SSTR5

Summary

SSTR5 (somatostatin receptor 5, HGNC:11334) is a protein-coding gene on chromosome 16p13.3, encoding Somatostatin receptor type 5 (P35346). Receptor for somatostatin 28 and to a lesser extent for somatostatin-14. In precision oncology, SSTR5 Overexpression confers sensitivity to Pasireotide in Neuroendocrine Tumor (CIViC Level B).

Somatostatin and its related peptide cortistatin exert multiple biological actions on normal and tumoral tissue targets by interacting with somatostatin receptors (SSTRs). The protein encoded by this gene is one of the SSTRs, which is a multi-pass membrane protein and belongs to the G-protein coupled receptor 1 family. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase, and different regions of this receptor molecule are required for the activation of different signaling pathways. A mutation in this gene results in somatostatin analog resistance. Alternatively spliced transcript variants have been identified in this gene.

Source: NCBI Gene 6755 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 105 total
• Druggable target: yes — 11 molecules with ChEMBL bioactivity
• Precision-oncology evidence (CIViC): 1 curated variant–drug association
• MANE Select transcript: NM_001172560

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11334
Approved symbol	SSTR5
Name	somatostatin receptor 5
Location	16p13.3
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000162009
Ensembl biotype	protein_coding
OMIM	182455
Entrez	6755

Gene structure

Transcript identifiers

Ensembl transcripts: 9 — 9 protein_coding

ENST00000293897, ENST00000689027, ENST00000711615, ENST00000711616, ENST00000886519, ENST00000964274, ENST00000964275, ENST00000964276, ENST00000964277

RefSeq mRNA: 2 — MANE Select: NM_001172560 NM_001053, NM_001172560

CCDS: CCDS10429

Canonical transcript exons

ENST00000689027 — 2 exons

Exon	Start	End
ENSE00003933921	1078842	1081454
ENSE00003935279	1072747	1072822

Expression profiles

Bgee: expression breadth broad, 75 present calls, max score 78.10.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.0964 / max 23.3876, expressed in 39 samples.

FANTOM5 promoters (3 alternative TSS)

Promoter ID	TPM avg	Samples expressed
152019	0.0918	38
152020	0.0028	1
152021	0.0017	2

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
tendon of biceps brachii	UBERON:0008188	78.10	silver quality
right atrium auricular region	UBERON:0006631	75.42	gold quality
cardiac atrium	UBERON:0002081	74.53	gold quality
apex of heart	UBERON:0002098	72.11	gold quality
adenohypophysis	UBERON:0002196	71.74	gold quality
pituitary gland	UBERON:0000007	71.45	gold quality
right adrenal gland cortex	UBERON:0035827	69.79	gold quality
buccal mucosa cell	CL:0002336	69.51	silver quality
heart left ventricle	UBERON:0002084	69.41	gold quality
cardiac ventricle	UBERON:0002082	68.80	gold quality
descending thoracic aorta	UBERON:0002345	68.27	gold quality
left adrenal gland cortex	UBERON:0035825	67.21	gold quality
thoracic aorta	UBERON:0001515	66.68	gold quality
ascending aorta	UBERON:0001496	66.58	gold quality
heart	UBERON:0000948	66.30	gold quality
right adrenal gland	UBERON:0001233	66.12	gold quality
left adrenal gland	UBERON:0001234	65.98	gold quality
adrenal cortex	UBERON:0001235	65.83	gold quality
secondary oocyte	CL:0000655	65.17	gold quality
parotid gland	UBERON:0001831	63.93	gold quality
cartilage tissue	UBERON:0002418	63.15	silver quality
trabecular bone tissue	UBERON:0002483	62.77	gold quality
Brodmann (1909) area 46	UBERON:0006483	62.12	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	61.02	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	60.73	gold quality
decidua	UBERON:0002450	60.17	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	59.84	gold quality
inferior olivary complex	UBERON:0002127	59.71	gold quality
endothelial cell	CL:0000115	59.68	gold quality
adrenal gland	UBERON:0002369	59.56	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 0.

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.46

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): PDX1, POU1F1

miRNA regulators (miRDB)

47 targeting SSTR5, 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-6870-5P	99.99	68.55	2115
HSA-MIR-7111-5P	99.97	68.48	2062
HSA-MIR-4723-5P	99.97	68.70	2034
HSA-MIR-5698	99.97	68.49	2029
HSA-MIR-6778-3P	99.96	67.29	2693
HSA-MIR-4447	99.85	67.81	2900
HSA-MIR-6756-5P	99.82	67.97	2466
HSA-MIR-6842-5P	99.80	67.54	1587
HSA-MIR-7110-5P	99.80	67.84	1712
HSA-MIR-6817-3P	99.79	68.35	2126
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-92A-2-5P	99.75	67.01	2164
HSA-MIR-1976	99.74	65.48	1127
HSA-MIR-6766-5P	99.68	67.70	2325
HSA-MIR-6132	99.60	65.83	1554
HSA-MIR-6836-5P	99.60	65.62	1538
HSA-MIR-6752-5P	99.59	67.32	1243
HSA-MIR-302B-5P	99.50	69.49	1857
HSA-MIR-302D-5P	99.50	69.34	1863
HSA-MIR-128-1-5P	99.33	60.46	332
HSA-MIR-128-2-5P	99.33	60.83	311
HSA-MIR-1227-5P	98.65	65.32	1549
HSA-MIR-6852-3P	98.54	67.60	1468
HSA-MIR-4290	98.51	65.17	907
HSA-MIR-3187-5P	98.36	65.74	1776
HSA-MIR-506-5P	98.02	67.41	1065
HSA-MIR-4736	97.96	65.89	1287
HSA-MIR-5189-5P	97.72	66.96	1814
HSA-MIR-1285-3P	97.72	67.02	1932
HSA-MIR-665	97.60	65.64	1781

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)
• SSTRs 1-5 are heterogeneously expressed in gastroenteropancreatic endocrine tumors (PMID:12021920)
• identified an upstream promoter of the somatostatin receptor 5 gene with tissue-specific activity (PMID:12072395)
• the SSTR5 gene is involved in the etiology of bipolar affective disorder or may exist in linkage disequilibrium with a susceptibility gene close to SSTR5. (PMID:12192619)
• 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)
• Results do not suggest the SSTR5 gene as a susceptibility gene for autism (PMID:12898583)
• Sst2 and sst5 were expressed in 70%, sst1 in 50%, and sst3 and sst4 subtypes only in 15-20% of insulinomas (PMID:14602773)
• 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)
• activation of hSSTR5 but not hSSTR1 is necessary for heterodimeric assembly (PMID:15247250)
• role for SSTR5 t-461c and c1004t alleles in influencing GH and IGF-I levels in patients with acromegaly, whereas SSTR2 and SSTR5 variants seem to have a minor role in determining the responsiveness to somatostatin analogs (PMID:15914528)
• intracellular sorting of the somatostatin receptor subtype 5 is regulated by interactions with PDZ domain proteins PIST/GOPC and PDZK1 (PMID:16012170)
• Results suggest that the expression pattern of dopamine receptor 2 and somatostatin receptor 5 may influence the effects of SRIF analogs in growth hormone-secreting pituitary adenomas. (PMID:16216913)
• nNOS is a new p60(src) kinase substrate essential for SST5-mediated anti-proliferative action (PMID:16690617)
• Cytostatic action exerted by SSTR2 analogs might account for the tumor shrinkage observed in acromegalic patients treated with long-acting somatostatin analogs. (PMID:16954443)
• The expression of SSTR5 in TSHoma may be a useful marker for predicting the outcome of octreotide therapy. (PMID:17159301)
• The majority of all benign, premalignant and malignant laryngeal specimens expressed moderate to high levels of expression of SSTR5. (PMID:18066572)
• Data show that human somatostatin receptors (SSTR)2 and SSTR5 heterodimerize, and that selective activation of SSTR2 and not SSTR5, or their costimulation, modulates the association. (PMID:18653781)
• Immunohistochemistry stufy of SSTR5 in prostate tissue from patients with bladder outlet obstruction showed that close to 90% of secretory cells showed a weak positivity in the cytoplasm. (PMID:18936524)
• To the best of our knowledge, this is the first report describing crosstalk/interactions between SSTRs and ErbBs. (PMID:19070659)
• SSTR5 mRNA levels in Cushing disease were greater than silent corticotroph adenoma (SCA) but did not differ between non-functioning pituitary tumor and SCA. (PMID:19318729)
• In somatotrophinomas patients treated with somatostatin analogs, the most expressed SSTR was SSTR5, SSTR3, SSTR2, SSTR1, and SSTR4, respectively. (PMID:19330452)
• investigation of the role of BBXXB and DRY motifs of SST5 in the transduction of intracellular signals involved in the regulation of GH secretion and cell proliferation (PMID:19342453)
• The existence of two previously unidentified sst5 spliced variants with distinct distribution in normal tissues and pituitary tumors. (PMID:19401364)
• Genetic variation in the SSTR5 gene and, particularly, the rs4988483 single nucleotide polymorphism influence circulating IGFI and IGFBP3 hormone levels with no measurable effect on prostate cancer risk. (PMID:19423539)
• heterodimerisation between hSSTR2 and hSSTR5 is potentiated in the absence of receptor-stimulation (PMID:19748526)
• This study demonstrated negative immunoreactivity for SSTR-5 in the adenomatous tissue. (PMID:19894022)
• SSTR5 and CCR7 have a role in Crohn’s disease pathogenesis (PMID:20150960)
• Studies show that this study may be the basis for further functional studies to evaluate the role of somatostatin receptors sst1 to sst5 in the diabetic state. (PMID:20182388)
• importance of Asn13 and/or Asn26 residues in the agonist-specific signalling of hSSTR5 (PMID:20207824)
• Potential role of SSTR5 in the response of some tumors to somatostatin receptors. (PMID:20233783)
• The summarized expression pattern of SSTR in the investigated neuroendocrine tumors in our material was: SSTR 1> SSTR 5> SSTR 3> SSTR 2A> SSTR 2B. (PMID:20529830)
• Data show that the mRNA levels of SSTR1, SSTR2, SSTR3, and SSTR5 were high in PET compared with AC, whereas the expression of SSTR4 was low in PET and AC. (PMID:20717067)
• Overexpressed in endomterium inendometriosis. (PMID:20739383)
• Common genetic variation in the IGF1 and SSTR5 genes seems to influence circulating IGF-I levels (PMID:20810604)
• These data indicate that the activation and/or overexpression of SST receptors along with the inhibition of EGFR will serve as an important therapeutic approach in the treatment of ErbB-positive tumors. (PMID:21190959)
• The heterodimerization of somatostatin receptor-5 not only indicate the receptor’s specificity of interaction but also provide new insight to understand the molecular mechanism in regulation of signaling pathway in receptor specific manner. (PMID:21238583)
• SSTR5 P335L is a hypofunctional protein with a potentially harmful effect on function, as well as potential latent effect, and therefore it could affect the clinical response to somatostatin analog therapy for patients with pancreatic cancer. (PMID:21249361)
• differential gene expression profiles revealed more abundant mRNA expression in ectopic ACTH syndrome than in Cushing disease of SSTR-5 (PMID:21383526)
• demonstrate that cells transfected with SSTR1 or SSTR1/5 negatively regulates EGF mediated effects attributed to the inhibition of EGFR phosphorylation. (PMID:21419811)
• mRNA levels of SSTR2a, SSTR3 and SSTR5 in neuroendocrine lung cancer affected patients, were determined (PMID:21503779)

Cross-species orthologs

6 orthologs

Organism	Symbol	Gene ID
danio_rerio	sstr3	ENSDARG00000014477
danio_rerio	si:zfos-169g10.2	ENSDARG00000103662
mus_musculus	Sstr5	ENSMUSG00000050824
rattus_norvegicus	Sstr5	ENSRNOG00000018834
drosophila_melanogaster	Rh7	FBGN0036260
caenorhabditis_elegans	trhr-1	WBGENE00016265

Paralogs (17): OPRK1 (ENSG00000082556), OPRM1 (ENSG00000112038), KISS1R (ENSG00000116014), OPRD1 (ENSG00000116329), OPRL1 (ENSG00000125510), NPBWR2 (ENSG00000125522), SSTR4 (ENSG00000132671), SSTR1 (ENSG00000139874), GPR149 (ENSG00000174948), SSTR2 (ENSG00000180616), UTS2R (ENSG00000181408), PTGDR2 (ENSG00000183134), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Somatostatin receptor type 5 — P35346 (reviewed: P35346)

All UniProt accessions (2): A0AAA9YHT9, P35346

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for somatostatin 28 and to a lesser extent for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Increases cell growth inhibition activity of SSTR2 following heterodimerization.

Subunit / interactions. Heterodimer with SSTR2. Heterodimerization with SSTR2 increases cell growth inhibition activity of SSTR2.

Subcellular location. Cell membrane.

Tissue specificity. Adult pituitary gland, heart, small intestine, adrenal gland, cerebellum and fetal hypothalamus. No expression in fetal or adult kidney, liver, pancreas, uterus, spleen, lung, thyroid or ovary.

Post-translational modifications. Palmitoylated by ZDHHC5, but not ZDHHC3, nor ZDHHC8. Palmitoylation creates an additional intracellular loop which is thought to be important for efficient coupling to G-proteins and may target the protein to lipid rafts.

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

RefSeq proteins (2): NP_001044, NP_001166031* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000586	Somatstn_rcpt	Family
IPR001184	Somatstn_rcpt_5	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (54 total): sequence variant 12, helix 11, topological domain 8, transmembrane region 7, turn 4, glycosylation site 3, region of interest 2, chain 1, compositionally biased region 1, modified residue 1, lipid moiety-binding region 1, disulfide bond 1, sequence conflict 1, strand 1

Structure

Experimental structures (PDB)

7 structures.

PDB	Method	Resolution (Å)
9W32	ELECTRON MICROSCOPY	2.59
9W33	ELECTRON MICROSCOPY	2.69
8X8L	ELECTRON MICROSCOPY	2.7
8X8N	ELECTRON MICROSCOPY	2.9
8ZBJ	ELECTRON MICROSCOPY	2.94
8ZCJ	ELECTRON MICROSCOPY	3.09
8ZBE	ELECTRON MICROSCOPY	3.24

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P35346-F1	81.91	0.63

Antibody-complex structures (SAbDab): 5 — 8X8L, 8X8N, 8ZBE, 8ZBJ, 8ZCJ

Functional residue map

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

Post-translational modifications (2): 325, 320

Disulfide bonds (1): 112–186

Glycosylation sites (3): 13, 26, 187

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: 161 (showing top): GSE18804_BRAIN_VS_COLON_TUMORAL_MACROPHAGE_UP, MORF_RAGE, MORF_FLT1, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_RESPONSE_TO_CORTICOSTEROID, GOBP_INSULIN_SECRETION, MORF_ATRX, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_HORMONE_TRANSPORT, MORF_ESR1, GOBP_CELL_CELL_SIGNALING, GOBP_REGULATION_OF_PROTEIN_SECRETION, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_HORMONE_MEDIATED_SIGNALING_PATHWAY, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS

GO Biological Process (10): G protein-coupled receptor signaling pathway (GO:0007186), G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger (GO:0007187), neuropeptide signaling pathway (GO:0007218), negative regulation of cell population proliferation (GO:0008285), positive regulation of cytokinesis (GO:0032467), glucose homeostasis (GO:0042593), regulation of insulin secretion (GO:0050796), cellular response to glucocorticoid stimulus (GO:0071385), signal transduction (GO:0007165), somatostatin signaling pathway (GO:0038170)

GO Molecular Function (4): somatostatin receptor activity (GO:0004994), neuropeptide binding (GO:0042923), G protein-coupled receptor activity (GO:0004930), protein binding (GO:0005515)

GO Cellular Component (3): plasma membrane (GO:0005886), neuron projection (GO:0043005), 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
G protein-coupled receptor signaling pathway	3
G protein-coupled receptor activity	1
signal transduction	1
cell population proliferation	1
regulation of cell population proliferation	1
negative regulation of cellular process	1
cytokinesis	1
regulation of cytokinesis	1
positive regulation of cell division	1
positive regulation of cell cycle process	1
carbohydrate homeostasis	1
insulin secretion	1
regulation of protein secretion	1
regulation of peptide hormone secretion	1
response to glucocorticoid	1
cellular response to corticosteroid stimulus	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
hormone-mediated signaling pathway	1
somatostatin receptor signaling pathway	1
neuropeptide receptor activity	1
somatostatin signaling pathway	1
peptide binding	1
transmembrane signaling receptor activity	1
binding	1
membrane	1
cell periphery	1
plasma membrane bounded cell projection	1
cellular anatomical structure	1

Protein interactions and networks

STRING

0 interactions, top by confidence (×1000):

IntAct

142 interactions, top by confidence:

A	B	Type	Score
ARMC6	SLC27A2	psi-mi:“MI:0914”(association)	0.530
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
SSTR1	SSTR5	psi-mi:“MI:2364”(proximity)	0.520
SSTR1	SSTR5	psi-mi:“MI:0403”(colocalization)	0.520
SSTR1	SSTR5	psi-mi:“MI:0915”(physical association)	0.520
SSTR4	SSTR5	psi-mi:“MI:2364”(proximity)	0.520
SSTR4	SSTR5	psi-mi:“MI:0915”(physical association)	0.520
SSTR4	SSTR5	psi-mi:“MI:0403”(colocalization)	0.520
SSTR5	SNX27	psi-mi:“MI:0407”(direct interaction)	0.440
MAST2	SSTR5	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	PDZK1	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	GOPC	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	TAMALIN	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	SHANK1	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	NHERF2	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	MAST1	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	ARHGEF12	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	GRID2IP	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	RHPN1	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	WHRN	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	NHERF4	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	PDZD7	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	PARD3B	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	TAX1BP3	psi-mi:“MI:0407”(direct interaction)	0.440
SSTR5	PTPN3	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (14): GOPC (Reconstituted Complex), SSTR5 (Negative Genetic), SSTR5 (Negative Genetic), SSTR5 (Negative Genetic), SSTR5 (Negative Genetic), SSTR5 (Negative Genetic), SSTR5 (Negative Genetic), SSTR5 (Affinity Capture-Western), SSTR5 (FRET), SSTR5 (FRET), SSTR5 (Protein-peptide), SSTR5 (Reconstituted Complex), SSTR5 (FRET), SSTR5 (Affinity Capture-MS)

ESM2 similar proteins: A0A287A2K5, F1MV99, O08858, O43193, O77808, O97772, P28646, P30098, P30552, P30553, P30796, P30872, P30873, P30937, P30938, P31391, P32239, P32300, P32307, P32745, P33533, P35346, P35370, P35377, P41143, P41146, P46095, P46627, P47748, P48044, P49660, P51651, P56481, P58406, P79266, P79292, Q49LX5, Q5D0K2, Q6W5G4, Q6YNI2

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

5 interactions.

A	Effect	B	Mechanism
SSTR5	“up-regulates activity”	GNAI1	binding
SSTR5	“up-regulates activity”	GNAI3	binding
SSTR5	“up-regulates activity”	GNAO1	binding
somatostatin	“up-regulates activity”	SSTR5	“chemical activation”
lanreotide	“up-regulates activity”	SSTR5	“chemical activation”

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 87 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	48.4×	3e-06
Unblocking of NMDA receptors, glutamate binding and activation	5	46.1×	3e-06
Negative regulation of NMDA receptor-mediated neuronal transmission	5	46.1×	3e-06
Long-term potentiation	5	40.3×	4e-06
Assembly and cell surface presentation of NMDA receptors	9	38.7×	1e-10
Neurexins and neuroligins	10	33.4×	6e-11
Protein-protein interactions at synapses	6	27.0×	3e-06

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	11	76.1×	4e-16
protein localization to synapse	6	54.7×	1e-07
receptor clustering	7	52.0×	9e-09
regulation of postsynaptic membrane neurotransmitter receptor levels	8	47.2×	1e-09
bicellular tight junction assembly	5	19.7×	3e-04
protein-containing complex assembly	9	12.2×	4e-06
cell-cell adhesion	10	12.1×	9e-07
protein localization to plasma membrane	8	10.3×	6e-05

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	82
Likely benign	8
Benign	12

Top pathogenic / likely-pathogenic (0)

SpliceAI

104 predictions. Top by Δscore:

Variant	Effect	Δscore
16:1079734:T:TA	acceptor_gain	0.6100
16:1079689:T:TA	acceptor_gain	0.6000
16:1079641:C:CA	acceptor_gain	0.5800
16:1079758:GCT:G	acceptor_gain	0.5800
16:1079642:G:A	acceptor_gain	0.5700
16:1079822:T:A	donor_gain	0.5400
16:1079666:C:A	acceptor_gain	0.5200
16:1079780:C:CA	acceptor_gain	0.5200
16:1079673:A:AG	acceptor_gain	0.5000
16:1079547:AAG:A	donor_gain	0.4900
16:1079823:CT:C	donor_gain	0.4900
16:1079545:TGAAG:T	donor_loss	0.4800
16:1079546:GAAGG:G	donor_loss	0.4800
16:1079547:AAGGT:A	donor_loss	0.4800
16:1079548:AGGT:A	donor_loss	0.4800
16:1079549:GGTGA:G	donor_loss	0.4800
16:1079550:GTGAG:G	donor_loss	0.4800
16:1079551:T:G	donor_loss	0.4800
16:1079735:G:GA	donor_gain	0.4800
16:1079670:A:AG	acceptor_gain	0.4700
16:1079683:T:TA	acceptor_gain	0.4700
16:1079552:GAGG:G	donor_loss	0.4600
16:1079673:ATC:A	acceptor_gain	0.4500
16:1079674:T:G	acceptor_gain	0.4500
16:1079820:GT:G	donor_gain	0.4400
16:1079821:TT:T	donor_gain	0.4400
16:1079632:T:A	acceptor_gain	0.4200
16:1079545:TGA:T	donor_gain	0.4100
16:1079779:AC:A	acceptor_gain	0.4000
16:1079750:C:CA	acceptor_gain	0.3900

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000032817 (16:1080688 G>A), RS1000375476 (16:1074745 G>A,C), RS1000579844 (16:1070782 G>A,T), RS1000829589 (16:1074919 G>A), RS1000854521 (16:1077386 CA>C), RS1000989928 (16:1077613 G>A), RS1001149593 (16:1072908 G>A), RS1001458174 (16:1072649 G>A,C,T), RS1001520439 (16:1081689 C>T), RS1001527722 (16:1079121 G>A), RS1001879002 (16:1074471 T>C), RS1001931479 (16:1074659 G>A), RS1001990220 (16:1078448 G>A), RS1002364818 (16:1081520 T>C), RS1002519548 (16:1081297 G>A)

Disease associations

OMIM: gene MIM:182455 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST002741_1	Polycystic ovary syndrome	6.000000e-06
GCST007005_8	Logical memory (immediate recall) in normal cognition	3.000000e-07

EFO canonical traits (1, from GWAS)

EFO ID	Trait name
EFO:0004874	memory performance

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (3): CHEMBL1792 (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: 64,161 (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
CHEMBL296419	ASTEMIZOLE	4	21,577
CHEMBL3349607	PASIREOTIDE	4	109
CHEMBL841	LOPERAMIDE	4	22,587
CHEMBL1823872	SOMATOSTATIN	3	2,276
CHEMBL3349523	VAPREOTIDE	3	14,736
CHEMBL408350	EDOTREOTIDE	3	880
CHEMBL311695	SEGLITIDE	2	820
CHEMBL386768	EDOTREOTIDE YTTRIUM	2

Clinical evidence (CIViC)

Drug × variant × indication: 1 predictive associations from 1 curated evidence items.

Variant	Therapy	Indication	Effect	Level	CIViC
SSTR5 Overexpression	Pasireotide	Neuroendocrine Tumor	Sensitivity/Response	CIViC B	EID10193

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 (48 total), top 25:

Ligand	Action	Affinity	Parameter
[125I]LTT-SRIF-28	Full agonist	10.5	pKd
SRIF-28	Full agonist	10.3	pKi
[125I]Tyr10-CST14	Full agonist	10.3	pKd
CST-17	Full agonist	10.2	pKi
seglitide	Full agonist	10.2	pKi
[125I]Tyr11-SRIF-14	Full agonist	10.0	pKd
SRIF-14	Full agonist	9.9	pKi
pasireotide	Full agonist	9.8	pIC50
cortistatin-14	Full agonist	9.7	pKi
[125I]Tyr3 SMS 201-995	Full agonist	9.64	pKd
BIM 23052	Full agonist	9.6	pKi
BIM 23059	Full agonist	9.6	pKi
BIM 23313	Full agonist	9.6	pKi
[125I]CGP 23996	Full agonist	9.5	pKd
L-363,301	Full agonist	9.5	pKi
octreotide	Full agonist	9.5	pKi
L-817,818	Full agonist	9.4	pKi
BIM 23023	Full agonist	9.4	pKi
lanreotide	Full agonist	9.3	pKi
S5A1	Antagonist	9.27	pKi
L-362,855	Full agonist	9.2	pKi
KE 108	Full agonist	9.2	pIC50
vapreotide	Full agonist	9.2	pKi
[L-Tyr8]CYN 154806	Antagonist	9.1	pKi
zavolosotine	Agonist	9.0	pEC50

Binding affinities (BindingDB)

294 measured of 307 human assays (308 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
4-[8-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]-2-methoxybenzoic acid	IC50	0.129 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-4-methyl-2-(2,4,5-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.152 nM	US-8742110: Spiroxazolidinone compounds
4-[2-oxo-8-[[5-(trifluoromethoxy)-2-(2,3,4-trifluorophenyl)phenyl]methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.165 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[(4,8-dimethoxynaphthalen-2-yl)methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.172 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-4-methyl-2-(2,3,4-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]-2-methylbenzoic acid	IC50	0.188 nM	US-8742110: Spiroxazolidinone compounds
4-[2-oxo-8-[(4-phenylmethoxy-1-propan-2-ylindol-3-yl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.225 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-4-methyl-2-(2,3,4-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]-2-methoxybenzoic acid	IC50	0.228 nM	US-8742110: Spiroxazolidinone compounds
SRIF-D-Trp8	KI	0.23 nM
4-[8-[(5-chloro-4-ethoxy-8-methoxynaphthalen-2-yl)methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.233 nM	US-8742110: Spiroxazolidinone compounds
4-[2-oxo-8-[[6-(2,4,5-trifluorophenyl)-2,3-dihydro-1H-inden-5-yl]methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.243 nM	US-8742110: Spiroxazolidinone compounds
Cortistatin	KI	0.25 nM
4-[2-oxo-8-[(5-phenylmethoxy-1-propan-2-ylindazol-3-yl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.26 nM	US-8742110: Spiroxazolidinone compounds
4-[2-oxo-8-[[5-propan-2-yloxy-2-(2,4,5-trifluorophenyl)phenyl]methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.272 nM	US-8742110: Spiroxazolidinone compounds
4-[2-oxo-8-[(4,4,8-trimethyl-2,3-dihydrochromen-6-yl)methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.317 nM	US-8742110: Spiroxazolidinone compounds
8-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-3-[4-(2H-tetrazol-5-yl)phenyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one	IC50	0.323 nM	US-8742110: Spiroxazolidinone compounds
4-[2-oxo-8-[[1-propan-2-yl-5-(2,3,4-trifluorophenyl)indol-3-yl]methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.342 nM	US-8742110: Spiroxazolidinone compounds
3-chloro-4-[8-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.359 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-4-methyl-2-(4-methylpyrazol-1-yl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.395 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-4-methyl-2-(2,3,4-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]-3-fluorobenzoic acid	IC50	0.397 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-2-(6-fluoro-3-pyridinyl)-4-methylphenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.407 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-4-methyl-2-(2,3,4-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.409 nM	US-8742110: Spiroxazolidinone compounds
Leu8, D-Trp22, Tyr25 SST-28	KI	0.41 nM
4-[8-[[1-tert-butyl-3-(3-chloro-4-fluorophenyl)pyrazol-4-yl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.421 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-3-(trifluoromethyl)isoquinolin-7-yl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.424 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]-3-fluorobenzoic acid	IC50	0.437 nM	US-8742110: Spiroxazolidinone compounds
4-[2-oxo-8-[[5-(trifluoromethyl)-2-(2,3,4-trifluorophenyl)phenyl]methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.439 nM	US-8742110: Spiroxazolidinone compounds
3-chloro-4-[8-[[5-ethoxy-4-methyl-2-(2,3,4-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.468 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-4-methyl-2-(2,3,4-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]-3-methylbenzoic acid	IC50	0.474 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[2-(2,4-difluorophenyl)-5-ethoxyphenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.49 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[2-(3,4-difluorophenyl)-5-ethoxyphenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.502 nM	US-8742110: Spiroxazolidinone compounds
LTT-SRIF28	KI	0.52 nM
4-[2-oxo-8-[[5-propan-2-yloxy-2-(2,3,4-trifluorophenyl)phenyl]methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.546 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[(5-bromo-1-propan-2-ylindol-3-yl)methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.55 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[5-ethoxy-2-(2,3,4-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.556 nM	US-8742110: Spiroxazolidinone compounds
8-[[1-tert-butyl-3-(4-chloro-2,5-difluorophenyl)pyrazol-4-yl]methyl]-3-[4-(2H-tetrazol-5-yl)phenyl]-1-oxa-3,8-diazaspiro[4.5]decan-2-one	IC50	0.582 nM	US-8742110: Spiroxazolidinone compounds
SRIF-14	KI	0.63 nM
4-[8-[[5-ethoxy-4-methyl-2-[6-(trifluoromethyl)-3-pyridinyl]phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.632 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[(6-chloro-4-ethoxy-8-methoxynaphthalen-2-yl)methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.65 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[(4-ethoxy-8-methoxynaphthalen-2-yl)methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.704 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[2-tert-butyl-4-(4-methoxyphenyl)-1,3-thiazol-5-yl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.705 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[1-(3,3-dimethyl-2-bicyclo[2.2.1]heptanyl)-3-(2,3,4-trifluorophenyl)pyrazol-4-yl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.74 nM	US-8742110: Spiroxazolidinone compounds
4-[8-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.768 nM	US-8742110: Spiroxazolidinone compounds
SS-25	KI	0.79 nM
4-[8-[[5-ethoxy-2-(2,4,5-trifluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.793 nM	US-8742110: Spiroxazolidinone compounds
Cortistatin(1-14)	KI	0.85 nM
4-[8-[(6-methoxy-1-propan-2-ylindol-3-yl)methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	IC50	0.851 nM	US-8742110: Spiroxazolidinone compounds

ChEMBL bioactivities

1104 potent at pChembl≥5 of 1135 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.33	EC50	0.047	nM	CHEMBL5208674
10.30	EC50	0.05012	nM	CHEMBL5208674
10.19	EC50	0.065	nM	SOMATOSTATIN
10.15	EC50	0.071	nM	CHEMBL5179782
10.11	EC50	0.077	nM	CHEMBL5178891
10.10	Ki	0.08	nM	CHEMBL3647691
10.10	EC50	0.07943	nM	CHEMBL5178891
10.10	EC50	0.07943	nM	CHEMBL5169724
10.10	EC50	0.07943	nM	CHEMBL5179782
10.06	EC50	0.088	nM	CHEMBL5169724
10.05	Ki	0.09	nM	CHEMBL4110066
10.00	IC50	0.1	nM	CHEMBL4286244
10.00	Ki	0.1	nM	CHEMBL3349606
9.92	Ki	0.12	nM	SOMATOSTATIN
9.90	Ki	0.1259	nM	PASIREOTIDE
9.89	IC50	0.129	nM	CHEMBL3665819
9.85	Ki	0.14	nM	SOMATOSTATIN
9.82	Ki	0.15	nM	SOMATOSTATIN
9.82	IC50	0.1523	nM	CHEMBL3665831
9.80	Ki	0.16	nM	CHEMBL3647687
9.80	Ki	0.1585	nM	CHEMBL3349521
9.78	IC50	0.1645	nM	CHEMBL3665837
9.77	IC50	0.1715	nM	CHEMBL3665853
9.73	IC50	0.1881	nM	CHEMBL3665832
9.72	EC50	0.19	nM	SOMATOSTATIN
9.70	Ki	0.2	nM	CHEMBL3098601
9.70	IC50	0.2	nM	SOMATOSTATIN
9.70	IC50	0.2	nM	CHEMBL437296
9.70	IC50	0.2	nM	CHEMBL4293458
9.70	IC50	0.2	nM	CHEMBL4287248
9.70	EC50	0.2	nM	CHEMBL5180885
9.70	EC50	0.1995	nM	CHEMBL5180885
9.65	IC50	0.2245	nM	CHEMBL3670748
9.64	Ki	0.23	nM	SOMATOSTATIN
9.64	Ki	0.23	nM	CHEMBL3647689
9.64	IC50	0.2277	nM	CHEMBL3665838
9.64	EC50	0.23	nM	CHEMBL5174433
9.63	IC50	0.2329	nM	CHEMBL3665854
9.61	IC50	0.2432	nM	CHEMBL3665839
9.60	EC50	0.2512	nM	CHEMBL5192315
9.60	EC50	0.2512	nM	CHEMBL5176490
9.60	EC50	0.2512	nM	CHEMBL5174433
9.60	Ki	0.2512	nM	CHEMBL3349605
9.59	Ki	0.26	nM	SOMATOSTATIN
9.59	IC50	0.2602	nM	CHEMBL3670744
9.57	IC50	0.2715	nM	CHEMBL3665836
9.57	EC50	0.27	nM	CHEMBL5192315
9.57	EC50	0.27	nM	CHEMBL5176490
9.52	IC50	0.3	nM	CHEMBL4286244
9.52	IC50	0.3	nM	CHEMBL457245

PubChem BioAssay actives

884 with measured affinity, of 1377 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
3-[4-[(3S)-3-amino-3-methylpyrrolidin-1-yl]-5-(4-fluoro-1H-benzimidazol-2-yl)-3-pyridinyl]benzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	<0.0001	uM
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3,15-dibenzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-[2-(dimethylamino)ethyl]carbamate	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0001	uM
1-[1-[3-(4,6-difluoro-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methylphenyl)-4-pyridinyl]azetidin-3-yl]ethanamine	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0001	uM
3-[4-(3-amino-3-methylpyrrolidin-1-yl)-5-(4-fluoro-1H-benzimidazol-2-yl)-3-pyridinyl]benzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	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	203243: Effective concentration on human somatostatin receptor 5	ec50	0.0001	uM
1-[1-[3-(4,7-difluoro-1H-benzimidazol-2-yl)-5-[3-fluoro-5-(trifluoromethyl)phenyl]-4-pyridinyl]azetidin-3-yl]ethanamine	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0001	uM
4-[8-[(4-cyclopropyl-1-propan-2-ylindol-3-yl)methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	1423700: Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay	ic50	0.0001	uM
Pasireotide	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0001	uM
3-[4-[3-(1-aminoethyl)azetidin-1-yl]-5-(4,6-difluoro-1H-benzimidazol-2-yl)-3-pyridinyl]-5-fluorobenzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0002	uM
3-[4-[(3S)-3-aminopyrrolidin-1-yl]-5-(7-fluoro-4-methyl-1H-benzimidazol-2-yl)-3-pyridinyl]-5-fluorobenzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0002	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	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0002	uM
(2S)-2-[[(2S,3R)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-amino-3-[[2-[2-[(2R,5S,8S,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]ethylsulfanyl]acetyl]amino]propanoyl]amino]-3-(4-aminophenyl)propanoyl]amino]-3-sulfanylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoic acid	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0002	uM
(2S,5S,8S,11S,14S,17S,20S,23S,26S,29S,32S,34Z,37S)-2,17-bis(4-aminobutyl)-5-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-8,11,23-tribenzyl-20,26-bis[(1R)-1-hydroxyethyl]-29-(hydroxymethyl)-14-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,30,38-undecaoxo-1,4,7,10,13,16,19,22,25,28,31-undecazacyclooctatriacont-34-ene-32-carboxamide	1061943: Displacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cells	ki	0.0002	uM
4-[2-oxo-8-[[1-propan-2-yl-4-(2,3,4-trifluorophenyl)indol-3-yl]methyl]-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	1423690: Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes	ic50	0.0002	uM
4-[8-[[3-chloro-5-cyclopropyl-4-(2,4-difluorophenyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	1423690: Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes	ic50	0.0002	uM
(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3,15-dibenzyl-20-hydroxy-12-(1H-indol-3-ylmethyl)-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosane-2,5,8,11,14,17-hexone	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0003	uM
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3-benzyl-15-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0003	uM
1-[1-[3-(4,6-difluoro-1H-benzimidazol-2-yl)-5-[3-fluoro-5-(trifluoromethyl)phenyl]-4-pyridinyl]azetidin-3-yl]ethanamine	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0003	uM
(3S)-1-[3-(3-chloro-5-fluorophenyl)-5-(4-fluoro-1H-benzimidazol-2-yl)-4-pyridinyl]pyrrolidin-3-amine	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0003	uM
1-[1-[3-(3-chloro-5-fluorophenyl)-5-(4,6-difluoro-1H-benzimidazol-2-yl)-4-pyridinyl]azetidin-3-yl]ethanamine	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0003	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	1638708: Displacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 mins	kd	0.0003	uM
(2S)-6-amino-2-[[(2S)-2-amino-3-[[2-[2-[(2R,5S,8S,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]ethylsulfanyl]acetyl]amino]propanoyl]amino]-N-[(2R)-1-[[(2R,3R)-1,3-dihydroxybutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]hexanamide	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0003	uM
2-[(3S,5S)-5-[[3-(aminomethyl)phenyl]methyl]-2-oxo-1-[(4-phenylphenyl)methyl]-5H-4,1-benzoxazepin-3-yl]-N-[(2-fluorophenyl)methyl]acetamide	412313: Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells	ic50	0.0003	uM
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3-benzyl-15-[3-(diaminomethylideneamino)propyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0004	uM
3-[[4-(4-aminobutyl)-5-quinolin-2-yl-1,2,4-triazol-3-yl]sulfanyl]-1-(7-methyl-1H-indol-3-yl)propan-1-one	238339: Inhibitory constant against human sst5 receptor at a dose of 10 uM	ki	0.0004	uM
[1-[3-(3-chlorophenyl)-5-(4,6-difluoro-1H-benzimidazol-2-yl)-4-pyridinyl]azetidin-3-yl]methanamine	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0004	uM
3-[4-[(3S)-3-aminopyrrolidin-1-yl]-5-(4-methyl-1H-benzimidazol-2-yl)-3-pyridinyl]-5-fluorobenzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0004	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-16-[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-10-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	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0004	uM
(4R,7S,10R,13S,16R,19S,22R,25S,28R,31S,34R,37S)-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[(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	203580: Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells	ki	0.0004	uM
[(2S)-2-aminopropyl] (2S)-6-amino-2-[[2-(2-naphthalen-2-yl-1H-benzo[g]indol-3-yl)acetyl]amino]hexanoate	313082: Binding affinity to sst5 receptor	ic50	0.0004	uM
4-[8-[[4-chloro-2-cyclopropyl-5-(trifluoromethyl)phenyl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	1423700: Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay	ic50	0.0004	uM
4-[8-[[4-(4-fluorophenyl)-1-propan-2-ylpyrrolo[2,3-b]pyridin-3-yl]methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	1423690: Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes	ic50	0.0004	uM
[(2S)-2-aminopropyl] (2R)-6-amino-2-[[2-(2-naphthalen-2-yl-1H-benzo[g]indol-3-yl)acetyl]amino]hexanoate	412313: Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells	ic50	0.0004	uM
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3,15-dibenzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0004	uM
3-[4-[(3S)-3-aminopyrrolidin-1-yl]-5-(4-chloro-1H-benzimidazol-2-yl)-3-pyridinyl]-5-fluorobenzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0005	uM
3-[4-[(3S)-3-aminopyrrolidin-1-yl]-5-(4-fluoro-1H-benzimidazol-2-yl)-3-pyridinyl]benzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0005	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	1061943: Displacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cells	ki	0.0005	uM
(2S)-2-[[(2S)-2-amino-3-[[2-[2-[(2R,5S,8S,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]ethylsulfanyl]acetyl]amino]propanoyl]amino]-3-(4-aminophenyl)-N-[(2R)-1-[[(2R,3R)-1,3-dihydroxybutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]propanamide	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0005	uM
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3,15-dibenzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(5-aminopentyl)carbamate	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0006	uM
5-[4-[(3S)-3-aminopyrrolidin-1-yl]-5-(4-fluoro-1H-benzimidazol-2-yl)-3-pyridinyl]-2-fluorobenzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0006	uM
3-[4-[(3S)-3-aminopyrrolidin-1-yl]-5-(5-fluoro-4-methyl-1H-benzimidazol-2-yl)-3-pyridinyl]-5-fluorobenzonitrile	1860926: Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level	ec50	0.0006	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-[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-16-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	203709: Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell	ki	0.0006	uM
(2S)-2-[(4R)-4-acetamido-3-oxo-1,4,5,10-tetrahydroazepino[3,4-b]indol-2-yl]-6-amino-N-(2-phenylethyl)hexanamide;2,2,2-trifluoroacetic acid	412313: Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells	ic50	0.0006	uM
(2S)-6-amino-2-[(4R)-3-oxo-4-[(2-phenylacetyl)amino]-1,4,5,10-tetrahydroazepino[3,4-b]indol-2-yl]-N-(2-phenylethyl)hexanamide;2,2,2-trifluoroacetic acid	412313: Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells	ic50	0.0006	uM
(4R,7S,10S,13S,16S,19S)-10-(4-aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-14-methyl-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	203578: Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)	kd	0.0006	uM
(4S,7R,10S,13R,16S,19R)-19-[[(2S)-2-amino-3-(4-amino-3-iodophenyl)propanoyl]amino]-10-(4-aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-16-[(4-hydroxy-3-iodophenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	254878: Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells	ic50	0.0006	uM
(2S,3R)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-amino-3-[[2-[2-[(2R,5S,8S,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]ethylsulfanyl]acetyl]amino]propanoyl]amino]-3-(4-aminophenyl)propanoyl]amino]-3-sulfanylpropanoyl]amino]-3-hydroxybutanoic acid	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0006	uM
4-[8-[(4,4-dimethyl-2,3-dihydrothiochromen-6-yl)methyl]-2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-3-yl]benzoic acid	1423690: Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes	ic50	0.0006	uM
4-[8-[(4-cyclopropyl-1-propan-2-ylindol-3-yl)methyl]-3-oxo-2,8-diazaspiro[4.5]decan-2-yl]benzoic acid	1423700: Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay	ic50	0.0007	uM
4-[1-(benzenesulfonyl)piperidin-4-yl]-1-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]piperidine	1423616: Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay	ic50	0.0007	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Benzo(a)pyrene	affects methylation	2
dicrotophos	increases expression	1
trichostatin A	affects expression, affects cotreatment	1
tris(2-butoxyethyl) phosphate	affects expression	1
dimethylselenide	increases expression, increases oxidation, decreases expression	1
beta-lapachone	decreases expression	1
sodium arsenite	affects methylation	1
AN 238	affects binding	1
abrine	decreases expression	1
ormosil	affects binding, increases expression	1
pasireotide	affects binding	1
BIM 23206	increases activity, increases expression, decreases expression	1
jinfukang	affects cotreatment, increases expression	1
Resveratrol	affects cotreatment, decreases expression	1
Decitabine	affects cotreatment, affects expression	1
Acetaminophen	decreases expression	1
Air Pollutants	increases abundance, increases expression	1
Camptothecin	increases expression	1
Cisplatin	affects cotreatment, increases expression	1
Drugs, Chinese Herbal	decreases expression	1
Endosulfan	decreases expression	1
Estradiol	decreases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Polyethylene Glycols	affects binding, increases expression	1
Silicon Dioxide	increases expression	1
Somatostatin	increases expression	1
Tobacco Smoke Pollution	decreases expression	1
Urethane	decreases expression	1
Valproic Acid	increases methylation	1
Cyclosporine	decreases methylation	1

ChEMBL screening assays

151 unique, capped per target: 123 binding, 24 functional, 4 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1009182	Binding	Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells	Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities. — J Med Chem
CHEMBL1009183	Functional	Antagonist activity at human recombinant sst5 receptor expressed in chinese hamster CCL39 cells assessed as effect on 100 nM somatostatin-28-induced [35S]GTP-gamma-S-binding	Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities. — J Med Chem
CHEMBL4195977	ADMET	Drug uptake in HEK293 cells co-expressing SSTR5 (unknown origin) and RFP assessed as SSTR5-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

8 cell lines: 4 cancer cell line, 3 spontaneously immortalized cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_C0TS	ACTOne SSTR5	Transformed cell line	Female
CVCL_D8W9	Ubigene HCT 116 SSTR5 KO	Cancer cell line	Male
CVCL_E2L3	HAP1 SSTR5 (-)	Cancer cell line	Male
CVCL_H503	CHO-K1/SST5/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV84	cAMP Hunter CHO-K1 SSTR5 Gi	Spontaneously immortalized cell line	Female
CVCL_KZ15	PathHunter CHO-K1 SSTR5 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_LB34	PathHunter U2OS SSTR5 beta-arrestin	Cancer cell line	Female
CVCL_ZK23	Tango SSTR5-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

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