSCANPILYAFLSDNFKKSFQNVLCLVKVSGTDDGERSDSKQDKSRLNETTETQRTLLNGDLQTSI
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family A G protein-coupled receptor
>
Peptide receptor (family A GPCR)
>
Short peptide receptor (family A GPCR)
>
Somatostatin receptor
Function
Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and PLC via pertussis toxin insensitive as well as sensitive G proteins. Inhibits calcium entry by suppressing voltage-dependent calcium channels. Acts as the functionally dominant somatostatin receptor in pancreatic alpha- and beta-cells where it mediates the inhibitory effect of somatostatin-14 on hormone secretion. Inhibits cell growth through enhancement of MAPK1 and MAPK2 phosphorylation and subsequent up-regulation of CDKN1B. Stimulates neuronal migration and axon outgrowth and may participate in neuron development and maturation during brain development. Mediates negative regulation of insulin receptor signaling through PTPN6. Inactivates SSTR3 receptor function following heterodimerization.
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Uniprot ID
Primary ID:
P30874

Secondarily ID:
A8K3Y0
B2R9P7
Q4VBP0
Q96GE0
Q96TF2
Q9BWH1
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Ensembl ID
ENSG00000180616
HGNC ID
HGNC:11331
Subcellular Location
Cell membrane
Cytoplasm
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: CL000383 , AR42J
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0522300
 Compound Info 
(3R,6S,9S,12S,15S,18S,21S,24S,27S,30S,33S,36R)-21-((1H-indol-3-yl)methyl)-30-(2-amino-2-oxoethyl)-18,33-bis(4-aminobutyl)-36-(2-((S)-2-aminopropanamido)acetamido)-12,24,27-tribenzyl-9,15-bis((R)-1-hydroxyethyl)-6-(hydroxymethyl)-5,8,11,14,17,20,23,26,29,32,35-undecaoxo-1,2-dithia-4,7,10,13,16,19,22,25,28,31,34-undecaazacycloheptatriacontane-3-carboxylic acid
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C75H102N18O19S2
  1
1
IC50 = 0.4 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0845169
 Compound Info 
(2E,8S,11S,14S,17S,20S,23S,26S,29S,32S,35S,38S,41S)-23,38-bis(4-aminobutyl)-41-{2-[(2S)-2-aminopropanamido]acetamido}-17,29,32-tribenzyl-35-(carbamoylmethyl)-49-hydroxy-14,20-bis[(1R)-1-hydroxyethyl]-11-(hydroxymethyl)-26-(1H-indol-3-ylmethyl)-10,13,16,19,22,25,28,31,34,37,40-undecaoxo-2,3,9,12,15,18,21,24,27,30,33,36,39-tridecaazatricyclo[41.2.2.2^{4,7}]nonatetraconta-1(45),2,4,6,43,46,48-heptaene-8-carboxylic acid
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C87H110N20O20
  1
1
IC50 > 600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000443 , CC531
 Cell Line Info 
Cell Line ID: CL000011 , CHO
 Cell Line Info 
Cell Line ID: CL000389 , CHO-DXB11
 Cell Line Info 
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Cell Line ID: CL000351 , Dede
 Cell Line Info 
Cell Line ID: CL000029 , GH4C1
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000050 , HEK293-A
 Cell Line Info 
Cell Line ID: CL000020 , Neuro-2a
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0760763
 Compound Info 
6-(3-carbamoyl-5-fluorophenyl)-3-(3-chloro-5-methylphenyl)-N,7-dimethyl-N-((S)-pyrrolidin-2-ylmethyl)-3,4-dihydroquinazoline-4-carboxamide
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C30H31ClFN5O2
  1
1 EC50 = 0.1585 nM
CP0702080
 Compound Info 
3-(3-chloro-5-methylphenyl)-6-(3-fluoro-2-hydroxyphenyl)-N,7-dimethyl-N-{[(2S)-pyrrolidin-2-yl]methyl}-3,4-dihydroquinazoline-4-carboxamide
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C29H30ClFN4O2
  1
1 EC50 = 0.7943 nM
CP0765978
 Compound Info 
3-(3-chloro-5-methylphenyl)-6-(3-cyano-5-fluorophenyl)-N,7-dimethyl-N-((S)-pyrrolidin-2-ylmethyl)-3,4-dihydroquinazoline-4-carboxamide
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C30H29ClFN5O
  1
1 EC50 = 1.259 nM
CP0049566
 Compound Info 
15-28-Somatostatin-28
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C76H104N18O19S2
  4
1 IC50 = 0.7 nM
2 Ki = 0.04 nM
3 Ki = 0.083 nM
4 Ki = 0.23 nM
CP0151093
 Compound Info 
(3S,6S,9S,12R,15S,18S)-9-(4-Amino-butyl)-3-benzyl-15-(4-hydroxy-benzyl)-12-(1H-indol-3-ylmethyl)-6-isopropyl-1,18-dimethyl-1,4,7,10,13,16hexaaza-cyclooctadecane-2,5,8,11,14,17-hexaone
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C44H56N8O7
  1
1 IC50 = 1.6 nM
CP0042009
 Compound Info 
(4R,7S,10S,13R,16S,19R)-13-((1H-indol-3-yl)methyl)-N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-19-((R)-2-amino-3-phenylpropanamido)-10-(4-aminobutyl)-16-benzyl-7-((R)-1-hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide
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C49H65N11O10S2
  2
1 IC50 = 1.9 nM
2 IC50 = 2.2 nM
CP0038580
 Compound Info 
(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-37-[[2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-carboxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]propanoyl]amino]acetyl]amino]-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-10,16-bis[(1S)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-2-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid
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C137H207N41O39S3
  3
1 IC50 = 2.3 nM
2 IC50 = 2.7 nM
3 IC50 = 3.3 nM
CP0050675
 Compound Info 
(4R,7R,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-37-{2-[(2S)-2-[(2S)-6-amino-2-[(2S)-2-[(2S)-2-[(2S)-2-{[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-{[(2S)-1-[(2R)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-amino-3-hydroxypropanamido]propanamido]-3-carbamoylpropanamido]-3-hydroxypropanamido]-3-carbamoylpropanoyl]pyrrolidin-2-yl]formamido}propanamido]-4-(methylsulfanyl)butanamido]propanoyl]pyrrolidin-2-yl]formamido}-5-carbamimidamidopentanamido]-4-carboxybutanamido]-5-carbamimidamidopentanamido]hexanamido]propanamido]a
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C137H207N41O39S3
  5
1 IC50 = 2.3 nM
2 IC50 = 2.4 nM
3 IC50 = 2.6 nM
4 IC50 = 2.7 nM
5 IC50 = 3 nM
CP0036365
 Compound Info 
H-c(Cys3-Phe6-Phe7-DTrp8-Lys9-Thr10-Phe11-Cys14)-OH
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C54H66N10O10S2
  1
1 IC50 = 41 nM
CP0046225
 Compound Info 
(4R,7S,10S,13S,16S,19S,22S,25R)-25-amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid
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C54H66N10O10S2
  1
1 IC50 = 130 nM
CP0670712
 Compound Info 
(S)-methyl 2-(4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)butanamido)-5-guanidinopentanoate
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C25H29F2N5O3
  2
1 IC50 > 1000 nM
2 IC50 > 10000 nM
CP0049568
 Compound Info 
(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-N-[(2S,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
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C49H66N10O10S2
  4
1 Kd = 0.61 nM
2 Ki = 0.57 nM
3 Ki = 0.645 nM
4 Ki = 2.1 nM
CP0193446
 Compound Info 
6-Amino-2-(3-(1H-indol-3-yl)-2-{[4-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidine-1-carbonyl]-amino}-butyrylamino)-hexanoic acid tert-butyl ester
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C35H47N7O5
  1
1 Ki = 0.01 nM
CP0141396
 Compound Info 
10-(4-Amino-butyl)-19-(2-amino-3-phenyl-propionylamino)-16-benzyl-7-(1-hydroxy-ethyl)-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaaza-cycloicosane-4-carboxylic acid (2-hydroxy-1-
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C49H66N10O10S2
  1
1 Ki = 0.4 nM
CP0050325
 Compound Info 
4-{3-[2-(7-Methyl-1H-indol-3-yl)-ethylsulfanyl]-5-quinolin-2-yl-[1,2,4]triazol-4-yl}-butylamine
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C26H28N6S
  1
1 Ki = 1.8 nM
CP0198320
 Compound Info 
3-[4-(4-Amino-butyl)-5-quinolin-2-yl-4H-[1,2,4]triazol-3-ylsulfanyl]-1-(7-methyl-1H-indol-3-yl)-propan-1-one
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C27H28N6OS
  1
1 Ki = 2 nM
CP0152283
 Compound Info 
4-{3-[2-(6-Fluoro-1H-indol-3-yl)-ethylsulfanyl]-5-quinolin-2-yl-[1,2,4]triazol-4-yl}-butylamine
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C25H25FN6S
  1
1 Ki = 2.7 nM
CP0255232
 Compound Info 
4-{3-[2-(5-Chloro-1H-indol-3-yl)-ethylsulfanyl]-5-quinolin-2-yl-[1,2,4]triazol-4-yl}-butylamine
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C25H25ClN6S
  1
1 Ki = 5.6 nM
CP0136960
 Compound Info 
(4R,7S,10S,13R,16S,19S)-10-(4-aminobutyl)-19-[[(2S)-2-amino-3-(4-chlorophenyl)propanoyl]amino]-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
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C58H68ClN11O10S2
  1
1 Ki = 26 nM
Clinical Information about the Protein
Target 1 ( Somatostatin receptor type 2 (SSTR2) )
Target Type Successful Target
Disease 2 Target-related Diseases  2
1 Acromegaly [ICD-11: 5A60.0]
2 Cushing disease [ICD-11: 5A70]
Approved Drug(s) 2 Approved Drugs  2
1 Octreotide
 Drug Info 
Approved
Acromegaly
2 Pasireotide
 Drug Info 
Approved
Cushing disease
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 Paltusotine
 Drug Info 
Phase 3
Acromegaly