SSTR4

Summary

SSTR4 (somatostatin receptor 4, HGNC:11333) is a protein-coding gene on chromosome 20p11.21, encoding Somatostatin receptor type 4 (P31391). Receptor for somatostatin-14.

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. SSTR4 is a member of the superfamily of receptors having seven transmembrane segments and is expressed in highest levels in fetal and adult brain and lung.

Source: NCBI Gene 6754 — RefSeq curated summary.

At a glance

• GWAS associations: 8
• Clinical variants (ClinVar): 69 total
• GTEx eGene: eQTL in 7 tissues, sQTL in 0 (q < 0.05)
• Drug target: yes — 1 curated mechanism-of-action drug, 3 via a complex or family; 6 molecules with ChEMBL bioactivity
• Approved drugs acting on a complex or family including it: 2 — Lutetium Oxodotreotide Lu-177, Octreotide Acetate (Somatostatin receptor)
• MANE Select transcript: NM_001052
• Notable: 69 clinical variants but no curated precision-oncology (CIViC) evidence yet

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11333
Approved symbol	SSTR4
Name	somatostatin receptor 4
Location	20p11.21
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000132671
Ensembl biotype	protein_coding
OMIM	182454
Entrez	6754

Gene structure

Transcript identifiers

Ensembl transcripts: 1 — 1 protein_coding

MANE Select: ENST00000255008

ENST00000255008

RefSeq mRNA: 1 — MANE Select: NM_001052 NM_001052

CCDS: CCDS42856

Canonical transcript exons

ENST00000255008 — 1 exons

Exon	Start	End
ENSE00000906832	23035312	23039237

Expression profiles

Bgee: expression breadth broad, 35 present calls, max score 68.44.

Highest expression (Bgee): endometrium epithelium, metanephric glomerulus, prefrontal cortex, heart right ventricle, frontal cortex.

Genetic regulation across tissues (GTEx eQTL / sQTL)

SSTR4 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 7 tissues and its splicing (sQTL) in 0 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

7 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Brain Cerebellar Hemisphere	eqtl	5.7e-18	+0.63	20:23039366:A:G
Brain Nucleus accumbens basal ganglia	eqtl	3.3e-16	+0.47	20:23022033:C:A
Brain Cerebellum	eqtl	4.7e-16	+0.59	20:23039366:A:G
Testis	eqtl	1.0e-12	+0.50	20:23031540:T:C
Brain Caudate basal ganglia	eqtl	7.7e-04	+0.25	20:23022033:C:A
Brain Cortex	eqtl	5.7e-03	+0.17	20:23046984:T:C
Brain Spinal cord cervical c-1	eqtl	3.3e-02	+1.64	20:23272973:T:G

Top tissues by expression

showing 100 of 238 tissues by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
endometrium epithelium	UBERON:0004811	68.44	gold quality
metanephric glomerulus	UBERON:0004736	65.85	gold quality
prefrontal cortex	UBERON:0000451	59.75	gold quality
heart right ventricle	UBERON:0002080	57.36	gold quality
frontal cortex	UBERON:0001870	55.82	gold quality
neocortex	UBERON:0001950	54.75	gold quality
right frontal lobe	UBERON:0002810	54.57	gold quality
anterior cingulate cortex	UBERON:0009835	54.47	gold quality
quadriceps femoris	UBERON:0001377	53.62	gold quality
vastus lateralis	UBERON:0001379	53.46	gold quality
cerebellar hemisphere	UBERON:0002245	52.84	gold quality
cerebellar cortex	UBERON:0002129	52.63	gold quality
right hemisphere of cerebellum	UBERON:0014890	52.38	gold quality
Brodmann (1909) area 9	UBERON:0013540	52.15	gold quality
cerebellum	UBERON:0002037	52.05	gold quality
cerebral cortex	UBERON:0000956	51.30	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	51.23	gold quality
Brodmann (1909) area 10	UBERON:0013541	51.03	gold quality
amygdala	UBERON:0001876	50.94	gold quality
frontal pole	UBERON:0002795	50.41	gold quality
middle frontal gyrus	UBERON:0002702	50.30	gold quality
paraflocculus	UBERON:0005351	50.18	gold quality
cerebellar vermis	UBERON:0004720	49.25	gold quality
islet of Langerhans	UBERON:0000006	49.24	gold quality
thymus	UBERON:0002370	47.61	gold quality
temporal lobe	UBERON:0001871	46.47	gold quality
Ammon’s horn	UBERON:0001954	46.24	gold quality
primary visual cortex	UBERON:0002436	46.01	silver quality
brain	UBERON:0000955	45.80	gold quality
forebrain	UBERON:0001890	45.50	gold quality
central nervous system	UBERON:0001017	45.38	gold quality
colonic epithelium	UBERON:0000397	45.16	gold quality
cardia of stomach	UBERON:0001162	45.07	gold quality
occipital lobe	UBERON:0002021	44.50	silver quality
nucleus accumbens	UBERON:0001882	44.40	gold quality
deltoid	UBERON:0001476	43.68	gold quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	43.37	gold quality
amniotic fluid	UBERON:0000173	42.92	gold quality
superior frontal gyrus	UBERON:0002661	42.68	gold quality
secondary oocyte	CL:0000655	42.57	gold quality
oviduct epithelium	UBERON:0004804	42.43	gold quality
myocardium	UBERON:0002349	42.12	gold quality
substantia nigra pars compacta	UBERON:0001965	41.91	gold quality
lymph node	UBERON:0000029	41.61	gold quality
sural nerve	UBERON:0015488	41.55	gold quality
superficial temporal artery	UBERON:0001614	41.33	gold quality
esophagus squamous epithelium	UBERON:0006920	41.12	gold quality
palpebral conjunctiva	UBERON:0001812	41.10	gold quality
parotid gland	UBERON:0001831	41.00	gold quality
mucosa of paranasal sinus	UBERON:0005030	40.98	gold quality
jejunal mucosa	UBERON:0000399	40.59	gold quality
biceps brachii	UBERON:0001507	40.57	gold quality
epithelium of nasopharynx	UBERON:0001951	40.45	gold quality
gingival epithelium	UBERON:0001949	40.43	gold quality
germinal epithelium of ovary	UBERON:0001304	40.33	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	40.27	gold quality
medial globus pallidus	UBERON:0002477	40.21	gold quality
jejunum	UBERON:0002115	40.18	gold quality
skeletal muscle tissue	UBERON:0001134	40.10	gold quality
cartilage tissue	UBERON:0002418	40.06	gold quality
epithelium of bronchus	UBERON:0002031	40.03	gold quality
bronchus	UBERON:0002185	40.00	gold quality
mammary duct	UBERON:0001765	39.98	gold quality
globus pallidus	UBERON:0001875	39.97	gold quality
mucosa of sigmoid colon	UBERON:0004993	39.95	gold quality
saphenous vein	UBERON:0007318	39.83	gold quality
oocyte	CL:0000023	39.80	gold quality
urethra	UBERON:0000057	39.80	gold quality
pericardium	UBERON:0002407	39.77	gold quality
layer of synovial tissue	UBERON:0007616	39.77	gold quality
muscle tissue	UBERON:0002385	39.76	gold quality
cortical plate	UBERON:0005343	39.76	gold quality
endothelial cell	CL:0000115	39.75	gold quality
synovial joint	UBERON:0002217	39.70	gold quality
dorsal root ganglion	UBERON:0000044	39.68	gold quality
nipple	UBERON:0002030	39.68	gold quality
bronchial epithelial cell	CL:0002328	39.65	gold quality
decidua	UBERON:0002450	39.65	gold quality
penis	UBERON:0000989	39.64	gold quality
gingiva	UBERON:0001828	39.64	gold quality
trigeminal ganglion	UBERON:0001675	39.63	gold quality
tendon of biceps brachii	UBERON:0008188	39.60	gold quality
inferior vagus X ganglion	UBERON:0005363	39.57	gold quality
superior surface of tongue	UBERON:0007371	39.56	gold quality
pylorus	UBERON:0001166	39.55	gold quality
renal medulla	UBERON:0000362	39.53	gold quality
pons	UBERON:0000988	39.51	gold quality
medulla oblongata	UBERON:0001896	39.48	gold quality
superior vestibular nucleus	UBERON:0007227	39.47	gold quality
colonic mucosa	UBERON:0000317	39.45	gold quality
parietal pleura	UBERON:0002400	39.45	gold quality
Brodmann (1909) area 23	UBERON:0013554	39.40	gold quality
dorsal plus ventral thalamus	UBERON:0001897	39.38	gold quality
tongue	UBERON:0001723	39.37	gold quality
oral cavity	UBERON:0000167	39.35	gold quality
subthalamic nucleus	UBERON:0001906	39.35	gold quality
ventral tegmental area	UBERON:0002691	39.35	gold quality
trachea	UBERON:0003126	39.33	gold quality
parietal lobe	UBERON:0001872	39.32	gold quality
vena cava	UBERON:0004087	39.31	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	0.82

HPA expression

RNA tissue specificity: Not detected

30 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM
Hippocampal formation	tissue	17.0
Cerebral cortex	tissue	13.5
Retrosplenial and cingulate cortex	tissue	13.5
Occipital cortex	tissue	12.2
Entorhinal cortex	tissue	11.9
Frontal cortex	tissue	10.5
Somatosensory cortex	tissue	8.3
Amygdala	tissue	6.6
Corpus callosum	tissue	6.4
Basal ganglia	tissue	5.8
Ventral forebrain	tissue	5.8
Septum	tissue	5.5
Caudate putamen	tissue	4.9
Olfactory bulb	tissue	4.8
Hypothalamus	tissue	2.9
Thalamus	tissue	1.9
Retrosplenial cortex	tissue	1.7
Hippocampus	tissue	1.5
Midbrain	tissue	1.4
Pons	tissue	1.0
Postcentral gyrus	tissue	0.7
Nucleus accumbens	tissue	0.6
Cerebellum	tissue	0.5
Locus coeruleus	tissue	0.4
Medulla oblongata	tissue	0.3
Putamen	tissue	0.2
Substantia nigra	tissue	0.2
Spinal cord	tissue	0.2
Choroid plexus	tissue	0.1
Lung	tissue	0.1

Brain sub-regions (HPA Brain Atlas): detected in 173; highest nTPM — White matter (6.4), Hippocampus, CA3 (2.5), Hippocampus, CA1 (2.4), Posterior cingulate cortex (2.1), Hippocampus, CA2 (1.8).

Regulation

Is transcription factor: no

Functional genomics

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000255008 — one region, missense o/e 1.20.

Literature-anchored findings (GeneRIF, showing 22)

• This suggests that Nbs and the Mre11/Rad50 complex play partially independent roles in telomere protection and that Nbs functions in both ATR- and ATM-controlled telomere protection pathways. (PMID:16648644)
• Study identified a stringent requirement for Mre11-Rad50-Nbs (MRN) function in telomere protection during early embryonic development. (PMID:19520832)
• Drosophila telomere capping protein HOAP interacts with DSB sensor proteins Mre11 and Nbs. (PMID:33556205)
• 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)
• expression of SSTR4 transcripts up-regulated in prostatic carcinoma cells; SSTR4 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)
• A variable degree of SSTR4 was detected in laryngeal benign, premalignant and malignant specimens, with the greatest percentage in teh malignant specimens. (PMID:18066572)
• Immunohistochemistry stufy of SSTR4 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)
• In somatotrophinomas patients treated with somatostatin analogs, the most expressed SSTR was SSTR5, SSTR3, SSTR2, SSTR1, and SSTR4, respectively. (PMID:19330452)
• Heterodimerization between somatostatin receptor 4 and somatostatin receptor 5 exerted receptor and ligand specific changes in receptor coupling to adenylyl cyclase and the downstream signaling pathway. (PMID:19426801)
• the expression, localization, and inflammation-induced alterations of sst(4) receptors in murine and human lungs (PMID:19687471)
• 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)
• Evaluation of the potential use of sst5TMD4 expression in surgically removed pituitary adenomas as a predictor of the subsequent response of different pituitary tumors to somatostatin therapy. (PMID:20233783)
• 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)
• High SSTR4 expression is associated with lymph node metastasis in gallbladder cancer. (PMID:23991955)
• deregulated somatostatin signaling in the Alzheimer disease cortices studied cannot be explained by hypermethylation of the SST or SSTR4 promoter CpG islands. (PMID:24602981)
• this study shows that CD26 is associated with SSTR4 in malignant pleural mesothelioma cells, and this interaction inhibits SSTR4-mediated cytostatic effects. (PMID:24743707)
• An immunohistochemical investigation of the expression of somatostatin receptor subtypes (PMID:25962406)
• Data showed that the distribution of somatostatin receptor (SSTR) subtypes among the 199 pancreatic neuroendocrine tumors (PNETs) was: SSTR2 (54.8%), SSTR1 (53.3%), SSTR4 (51.8%), SSTR5 (33.7%), and SSTR3 (28.6%). (PMID:26474434)
• Characterization of Neurons Expressing the Novel Analgesic Drug Target Somatostatin Receptor 4 in Mouse and Human Brains. (PMID:33096776)
• Human Somatostatin SST4 Receptor Transgenic Mice: Construction and Brain Expression Pattern Characterization. (PMID:33916620)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
mus_musculus	Sstr4	ENSMUSG00000037014
rattus_norvegicus	Sstr4	ENSRNOG00000004641
drosophila_melanogaster	Rh7	FBGN0036260
caenorhabditis_elegans	trhr-1	WBGENE00016265

Paralogs (17): OPRK1 (ENSG00000082556), OPRM1 (ENSG00000112038), KISS1R (ENSG00000116014), OPRD1 (ENSG00000116329), OPRL1 (ENSG00000125510), NPBWR2 (ENSG00000125522), SSTR1 (ENSG00000139874), SSTR5 (ENSG00000162009), GPR149 (ENSG00000174948), SSTR2 (ENSG00000180616), UTS2R (ENSG00000181408), PTGDR2 (ENSG00000183134), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:105372) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 10 distinct phenotype terms.

Mouse phenotype (MP)	Records
edema	1
increased airway responsiveness	1
abnormal granulocyte morphology	1
abnormal neutrophil physiology	1
pulmonary edema	1
hyperalgesia	1
increased susceptibility to type IV hypersensitivity reaction	1
increased tumor necrosis factor secretion	1
increased interferon-gamma secretion	1
increased interleukin-1 beta secretion	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Pan troglodytes	Q5IJ49	100.0%	Diamond
Chlorocebus pygerythrus	Q8HZP3	99.7%	Diamond
Chlorocebus aethiops	Q95L01	99.7%	Diamond
Sus scrofa	P79291	99.6%	Diamond
Bos taurus	Q5E9H8	99.5%	Diamond
Macaca mulatta	Q8MJ88	99.4%	Diamond
Macaca fascicularis	Q8SQ54	99.4%	Diamond
Cavia porcellus	P97266	99.0%	Diamond
Canis lupus familiaris	Q49LX5	99.0%	Diamond
Saimiri boliviensis boliviensis	Q5IS84	99.0%	Diamond
Gorilla gorilla gorilla	P79175	98.3%	Diamond
Pongo pygmaeus	P79234	97.9%	Diamond
Meleagris gallopavo	O93361	97.6%	Diamond
Gallus gallus	Q98907	97.6%	Diamond
Xenopus laevis	P79960	97.4%	Diamond
Xenopus tropicalis	Q4VA82	97.4%	Diamond
Cricetulus griseus	P58826	94.5%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
THBD	protein-coding	7056
LINC00656	ncRNA	200261
CD93	protein-coding	22918

Protein

Protein identifiers

Somatostatin receptor type 4 — P31391 (reviewed: P31391)

All UniProt accessions (1): P31391

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. It is functionally coupled not only to inhibition of adenylate cyclase, but also to activation of both arachidonate release and mitogen-activated protein (MAP) kinase cascade. Mediates antiproliferative action of somatostatin in tumor cells.

Subcellular location. Cell membrane.

Tissue specificity. Specifically expressed in fetal and adult brain, lung tissue, stomach, and in lesser quantities in the kidney, pituitary and adrenals.

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

RefSeq proteins (1): NP_001043* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000586	Somatstn_rcpt	Family
IPR001512	Somatstn_rcpt_4	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (46 total): helix 15, topological domain 8, transmembrane region 7, sequence variant 4, strand 4, turn 3, chain 1, lipid moiety-binding region 1, glycosylation site 1, disulfide bond 1, sequence conflict 1

Structure

Experimental structures (PDB)

2 structures by resolution:

PDB	Title	Method	Resolution (Å)
7XMT	CryoEM structure of somatostatin receptor 4 (SSTR4) with Gi1 and J-2156	ELECTRON MICROSCOPY	2.8
7XMS	CryoEM structure of somatostatin receptor 4 (SSTR4) in complex with Gi1 and its …	ELECTRON MICROSCOPY	2.9

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P31391-F1	78.72	0.54

Antibody-complex structures (SAbDab)

2 antibodies co-crystallized with this protein: 7XMS, 7XMT

Human Protein Atlas

Protein class: G-protein coupled receptors, GPCRs excl olfactory receptors, Predicted membrane proteins, GPCRHMM predicted membrane proteins, FDA approved drug targets, Small molecule drugs

Protein evidence: Evidence at protein level

Antibody reliability (HPA): IH uncertain

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 (1)

Type	Positions
S-palmitoyl cysteine	327

Disulfide bonds (1)

Type	Positions
Disulfide bond	119–198

Glycosylation sites (1)

Type	Positions
N-linked (glcnac…) asparagine	24

Function

Pathways and Gene Ontology

Reactome pathways

2 curated (TAS) of 7; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

7 pathways:

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

MSigDB gene sets: 71 (showing top): BROWNE_HCMV_INFECTION_30MIN_DN, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_RESPONSE_TO_CORTICOSTEROID, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_HORMONE_MEDIATED_SIGNALING_PATHWAY, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, GOBP_CELLULAR_RESPONSE_TO_CORTICOSTEROID_STIMULUS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_RESPONSE_TO_STEROID_HORMONE, GOBP_RESPONSE_TO_HORMONE, GOBP_RESPONSE_TO_LIPID, GOBP_CELLULAR_RESPONSE_TO_STEROID_HORMONE_STIMULUS, GOMF_PEPTIDE_RECEPTOR_ACTIVITY, GOCC_NEURON_PROJECTION, SAKAI_CHRONIC_HEPATITIS_VS_LIVER_CANCER_DN

GO Biological Process (7): 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), 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

5 top-level categories:

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

24 GO namespaces:

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
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

showing 16 of 652 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SSTR4	SST	P01166	886
SSTR4	UTS2	O95399	743
SSTR4	PYGB	P11216	727
SSTR4	EPB41L1	Q9H4G0	618
SSTR4	PCSK2	P16519	593
SSTR4	PYGL	P06737	551
SSTR4	HIVEP2	P31629	513
SSTR4	SLC32A1	Q9H598	492
SSTR4	THBD	P07204	449
SSTR4	RET	P07949	447
SSTR4	CORT	O00230	441
SSTR4	TCF4	P15884	388
SSTR4	GIPR	P48546	373
SSTR4	SMURF1	Q9HCE7	365
SSTR4	CENPM	Q9NSP4	364
SSTR4	HAPLN4	Q86UW8	364

IntAct

Human interaction partners of SSTR4 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

5 partners by confidence:

Partner	Interaction type	MIscore	Records
SSTR5	proximity	0.520	3
RAMP3	physical association	0.400	5
RAMP2	physical association	0.400	3
RAMP1	physical association	0.400	1
YWHAB	association	0.350	1

BioGRID (6 interactions; top human partners by supporting records): CORT (Protein-peptide), JAK3 (Positive Genetic), OPRD1 (Affinity Capture-Western), PRKDC (Negative Genetic), PTPN18 (Affinity Capture-MS), SETD3 (Affinity Capture-MS)

SIGNOR signaling

6 signaling interactions:

A	Effect	B	Mechanism
SSTR4	“up-regulates activity”	GNAI1	binding
SSTR4	“up-regulates activity”	GNAI3	binding
SSTR4	“up-regulates activity”	GNA12	binding
somatostatin	“up-regulates activity”	SSTR4	“chemical activation”
CORT	up-regulates	SSTR4	binding
SST	up-regulates	SSTR4	binding

Protein complexes (CORUM) (3)

Experimentally-characterized complexes this protein is a subunit of (★ = the complex contains a known drug target).

3 complexes by size:

Complex	Subunits	Members
★ PDZK1-PLCB3-SSTR4 complex	3	PDZK1, PLCB3, SSTR4
★ SSTR4-SSTR5 complex	2	SSTR4, SSTR5
★ Somatostatin receptor type 4	1	SSTR4

Ligand–receptor pairs (CellPhoneDB) (2)

Curated ligand–receptor partners (cell-cell communication), distinct from the protein–protein interactions above.

2 ligand–receptor pairs:

Partner	This gene’s role	Signaling class
CORT	receptor	Signaling by Somatostatin
SST	receptor	Signaling by Somatostatin

Disease & clinical

Genetic variants

Variant evidence for SSTR4: 69 ClinVar records (0 pathogenic / likely pathogenic); 8 GWAS associations.

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	62
Likely benign	3
Benign	4

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 24 predictions of 187):

Position(s)	Effect	Δscore	Sites
20:23038295	donor_gain	0.8000
20:23036789	donor_gain	0.6800
20:23037139	donor_gain	0.6100
20:23038311	donor_gain	0.5600
20:23038887	acceptor_gain	0.5500
20:23039053–23039055	acceptor_loss	0.5300	7
20:23039043	acceptor_loss	0.5100
20:23039053	acceptor_loss	0.5100
20:23036546–23036548	donor_loss	0.5000	9
20:23039038	acceptor_loss	0.5000

AlphaMissense

845 missense substitutions predicted likely pathogenic (of 2,480 scored), across 226 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
M130	9	0.815	0.966
N65	8	0.978	0.993
D126	8	0.976	0.987
D93	8	0.973	0.984
D143	8	0.962	0.980
F220	8	0.951	0.996
F131	8	0.947	0.995
F268	8	0.946	0.995
F275	8	0.932	0.996
F211	8	0.931	0.988
F114	8	0.916	0.982
F102	8	0.905	0.963
N307	8	0.899	0.981
F318	8	0.893	0.977
F96	8	0.859	0.925
S304	8	0.851	0.989
C119	7	0.985	0.995
W112	7	0.980	0.998
C198	7	0.979	0.991
W272	7	0.969	0.985

HPA cancer prognostics

RNA cancer specificity: Not detected

Disease associations

OMIM: gene MIM:182454 | disease phenotypes:

GWAS associations

8 associations:

Study	Trait	p-value
GCST006002_15	Blood sugar levels	2e-13
GCST003988_18	Hypothyroidism	5e-10
GCST003191_1	Vitamin D levels	4e-9
GCST007393_1	Mitochondrial DNA copy number	6e-9
GCST002337_24	Amyotrophic lateral sclerosis (sporadic)	9e-7
GCST004250_20	Alanine aminotransferase (ALT) levels after remission induction therapy in actute lymphoblastic leukemia (ALL)	2e-6
GCST001762_306	Obesity-related traits	3e-6
GCST004250_6	Alanine aminotransferase (ALT) levels after remission induction therapy in actute lymphoblastic leukemia (ALL)	3e-6

EFO canonical traits (from GWAS)

4 canonical traits:

EFO ID	Trait name
EFO:0003939	energy intake
EFO:0007965	response to combination chemotherapy
EFO:0004468	glucose measurement
EFO:0006312	mitochondrial DNA measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL1853 (SINGLE PROTEIN), CHEMBL2111436 (PROTEIN FAMILY)

Drugs by curated mechanism of action (ChEMBL)

Drugs whose curated ChEMBL mechanism of action targets the SSTR4 protein itself — single-protein targets only (drugs acting on a protein family or complex that merely includes it are excluded). Includes antibodies and oligonucleotides that bioactivity screening does not capture.

1 curated-mechanism drugs:

Drug	Modality	Max phase
VELDOREOTIDE	Protein	2

Drugs acting on a complex or family that includes this protein

Curated ChEMBL mechanism-of-action drugs whose target is a protein complex or family of ≤10 members that includes SSTR4 — the drug acts on the assembly or class, not necessarily on this subunit alone.

3 drugs via a complex or family:

Drug	Target (ChEMBL)	Members	Max phase
LUTETIUM OXODOTREOTIDE LU-177	Somatostatin receptor	5	4
OCTREOTIDE ACETATE	Somatostatin receptor	5	4
SOMATOSTATIN	Somatostatin receptor	5	3

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 19,204 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

6 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL262135	GALLIUM OXODOTREOTIDE	4
CHEMBL1680	OCTREOTIDE	4	1,041
CHEMBL5267842	PALTUSOTINE	3	89
CHEMBL1823872	SOMATOSTATIN	3	2,376
CHEMBL3349523	VAPREOTIDE	3	14,872
CHEMBL311695	SEGLITIDE	2	826

PharmGKB: 1 entry (CPIC guideline: no)

GtoPdb / IUPHAR curated pharmacology

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

Target class: gpcr — Somatostatin receptors

Most potent curated ligand interactions (31 total), top 25:

Ligand	Action	Affinity	Parameter
CST-17	Full agonist	9.6	pKi
[125I]LTT-SRIF-28	Full agonist	9.6	pIC50
[125I]Tyr10-CST14	Full agonist	9.4	pKd
[125I]CGP 23996	Full agonist	9.4	pKd
SRIF-14	Full agonist	9.3	pKi
SRIF-28	Full agonist	9.2	pKi
L-803,087	Full agonist	9.2	pKi
[125I]Tyr11-SRIF-14	Full agonist	9.0	pKd
J-2156	Agonist	8.92	pKi
Des-AA5-[D-Trp8]SRIF	Full agonist	8.9	pIC50
CGP 23996	Full agonist	8.8	pKi
cortistatin-14	Full agonist	8.8	pKi
KE 108	Full agonist	8.8	pIC50
BIM 23052	Full agonist	8.6	pKi
H-c[Cys-Phe-LAgl(NβMe,benzoyl)-Trp-Lys-Thr-Phe-Cys]-OH	Full agonist	8.6	pIC50
BIM 23295	Full agonist	8.5	pKi
H-c[DCys-Phe-LAgl(NβMe,benzoyl)-DTrp-Lys-Thr-Phe-Cys]-OH	Full agonist	8.5	pIC50
H-c[Cys-Phe-LAgl(NβMe,benzoyl)-DTrp-Lys-Thr-Phe-Cys]-OH	Full agonist	8.3	pIC50
NNC269100	Full agonist	8.2	pKi
veldoreotide	Agonist	8.15	pIC50
BIM 23068	Full agonist	8.0	pKi
β3-tetrapeptide	Full agonist	7.8	pKd
consomatin Fj1	Agonist	7.66	pEC50
LY3556050	Agonist	7.4	pKi
L-362,855	Full agonist	7.3	pKi

Binding affinities (BindingDB)

1040 measured of 1438 human assays (1443 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
CHEMBL3781796	KI	0.03 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
(1S,5R)-N-[2-(7-chloro-1-methylindazol-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.1 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
CHEMBL3349516	KI	0.158 nM
CHEMBL3349522	KI	0.2 nM
SRIF	KI	0.2 nM
CHEMBL437296	IC50	0.2 nM
SRIF-D-Trp8	KI	0.23 nM
Cortistatin	KI	0.24 nM
CHEMBL3349521	KI	0.251 nM
CHEMBL440072	KD	0.29 nM
(1R,5S)-N-[2-(7-chloro-1,2-benzoxazol-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.3 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1R,5S)-N-[2-(7-fluoro-2H-indazol-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.3 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1S,5R)-N-[2-(1,8-dimethylimidazo[1,5-a]pyridin-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.3 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1R,5S)-N-[2-(8-chloroimidazo[1,5-a]pyridin-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.3 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(12S,15R,18S)-9-(4-Amino-butyl)-3-benzyl-15-(4-hydroxy-benzyl)-12-(1H-indol-3-ylmethyl)-6-isopropyl-1,18-dimethyl-1,4,7,10,13,16hexaaza-cyclooctadecane-2,5,8,11,14,17-hexaone	KI	0.3 nM
CHEMBL3098601	KI	0.31 nM
CHEMBL376485	IC50	0.35 nM
(4R,7S,10S,13R,16S,19R)-19-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-N-((2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-7,16-dibenzyl-10-(4-((isopropylamino)methyl)benzyl)-13-(N-methyl-2-naphthamido)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide	EC50	0.37 nM
Ala-Gly-cyclo[Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys] (SRIF14)	KI	0.38 nM
(1S,5R)-N-[2-(6-fluoro-1-methylindazol-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.4 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1R,5S)-N-[2-(7-methyl-1,2-benzoxazol-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.4 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1S,5R)-N-[2-(7-fluoro-1-methylindazol-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.4 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1S,5R)-N-[2-(8-methylindolizin-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.4 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
Leu8, D-Trp22, Tyr25 SST-28	KI	0.41 nM
Sandostatinm	IC50	0.46 nM
(1S,5R)-N-[2-(4-methylphthalazin-1-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.5 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
CHEMBL376484	IC50	0.5 nM
CHEMBL3349517	KI	0.501 nM
LTT-SRIF28	KI	0.52 nM
(1S,5R)-N-[2-methyl-1-[2-(trifluoromethyl)phenoxy]propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.6 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1R,5S)-N-[2-(3-methylindolizin-1-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.6 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1R,5S)-N-[2-(8-methoxyimidazo[1,5-a]pyridin-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.6 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1R,5S)-N-[2-(8-fluoro-1-methylimidazo[1,5-a]pyridin-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.6 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
N-[2-(1-methylisoquinolin-4-yl)propan-2-yl]-2,3,4,5-tetrahydro-1,4-benzoxazepine-9-carboxamide	EC50	0.6 nM	US-10183940: Aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amides as somatostatin receptor subtype 4 (SSTR4) agonists
SRIF-14	KI	0.63 nM
CHEMBL3349518	KI	0.631 nM
CHEMBL426548	IC50	0.64 nM
N-[2-(1-methylisoquinolin-4-yl)propan-2-yl]-1,4-oxazepane-6-carboxamide	EC50	0.7 nM	US-10071974: Morpholine and 1,4-oxazepane amides as somatostatin receptor subtype 4 (SSTR4) agonists
(1S,5R)-N-[2-[7-(trifluoromethyl)-2H-indazol-3-yl]propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.7 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
SS-25	KI	0.79 nM
CHEMBL3349513	KI	0.794 nM
(1R,5S)-N-[2-[1-methyl-7-(trifluoromethyl)indazol-3-yl]propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.8 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1S,5R)-N-[2-(8-methylquinazolin-4-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.8 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1S,5R)-N-[1-(8-methylimidazo[1,5-a]pyridin-3-yl)cyclobutyl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.8 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(1S,5R)-N-[2-(6-fluoro-8-methylimidazo[1,5-a]pyridin-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	EC50	0.8 nM	US-10166214: Somatostatin receptor subtype 4 (SSTR4) agonists
(4R,7S,10S,13R,16S,19R)-19-((S)-2-amino-3-(4-hydroxy-2-iodophenyl)propanamido)-N-((2R,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl)-7,16-dibenzyl-10-(4-((isopropylamino)methyl)benzyl)-13-(N-methyl-2-naphthamido)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide	IC50	0.8 nM
Cortistatin(1-14)	KI	0.85 nM

ChEMBL bioactivities

2044 potent at pChembl≥5 of 2074 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.10	IC50	0.08	nM	SOMATOSTATIN
10.00	EC50	0.1	nM	CHEMBL5197201
10.00	EC50	0.1	nM	CHEMBL5994657
10.00	EC50	0.1	nM	CHEMBL5981217
9.97	EC50	0.1072	nM	CHEMBL5563332
9.90	EC50	0.126	nM	CHEMBL5745719
9.80	EC50	0.158	nM	CHEMBL6005000
9.70	IC50	0.2	nM	CHEMBL437296
9.70	Kd	0.2	nM	CHEMBL440072
9.70	EC50	0.2	nM	CHEMBL5193727
9.70	EC50	0.2	nM	CHEMBL5209180
9.70	EC50	0.2	nM	CHEMBL5805146
9.70	EC50	0.2	nM	CHEMBL6142794
9.52	EC50	0.3	nM	CHEMBL5180543
9.52	EC50	0.3	nM	CHEMBL5190457
9.52	EC50	0.3	nM	CHEMBL5791465
9.52	EC50	0.3	nM	CHEMBL5942606
9.52	EC50	0.3	nM	CHEMBL5868096
9.52	EC50	0.3	nM	CHEMBL5850161
9.52	EC50	0.3	nM	CHEMBL5895650
9.46	IC50	0.35	nM	CHEMBL376485
9.40	EC50	0.4	nM	CHEMBL3421843
9.40	EC50	0.4	nM	CHEMBL3421842
9.40	EC50	0.4	nM	CHEMBL5991272
9.40	EC50	0.4	nM	CHEMBL5813716
9.40	EC50	0.4	nM	CHEMBL6061544
9.40	EC50	0.4	nM	CHEMBL5934220
9.40	EC50	0.4	nM	CHEMBL6037535
9.40	EC50	0.4	nM	CHEMBL6014424
9.40	EC50	0.398	nM	CHEMBL5977345
9.40	Ki	0.4	nM	CHEMBL6161926
9.40	EC50	0.4	nM	CHEMBL6161926
9.34	IC50	0.46	nM	SANDOSTATIN
9.30	IC50	0.5	nM	CHEMBL262379
9.30	IC50	0.5	nM	CHEMBL376484
9.30	EC50	0.5012	nM	CHEMBL4778342
9.30	EC50	0.5	nM	CHEMBL5183772
9.30	Ki	0.5	nM	CHEMBL5197201
9.30	Ki	0.5	nM	CHEMBL5183772
9.30	Ki	0.5	nM	CHEMBL5174969
9.30	EC50	0.5	nM	CHEMBL5966099
9.30	EC50	0.5	nM	CHEMBL5791074
9.29	IC50	0.51	nM	CHEMBL3350911
9.28	IC50	0.53	nM	CHEMBL415582
9.26	IC50	0.55	nM	CHEMBL2371100
9.23	Ki	0.59	nM	SOMATOSTATIN
9.22	IC50	0.6	nM	CHEMBL216992
9.22	EC50	0.6	nM	CHEMBL5177487
9.22	Ki	0.6	nM	CHEMBL5185547
9.22	EC50	0.6	nM	CHEMBL5985852

PubChem BioAssay actives

825 with measured affinity, of 1270 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
(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	203233: Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4	ic50	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	203570: Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0001	uM
3-[[5-[(3-chlorophenyl)methyl]-4-[3-(1H-imidazol-5-yl)propyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881329: Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ec50	0.0001	uM
2-(4-chlorophenoxy)-2,2-difluoro-N-[(3S,4S)-3-methylpiperidin-4-yl]acetamide	2094787: Agonist activity at SSTR4 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cellular cAMP level incubated for 30 mins by HTRF analysis	ec50	0.0001	uM
6-fluoro-3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-[[3-(trifluoromethyl)phenyl]methyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881329: Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	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	203570: Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0002	uM
(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]propanoyl]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-carboxamide	203570: Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0002	uM
6-fluoro-3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-[(2-methoxyphenyl)methyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881329: Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ec50	0.0002	uM
6-fluoro-3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-(3-methylsulfonylphenyl)sulfanyl-1,2,4-triazol-3-yl]methyl]-1H-indole	2241922: Agonist activity at human SST4 expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured at 2.5 to 20 hrs by TR-FRET LANCE assay	ec50	0.0002	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	1638707: Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins	kd	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
(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19-(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)-34-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-carboxylic acid	203570: Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0003	uM
3-[[5-[(3-bromophenyl)methyl]-4-[3-(1H-imidazol-5-yl)propyl]-1,2,4-triazol-3-yl]methyl]-6-fluoro-1H-indole	1881329: Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ec50	0.0003	uM
3-[[5-[(3,4-dichlorophenyl)methyl]-4-[3-(1H-imidazol-5-yl)propyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881329: Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ec50	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
3-(benzenesulfonyl)-4-[3-(1H-imidazol-5-yl)propyl]-5-(naphthalen-1-ylmethyl)-1,2,4-triazole	2241921: Displacement of [125I]-Tyr- SRIF-14 from human SST4 assessed as inhibition constant incubated for 90 mins by gamma counter based competitive radioligand binding assay	ki	0.0004	uM
(1R,5S)-N-[2-(3-methylisoquinolin-1-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	1203033: Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay	ec50	0.0004	uM
(1R,5S)-N-[2-(1-methylindazol-3-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	1203033: Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay	ec50	0.0004	uM
(4R,7S,10S,13S,16R,19S,22S,25R)-25-amino-13-(4-aminobutyl)-19,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-7-[(4-hydroxyphenyl)methyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203556: Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	ic50	0.0005	uM
6-(3-chloro-5-methylphenyl)-3-(3-fluoro-5-hydroxyphenyl)-5-[[methyl-[[(2S)-pyrrolidin-2-yl]methyl]amino]methyl]pyrido[2,3-d]pyrimidin-4-one	1675440: Agonist activity at human SST4	ec50	0.0005	uM
3-[[5-[(3-chlorophenyl)methyl]-4-[3-(1H-imidazol-5-yl)propyl]-1,2,4-triazol-3-yl]methyl]-6-fluoro-1H-indole	1881330: Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis	ki	0.0005	uM
3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-[(3-methoxyphenyl)methyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881329: Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ec50	0.0005	uM
(4R,7S,10R,13S,16R,19S,22R,25S)-25-amino-13-(4-aminobutyl)-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-19-[(4-hydroxyphenyl)methyl]-16-[(1S)-1-naphthalen-2-ylethyl]-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203555: Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.	ic50	0.0005	uM
(4R,7S,10R,13S,16R,19S,22S,25S,28R,31R,34S)-34-amino-19,31-bis(4-aminobutyl)-25,28-dibenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-13-[(4-hydroxyphenyl)methyl]-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid	242521: Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4	ic50	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
(4R,7S,10S,13S,16R,19S,22S,25S)-25-amino-13-(4-aminobutyl)-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-19-[(4-hydroxyphenyl)methyl]-16-[(1S)-1-naphthalen-2-ylethyl]-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203557: Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand	ic50	0.0006	uM
3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-[[3-(trifluoromethyl)phenyl]methyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881329: Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ec50	0.0006	uM
6-fluoro-3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-(3-methoxyphenyl)sulfanyl-1,2,4-triazol-3-yl]methyl]-1H-indole	2241921: Displacement of [125I]-Tyr- SRIF-14 from human SST4 assessed as inhibition constant incubated for 90 mins by gamma counter based competitive radioligand binding assay	ki	0.0006	uM
6-fluoro-3-[[5-(4-fluorophenyl)sulfanyl-4-[3-(1H-imidazol-5-yl)propyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	2241921: Displacement of [125I]-Tyr- SRIF-14 from human SST4 assessed as inhibition constant incubated for 90 mins by gamma counter based competitive radioligand binding assay	ki	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-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	203570: Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0006	uM
3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-phenylsulfanyl-1,2,4-triazol-3-yl]methyl]-1H-indole	2241922: Agonist activity at human SST4 expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured at 2.5 to 20 hrs by TR-FRET LANCE assay	ec50	0.0006	uM
6-fluoro-3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-[(3-methoxyphenyl)methyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881330: Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis	ki	0.0006	uM
(4R,7S,10R,13S,16S,19S,22R,25R,28S)-28-amino-13,25-bis(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27-octaoxo-1,2-dithia-5,8,11,14,17,20,23,26-octazacyclononacosane-4-carboxylic acid	242520: Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4	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
(4R,7S,10S,13S,16S,19S,22S,25R)-25-amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203556: Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	ic50	0.0007	uM
6-fluoro-3-[[5-[(6-fluoro-1H-indol-3-yl)methyl]-4-[3-(1H-imidazol-5-yl)propyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881329: Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ec50	0.0007	uM
3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-(3-methylsulfonylphenyl)sulfanyl-1,2,4-triazol-3-yl]methyl]-1H-indole	2241921: Displacement of [125I]-Tyr- SRIF-14 from human SST4 assessed as inhibition constant incubated for 90 mins by gamma counter based competitive radioligand binding assay	ki	0.0007	uM
3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-[(2-methoxyphenyl)methyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881330: Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis	ki	0.0007	uM
6-fluoro-3-[[4-[3-(1H-imidazol-5-yl)propyl]-5-[(3-methylsulfonylphenyl)methyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881330: Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis	ki	0.0007	uM
(4R,7S,10S,13S,16R,19S,22S,25S)-25-acetamido-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	384716: Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells	ic50	0.0007	uM
(4S,7R,10S,13R,16S,19R,22R,25S)-25-amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203554: Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand	ic50	0.0007	uM
methyl (2S)-5-(diaminomethylideneamino)-2-[4-(5,7-difluoro-2-phenyl-1H-indol-3-yl)butanoylamino]pentanoate	1571205: Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method	ki	0.0007	uM
1-[(3-chlorophenyl)methyl]-N-[(3S,4S)-3-methylpiperidin-4-yl]cyclopropane-1-carboxamide	2094787: Agonist activity at SSTR4 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cellular cAMP level incubated for 30 mins by HTRF analysis	ec50	0.0008	uM
(4R,7S,10S,13S,16S,19S,22S,25R)-25-amino-13-(4-aminobutyl)-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203556: Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	ic50	0.0008	uM
(4R,7S,10S,13S,16R,19S,22S,25R)-25-amino-13-(4-aminobutyl)-19-[(4-aminophenyl)methyl]-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203556: Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	ic50	0.0009	uM
6-fluoro-3-[[5-[(4-fluorophenyl)methyl]-4-[3-(1H-imidazol-5-yl)propyl]-1,2,4-triazol-3-yl]methyl]-1H-indole	1881330: Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis	ki	0.0009	uM
(4R,7S,10S,13S,16S,19S,22S,25R)-13-(4-aminobutyl)-25-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-[(1S)-1-(1H-indol-3-yl)ethyl]-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203556: Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	ic50	0.0009	uM
(4R,7S,10S,13S,16R,19S,22S,25R)-25-acetamido-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacycloheptacosane-4-carboxylic acid	384716: Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cells	ic50	0.0009	uM
(4R,7S,10S,13S,16S,19R,22S,25S,28R)-16-(4-aminobutyl)-10,22,25-tribenzyl-28-[[(2S)-5-carbamimidamido-2-[[2-[2-[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetyl]amino]ethoxy]ethoxy]acetyl]amino]pentanoyl]amino]-13-[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-19-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27-octaoxo-1,2-dithia-5,8,11,14,17,20,23,26-octazacyclononacosane-4-carboxylic acid	1071306: Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysis	ic50	0.0009	uM
(4R,7S,10S,13S,16R,19S,22S,25R)-25-amino-13-(4-aminobutyl)-7,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-16-(1H-indol-3-ylmethyl)-19-methyl-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	203556: Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	ic50	0.0010	uM

CTD chemical–gene interactions

12 total (human), top 12 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
propionaldehyde	decreases expression	1
bisphenol A	increases methylation	1
CGP 52608	affects binding, increases reaction	1
pasireotide	affects binding	1
Resveratrol	affects cotreatment, decreases expression	1
Air Pollutants	increases abundance, increases expression	1
Benzo(a)pyrene	affects methylation, increases methylation	1
Diazinon	increases methylation	1
Ozone	increases abundance, increases expression	1
Plant Extracts	affects cotreatment, decreases expression	1
Somatostatin	increases expression	1
Valproic Acid	increases methylation	1

ChEMBL screening assays

174 unique, capped per target: 153 binding, 19 functional, 2 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1009181	Binding	Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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*
CHEMBL1177481	Functional	Agonist activity against human SST4 receptor expressed in human NIH373 cells assessed as beta-galactosidase activity at 3 uM after 5 days by R-SAT assay	Optimization of isochromanone based urotensin II receptor agonists. — *Bioorg Med Chem*
CHEMBL4195976	ADMET	Drug uptake in HEK293 cells co-expressing SSTR4 (unknown origin) and RFP assessed as SSTR4-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

3 cell lines: 3 spontaneously immortalized cell line

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

Cellosaurus	Name	Category	Sex
CVCL_H502	CHO-K1/SST4/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV83	cAMP Hunter CHO-K1 SSTR4 Gi	Spontaneously immortalized cell line	Female
CVCL_KZ14	PathHunter CHO-K1 SSTR4 beta-arrestin	Spontaneously immortalized cell line	Female

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for SSTR4 across ~30M SureChEMBL compounds — explore on Sugi Predict.