SSTR2

Summary

SSTR2 (somatostatin receptor 2, HGNC:11331) is a protein-coding gene on chromosome 17q25.1, encoding Somatostatin receptor type 2 (P30874). Receptor for somatostatin-14 and -28.

Somatostatin acts at many sites to inhibit the release of many hormones and other secretory proteins. The biologic effects of somatostatin are probably mediated by a family of G protein-coupled receptors that are expressed in a tissue-specific manner. SSTR2 is a member of the superfamily of receptors having seven transmembrane segments and is expressed in highest levels in cerebrum and kidney.

Source: NCBI Gene 6752 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 40 total
• Druggable target: yes — 11 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001050

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11331
Approved symbol	SSTR2
Name	somatostatin receptor 2
Location	17q25.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000180616
Ensembl biotype	protein_coding
OMIM	182452
Entrez	6752

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 1 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000357585, ENST00000579323

RefSeq mRNA: 1 — MANE Select: NM_001050 NM_001050

CCDS: CCDS11691

Canonical transcript exons

ENST00000357585 — 2 exons

Exon	Start	End
ENSE00001425722	73169228	73176633
ENSE00003847255	73165010	73165288

Expression profiles

Bgee: expression breadth ubiquitous, 186 present calls, max score 90.60.

FANTOM5 (CAGE): breadth broad, TPM avg 9.2622 / max 947.8504, expressed in 629 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
162561	9.1891	629
162562	0.0730	41

Top tissues by expression

281 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
buccal mucosa cell	CL:0002336	90.60	gold quality
ganglionic eminence	UBERON:0004023	90.13	gold quality
cortical plate	UBERON:0005343	84.51	gold quality
cerebellar cortex	UBERON:0002129	84.38	gold quality
cerebellar hemisphere	UBERON:0002245	84.32	gold quality
cerebellum	UBERON:0002037	83.70	gold quality
islet of Langerhans	UBERON:0000006	83.29	gold quality
right hemisphere of cerebellum	UBERON:0014890	83.05	gold quality
cerebellar vermis	UBERON:0004720	80.03	silver quality
paraflocculus	UBERON:0005351	79.51	gold quality
superior frontal gyrus	UBERON:0002661	79.07	gold quality
prefrontal cortex	UBERON:0000451	78.09	gold quality
postcentral gyrus	UBERON:0002581	78.00	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	77.43	gold quality
frontal cortex	UBERON:0001870	77.25	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	76.96	gold quality
neocortex	UBERON:0001950	76.86	gold quality
parietal lobe	UBERON:0001872	76.39	gold quality
cingulate cortex	UBERON:0003027	76.31	gold quality
cerebral cortex	UBERON:0000956	76.29	gold quality
anterior cingulate cortex	UBERON:0009835	76.15	gold quality
Brodmann (1909) area 9	UBERON:0013540	75.95	gold quality
entorhinal cortex	UBERON:0002728	75.84	gold quality
Brodmann (1909) area 46	UBERON:0006483	75.38	gold quality
right frontal lobe	UBERON:0002810	75.19	gold quality
cartilage tissue	UBERON:0002418	74.79	gold quality
embryo	UBERON:0000922	74.19	gold quality
telencephalon	UBERON:0001893	74.07	gold quality
nucleus accumbens	UBERON:0001882	74.03	gold quality
Ammon’s horn	UBERON:0001954	73.86	gold quality

Single-cell (SCXA)

Detected in 5 experiment(s), a significant marker in 5.

Experiment	Marker?	Max mean expression
E-HCAD-5	yes	869.82
E-MTAB-5061	yes	25.92
E-GEOD-81547	yes	25.20
E-GEOD-135922	yes	25.16
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): HIVEP2, PITX1, SMAD3, SMAD4, SP1, TCF4, TP53

miRNA regulators (miRDB)

62 targeting SSTR2, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-4673	100.00	66.64	1490
HSA-MIR-4482-3P	99.98	72.50	3147
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-9983-3P	99.94	71.48	3631
HSA-MIR-548J-3P	99.94	72.61	4881
HSA-MIR-548AE-3P	99.93	72.66	4867
HSA-MIR-548AQ-3P	99.93	72.66	4867
HSA-MIR-381-3P	99.93	71.87	2854
HSA-MIR-548AH-3P	99.93	72.54	4872
HSA-MIR-548AM-3P	99.93	72.54	4872
HSA-MIR-300	99.92	71.76	2856
HSA-MIR-515-5P	99.92	69.82	2343
HSA-MIR-519E-5P	99.92	69.62	2358
HSA-MIR-4302	99.89	67.94	1187
HSA-MIR-129-5P	99.88	70.26	3273
HSA-MIR-3919	99.87	69.45	2489
HSA-MIR-548AC	99.84	70.77	4351
HSA-MIR-548H-3P	99.84	70.80	4349
HSA-MIR-548Z	99.84	70.80	4349
HSA-MIR-3934-3P	99.76	65.51	1351
HSA-MIR-200A-5P	99.76	69.10	949
HSA-MIR-200B-5P	99.76	69.05	948
HSA-MIR-6885-3P	99.75	70.36	3187
HSA-MIR-4306	99.72	70.50	3630
HSA-MIR-5580-3P	99.70	69.41	2052
HSA-MIR-29B-2-5P	99.67	68.98	1726
HSA-MIR-26A-1-3P	99.64	66.81	788

Literature-anchored findings (GeneRIF, showing 40)

• SSTR transcripts are expressed and functional in retroorbital fibroblasts. SSTR1 is expressed in Grave’s disease and octreotide inhibits retroorbital cell growth, explaining the SRIH therapeutic effect. (PMID:11753241)
• Quantitative evaluation of somatostatin receptor subtype 2 expression in sporadic colorectal tumor and in the corresponding normal mucosa (PMID:11839658)
• Somatostatin modulates G-CSF-induced but not interleukin-3-induced proliferative responses in myeloid 32D cells via activation of somatostatin receptor subtype 2. (PMID:11920268)
• SSTRs 1-5 are heterogeneously expressed in gastroenteropancreatic endocrine tumors (PMID:12021920)
• expression of SSTR2 transcripts up-regulated in prostatic carcinoma cells; SSTR2 agonists may have role in treatment of prostate cancer (PMID:12210479)
• somatostatin receptor transcripts were found in lymphocytes both from Graves’ ophthalmopathy retroorbital tissues and blood samples, with levels of expression of SST1, -2, and -4 mRNA higher than those of the SST3 and -5 transcripts (PMID:12414882)
• localization and expression in human prostatic tissue and prostate cancer cell lines (PMID:12474541)
• sensitizes human pancreatic cancer cells to death ligand-induced apoptosis (PMID:12490654)
• Presence and intracellular localization of the spliced variant SSR2(a) and its endogenous ligand SS in the cultured human neuroblastoma (NB) cell line, SH-SY5Y. (PMID:12675130)
• study demonstrates for the first time a selective and inducible expression of the recently discovered cortistatin, as well as somatostatin receptor 2, in human monocyte-derived cells (PMID:12684217)
• Expression of somatostatin receptor 2 by human pancreatic cancer causes significant slowing of tumor growth by a mechanism independent of exogenous somatostatin (PMID:14572771)
• Activation of SSTR 2 by SSTR 2 agonist significantly suppressed insulin secretion. (PMID:14576502)
• Sst2 and sst5 were expressed in 70%, sst1 in 50%, and sst3 and sst4 subtypes only in 15-20% of insulinomas (PMID:14602773)
• The receptor from somatostatinoma was completely phosphorylated. Only unphosphorylated sst2A was present in human tumors not exposed to autocrine stimulation. (PMID:14671213)
• SST2R gene together with p53 and ras genes may participate in pancreatic cancerous angiogenesis. (PMID:14695784)
• Expression of reintroduced human SSTR2 gene exerts its antiangiogenic effects by down-regulating expressions of factors involved in tumor angiogenesis and metastasis, suggesting SSTR2 gene transfer as new strategy of gene therapy for pancreatic cancer. (PMID:14760765)
• The degree (or level) of sst2 and sst5 expression is critical for the ultimate GH response of somatotropinomas to endogenous SRIF tone and exogenous SRIF analogue therapy. (PMID:15118275)
• Epithelial sst2A cells, identified as neuroendocrine, gastrin-producing cells, were found in large numbers in the antrum and the duodenum, but not in the gastric corpus. (PMID:15153427)
• SSTR2 provides an anti-angiogenic effect on pancreatic cancer xenografts, susgesting gene transfer as a promising strategy of gene therapy for pancreatic cancer. (PMID:15205362)
• human somatostatin receptor 2 dimers have a role in receptor trafficking (PMID:15231824)
• Expression of the SSTR2 gene in pancreatic adenocarcinoma cells induces apoptosis, which may be mediated via down-regulation of Bcl-2 & up-regulation of Bax (alteration of Bcl-2/Bax ratio) & inhibits tumor angiogenesis, inhibiting of tumor growth. (PMID:15257106)
• gene transfer into pancreatic neoplasm cells resulted in no apoptosis, but a significant cell proliferation inhibition (PMID:15754023)
• SSTR2 and SSTR5 variants seem to have a minor role in determining the responsiveness to somatostatin analogs in acromegaly (PMID:15914528)
• activation of the IKK/NFkappaB signaling cascade by SSTR2 requires a complicated network consisting of Galpha(14), protein kinase C, CamkII, ERK, and c-Src (PMID:16115892)
• In the temporal lobe epilepsy, dentate gyrus, sst2 receptor mRNA expression was strongly increased in the granule cell layer, sst2 receptor-binding sites and immunoreactivity was preserved in the inner but decreased in the outer molecular layer. (PMID:16254490)
• the subtype 2 receptor-mediated antiproliferative effect of SRIH on TT cell proliferation may be exerted through a decrease in cyclin D1 and cdk4 levels (PMID:16601140)
• Sst2 sensitized NIH3T3 cells to TNFalpha-induced apoptosis, enhanced TNFalpha-mediated activation of NF-kappaB, resulting in JNK inhibition and subsequent executioner caspase activation and cell death. (PMID:16645635)
• Physical interaction between a sst2 and p85, revealing a novel mechanism for negative regulation by ligand-activated GPCR of PI3K-dependent survival pathways, which may be an important molecular target for antineoplastic therapy. (PMID:16917505)
• Cytostatic action exerted by SSTR2 analogs might account for the tumor shrinkage observed in acromegalic patients treated with long-acting somatostatin analogs. (PMID:16954443)
• results show that Somatostatin receptor 2 is predominantly expressed on thyroid tissue and is a valid target for treatment of thyroid tumours (PMID:16996150)
• We conclude that the somatostatin receptor plays a role in the total renal uptake of radiolabelled somatostatin analogues. (PMID:17546456)
• Somatostatin caused rapid sst(2a) receptor phosphorylation and desensitization of epithelial antisecretory responses. (PMID:17603546)
• 17q gain and promoter polymorphisms can play a role into the regulation of sst2 expression in neuroblastomas (PMID:17678886)
• The functional interactions between human somatostatin receptor 2 (hSSTR2) and human dopamine receptor 2 (hD2R) in both co-transfected CHO-K1 or HEK-293 cells as well as in cultured neuronal cells which express both the receptors endogenously. (PMID:17706924)
• Analysis of orbital tissues reveals upregulation of SSTR1 and -2 in a group of Graves’ ophthalmopathy (GO) patients. Adipogenesis, a process occurring in GO orbits, provides one possible explanation for some of the observed increase. (PMID:17848636)
• Sst(2) is the best target for visualization of neuroendocrine tumors(NE) tumors, whereas noradrenaline transporter is only a useful target in a subpopulation of NE tumors. (PMID:18196892)
• This study was undertaken to investigate molecular mechanism of transcriptional regulation of the human sst2 gene, for which an additional exon (exon 1) in the 5’-untranslated region was recently found. (PMID:18234910)
• sst2 was expressed in 67% of the patients with HCC (PMID:18292657)
• Existence of a novel upstream promoter for the hSSTR2 gene that is regulated by epigenetic modifications, suggesting for complex control of the hSSTR2 transcription. (PMID:18325993)
• SSTR2 is the predominant mediator of functional ocular antiangiogenic effects. (PMID:18599562)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	sstr2a	ENSDARG00000059090
danio_rerio	sstr2b	ENSDARG00000069806
mus_musculus	Sstr2	ENSMUSG00000047904
rattus_norvegicus	Sstr2	ENSRNOG00000002793
drosophila_melanogaster	AstC-R2	FBGN0036789

Paralogs (17): OPRK1 (ENSG00000082556), OPRM1 (ENSG00000112038), KISS1R (ENSG00000116014), OPRD1 (ENSG00000116329), OPRL1 (ENSG00000125510), NPBWR2 (ENSG00000125522), SSTR4 (ENSG00000132671), SSTR1 (ENSG00000139874), SSTR5 (ENSG00000162009), GPR149 (ENSG00000174948), UTS2R (ENSG00000181408), PTGDR2 (ENSG00000183134), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Somatostatin receptor type 2 — P30874 (reviewed: P30874)

Alternative names: SRIF-1

All UniProt accessions (1): P30874

UniProt curated annotations — full annotation on UniProt →

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.

Subunit / interactions. Homodimer and heterodimer with SSTR3 and SSTR5. Heterodimerization with SSTR3 inactivates SSTR3 receptor function. Heterodimerization with SSTR5 is enhanced by agonist stimulation of SSTR2 and increases SSTR2 cell growth inhibition activity. Following agonist stimulation, homodimers dissociate into monomers which is required for receptor internalization. Interacts with beta-arrestin; this interaction is necessary for receptor internalization and is destabilized by heterodimerization with SSTR5 which results in increased recycling of SSTR2 to the cell surface. Interacts (via C-terminus) with SHANK1 (via PDZ domain).

Subcellular location. Cell membrane. Cytoplasm.

Tissue specificity. Expressed in both pancreatic alpha- and beta-cells (at protein level). Expressed at higher levels in the pancreas than other somatostatin receptors. Also expressed in the cerebrum and kidney and, in lesser amounts, in the jejunum, colon and liver. In the developing nervous system, expressed in the cortex where it is located in the preplate at early stages and is enriched in the outer part of the germinal zone at later stages. In the cerebellum, expressed in the deep part of the external granular layer at gestational week 19. This pattern persists until birth but disappears at adulthood.

Post-translational modifications. Phosphorylated on serine and threonine residues in response to agonist stimulation, leading to receptor desensitization and rapid internalization. Phosphorylated to a greater extent on serine than threonine residues. Threonine phosphorylation is required for arrestin binding and receptor endocytosis but is not necessary for desensitization.

Similarity. Belongs to the G-protein coupled receptor 1 family.

Isoforms (2)

UniProt ID	Names	Canonical?
P30874-1	A, SSTR2A	yes
P30874-2	B, SSTR2B

RefSeq proteins (1): NP_001041* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000586	Somatstn_rcpt	Family
IPR002074	Somatstn_rcpt_2	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (65 total): helix 17, topological domain 8, mutagenesis site 8, transmembrane region 7, modified residue 5, strand 5, glycosylation site 4, sequence conflict 3, turn 3, chain 1, site 1, lipid moiety-binding region 1, disulfide bond 1, splice variant 1

Structure

Experimental structures (PDB)

17 structures.

PDB	Method	Resolution (Å)
7T10	ELECTRON MICROSCOPY	2.5
7XN9	X-RAY DIFFRACTION	2.6
7XNA	X-RAY DIFFRACTION	2.65
7T11	ELECTRON MICROSCOPY	2.7
7WIG	ELECTRON MICROSCOPY	2.7
7WIC	ELECTRON MICROSCOPY	2.8
7XAT	ELECTRON MICROSCOPY	2.85
7XAV	ELECTRON MICROSCOPY	2.87
7XAU	ELECTRON MICROSCOPY	2.97
7UL5	ELECTRON MICROSCOPY	3.1
7XMR	ELECTRON MICROSCOPY	3.1
7YAC	ELECTRON MICROSCOPY	3.24
7Y24	ELECTRON MICROSCOPY	3.25
7Y26	ELECTRON MICROSCOPY	3.3
7YAE	ELECTRON MICROSCOPY	3.37
7Y27	ELECTRON MICROSCOPY	3.48
7WJ5	ELECTRON MICROSCOPY	3.72

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P30874-F1	81.75	0.54

Antibody-complex structures (SAbDab): 14 — 7T10, 7T11, 7UL5, 7WIC, 7WIG, 7WJ5, 7XAT, 7XAU, 7XAV, 7Y24, 7Y26, 7Y27, 7YAC, 7YAE

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Catalytic / active sites (1): 89 (important for ligand binding)

Post-translational modifications (6): 341, 343, 348, 353, 354, 328

Disulfide bonds (1): 115–193

Glycosylation sites (4): 9, 22, 29, 32

Mutagenesis-validated functional residues (8):

Position	Phenotype
89	expression levels reduced by 60%.
89	expression levels reduced by 80%.
89	slightly reduced expression levels. remains localized in membrane. abolishes ligand binding and g protein-mediated calci
139	expression levels reduced by 50%. significantly reduced ligand binding capacity but increased affinity. reduced g protei
139	expression levels reduced by 40%. no significant change in ligand binding capacity or affinity. reduced g protein-mediat
140	slightly reduced expression levels. no significant change in ligand binding capacity or affinity. no significant change
140	almost abolishes expression. abolishes membrane localization.
140	slightly reduced expression levels. significantly reduced ligand binding capacity but increased affinity. reduced g prot

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

ID	Pathway
R-HSA-375276	Peptide ligand-binding receptors
R-HSA-418594	G alpha (i) signalling events
R-HSA-162582	Signal Transduction
R-HSA-372790	Signaling by GPCR
R-HSA-373076	Class A/1 (Rhodopsin-like receptors)
R-HSA-388396	GPCR downstream signalling
R-HSA-500792	GPCR ligand binding

MSigDB gene sets: 176 (showing top): BENPORATH_ES_WITH_H3K27ME3, GOBP_RESPONSE_TO_ESTRADIOL, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_RESPONSE_TO_CORTICOSTEROID, MODULE_64, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, CREB_Q4, MODULE_66, GOBP_ADENYLATE_CYCLASE_MODULATING_G_PROTEIN_COUPLED_RECEPTOR_SIGNALING_PATHWAY, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_HORMONE_MEDIATED_SIGNALING_PATHWAY, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, MODULE_379, GOBP_CELLULAR_RESPONSE_TO_CORTICOSTEROID_STIMULUS, SHETH_LIVER_CANCER_VS_TXNIP_LOSS_PAM1

GO Biological Process (9): G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger (GO:0007187), adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway (GO:0007193), neuropeptide signaling pathway (GO:0007218), negative regulation of cell population proliferation (GO:0008285), cellular response to glucocorticoid stimulus (GO:0071385), cellular response to estradiol stimulus (GO:0071392), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), somatostatin signaling pathway (GO:0038170)

GO Molecular Function (5): somatostatin receptor activity (GO:0004994), PDZ domain binding (GO:0030165), neuropeptide binding (GO:0042923), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)

GO Cellular Component (6): nucleoplasm (GO:0005654), cytosol (GO:0005829), plasma membrane (GO:0005886), neuron projection (GO:0043005), cytoplasm (GO:0005737), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Signaling by GPCR	2
Class A/1 (Rhodopsin-like receptors)	1
GPCR downstream signalling	1
Signal Transduction	1
GPCR ligand binding	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
cellular anatomical structure	4
G protein-coupled receptor signaling pathway	3
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	1
adenylate cyclase inhibitor activity	1
cell population proliferation	1
regulation of cell population proliferation	1
negative regulation of cellular process	1
response to glucocorticoid	1
cellular response to corticosteroid stimulus	1
response to estradiol	1
cellular response to lipid	1
cellular response to oxygen-containing compound	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
hormone-mediated signaling pathway	1
somatostatin receptor signaling pathway	1
neuropeptide receptor activity	1
somatostatin signaling pathway	1
protein domain specific binding	1
peptide binding	1
transmembrane signaling receptor activity	1
binding	1
nuclear lumen	1
cytoplasm	1
membrane	1
cell periphery	1
plasma membrane bounded cell projection	1
intracellular anatomical structure	1

Protein interactions and networks

STRING

1212 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SSTR2	SST	P01166	999
SSTR2	DRD2	P14416	821
SSTR2	CORT	O00230	717
SSTR2	HIVEP2	P31629	702
SSTR2	GAST	P01350	699
SSTR2	CHGA	P10645	621
SSTR2	GCG	P01275	600
SSTR2	TCF4	P15884	548
SSTR2	GHRH	P01286	519
SSTR2	POMC	P01189	513
SSTR2	GAL	P22466	512
SSTR2	UTS2B	Q765I0	512
SSTR2	MEN1	O00255	508
SSTR2	FOLH1	Q04609	507
SSTR2	SNED1	Q8TER0	507

IntAct

19 interactions, top by confidence:

A	B	Type	Score
PIK3R1	SSTR2	psi-mi:“MI:0407”(direct interaction)	0.640
PIK3R1	SSTR2	psi-mi:“MI:0915”(physical association)	0.640
SSTR2	PIK3R1	psi-mi:“MI:0915”(physical association)	0.640
SSTR5	SSTR2	psi-mi:“MI:0915”(physical association)	0.520
SSTR5	SSTR2	psi-mi:“MI:2364”(proximity)	0.520
SSTR5	SSTR2	psi-mi:“MI:0403”(colocalization)	0.520
SSTR2	SSTR3	psi-mi:“MI:0915”(physical association)	0.520
SSTR2	SSTR3	psi-mi:“MI:2364”(proximity)	0.520
SSTR3	SSTR2	psi-mi:“MI:0403”(colocalization)	0.520
ARRB2	SSTR2	psi-mi:“MI:0403”(colocalization)	0.430
RAMP1	SSTR2	psi-mi:“MI:0915”(physical association)	0.400
SSTR2	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	SSTR2	psi-mi:“MI:0915”(physical association)	0.400
SSTR2	PJA2	psi-mi:“MI:0914”(association)	0.350

BioGRID (15): SSTR2 (Protein-peptide), SSTR2 (Reconstituted Complex), PIK3R1 (Affinity Capture-MS), PIK3R1 (Affinity Capture-Western), SSTR2 (FRET), SSTR2 (Affinity Capture-Western), SSTR2 (Reconstituted Complex), SSTR2 (Reconstituted Complex), SHANK1 (Affinity Capture-Western), SSTR2 (Affinity Capture-Western), SSTR2 (Protein-peptide), SSTR2 (Affinity Capture-MS), SSTR2 (Co-fractionation), SSTR2 (Affinity Capture-RNA), APP (Reconstituted Complex)

ESM2 similar proteins: A0A287A2K5, F1MV99, O08858, O42179, P28646, P30552, P30553, P30680, P30796, P30872, P30873, P30874, P30875, P30936, P30937, P30938, P31391, P32239, P32300, P32745, P33533, P33534, P33535, P34975, P34993, P34994, P35346, P35370, P35377, P41143, P41144, P41145, P41146, P42866, P46627, P47748, P48145, P48146, P49660, P49681

Diamond homologs: A0T2N3, F1MV99, O00155, O00590, O08707, O08858, O09027, O35210, O77590, O88410, O89039, O97666, P0C5I1, P0C7U4, P11613, P21109, P25024, P25025, P25095, P25104, P25106, P29089, P29754, P29755, P30555, P30556, P30680, P30874, P30875, P30935, P30936, P30937, P30938, P31391, P32303, P32745, P33396, P33535, P34976, P34993

SIGNOR signaling

7 interactions.

A	Effect	B	Mechanism
SSTR2	“up-regulates activity”	GNAI1	binding
SSTR2	“up-regulates activity”	GNAI3	binding
SSTR2	“up-regulates activity”	GNA14	binding
somatostatin	“up-regulates activity”	SSTR2	“chemical activation”
lanreotide	“up-regulates activity”	SSTR2	“chemical activation”
HIVEP2	“up-regulates quantity by expression”	SSTR2	“transcriptional regulation”
TCF4	“up-regulates quantity by expression”	SSTR2	“transcriptional regulation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

40 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	38
Likely benign	2
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

484 predictions. Top by Δscore:

Variant	Effect	Δscore
17:73165289:G:C	donor_loss	1.0000
17:73171615:GGCAT:G	donor_gain	1.0000
17:73165289:G:GG	donor_gain	0.9900
17:73171616:GCAT:G	donor_gain	0.9900
17:73169227:GAT:G	acceptor_gain	0.9800
17:73174310:T:TA	acceptor_gain	0.9800
17:73170422:G:GG	donor_gain	0.9700
17:73171612:C:G	donor_gain	0.9700
17:73169222:TTCCA:T	acceptor_loss	0.9600
17:73169223:TCCA:T	acceptor_loss	0.9600
17:73169224:CCA:C	acceptor_loss	0.9600
17:73169225:CA:C	acceptor_loss	0.9600
17:73169226:A:G	acceptor_loss	0.9600
17:73174310:T:G	acceptor_gain	0.9600
17:73169226:A:AG	acceptor_gain	0.9400
17:73169227:G:GG	acceptor_gain	0.9400
17:73171666:A:AG	donor_gain	0.9300
17:73174309:AT:A	acceptor_gain	0.9200
17:73174309:ATGAT:A	acceptor_gain	0.9200
17:73166299:G:GT	donor_gain	0.8900
17:73170421:A:AG	donor_gain	0.8900
17:73165287:AG:A	donor_gain	0.8400
17:73165288:GG:G	donor_gain	0.8400
17:73174313:T:TA	acceptor_gain	0.8200
17:73166291:GCCC:G	donor_gain	0.8100
17:73166300:G:T	donor_gain	0.8000
17:73169227:GA:G	acceptor_gain	0.7900
17:73169227:GATGT:G	acceptor_gain	0.7800
17:73174309:A:AG	acceptor_gain	0.7800
17:73171001:G:GG	donor_gain	0.7700

AlphaMissense

2440 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
17:73169488:G:A	G57R	0.999
17:73169488:G:C	G57R	0.999
17:73169488:G:T	G57W	0.999
17:73169489:G:A	G57E	0.999
17:73169502:C:A	N61K	0.999
17:73169502:C:G	N61K	0.999
17:73169573:T:C	L85P	0.999
17:73169584:G:C	D89H	0.999
17:73169585:A:C	D89A	0.999
17:73169643:G:C	W108C	0.999
17:73169643:G:T	W108C	0.999
17:73169704:A:C	S129R	0.999
17:73169706:C:A	S129R	0.999
17:73169706:C:G	S129R	0.999
17:73169717:T:C	L133P	0.999
17:73169728:A:C	S137R	0.999
17:73169730:C:A	S137R	0.999
17:73169730:C:G	S137R	0.999
17:73169735:A:C	D139A	0.999
17:73169735:A:T	D139V	0.999
17:73169738:G:C	R140P	0.999
17:73169818:T:A	W167R	0.999
17:73169818:T:C	W167R	0.999
17:73169896:T:A	C193S	0.999
17:73169897:G:C	C193S	0.999
17:73170112:T:C	F265L	0.999
17:73170114:C:A	F265L	0.999
17:73170114:C:G	F265L	0.999
17:73170244:C:T	P309S	0.999
17:73170245:C:A	P309H	0.999

dbSNP variants (sampled 300 via entrez): RS1000010817 (17:73165518 C>CTGTGGGTAGAG), RS1000234307 (17:73170732 G>T), RS1000446017 (17:73176354 C>A,T), RS1000497807 (17:73163931 G>T), RS1000656563 (17:73164411 G>A), RS1000959684 (17:73170819 A>G), RS1001339582 (17:73163488 T>A), RS1001497716 (17:73169882 G>A,C,T), RS1001545849 (17:73174932 C>T), RS1001557447 (17:73175900 G>T), RS1001641912 (17:73168266 C>A,G,T), RS1001850859 (17:73170291 G>A), RS1001880383 (17:73163183 C>A), RS1001982169 (17:73170150 T>C), RS1002010280 (17:73163558 C>T)

Disease associations

OMIM: gene MIM:182452 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST004735_39	Epstein-Barr virus copy number in lymphoblastoid cell lines	3.000000e-06
GCST009391_381	Metabolite levels	8.000000e-07
GCST009391_953	Metabolite levels	5.000000e-06

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0010437	triacylglycerol 58:10 measurement
EFO:0010443	triacylglycerol 58:9 measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL1804 (SINGLE PROTEIN), CHEMBL2111436 (PROTEIN FAMILY), CHEMBL4296070 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

11 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 20,098 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1201185	LANREOTIDE	4	177
CHEMBL1680	OCTREOTIDE	4	999
CHEMBL262135	GALLIUM OXODOTREOTIDE	4
CHEMBL3349607	PASIREOTIDE	4	109
CHEMBL1823872	SOMATOSTATIN	3	2,276
CHEMBL3349523	VAPREOTIDE	3	14,736
CHEMBL408350	EDOTREOTIDE	3	880
CHEMBL5267842	PALTUSOTINE	3	87
CHEMBL311695	SEGLITIDE	2	820
CHEMBL386768	EDOTREOTIDE YTTRIUM	2
CHEMBL5314924	MK-8189	2	14

PharmGKB: 1 entry (VIP=true, CPIC=false)

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: gpcr — Somatostatin receptors

Most potent curated ligand interactions (77 total), top 25:

Ligand	Action	Affinity	Parameter
L-363,409	Full agonist	12.0	pIC50
L-054,522	Full agonist	11.0	pKi
BIM 23027	Agonist	10.85	pIC50
EC 5-21	Full agonist	10.6	pKi
NC 8-12	Full agonist	10.6	pKi
SRIF-14	Full agonist	10.5	pKi
L-779,976	Full agonist	10.3	pKi
seglitide	Full agonist	10.3	pKi
SRIF-28	Full agonist	10.2	pKi
vapreotide	Full agonist	10.1	pKi
[125I]LTT-SRIF-28	Full agonist	10.0	pKd
octreotide	Full agonist	9.9	pKi
[125I]CGP 23996	Full agonist	9.8	pKd
[Ga-DOTA,Tyr3,Thr8]octreotide	Full agonist	9.7	pIC50
BIM 23197	Full agonist	9.7	pIC50
[125I]BIM23027	Full agonist	9.7	pIC50
paltusotine	Agonist	9.6	pEC50
lanreotide	Full agonist	9.6	pKi
DC 23-60	Full agonist	9.6	pKi
[125I]MK-678	Full agonist	9.6	pKd
BASS antagonist	Antagonist	9.52	pKi
[125I]Tyr10-CST14	Full agonist	9.4	pKd
BIM 23023	Full agonist	9.4	pKi
BIM 23059	Full agonist	9.4	pKi
[125I][Tyr3,Thr8]octreotide	Full agonist	9.33	pIC50

Binding affinities (BindingDB)

219 measured of 448 human assays (448 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[[(2R,3S)-2-[[4-[(2-Oxo-2,3-dihydro-1H-benzimidazole)-1-yl]piperidino]carbonylamino]-3-(1H-indole-3-yl)butyryl]amino]-6-aminohexanoic acid tert-butyl ester	KI	0.01 nM
somatostatin-28	KI	0.07 nM
L-Ser-L-Ala-L-Asn-L-Ser-L-Asn-L-Pro-L-Ala-L-Met-L-Ala-L-Pro-L-Arg-L-Glu-L-Arg-L-Lys-L-Ala-Gly-L-Cys(1)-L-Lys-L-Asn-L-Phe-L-Phe-L-Trp-L-Lys-L-Thr-L-Phe-L-Thr-L-Ser-L-Cys(1)-OH	KI	0.07 nM
15-28-Somatostatin-28	KI	0.1 nM
SRIF-D-Trp8	KI	0.23 nM
Cortistatin	KI	0.25 nM
Leu8, D-Trp22, Tyr25 SST-28	KI	0.41 nM
LTT-SRIF28	KI	0.52 nM
4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-3-(4,6-difluoro-1H-benzimidazol-2-yl)-5-(3,5-difluorophenyl)pyridin-2-amine	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-3-(4,6-difluoro-1H-benzimidazol-2-yl)-5-(3-fluorophenyl)pyridin-2-amine	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-3-(4,6-difluoro-1H-benzimidazol-2-yl)-5-(3,5-difluorophenyl)-N-methylpyridin-2-amine	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-5-(3-fluorophenyl)pyridin-2-amine	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-5-(3-fluorophenyl)-N-methylpyridin-2-amine	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
2-[4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-2-amino-5-(3-fluorophenyl)-3-pyridinyl]-7-methoxy-3H-benzimidazole-5-carbonitrile	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-5-(3-chloro-5-fluorophenyl)-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-N-methylpyridin-2-amine	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
2-[4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-2-amino-5-(3,5-difluorophenyl)-3-pyridinyl]-7-methoxy-3H-benzimidazole-5-carbonitrile	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
2-[4-(1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl)-2-amino-5-(3,5-difluorophenyl)-3-pyridinyl]-7-fluoro-3H-benzimidazole-5-carbonitrile	EC50	0.55 nM	US-10696689: Somatostatin modulators and uses thereof
4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-3-(4,6-difluoro-1H-benzimidazol-2-yl)-5-(3,5-difluorophenyl)pyridin-2-amine	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-3-(4,6-difluoro-1H-benzimidazol-2-yl)-5-(3-fluorophenyl)pyridin-2-amine	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-3-(4,6-difluoro-1H-benzimidazol-2-yl)-5-(3,5-difluorophenyl)-N-methylpyridin-2-amine	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-5-(3-fluorophenyl)pyridin-2-amine	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-5-(3-fluorophenyl)-N-methylpyridin-2-amine	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
2-[4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-2-amino-5-(3-fluorophenyl)-3-pyridinyl]-7-methoxy-3H-benzimidazole-5-carbonitrile	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-5-(3-chloro-5-fluorophenyl)-3-(6-fluoro-4-methoxy-1H-benzimidazol-2-yl)-N-methylpyridin-2-amine	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
2-[4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-2-amino-5-(3,5-difluorophenyl)-3-pyridinyl]-7-methoxy-3H-benzimidazole-5-carbonitrile	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
2-[4-[(4aS,8aS)-1,2,3,4a,5,7,8,8a-octahydropyrido[3,4-b][1,4]oxazin-6-yl]-2-amino-5-(3,5-difluorophenyl)-3-pyridinyl]-7-fluoro-3H-benzimidazole-5-carbonitrile	EC50	0.55 nM	US-11186590: Somatostatin modulators and uses thereof
SRIF-14	KI	0.63 nM
SS-25	KI	0.79 nM
Cortistatin(1-14)	KI	0.85 nM
Tyr10-cortistatin	KI	0.91 nM
CST14-Tyr10	KI	0.91 nM
L-797591	KI	1.4 nM
CH-275	KI	1.8 nM
CAS_183658-72-2	KI	2.63 nM
L-817,818	KI	3.3 nM
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[4-[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]butylamino]-14-(4-aminobutyl)-5,8-dibenzyl-20-[(4-fluorophenyl)methyl]-17-[(1R)-1-hydroxyethyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	6.9 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(2R)-1-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-3,15,18-tribenzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]acetamide	KI	8.5 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[3-[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]propylamino]-14-(4-aminobutyl)-5,8-dibenzyl-20-[(4-fluorophenyl)methyl]-17-[(1R)-1-hydroxyethyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	10.8 nM	US-8952128: Somatostatin-dopamine chimeric analogs
octreotide	KI	12 nM
N-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methyl]-N-[3-[[(2R)-1-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-15,18-dibenzyl-21-(3-carbamimidamidopropyl)-3-[(4-fluorophenyl)methyl]-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]amino]propyl]acetamide	KI	14 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(2S)-1-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-15,18-dibenzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]acetamide	KI	15 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]ethylamino]-14-(4-aminobutyl)-5,8-dibenzyl-20-[(3,4-difluorophenyl)methyl]-17-[(1R)-1-hydroxyethyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	16.9 nM	US-8952128: Somatostatin-dopamine chimeric analogs
BIM 23268	KI	18.4 nM
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[3-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfonyl]propylamino]-14-(4-aminobutyl)-5,8-dibenzyl-20-[(4-fluorophenyl)methyl]-17-[(1R)-1-hydroxyethyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	19.4 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfinyl]-N-[(5S)-5-[[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfinyl]acetyl]amino]-6-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-18-benzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-15-(pyridin-4-ylmethyl)-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]hexyl]acetamide	KI	22.5 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(2S)-1-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-3,15,18-tribenzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]acetamide	KI	24.2 nM	US-8952128: Somatostatin-dopamine chimeric analogs
(2R)-2-[[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]acetyl]amino]-N-[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-3,15,18-tribenzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]-3-(4-hydroxyphenyl)propanamide	KI	25.3 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]ethylamino]-14-(4-aminobutyl)-5,8-dibenzyl-20-[(3,5-difluorophenyl)methyl]-17-[(1R)-1-hydroxyethyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	25.4 nM	US-8952128: Somatostatin-dopamine chimeric analogs
H-c(Cys3-Phe6-Phe7-DTrp8-Lys9-Thr10-Phe11-Cys14)-OH	KI	28 nM
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(2S)-1-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-15,18-dibenzyl-21-(3-carbamimidamidopropyl)-3-[(4-fluorophenyl)methyl]-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]acetamide	KI	28.5 nM	US-8952128: Somatostatin-dopamine chimeric analogs

ChEMBL bioactivities

1232 potent at pChembl≥5 of 1256 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
11.00	Ki	0.01	nM	CHEMBL99895
10.89	Ki	0.013	nM	CHEMBL4590517
10.89	EC50	0.013	nM	CHEMBL4861425
10.89	EC50	0.013	nM	CHEMBL4872591
10.89	EC50	0.013	nM	CHEMBL4866325
10.85	EC50	0.014	nM	CHEMBL4849848
10.82	Ki	0.015	nM	CHEMBL4541310
10.82	Ki	0.015	nM	CHEMBL4550617
10.82	Ki	0.015	nM	CHEMBL4584764
10.82	EC50	0.015	nM	CHEMBL4860633
10.77	EC50	0.017	nM	CHEMBL4873269
10.74	Ki	0.018	nM	CHEMBL4564727
10.72	EC50	0.019	nM	CHEMBL4853282
10.70	IC50	0.02	nM	CHEMBL3350037
10.70	Ki	0.02	nM	CHEMBL3647695
10.70	Ki	0.02	nM	CHEMBL3647691
10.70	Ki	0.02	nM	CHEMBL3647696
10.66	Ki	0.022	nM	CHEMBL4527856
10.60	Ki	0.025	nM	CHEMBL1766100
10.60	Ki	0.025	nM	CHEMBL1766103
10.57	EC50	0.027	nM	CHEMBL4858892
10.52	Ki	0.03	nM	CHEMBL4299281
10.52	EC50	0.03	nM	CHEMBL4863880
10.52	EC50	0.03	nM	OCTREOTIDE
10.46	Ki	0.035	nM	SOMATOSTATIN
10.43	Ki	0.037	nM	CHEMBL1766097
10.42	Ki	0.038	nM	CHEMBL1766099
10.40	Ki	0.04	nM	CHEMBL3647673
10.40	Ki	0.04	nM	CHEMBL3647704
10.40	Ki	0.04	nM	CHEMBL3647689
10.40	Ki	0.04	nM	CHEMBL3647692
10.40	EC50	0.04	nM	CHEMBL4845867
10.40	Ki	0.04	nM	CHEMBL408362
10.40	Ki	0.04	nM	SOMATOSTATIN
10.39	EC50	0.041	nM	CHEMBL4870834
10.32	EC50	0.048	nM	CHEMBL4862195
10.31	Ki	0.049	nM	SOMATOSTATIN
10.30	Ki	0.05	nM	CHEMBL4110066
10.30	Ki	0.05	nM	CHEMBL3647690
10.30	Ki	0.05	nM	CHEMBL3647700
10.28	Ki	0.053	nM	CHEMBL3350037
10.22	Ki	0.06	nM	CHEMBL3647688
10.21	Ki	0.061	nM	CHEMBL4592483
10.21	Ki	0.062	nM	CHEMBL1766109
10.12	Ki	0.075	nM	CHEMBL4581874
10.11	EC50	0.078	nM	CHEMBL4876263
10.10	Ki	0.08	nM	CHEMBL3647693
10.10	Ki	0.08	nM	CHEMBL3647699
10.10	Ki	0.08	nM	CHEMBL3647684
10.10	EC50	0.08	nM	CHEMBL4851978

PubChem BioAssay actives

973 with measured affinity, of 1536 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
N-[4-(4-aminopiperidin-1-yl)-5-(3,5-dimethylphenyl)-3-pyridinyl]-3,5-dimethylbenzamide	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
1-[3-(3-fluoro-5-methoxyphenyl)-5-(6-methyl-1H-benzimidazol-2-yl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
1-[3-(6-fluoro-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methylphenyl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
(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	254874: Inhibitory concentration against human somatostatin receptor type 2 in CC531 cells	ic50	<0.0001	uM
(4S,7S,10R,13R,16R,19R,22S,25R,28R,31R,34S,37S)-37-[[2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-1-[(2R)-4-amino-2-[[(2R)-2-[[(2R)-4-amino-2-[[(2R)-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-carbamimidamidopentanoyl]amino]-4-carboxybutanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]propanoyl]amino]acetyl]amino]-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-16,22-bis[(1R)-1-hydroxyethyl]-10-[(1S)-1-hydroxyethyl]-7-(hydroxymethyl)-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	1288210: Displacement of [125I]tyr11-SRIF from human sst2 receptor after 60 mins by liquid scintillation counting method	ki	<0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[[(2R)-3-amino-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-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-carbonyl]amino]-3-oxopropyl]disulfanyl]propanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	<0.0001	uM
(2S,3R)-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-[3-[[3-[[(2S)-1-[[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl]oxy]-1-oxopropan-2-yl]-methylamino]-3-oxopropyl]disulfanyl]propylamino]-3-phenylpropanoyl]amino]-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-carbonyl]amino]-3-hydroxybutanoic acid	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	<0.0001	uM
(2S,3R)-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-[4-[2-[[3-[[(2S)-1-[[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl]oxy]-1-oxopropan-2-yl]-methylamino]-3-oxopropyl]disulfanyl]ethoxy]phenyl]propanoyl]amino]-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-carbonyl]amino]-3-hydroxybutanoic acid	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	<0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[[(2R)-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-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-carbonyl]amino]-3-hydroxypropyl]disulfanyl]propanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	<0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[[(3R)-4-amino-3-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-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-carbonyl]amino]-2-methyl-4-oxobutan-2-yl]disulfanyl]propanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	<0.0001	uM
(2R)-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-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-carbonyl]amino]-3-[[3-[[(2S)-1-[[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl]oxy]-1-oxopropan-2-yl]-methylamino]-3-oxopropyl]disulfanyl]propanoic acid	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	<0.0001	uM
tert-butyl (2S)-6-amino-2-[[(2R,3S)-3-(1H-indol-3-yl)-2-[[4-(2-oxo-3H-benzimidazol-1-yl)piperidine-1-carbonyl]amino]butanoyl]amino]hexanoate	1954038: Binding affinity to human somatostatin receptor type 2	ki	<0.0001	uM
(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-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	1061946: Displacement of [125I]-somatostatin from human SSTR2 expressed in CHO-K1 cells	ki	<0.0001	uM
(4R,7S,10S,13S,16S,19S,22R,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-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	1061946: Displacement of [125I]-somatostatin from human SSTR2 expressed in CHO-K1 cells	ki	<0.0001	uM
1-[3-(3,5-dimethylphenyl)-5-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
1-[3-(6-chloro-1H-benzimidazol-2-yl)-5-(3,5-dimethylphenyl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
2-[4-(4-aminopiperidin-1-yl)-5-(3,5-dimethylphenyl)-3-pyridinyl]-3H-benzimidazole-5-carbonitrile	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
1-[3-(3,5-dimethoxyphenyl)-5-(6-methyl-1H-benzimidazol-2-yl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
1-[3-(3,5-dimethylphenyl)-5-(6-methyl-1H-benzimidazol-2-yl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
1-[3-(3,5-dimethylphenyl)-5-(6-fluoro-1H-benzimidazol-2-yl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
N-[4-(4-aminopiperidin-1-yl)-5-(3,5-dichlorophenyl)-3-pyridinyl]-2,5-dimethylpyrazole-3-carboxamide	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
4-[7-chloro-3-(3,5-dimethylphenyl)-4-[2-[(2R)-piperidin-2-yl]ethoxy]quinolin-6-yl]benzamide	593731: Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting	ki	<0.0001	uM
3-[7-chloro-3-(3,5-dimethylphenyl)-4-[2-[(2R)-piperidin-2-yl]ethoxy]quinolin-6-yl]phenol	593731: Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting	ki	<0.0001	uM
(4R,7S,10R,13S,16R,19S,22R,25S,28S,31S,34R,37S)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-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	203086: Binding affinity towards human sst2 receptor expressed in CHO-K1 cells	ki	<0.0001	uM
(4R,7S,10R,13S,16R,19S,22R,25S,28R,31S)-13,28-bis(4-aminobutyl)-25-(2-amino-2-oxoethyl)-31-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-19,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30-nonaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29-nonazacyclodotriacontane-4-carboxylic acid	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	<0.0001	uM
Octreotide	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
3-[4-(3-aminopropoxy)-7-chloro-3-(3,5-dimethylphenyl)quinolin-6-yl]phenol	593731: Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting	ki	<0.0001	uM
7-chloro-3-(3,5-dimethylphenyl)-6-(1-methylpyrazol-4-yl)-4-[2-[(2R)-piperidin-2-yl]ethoxy]quinoline	593731: Displacement of I125-somatostatin-14 from human SST2 expressed in CHO cells after 3 hrs by scintillation counting	ki	<0.0001	uM
4-(4-aminopiperidin-1-yl)-N,5-bis(3,5-dimethylphenyl)pyridine-3-carboxamide	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
1-[3-(4,6-dimethyl-1H-benzimidazol-2-yl)-5-(3,5-dimethylphenyl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	<0.0001	uM
1-[3-(1H-benzimidazol-2-yl)-5-(3,5-dimethylphenyl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	0.0001	uM
1-[3-(6-fluoro-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methoxyphenyl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	0.0001	uM
3-(3-chloro-5-methylphenyl)-6-(3-fluoro-5-hydroxyphenyl)-N,7-dimethyl-N-[[(2S)-pyrrolidin-2-yl]methyl]-4H-quinazoline-4-carboxamide	1675011: Agonist activity at SST2 (unknown origin)	ec50	0.0001	uM
6-(3-carbamoyl-5-fluorophenyl)-3-(3-chloro-5-methylphenyl)-N,7-dimethyl-N-[[(2S)-pyrrolidin-2-yl]methyl]-4H-quinazoline-4-carboxamide	1675016: Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation	ec50	0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[2-[[(2S,3R)-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-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-carbonyl]amino]-3-hydroxybutanoyl]amino]ethyldisulfanyl]propanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[3-[[(2R)-1-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-16-benzyl-4-[[(2R,3R)-1,3-dihydroxybutan-2-yl]carbamoyl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]propyldisulfanyl]propanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[1-[2-[[(2S)-3-amino-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-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-carbonyl]amino]-3-oxopropyl]amino]-2-oxoethyl]-2,5-dioxopyrrolidin-3-yl]sulfanylpropanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[[3-[4-[(2S,5S,8R,11S,14S,17S)-11-(4-aminobutyl)-17-benzyl-14-[(1R)-1-hydroxyethyl]-5-[(4-hydroxyphenyl)methyl]-8-(1H-indol-3-ylmethyl)-1-methyl-3,6,9,12,15,18-hexaoxo-1,4,7,10,13,16-hexazacyclooctadec-2-yl]butylamino]-3-oxopropyl]disulfanyl]propanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[1-[3-[[2-[[(2S)-2-[[(2S)-2-[[2-[6-[3-[3-[[(2R)-1-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-16-benzyl-4-[[(2R,3R)-1,3-dihydroxybutan-2-yl]carbamoyl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]propylsulfanyl]-2,5-dioxopyrrolidin-1-yl]hexanoylamino]acetyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]propyl]-2,5-dioxopyrrolidin-3-yl]sulfanylpropanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[[4-[[(2R)-3-amino-2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-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-carbonyl]amino]-3-oxopropyl]disulfanyl]-4-methylpentanoyl]-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	0.0001	uM
[(1S,2R,3S,5R,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[3-[2-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-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-carbonyl]amino]ethyldisulfanyl]propanoyl-methylamino]propanoate	1638693: Displacement of [125I]somatostatin from human SSTR2 expressed in CHO-K1 cell membranes after 240 mins	ki	0.0001	uM
(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-31-methyl-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-carboxamide	203409: Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0001	uM
(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-22-(1H-indol-3-ylmethyl)-7-methyl-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-carboxamide	203409: Binding affinity towards human Somatostatin receptor type 2 (sst2) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0001	uM
3-(3-chloro-5-methylphenyl)-6-(3-fluoro-2-hydroxyphenyl)-N,7-dimethyl-N-(pyrrolidin-2-ylmethyl)-4H-quinazoline-4-carboxamide	1675016: Agonist activity at human SST2 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP accumulation	ec50	0.0001	uM
N-[4-(4-aminopiperidin-1-yl)-5-(3,5-dichlorophenyl)-3-pyridinyl]-1-methyl-5-(trifluoromethyl)pyrazole-4-carboxamide	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	0.0001	uM
N-[4-(4-aminopiperidin-1-yl)-5-(3,5-dichlorophenyl)-3-pyridinyl]-1,3-dimethylpyrazole-4-carboxamide	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	0.0001	uM
N-[4-(4-aminopiperidin-1-yl)-5-(3,5-dichlorophenyl)-3-pyridinyl]imidazo[1,2-a]pyridine-2-carboxamide	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	0.0001	uM
1-[3-(3-chloro-5-fluorophenyl)-5-(6-fluoro-1H-benzimidazol-2-yl)-4-pyridinyl]piperidin-4-amine	1781889: Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay	ec50	0.0001	uM
3-[4-(4-aminopiperidin-1-yl)-3-(3-fluoro-5-methoxyphenyl)quinolin-6-yl]-2-hydroxybenzonitrile	1922701: Agonist activity at human SST2 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay	ec50	0.0001	uM
3-[4-(4-aminopiperidin-1-yl)-3-(3,5-difluorophenyl)quinolin-6-yl]benzamide	1922701: Agonist activity at human SST2 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay	ec50	0.0001	uM

CTD chemical–gene interactions

51 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	increases expression, affects expression, decreases expression	7
entinostat	increases expression, affects cotreatment	2
Benzo(a)pyrene	affects methylation, increases methylation	2
Phenylmercuric Acetate	affects cotreatment, decreases expression	2
Tretinoin	decreases expression	2
aristolochic acid I	increases expression	1
methylmercuric chloride	increases expression	1
propionaldehyde	increases expression	1
terbufos	increases methylation	1
butyraldehyde	increases expression	1
triadimefon	increases expression	1
S-(1,2-dichlorovinyl)cysteine	decreases reaction, increases expression	1
pentanal	increases expression	1
CGP 52608	affects binding, increases reaction	1
Edotreotide	affects binding, decreases reaction	1
AN 238	affects binding	1
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	affects cotreatment, increases expression, decreases expression	1
abrine	increases expression	1
111In-DOTA-TOC	affects binding	1
dorsomorphin	decreases expression, affects cotreatment, increases expression	1
pasireotide	affects binding	1
BIM 23120	decreases expression, increases activity, increases expression	1
64Cu-DOTA-Y3-TATE	affects binding, increases uptake	1
64Cu-CB-TE2A-Y3-TATE	affects cotreatment, decreases reaction, increases chemical synthesis, affects binding, increases uptake	1
64Cu-CB-TE2A-sst2-ANT	affects binding, increases uptake	1
4-(4-((5-(4,5-dimethyl-2-nitrophenyl)-2-furanyl)methylene)-4,5-dihydro-3-methyl-5-oxo-1H-pyrazol-1-yl)benzoic acid	increases expression	1
Celecoxib	increases expression	1
Arsenic Trioxide	decreases expression	1
Cyclic AMP	affects cotreatment, decreases reaction, increases chemical synthesis	1
Aldehydes	increases expression	1

ChEMBL screening assays

182 unique, capped per target: 149 binding, 28 functional, 5 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1007363	Binding	Binding affinity to human SSTR2A	A synthetic method for peptide-PEG-lipid conjugates: application of octreotide-PEG-DSPE synthesis. — Bioorg Med Chem Lett
CHEMBL1212342	Functional	Antagonist activity at human SST2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by FRET assay	Piperidinyl-nicotinamides as potent and selective somatostatin receptor subtype 5 antagonists. — Bioorg Med Chem Lett
CHEMBL4195974	ADMET	Drug uptake in HEK293 cells co-expressing SSTR2 (unknown origin) and RFP assessed as SSTR2-mediated drug accumulation by measuring mean fluorescence intensity measured after 30 mins by fluorescence microscopic analysis (Rvb = 1.1 No_unit)	New somatostatin-drug conjugates for effective targeting pancreatic cancer. — Bioorg Med Chem

Cellosaurus cell lines

9 cell lines: 5 cancer cell line, 4 spontaneously immortalized cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_D1QS	Abcam K-562 SSTR2 KO	Cancer cell line	Female
CVCL_D2MD	Abcam Raji SSTR2 KO	Cancer cell line	Male
CVCL_E2L2	HAP1 SSTR2 (-)	Cancer cell line	Male
CVCL_H500	CHO-K1/SST2/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV81	cAMP Hunter CHO-K1 SSTR2 Gi	Spontaneously immortalized cell line	Female
CVCL_KZ11	PathHunter CHO-K1 SSTR2 Activated GPCR Internalization	Spontaneously immortalized cell line	Female
CVCL_KZ12	PathHunter CHO-K1 SSTR2 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_WQ61	Abcam Jurkat SSTR2 KO	Cancer cell line	Male
CVCL_ZK22	Tango SSTR2-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

0 trials via MONDO — disease-level, not drug-specific.