SSTR3

Summary

SSTR3 (somatostatin receptor 3, HGNC:11332) is a protein-coding gene on chromosome 22q13.1, encoding Somatostatin receptor type 3 (P32745). Receptor for somatostatin-14 and -28.

This gene encodes a member of the somatostatin receptor protein family. Somatostatins are peptide hormones that regulate diverse cellular functions such as neurotransmission, cell proliferation, and endocrine signaling as well as inhibiting the release of many hormones and other secretory proteins. Somatostatin has two active forms of 14 and 28 amino acids. The biological effects of somatostatins are mediated by a family of G-protein coupled somatostatin receptors that are expressed in a tissue-specific manner. Somatostatin receptors form homodimers and heterodimers with other members of the superfamily as well as with other G-protein coupled receptors and receptor tyrosine kinases. This protein is functionally coupled to adenylyl cyclase. Alternate splicing results in multiple transcript variants.

Source: NCBI Gene 6753 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 77 total
• Druggable target: yes — 7 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001051

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11332
Approved symbol	SSTR3
Name	somatostatin receptor 3
Location	22q13.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000278195
Ensembl biotype	protein_coding
OMIM	182453
Entrez	6753

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000610913, ENST00000617123, ENST00000959749

RefSeq mRNA: 2 — MANE Select: NM_001051 NM_001051, NM_001278687

CCDS: CCDS13944

Canonical transcript exons

ENST00000610913 — 2 exons

Exon	Start	End
ENSE00003715012	37204237	37207839
ENSE00003753118	37211825	37212477

Expression profiles

Bgee: expression breadth broad, 90 present calls, max score 84.95.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.0238 / max 112.8107, expressed in 156 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
194017	0.5765	98
194021	0.1938	69
194019	0.0837	23
194020	0.0686	34
194018	0.0435	18
194022	0.0399	16
194016	0.0179	10

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
pancreatic ductal cell	CL:0002079	84.95	silver quality
buccal mucosa cell	CL:0002336	82.23	gold quality
tendon of biceps brachii	UBERON:0008188	81.69	silver quality
islet of Langerhans	UBERON:0000006	80.62	gold quality
vena cava	UBERON:0004087	78.46	gold quality
triceps brachii	UBERON:0001509	77.26	gold quality
cerebellar vermis	UBERON:0004720	75.69	silver quality
body of tongue	UBERON:0011876	75.15	gold quality
gluteal muscle	UBERON:0002000	74.37	gold quality
pons	UBERON:0000988	74.27	silver quality
lateral nuclear group of thalamus	UBERON:0002736	74.23	gold quality
endothelial cell	CL:0000115	74.16	gold quality
pericardium	UBERON:0002407	74.05	gold quality
medial globus pallidus	UBERON:0002477	74.05	silver quality
cardia of stomach	UBERON:0001162	73.94	gold quality
prefrontal cortex	UBERON:0000451	73.93	gold quality
globus pallidus	UBERON:0001875	73.88	gold quality
lateral globus pallidus	UBERON:0002476	73.77	gold quality
cartilage tissue	UBERON:0002418	73.47	gold quality
tongue	UBERON:0001723	73.13	gold quality
nipple	UBERON:0002030	72.85	gold quality
substantia nigra pars reticulata	UBERON:0001966	72.75	gold quality
trabecular bone tissue	UBERON:0002483	72.65	gold quality
subthalamic nucleus	UBERON:0001906	72.63	gold quality
dorsal plus ventral thalamus	UBERON:0001897	72.44	gold quality
inferior vagus X ganglion	UBERON:0005363	72.29	gold quality
pharyngeal mucosa	UBERON:0000355	72.23	gold quality
pylorus	UBERON:0001166	72.11	gold quality
right frontal lobe	UBERON:0002810	71.94	gold quality
substantia nigra pars compacta	UBERON:0001965	71.91	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	no	1.28

Regulation

Is transcription factor: no

miRNA regulators (miRDB)

91 targeting SSTR3, 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-3925-3P	100.00	69.95	1237
HSA-MIR-3667-3P	99.99	67.17	1636
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-2110	99.96	66.68	1930
HSA-MIR-1250-3P	99.96	70.04	4038
HSA-MIR-1236-3P	99.94	68.04	1695
HSA-MIR-497-5P	99.92	71.83	2674
HSA-MIR-15A-5P	99.90	72.80	2787
HSA-MIR-15B-5P	99.90	72.78	2798
HSA-MIR-16-5P	99.90	72.80	2780
HSA-MIR-195-5P	99.90	72.81	2805
HSA-MIR-4493	99.90	66.48	977
HSA-MIR-424-5P	99.89	71.90	2641
HSA-MIR-6838-5P	99.89	71.94	2690
HSA-MIR-345-3P	99.89	70.23	1421
HSA-MIR-221-5P	99.86	65.45	1052
HSA-MIR-8073	99.86	65.21	1118
HSA-MIR-10395-5P	99.86	67.35	676
HSA-MIR-4728-5P	99.85	69.39	4718
HSA-MIR-4698	99.84	71.41	4303
HSA-MIR-6785-5P	99.82	68.68	4428
HSA-MIR-6756-5P	99.82	67.97	2466
HSA-MIR-4319	99.76	69.83	2586
HSA-MIR-6764-5P	99.75	67.89	2304
HSA-MIR-149-3P	99.72	68.22	3963
HSA-MIR-4524A-3P	99.72	66.85	2406
HSA-MIR-6752-3P	99.72	66.71	1587
HSA-MIR-3059-5P	99.70	69.93	2491
HSA-MIR-6883-5P	99.69	68.05	3785
HSA-MIR-6892-3P	99.68	66.40	1178

Literature-anchored findings (GeneRIF, showing 29)

• 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 somatostatin (SS) and SS receptor (SSR) subtype 1 (sst1), sst2A, and sst3 in normal human thymic tissue (PMID:12376335)
• somatostatin receptor transcripts were found in lymphocytes both from Graves’ ophthalmopathy retroorbital tissues and blood samples, with levels of expression of SST1, -2, and -4 mRNA higher than those of the SST3 and -5 transcripts (PMID:12414882)
• localization and expression in human prostatic tissue and prostate cancer cell lines. (PMID:12474541)
• Reduced SSTR3 expression is associated with gastric cancers (PMID:15197339)
• Density of the SSTR3 receptor is decreased in gastric adenocarcinoma. H. pylori infection related reduction of the SSTR3 density in the antrum mucosa speaks for the need of eradication of these bacteria in the prevention of distal gastric cancer. (PMID:17679363)
• Determine the influence of H. pylori infection and a family history of gastric cancer on the expression of SSTR3 in the gastric mucosa of non-cancer patients with dyspepsia. (PMID:17683502)
• There was very little expression of SSTR3 in benign, premalignant, and cancerous laryngeal specimens; thus SSTR3 does not have an important role in laryngeal patholgy. (PMID:18066572)
• Immunohistochemistry stufy of SSTR3 in prostate tissue from patients with bladder outlet obstruction showed that greatest proportion of basal cells showed a moderate intensity, strong immunoreactivity being observed only in 15.8% of cells. (PMID:18936524)
• An interaction between the human somatostatin receptor 3 and the multiple PDZ protein MUPP1 was identified. (PMID:19071123)
• There was a positive correlation between the percentage of tumor reduction by octreotide-lar and SSTR3 expression. (PMID:19330452)
• 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)
• The cigarettes smoking and H. pylori infection are independent factors leading to decreasing of the SSTR3 mRNA level in gastric mucosa of patients with functional dyspepsia. (PMID:20570798)
• SST, presumably via SSTR3/MUPP1, regulates tight junction permeability in cultured keratinocytes (PMID:20629740)
• 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)
• mRNA levels of SSTR2a, SSTR3 and SSTR5 in neuroendocrine lung cancer affected patients, were determined (PMID:21503779)
• Determination of the expression of SSTR3 in an attempt to establish correlations and/or associations with clinical characteristics of patients with nonfunctioning pituitary adenomas. (PMID:22419713)
• High SSTR3 expression is associated with gallbladder cancer. (PMID:23991955)
• constitutive SSTR3 activity mediates transcriptional repression of GH. (PMID:24606125)
• In conclusions, in CNFAs, high expression of somatostatin receptors is much less common than that of D2R (PMID:25536318)
• SSTR2A and SSTR3 are more likely to be expressed in SDH-deficient pheochromocytomas/paragangliomas compared with tumors demonstrating normal SDHB staining pattern. (PMID:25554089)
• Data indicate that somatostatin receptor scintigraphy (SRS) and immunohistochemical results for somatostatin and dopamine receptors sstr2, sstr3, sstr5 and D2R were compared in neuroendocrine neoplasms tissues. (PMID:25808161)
• An immunohistochemical investigation of the expression of somatostatin receptor subtypes (PMID:25962406)
• findings provide new insights in understanding the antiproliferative role of SSTR3 in breast tumor biology. (PMID:26112183)
• 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)
• the C-terminal phosphorylation motif of the human sst3 receptor that regulates its agonist-promoted phosphorylation, beta-arrestin recruitment, and internalization of this clinically relevant receptor, is reported. (PMID:27101376)
• HTR6 and SSTR3 ciliary targeting relies on both IC3 loops and C-terminal tails. (PMID:33372037)
• Expression Analysis of SSTR 1, 2 and 3 in Small-cell Lung Cancer Patients as Targets for Future Peptide Receptor Radionuclide Therapy. (PMID:39197921)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
danio_rerio	sstr5	ENSDARG00000101655
mus_musculus	Sstr3	ENSMUSG00000044933
rattus_norvegicus	Sstr3	ENSRNOG00000007332
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), SSTR5 (ENSG00000162009), GPR149 (ENSG00000174948), SSTR2 (ENSG00000180616), UTS2R (ENSG00000181408), PTGDR2 (ENSG00000183134), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Somatostatin receptor type 3 — P32745 (reviewed: P32745)

Alternative names: SSR-28

All UniProt accessions (1): P32745

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase.

Subunit / interactions. Homodimer and heterodimer with SSTR2. Heterodimerization with SSTR2 inactivates SSTR3 receptor function.

Subcellular location. Cell membrane.

Tissue specificity. Brain, pituitary and pancreas.

Post-translational modifications. Phosphorylated. Phosphorylation increases upon somatostatin binding.

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

RefSeq proteins (2): NP_001042, NP_001265616 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000586	Somatstn_rcpt	Family
IPR001856	Somatstn_rcpt_3	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (35 total): topological domain 8, transmembrane region 7, sequence variant 6, compositionally biased region 5, modified residue 3, region of interest 2, glycosylation site 2, chain 1, disulfide bond 1

Structure

Experimental structures (PDB)

3 structures.

PDB	Method	Resolution (Å)
8XIR	ELECTRON MICROSCOPY	2.52
8XIQ	ELECTRON MICROSCOPY	2.71
8ZBI	ELECTRON MICROSCOPY	2.79

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P32745-F1	74.90	0.39

Antibody-complex structures (SAbDab): 3 — 8XIQ, 8XIR, 8ZBI

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 (3): 332, 337, 348

Disulfide bonds (1): 116–191

Glycosylation sites (2): 17, 30

Function

Pathways and Gene Ontology

Reactome pathways

11 pathways

ID	Pathway
R-HSA-375276	Peptide ligand-binding receptors
R-HSA-418594	G alpha (i) signalling events
R-HSA-5620922	BBSome-mediated cargo-targeting to cilium
R-HSA-162582	Signal Transduction
R-HSA-1852241	Organelle biogenesis and maintenance
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
R-HSA-5617833	Cilium Assembly
R-HSA-5620920	Cargo trafficking to the periciliary membrane

MSigDB gene sets: 133 (showing top): GSE37336_LY6C_POS_VS_NEG_NAIVE_CD4_TCELL_DN, GSE18804_SPLEEN_MACROPHAGE_VS_COLON_TUMORAL_MACROPHAGE_UP, GGGTGGRR_PAX4_03, SREBP1_02, GOBP_CELL_CELL_SIGNALING, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_HORMONE_MEDIATED_SIGNALING_PATHWAY, GATA3_01, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, GOBP_APOPTOTIC_SIGNALING_PATHWAY, GATA6_01, GATA1_01, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_RESPONSE_TO_HORMONE, GOMF_PEPTIDE_RECEPTOR_ACTIVITY

GO Biological Process (8): G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger (GO:0007187), neuropeptide signaling pathway (GO:0007218), cell-cell signaling (GO:0007267), negative regulation of cell population proliferation (GO:0008285), hormone-mediated apoptotic signaling pathway (GO:0008628), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), somatostatin signaling pathway (GO:0038170)

GO Molecular Function (5): G protein-coupled receptor activity (GO:0004930), somatostatin receptor activity (GO:0004994), signaling receptor binding (GO:0005102), neuropeptide binding (GO:0042923), protein binding (GO:0005515)

GO Cellular Component (6): plasma membrane (GO:0005886), cilium (GO:0005929), neuron projection (GO:0043005), ciliary membrane (GO:0060170), non-motile cilium (GO:0097730), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-8 pathways:

Category	Pathways
Signaling by GPCR	2
Class A/1 (Rhodopsin-like receptors)	1
GPCR downstream signalling	1
Cargo trafficking to the periciliary membrane	1
Signal Transduction	1
GPCR ligand binding	1
Organelle biogenesis and maintenance	1
Assembly of the 9+0 primary cilium	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	3
cell communication	2
signaling	2
hormone-mediated signaling pathway	2
plasma membrane bounded cell projection	2
cilium	2
cell population proliferation	1
regulation of cell population proliferation	1
negative regulation of cellular process	1
apoptotic signaling pathway	1
cellular process	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
somatostatin receptor signaling pathway	1
transmembrane signaling receptor activity	1
neuropeptide receptor activity	1
somatostatin signaling pathway	1
protein binding	1
peptide binding	1
binding	1
membrane	1
cell periphery	1
intraciliary transport particle	1
membrane-bounded organelle	1
cell projection membrane	1
bounding membrane of organelle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

984 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SSTR3	SST	P01166	978
SSTR3	BBS1	Q8NFJ9	841
SSTR3	BBS2	Q9BXC9	787
SSTR3	BBS4	Q96RK4	760
SSTR3	BBS7	Q8IWZ6	720
SSTR3	ARL13B	Q3SXY8	676
SSTR3	MPDZ	O75970	643
SSTR3	BBS9	P78514	639
SSTR3	SMO	Q99835	630
SSTR3	ADCY3	O60266	614
SSTR3	MCHR1	Q99705	605
SSTR3	TULP3	O75386	603
SSTR3	IFT88	Q13099	602
SSTR3	BBS5	Q8N3I7	595
SSTR3	TAS2R16	Q9NYV7	575

IntAct

21 interactions, top by confidence:

A	B	Type	Score
APP	SSTR3	psi-mi:“MI:0915”(physical association)	0.560
MPDZ	SSTR3	psi-mi:“MI:0915”(physical association)	0.540
SSTR3	MPDZ	psi-mi:“MI:0915”(physical association)	0.540
MPDZ	SSTR3	psi-mi:“MI:0403”(colocalization)	0.540
SSTR2	SSTR3	psi-mi:“MI:0915”(physical association)	0.520
SSTR2	SSTR3	psi-mi:“MI:2364”(proximity)	0.520
SSTR3	SSTR2	psi-mi:“MI:0403”(colocalization)	0.520
SSTR3	Mpdz	psi-mi:“MI:0915”(physical association)	0.500
SSTR3	Mpdz	psi-mi:“MI:0914”(association)	0.500
RAMP1	SSTR3	psi-mi:“MI:0915”(physical association)	0.400
SSTR3	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
SSTR3	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
SSTR3	RAMP1	psi-mi:“MI:0915”(physical association)	0.400
SSTR3	CSNK2A1	psi-mi:“MI:0914”(association)	0.350

BioGRID (15): SSTR3 (Protein-peptide), SST (Protein-peptide), MPDZ (Two-hybrid), SSTR3 (Affinity Capture-Western), Mpdz (Affinity Capture-Western), MPDZ (Affinity Capture-MS), TJP1 (Affinity Capture-MS), SCRIB (Affinity Capture-MS), TJP2 (Affinity Capture-MS), MAGI3 (Affinity Capture-MS), MAGI1 (Affinity Capture-MS), MPP6 (Affinity Capture-MS), HSPA4 (Affinity Capture-MS), GOPC (Affinity Capture-MS), SSTR3 (Two-hybrid)

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

3 interactions.

A	Effect	B	Mechanism
SSTR3	“up-regulates activity”	GNAI1	binding
SSTR3	“up-regulates activity”	GNAI3	binding
somatostatin	“up-regulates activity”	SSTR3	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	71
Likely benign	5
Benign	0

Top pathogenic / likely-pathogenic (0)

SpliceAI

484 predictions. Top by Δscore:

Variant	Effect	Δscore
22:37210473:C:A	donor_gain	0.9900
22:37207837:TGCC:T	acceptor_loss	0.9800
22:37207840:CTGGG:C	acceptor_loss	0.9800
22:37207841:T:A	acceptor_loss	0.9800
22:37210536:AAG:A	donor_gain	0.9800
22:37210690:C:CC	acceptor_gain	0.9800
22:37207835:TTTGC:T	acceptor_gain	0.9700
22:37207840:C:CC	acceptor_gain	0.9700
22:37207836:TTGC:T	acceptor_gain	0.9600
22:37207837:TGC:T	acceptor_gain	0.9600
22:37211952:TCTAG:T	donor_gain	0.9600
22:37210515:A:C	donor_gain	0.9400
22:37210519:CAG:C	donor_gain	0.9400
22:37207836:TTGCC:T	acceptor_gain	0.9300
22:37207837:TGCCT:T	acceptor_gain	0.9300
22:37207838:GCCT:G	acceptor_gain	0.9300
22:37210525:T:A	donor_gain	0.9200
22:37211949:A:AC	donor_gain	0.9200
22:37211950:C:CC	donor_gain	0.9200
22:37207840:C:A	acceptor_gain	0.9100
22:37208571:G:C	acceptor_gain	0.9100
22:37207838:GC:G	acceptor_gain	0.9000
22:37207839:CC:C	acceptor_gain	0.9000
22:37207839:CCT:C	acceptor_gain	0.9000
22:37210459:T:C	donor_gain	0.9000
22:37207841:T:G	acceptor_gain	0.8800
22:37210472:T:TA	donor_gain	0.8600
22:37211950:CTT:C	donor_gain	0.8400
22:37210532:A:AC	donor_gain	0.8300
22:37210533:C:CC	donor_gain	0.8300

AlphaMissense

2666 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
22:37207390:G:C	S138R	1.000
22:37207390:G:T	S138R	1.000
22:37207392:T:G	S138R	1.000
22:37207302:A:G	W168R	0.999
22:37207302:A:T	W168R	0.999
22:37207403:A:G	L134P	0.999
22:37207414:G:C	S130R	0.999
22:37207414:G:T	S130R	0.999
22:37207416:T:G	S130R	0.999
22:37207457:C:G	C116S	0.999
22:37207458:A:T	C116S	0.999
22:37207477:C:A	W109C	0.999
22:37207477:C:G	W109C	0.999
22:37207535:T:A	D90V	0.999
22:37207536:C:G	D90H	0.999
22:37207547:A:G	L86P	0.999
22:37207618:G:C	N62K	0.999
22:37207618:G:T	N62K	0.999
22:37207632:C:G	G58R	0.999
22:37206875:G:T	P310H	0.998
22:37206877:G:C	N309K	0.998
22:37206877:G:T	N309K	0.998
22:37206886:G:C	S306R	0.998
22:37206886:G:T	S306R	0.998
22:37206888:T:G	S306R	0.998
22:37207006:G:C	F266L	0.998
22:37207006:G:T	F266L	0.998
22:37207008:A:G	F266L	0.998
22:37207219:C:A	W195C	0.998
22:37207219:C:G	W195C	0.998

dbSNP variants (sampled 300 via entrez): RS1000286780 (22:37221813 G>A,T), RS1000338806 (22:37221541 C>G), RS1000442503 (22:37216046 G>A,T), RS1000569606 (22:37210711 A>G), RS1000837181 (22:37221665 C>T), RS1000883937 (22:37221363 C>T), RS1000896565 (22:37215889 C>A,G), RS1001033353 (22:37205920 G>A,T), RS1001284907 (22:37220380 C>A,T), RS1001392495 (22:37220809 G>A), RS1001853139 (22:37215275 TCTCC>T), RS1001958489 (22:37220374 A>C), RS1002263290 (22:37206714 C>A,G,T), RS1002396983 (22:37222190 G>A,T), RS1002516524 (22:37215010 C>G)

Disease associations

OMIM: gene MIM:182453 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL2028 (SINGLE PROTEIN), CHEMBL2111436 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

7 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 18,998 (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
CHEMBL3349607	PASIREOTIDE	4	109
CHEMBL1823872	SOMATOSTATIN	3	2,276
CHEMBL3349523	VAPREOTIDE	3	14,736
CHEMBL408350	EDOTREOTIDE	3	880
CHEMBL311695	SEGLITIDE	2	820
CHEMBL386768	EDOTREOTIDE YTTRIUM	2

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 (54 total), top 25:

Ligand	Action	Affinity	Parameter
[125I]LTT-SRIF-28	Full agonist	10.3	pKd
L-362,823	Full agonist	10.1	pIC50
[125I]Tyr10-CST14	Full agonist	10.1	pKd
SRIF-14	Full agonist	10.0	pKi
NC 8-12	Full agonist	10.0	pKi
CST-17	Full agonist	9.9	pKi
SRIF-28	Full agonist	9.9	pKi
cortistatin-14	Full agonist	9.9	pKi
[125I]CGP 23996	Full agonist	9.8	pKd
BIM 23052	Full agonist	9.7	pKi
[125I]Tyr7-Sst3-ODN-8	Full agonist	9.6	pKd
CGP 23996	Full agonist	9.3	pKi
BN-81,644	Full agonist	9.2	pKi
MK-4256	Antagonist	9.18	pIC50
BIM 23066	Full agonist	9.0	pIC50
BN-81,674	Full agonist	9.0	pKi
KE 108	Full agonist	8.8	pIC50
pasireotide	Full agonist	8.8	pIC50
BIM 23068	Full agonist	8.8	pKi
BIM 23058	Full agonist	8.8	pKi
octreotide	Full agonist	8.6	pKi
Des-AA5-[D-Trp8]SRIF	Full agonist	8.5	pIC50
L-362,855	Full agonist	8.3	pKi
[111In]DOTA-BOC-ATE	Full agonist	8.3	pIC50
sst3-ODN-8	Antagonist	8.2	pIC50

Binding affinities (BindingDB)

99 measured of 111 human assays (111 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
2-[[(2R,3S)-2-[[4-[(2-Oxo-2,3-dihydro-1H-benzimidazole)-1-yl]piperidino]carbonylamino]-3-(1H-indole-3-yl)butyryl]amino]-6-aminohexanoic acid tert-butyl ester	KI	0.01 nM
somatostatin-28	KI	0.07 nM
L-Ser-L-Ala-L-Asn-L-Ser-L-Asn-L-Pro-L-Ala-L-Met-L-Ala-L-Pro-L-Arg-L-Glu-L-Arg-L-Lys-L-Ala-Gly-L-Cys(1)-L-Lys-L-Asn-L-Phe-L-Phe-L-Trp-L-Lys-L-Thr-L-Phe-L-Thr-L-Ser-L-Cys(1)-OH	KI	0.07 nM
15-28-Somatostatin-28	KI	0.1 nM
SRIF-D-Trp8	KI	0.23 nM
Cortistatin	KI	0.25 nM
Leu8, D-Trp22, Tyr25 SST-28	KI	0.41 nM
LTT-SRIF28	KI	0.52 nM
SRIF-D-Trp8	KI	0.56 nM
SRIF-14	KI	0.63 nM
SS-25	KI	0.79 nM
Cortistatin(1-14)	KI	0.85 nM
Tyr10-cortistatin	KI	0.91 nM
CST14-Tyr10	KI	0.91 nM
2-[(3R)-3-[5-(5-fluoro-6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-1-(3-methoxy-6-bicyclo[3.1.0]hexanyl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,3,4-oxadiazole	IC50	1.2 nM	US-8754099: Oxadiazole beta carboline derivatives as antidiabetic compounds
L-797591	KI	1.4 nM
2-[(3R)-3-[5-(5-fluoro-6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-1-(oxan-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,3,4-oxadiazole	IC50	1.7 nM	US-8754099: Oxadiazole beta carboline derivatives as antidiabetic compounds
CH-275	KI	1.8 nM
2-[(1S,3R)-1-(ethoxymethyl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,3,4-oxadiazole	IC50	2.6 nM	US-8754099: Oxadiazole beta carboline derivatives as antidiabetic compounds
CAS_183658-72-2	KI	2.63 nM
L-817,818	KI	3.3 nM
2-[(3R)-3-[5-(5-fluoro-6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-1-(oxolan-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,3,4-oxadiazole	IC50	4.6 nM	US-8754099: Oxadiazole beta carboline derivatives as antidiabetic compounds
octreotide	KI	12 nM
BIM 23268	KI	18.4 nM
H-c(Cys3-Phe6-Phe7-DTrp8-Lys9-Thr10-Phe11-Cys14)-OH	KI	28 nM
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(2S)-1-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-15,18-dibenzyl-21-(3-carbamimidamidopropyl)-3-[(4-fluorophenyl)methyl]-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]acetamide	KI	28.5 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]ethylamino]-14-(4-aminobutyl)-5-benzyl-17-[(1R)-1-hydroxyethyl]-20-[(4-hydroxyphenyl)methyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-8-(pyridin-4-ylmethyl)-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	34.3 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(5S)-5-[[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]acetyl]amino]-6-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-3,18-dibenzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-15-(pyridin-4-ylmethyl)-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]hexyl]acetamide	KI	39.2 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[(1R,3R)-1-(ethoxymethyl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,3,4-oxadiazole	IC50	43.8 nM	US-8754099: Oxadiazole beta carboline derivatives as antidiabetic compounds
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfonyl]ethylamino]-14-(4-aminobutyl)-5,8-dibenzyl-20-[(4-fluorophenyl)methyl]-17-[(1R)-1-hydroxyethyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	56.4 nM	US-8952128: Somatostatin-dopamine chimeric analogs
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[2-[(R)-[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfinyl]ethylamino]-14-(4-aminobutyl)-5-benzyl-17-[(1R)-1-hydroxyethyl]-20-[(4-hydroxyphenyl)methyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-8-(pyridin-4-ylmethyl)-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	79.7 nM	US-8952128: Somatostatin-dopamine chimeric analogs
CHEMBL1202953	KI	84 nM
CAS_133073-82-2	KI	100 nM
L-362855	KI	100 nM
CGP-23996	KI	100 nM
BIM 23056	KI	100 nM
RC 160II	KI	100 nM
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]ethylamino]-14-(4-aminobutyl)-5,8-dibenzyl-20-[(4-fluorophenyl)methyl]-17-[(1R)-1-hydroxyethyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	101 nM	US-8952128: Somatostatin-dopamine chimeric analogs
BIM 23050	KI	107 nM
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(5S)-5-[[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]acetyl]amino]-6-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-18-benzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-15-(pyridin-4-ylmethyl)-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]hexyl]acetamide	KI	113 nM	US-8952128: Somatostatin-dopamine chimeric analogs
c[Aha-Phe-D-Trp-Lys-Thr(Bzl)]	KI	141 nM
3-(2-Naphtyl)-D-Ala-L-Cys(1)-L-Tyr-D-Trp-L-Lys-L-Val-L-Cys(1)-L-Thr-NH2	KI	178 nM
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(2S)-1-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-3,18-dibenzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-15-(pyridin-4-ylmethyl)-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]acetamide	KI	182 nM	US-8952128: Somatostatin-dopamine chimeric analogs
L-803,087	KI	199 nM
DC23-60	KI	241 nM
2-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-27-[2-[(S)-[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfinyl]ethylamino]-14-(4-aminobutyl)-5-benzyl-17-[(1R)-1-hydroxyethyl]-20-[(4-hydroxyphenyl)methyl]-11-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,28-octaoxo-8-(pyridin-4-ylmethyl)-1,4,7,10,13,16,19,22-octazacyclooctacos-2-yl]propyl]guanidine	KI	255 nM	US-8952128: Somatostatin-dopamine chimeric analogs
3-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methyl-acetylamino]-N-[(2R)-1-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-15,18-dibenzyl-21-(3-carbamimidamidopropyl)-3-[(4-fluorophenyl)methyl]-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]propanamide	KI	277 nM	US-8952128: Somatostatin-dopamine chimeric analogs
EC5-21	KI	382 nM
Lanreotide	KI	500 nM
(1R,5S)-N-[2-(1-methylisoquinolin-4-yl)propan-2-yl]-3-azabicyclo[3.1.0]hexane-6-carboxamide	KI	508 nM	US-9789082: Somatostatin receptor subtype 4 (SSTR4) agonists

ChEMBL bioactivities

1135 potent at pChembl≥5 of 1152 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
10.49	Kd	0.032	nM	CHEMBL440072
10.00	Ki	0.1	nM	SOMATOSTATIN
9.85	Ki	0.14	nM	SOMATOSTATIN
9.82	IC50	0.15	nM	CHEMBL3323076
9.70	IC50	0.2	nM	CHEMBL437296
9.64	EC50	0.23	nM	CHEMBL1824052
9.60	EC50	0.249	nM	CHEMBL5193727
9.60	Ki	0.2512	nM	SOMATOSTATIN
9.56	EC50	0.276	nM	CHEMBL5190457
9.52	IC50	0.3	nM	CHEMBL3582344
9.50	Ki	0.3162	nM	CHEMBL3349606
9.46	IC50	0.35	nM	CHEMBL376485
9.46	EC50	0.35	nM	CHEMBL1824051
9.40	IC50	0.4	nM	CHEMBL3582321
9.40	IC50	0.4	nM	CHEMBL3582339
9.40	IC50	0.4	nM	SOMATOSTATIN
9.34	EC50	0.46	nM	CHEMBL3775042
9.34	IC50	0.46	nM	SANDOSTATIN
9.30	IC50	0.5	nM	CHEMBL3582342
9.30	IC50	0.5	nM	CHEMBL376484
9.29	EC50	0.516	nM	CHEMBL3287628
9.28	Ki	0.53	nM	SOMATOSTATIN
9.28	IC50	0.52	nM	CHEMBL3323084
9.28	EC50	0.53	nM	CHEMBL1824056
9.23	EC50	0.585	nM	CHEMBL5177487
9.21	Ki	0.61	nM	CHEMBL1823873
9.21	EC50	0.619	nM	CHEMBL6025625
9.20	Ki	0.631	nM	CHEMBL3349516
9.20	Ki	0.631	nM	CHEMBL3349521
9.20	Ki	0.631	nM	CHEMBL3349605
9.20	Ki	0.631	nM	CHEMBL3349517
9.20	EC50	0.63	nM	CHEMBL1823873
9.19	Ki	0.64	nM	CHEMBL2069499
9.19	Ki	0.64	nM	CHEMBL1237140
9.19	IC50	0.64	nM	CHEMBL3323074
9.19	IC50	0.64	nM	CHEMBL426548
9.18	IC50	0.66	nM	CHEMBL2204935
9.18	Ki	0.66	nM	CHEMBL408362
9.18	Ki	0.66	nM	SOMATOSTATIN
9.15	IC50	0.7	nM	CHEMBL2204939
9.15	IC50	0.7	nM	CHEMBL2204935
9.15	IC50	0.7	nM	CHEMBL3582329
9.14	EC50	0.725	nM	CHEMBL5175637
9.13	IC50	0.74	nM	CHEMBL2204939
9.12	IC50	0.76	nM	CHEMBL2204934
9.11	IC50	0.78	nM	CHEMBL2204938
9.11	IC50	0.78	nM	CHEMBL3323076
9.11	IC50	0.78	nM	CHEMBL3323074
9.11	EC50	0.78	nM	SOMATOSTATIN
9.10	IC50	0.8	nM	CHEMBL2069500

PubChem BioAssay actives

1017 with measured affinity, of 1566 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,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	1638706: Displacement of [125I]somatostatin from human SSTR3 expressed in CHO-K1 cell membranes after 120 mins	kd	<0.0001	uM
ethyl 5-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylate	1184748: Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis	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]-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	203547: Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype	ki	0.0001	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,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-(naphthalen-2-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid	616823: Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay	ec50	0.0002	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	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0003	uM
2-[5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-2-oxo-1,3,4-oxadiazol-3-yl]acetamide	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	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
(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-(naphthalen-2-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid	616823: Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay	ec50	0.0003	uM
3-[(1R,3R)-1-[1-(cyclopropylmethyl)pyrazol-4-yl]-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	0.0004	uM
3-ethyl-5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,3,4-oxadiazol-2-one	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	0.0004	uM
(4R,7S,10S,13S,16R,19S,22S,25R)-25-amino-13-(4-aminobutyl)-7,19,22-tribenzyl-10-[(1R)-1-hydroxyethyl]-16-(naphthalen-2-ylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptazacyclohexacosane-4-carboxylic acid	616823: Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay	ec50	0.0005	uM
5-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-3-carboxylic acid	1184748: Antagonist activity at human SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis	ic50	0.0005	uM
3-[2-(dimethylamino)ethyl]-5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,3,4-oxadiazol-2-one	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	0.0005	uM
5-methyl-3-[(1R,3R)-1-(1-methylpyrazol-4-yl)-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-1,2,4-oxadiazole	1285054: Antagonist activity at human somatostatin receptor type 3 assessed as inhibition of cAMP levels	ec50	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
N-[(1R,2S)-2-[(3,4-dichlorophenyl)methylamino]cyclohexyl]naphthalene-2-carboxamide	1156205: Agonist activity at human SST3 expressed in CHO-K1 cells assessed as foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay	ec50	0.0005	uM
(3S)-1,1-dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole	1156202: Displacement of [125I]SS14 from human SST3 expressed in CHO membrane after 60 to 90 mins by scintillation counting	ki	0.0006	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	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0006	uM
ethyl 2-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-4-carboxylate	1184747: Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer	ic50	0.0006	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	1061945: Displacement of [125I]-somatostatin from human SSTR3 expressed in CHO-K1 cells	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	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0006	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	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	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-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	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	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
(3R)-1,1-dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole	203547: Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype	ki	0.0006	uM
2-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methylsulfanyl-1,3,4-oxadiazole	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	0.0007	uM
(4R,7S,10R,13S,16R,19S,22R,25S,28S,31S,34R,37S)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid	203226: Binding affinity towards human sst3 receptor expressed in CHO-K1 cells	ki	0.0007	uM
3-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole	1229170: Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay	ic50	0.0007	uM
(3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1,1-bis(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole	712054: Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins	ic50	0.0007	uM
(3R)-1-cyclohexyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole	1229170: Displacement of [125I]SS-14 from human recombinant SSTR3 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay	ic50	0.0008	uM
[(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3-benzyl-15-(1H-imidazol-5-ylmethyl)-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	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0008	uM
ethyl 6-[(1R,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]pyridine-2-carboxylate	1184747: Displacement of [125I]SS-14 from human SSTR3 expressed in CHO cells by TopCount analyzer	ic50	0.0008	uM
5-[(1R,3R)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-propan-2-yl-1,3,4-oxadiazol-2-one	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	0.0008	uM
2-[5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-2-oxo-1,3,4-oxadiazol-3-yl]acetic acid	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	0.0008	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	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0008	uM
(3S)-1,1-dibutyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole;oxalic acid	203547: Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype	ki	0.0008	uM
(3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1,1-diphenyl-2,3,4,9-tetrahydropyrido[3,4-b]indole	712055: Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins	ic50	0.0008	uM
3-[(1R,3S)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole	712054: Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins	ic50	0.0008	uM
(3S)-1,1-dipentyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole	203416: Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor.	ic50	0.0008	uM
Pasireotide	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0008	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	203551: Binding affinity towards human Somatostatin receptor type 3 (sst3) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0008	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-[(4-hydroxyphenyl)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	616823: Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay	ec50	0.0009	uM
(3S)-1-cyclohexyl-1-methyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indole	203547: Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-3) subtype	ki	0.0009	uM
5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-propan-2-yl-1,3,4-oxadiazol-2-one	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	0.0010	uM
3-[(3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(5-methyl-1,2,4-oxadiazol-3-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole	712055: Displacement of [125I]SS-28 from human SSTR3 transfected in CHO cells after 60 to 90 mins	ic50	0.0010	uM
5-[(1R,3R)-1-(1-ethylpyrazol-4-yl)-3-[5-(5-fluoro-2-pyridinyl)-1H-imidazol-2-yl]-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-3-methyl-1,3,4-oxadiazol-2-one	1229171: Antagonist activity against human recombinant SSTR3 expressed in CHO cells assessed as reduction in forskolin-induced cAMP accumulation in presence of SS-14 by time-resolved fluorescence assay	ic50	0.0011	uM
(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-N-[(2S,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0011	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	652544: Binding affinity to human sst3 by in vitro receptor autoradiography assay	ic50	0.0011	uM
3-[(1S,3R)-3-[5-(4-fluorophenyl)-1H-imidazol-2-yl]-1-(1-methylpyrazol-4-yl)-2,3,4,9-tetrahydropyrido[3,4-b]indol-1-yl]-5-methyl-1,2,4-oxadiazole	712054: Inhibition of human SSTR3 transfected in CHO cells assessed as inhibition of SRIF-induced reduction of cAMP accumulation after 45 mins	ic50	0.0011	uM

CTD chemical–gene interactions

18 total (human), top 18 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
bisphenol A	decreases expression, decreases methylation	2
aristolochic acid I	increases expression	1
ethyl-p-hydroxybenzoate	decreases expression	1
tetrabromobisphenol A	decreases expression	1
di-n-butylphosphoric acid	affects expression	1
3-(4’-hydroxy-3’-adamantylbiphenyl-4-yl)acrylic acid	decreases expression	1
pasireotide	affects binding	1
bisphenol S	decreases expression	1
3-hydroxy-4-prenyl-5-methoxystilbene-2-carboxylic acid	increases expression	1
Benzo(a)pyrene	increases methylation	1
Cadmium	decreases expression, increases abundance	1
Mercury	decreases expression	1
Somatostatin	increases expression	1
Tetrachlorodibenzodioxin	affects expression	1
Triclosan	increases expression	1
1-Methyl-4-phenylpyridinium	increases expression	1
Sodium Selenite	decreases expression	1
Cadmium Chloride	decreases expression, increases abundance	1

ChEMBL screening assays

147 unique, capped per target: 114 binding, 32 functional, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1009180	Binding	Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst3 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
CHEMBL1102026	Functional	Antagonist activity at human recombinant SST3 receptor expressed in CHO cells assessed as inhibition of SRIF14-induced cAMP accumulation	Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst(3) receptor antagonists. — Bioorg Med Chem Lett
CHEMBL4195975	ADMET	Drug uptake in HEK293 cells co-expressing SSTR3 (unknown origin) and RFP assessed as SSTR3-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

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

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

Cellosaurus	Name	Category	Sex
CVCL_H501	CHO-K1/SST3/Galpha15	Spontaneously immortalized cell line	Female
CVCL_KV82	cAMP Hunter CHO-K1 SSTR3 Gi	Spontaneously immortalized cell line	Female
CVCL_KZ13	PathHunter CHO-K1 SSTR3 beta-arrestin	Spontaneously immortalized cell line	Female
CVCL_KZ67	PathHunter HEK 293 SSTR3 beta-arrestin	Transformed cell line	Female

Clinical trials (associated diseases)

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