SSTR1

Summary

SSTR1 (somatostatin receptor 1, HGNC:11330) is a protein-coding gene on chromosome 14q21.1, encoding Somatostatin receptor type 1 (P30872). Receptor for somatostatin with higher affinity for somatostatin-14 than -28.

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. The protein encoded by this gene is a member of the superfamily of somatostatin receptors having seven transmembrane segments. 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 somatostatin receptor has greater affinity for somatostatin-14 than -28.

Source: NCBI Gene 6751 — RefSeq curated summary.

At a glance

• GWAS associations: 3
• Clinical variants (ClinVar): 62 total
• Druggable target: yes — 5 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_001049

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:11330
Approved symbol	SSTR1
Name	somatostatin receptor 1
Location	14q21.1
Locus type	gene with protein product
Status	Approved
Ensembl gene	ENSG00000139874
Ensembl biotype	protein_coding
OMIM	182451
Entrez	6751

Gene structure

Transcript identifiers

Ensembl transcripts: 2 — 2 protein_coding

ENST00000267377, ENST00000886873

RefSeq mRNA: 1 — MANE Select: NM_001049 NM_001049

CCDS: CCDS9666

Canonical transcript exons

ENST00000267377 — 3 exons

Exon	Start	End
ENSE00001336207	38208443	38208609
ENSE00001336209	38207904	38208104
ENSE00002510222	38209046	38213067

Expression profiles

Bgee: expression breadth ubiquitous, 173 present calls, max score 92.81.

FANTOM5 (CAGE): breadth broad, TPM avg 2.8386 / max 128.5940, expressed in 486 samples.

FANTOM5 promoters (6 alternative TSS)

Promoter ID	TPM avg	Samples expressed
139333	1.8225	387
139335	0.5369	234
139331	0.2055	87
139334	0.1347	57
139330	0.0998	36
139332	0.0391	18

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
stromal cell of endometrium	CL:0002255	92.81	gold quality
jejunal mucosa	UBERON:0000399	88.21	gold quality
Brodmann (1909) area 46	UBERON:0006483	85.35	gold quality
duodenum	UBERON:0002114	85.12	gold quality
prefrontal cortex	UBERON:0000451	81.53	gold quality
middle temporal gyrus	UBERON:0002771	80.34	gold quality
substantia nigra pars reticulata	UBERON:0001966	80.31	gold quality
substantia nigra pars compacta	UBERON:0001965	80.30	gold quality
Brodmann (1909) area 23	UBERON:0013554	78.95	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	78.53	gold quality
islet of Langerhans	UBERON:0000006	78.10	gold quality
anterior cingulate cortex	UBERON:0009835	77.70	gold quality
frontal cortex	UBERON:0001870	77.65	gold quality
frontal lobe	UBERON:0016525	77.65	gold quality
entorhinal cortex	UBERON:0002728	77.18	gold quality
right lung	UBERON:0002167	76.80	gold quality
right lobe of liver	UBERON:0001114	76.76	gold quality
neocortex	UBERON:0001950	76.44	gold quality
body of stomach	UBERON:0001161	76.38	gold quality
Brodmann (1909) area 9	UBERON:0013540	76.35	gold quality
superior frontal gyrus	UBERON:0002661	75.71	gold quality
cerebral cortex	UBERON:0000956	75.38	gold quality
ileal mucosa	UBERON:0000331	75.25	gold quality
temporal lobe	UBERON:0001871	74.89	gold quality
hypothalamus	UBERON:0001898	74.80	gold quality
parietal pleura	UBERON:0002400	74.75	gold quality
right frontal lobe	UBERON:0002810	74.31	gold quality
stomach	UBERON:0000945	74.16	gold quality
visceral pleura	UBERON:0002401	73.70	gold quality
amygdala	UBERON:0001876	73.56	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-MTAB-5061	yes	10.01
E-ANND-3	yes	3.24

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): E2F1, EZH2, PDX1, POU1F1, POU3F1, SREBF1

miRNA regulators (miRDB)

83 targeting SSTR1, 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-5011-5P	100.00	83.46	5820
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-3613-3P	100.00	76.36	7965
HSA-MIR-3120-5P	100.00	65.56	965
HSA-MIR-5692A	100.00	74.40	6850
HSA-MIR-4510	100.00	66.60	2050
HSA-MIR-6127	100.00	66.76	2188
HSA-MIR-6129	100.00	66.46	2080
HSA-MIR-6130	100.00	66.69	2012
HSA-MIR-6133	100.00	66.48	2064
HSA-MIR-4533	100.00	69.48	2758
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-4789-5P	99.98	70.76	2721
HSA-MIR-5696	99.98	72.36	4487
HSA-MIR-548P	99.98	72.25	3784
HSA-MIR-27A-3P	99.98	72.13	2955
HSA-MIR-27B-3P	99.98	72.13	2955
HSA-MIR-9985	99.98	72.11	2939
HSA-MIR-495-3P	99.96	72.81	4197
HSA-MIR-5688	99.96	73.23	4504
HSA-MIR-552-5P	99.93	68.56	1583
HSA-MIR-6835-3P	99.93	70.49	2904
HSA-MIR-10527-5P	99.91	72.28	3754
HSA-MIR-8062	99.88	68.43	995
HSA-MIR-4779	99.86	66.50	1583
HSA-MIR-4503	99.85	71.45	1869
HSA-MIR-4668-5P	99.79	70.58	3782
HSA-MIR-3934-3P	99.76	65.51	1351
HSA-MIR-1255A	99.74	68.09	744

Literature-anchored findings (GeneRIF, showing 37)

• 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)
• selective activation reduces cell growth and calcitonin secretion in a human medullary thyroid carcinoma cell line (PMID:12359227)
• the 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)
• SSTR1 selective activation inhibits hormone secretion and cell viability in GH- and PRL-secreting adenomas in. SRIF analogs with affinity for SSTR1 may be useful to control hormone hypersecretion and reduce neoplastic growth of pituitary adenomas. (PMID:12788890)
• activation of hSSTR1 is not necessary for heterodimeric assembly (PMID:15247250)
• transcriptional regulation of the human SST1 was analyzed in the present study (PMID:17533578)
• Analysis of orbital tissues reveals upregulation of SSTR1 and -2 in a group of Graves’ ophthalmopathy (GO)patients. Adipogenesis, a process occurring in GO orbits, provides one possible explanation for some of the observed increase. (PMID:17848636)
• The most prominent candidates associated with aggressive prostate cancer were SSTR1 and genes related to proliferation, including TOP2A. (PMID:18347174)
• the expression of SSTR-1 mRNA in human pancreatic cancer tissue specimens, and investigated the effect of SSTR-1 overexpression on cell proliferation, cell cycle, and tumor growth in a subcutaneous nude mouse model. (PMID:18823376)
• Immunohistochemistry stufy of SSTR1 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 18.1% of cells. (PMID:18936524)
• To the best of our knowledge, this is the first report describing crosstalk/interactions between SSTRs and ErbBs. (PMID:19070659)
• An autocrine and paracrine role of SST in the lacrimal system and at the ocular surface and a role of SST in corneal immunology. (PMID:19106227)
• Both SSTR1 and 2 mRNA levels in SCA were greater than Cushing disease, while SSTR1 mRNA levels, but not SSTR2, in silent corticotroph adenoma were also greater than non-functioning pituitary tumor. (PMID:19318729)
• SSTR1 had higher expression in patients that had normalized GH and IGF-I. There was a positive correlation between the percentage of tumor reduction by octreotide-lar and SSTR1 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 summarized expression pattern of SSTR in the investigated neuroendocrine tumors in our material was: SSTR 1> SSTR 5> SSTR 3> SSTR 2A> SSTR 2B. (PMID:20529830)
• Data show that the mRNA levels of SSTR1, SSTR2, SSTR3, and SSTR5 were high in PET compared with AC, whereas the expression of SSTR4 was low in PET and AC. (PMID:20717067)
• Overexpressed in endomterium inendometriosis. (PMID:20739383)
• Data demonstrate that cells transfected with SSTR1 or SSTR1/5 negatively regulates EGF mediated effects attributed to the inhibition of EGFR phosphorylation. (PMID:21419811)
• Activated/phosphorylated pMAPK 44/42 was detected in 82% of medulloblastomas, all subtypes, and in 62.5% of primitive neuroectodermal tumors with coexpression of SSR1 in one third. (PMID:23455179)
• The UMB-7 may prove of great value in the identification of sst1-expressing tumors during routine histopathological examinations. This may open up new routes for diagnostic and therapeutic intervention. (PMID:23466804)
• Somatostatin receptor 1 is a novel methylated gene driven by EBV infection in gastric cancer cells and acts as a potential tumour suppressor. (PMID:23722468)
• Somatostatin receptor imaging (SRI) using SPECT or PET as a whole-body imaging technique has become a crucial part of the management of Neuroendocrine tumors (PMID:24106690)
• SSTRs are overexpressed in primary pigmented nodular adrenocortical disease tissues in comparison with normal adrenal cortex (PMID:24512486)
• Tumor cells in the tissue samples of the patients diagnosed with advanced-stage hepatocellular carcinoma expressed a high proportion of SSTR1 and SSTR5. (PMID:24634938)
• SSTR-PET showed high sensitivity for imaging bone, soft tissue and brain metastases, and particularly in combination with CT had a significant impact on clinical stage and patient management. (PMID:24742330)
• Aberrant methylation inactivates somatostatin and SSTR1 in head and neck squamous cell carcinoma. (PMID:25734919)
• 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)
• High SSTR1 expression is associated with hepatocellular and cholangiocellular carcinomas in tumor capillaries. (PMID:29282035)
• Predictive and prognostic significance of tumour subtype, SSTR1-5 and e-cadherin expression in a well-defined cohort of patients with acromegaly. (PMID:33491286)
• The impact of SST2 trafficking and signaling in the treatment of pancreatic neuroendocrine tumors. (PMID:33675866)
• Selectivity Comparison of Tumor-Imaging Probes Designed Based on Various Tumor-Targeting Strategies: A Proof of Concept Study. (PMID:35014332)
• 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	sstr1a	ENSDARG00000104922
mus_musculus	Sstr1	ENSMUSG00000035431
rattus_norvegicus	Sstr1	ENSRNOG00000048145
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), SSTR5 (ENSG00000162009), GPR149 (ENSG00000174948), SSTR2 (ENSG00000180616), UTS2R (ENSG00000181408), PTGDR2 (ENSG00000183134), CMKLR2 (ENSG00000183671), LTB4R (ENSG00000213903), LTB4R2 (ENSG00000213906), SSTR3 (ENSG00000278195), NPBWR1 (ENSG00000288611)

Protein

Protein identifiers

Somatostatin receptor type 1 — P30872 (reviewed: P30872)

Alternative names: SRIF-2

All UniProt accessions (1): P30872

UniProt curated annotations — full annotation on UniProt →

Function. Receptor for somatostatin with higher affinity for somatostatin-14 than -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and Na(+)/H(+) exchanger via pertussis toxin insensitive G proteins.

Subunit / interactions. Interacts with SKB1.

Subcellular location. Cell membrane.

Tissue specificity. Fetal kidney, fetal liver, and adult pancreas, brain, lung, jejunum and stomach.

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

RefSeq proteins (1): NP_001040* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR000276	GPCR_Rhodpsn	Family
IPR000586	Somatstn_rcpt	Family
IPR001116	Somatstn_rcpt_1	Family
IPR017452	GPCR_Rhodpsn_7TM	Domain

Pfam: PF00001

UniProt features (24 total): topological domain 8, transmembrane region 7, glycosylation site 3, compositionally biased region 2, chain 1, region of interest 1, lipid moiety-binding region 1, disulfide bond 1

Structure

Experimental structures (PDB)

4 structures.

PDB	Method	Resolution (Å)
8XIO	ELECTRON MICROSCOPY	2.65
9IK8	ELECTRON MICROSCOPY	2.82
8XIP	ELECTRON MICROSCOPY	3.29
9IK9	ELECTRON MICROSCOPY	3.37

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-P30872-F1	79.74	0.54

Antibody-complex structures (SAbDab): 2 — 8XIO, 8XIP

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): 339

Disulfide bonds (1): 130–208

Glycosylation sites (3): 4, 44, 48

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

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

MSigDB gene sets: 125 (showing top): RNGTGGGC_UNKNOWN, GOBP_HINDBRAIN_DEVELOPMENT, GOBP_METENCEPHALON_DEVELOPMENT, BENPORATH_ES_WITH_H3K27ME3, GOBP_RESPONSE_TO_ESTRADIOL, GOBP_RESPONSE_TO_PEPTIDE, GOBP_CELLULAR_RESPONSE_TO_LIPID, GOBP_MALE_GAMETE_GENERATION, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_FOREBRAIN_DEVELOPMENT, REACTOME_PEPTIDE_LIGAND_BINDING_RECEPTORS, GOBP_HORMONE_MEDIATED_SIGNALING_PATHWAY, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, KEGG_NEUROACTIVE_LIGAND_RECEPTOR_INTERACTION, GOBP_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND

GO Biological Process (13): G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger (GO:0007187), glutamate receptor signaling pathway (GO:0007215), neuropeptide signaling pathway (GO:0007218), spermatogenesis (GO:0007283), negative regulation of cell population proliferation (GO:0008285), cerebellum development (GO:0021549), forebrain development (GO:0030900), response to starvation (GO:0042594), cellular response to estradiol stimulus (GO:0071392), cellular response to leukemia inhibitory factor (GO:1990830), signal transduction (GO:0007165), G protein-coupled receptor signaling pathway (GO:0007186), somatostatin signaling pathway (GO:0038170)

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

GO Cellular Component (3): plasma membrane (GO:0005886), neuron projection (GO:0043005), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

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

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
G protein-coupled receptor signaling pathway	3
anatomical structure development	2
cell surface receptor signaling pathway	1
glutamate receptor activity	1
developmental process involved in reproduction	1
male gamete generation	1
cell population proliferation	1
regulation of cell population proliferation	1
negative regulation of cellular process	1
metencephalon development	1
brain development	1
response to stress	1
response to nutrient levels	1
response to estradiol	1
cellular response to lipid	1
cellular response to oxygen-containing compound	1
cellular response to cytokine stimulus	1
response to leukemia inhibitory factor	1
cell communication	1
cellular process	1
signaling	1
regulation of cellular process	1
cellular response to stimulus	1
G protein-coupled receptor activity	1
signal transduction	1
hormone-mediated signaling pathway	1
somatostatin receptor signaling pathway	1
neuropeptide receptor activity	1
somatostatin signaling pathway	1
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

830 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SSTR1	SST	P01166	999
SSTR1	CORT	O00230	885
SSTR1	CHGA	P10645	552
SSTR1	PCSK2	P16519	520
SSTR1	GCG	P01275	512
SSTR1	NPY5R	Q15761	503
SSTR1	PYGB	P11216	472
SSTR1	CRH	P06850	462
SSTR1	BCL2L11	O43521	443
SSTR1	TACR2	P21452	443
SSTR1	KCNC4	Q03721	438
SSTR1	CSNK1D	P48730	436
SSTR1	SSTR5	P34988	435
SSTR1	CXCL6	P80162	433
SSTR1	CXCL14	O95715	433

IntAct

10 interactions, top by confidence:

A	B	Type	Score
SSTR1	SSTR5	psi-mi:“MI:2364”(proximity)	0.520
SSTR1	SSTR5	psi-mi:“MI:0403”(colocalization)	0.520
SSTR1	SSTR5	psi-mi:“MI:0915”(physical association)	0.520
SSTR1	GOPC	psi-mi:“MI:0915”(physical association)	0.400
SSTR1	RAMP2	psi-mi:“MI:0915”(physical association)	0.400
SSTR1	RAMP3	psi-mi:“MI:0915”(physical association)	0.400
RAMP3	SSTR1	psi-mi:“MI:0915”(physical association)	0.400
DND1	RPSA2	psi-mi:“MI:0914”(association)	0.350
SSTR1	SSRP1	psi-mi:“MI:0914”(association)	0.350

BioGRID (15): DLG1 (Reconstituted Complex), DLG1 (Affinity Capture-Western), SSTR1 (Affinity Capture-Western), SSTR1 (Protein-peptide), SUPT16H (Affinity Capture-MS), SLC27A3 (Affinity Capture-MS), LRRC8E (Affinity Capture-MS), TMEM259 (Affinity Capture-MS), ARL8B (Affinity Capture-MS), SSRP1 (Affinity Capture-MS), CYP51A1 (Affinity Capture-MS), RNF185 (Affinity Capture-MS), PRMT5 (Affinity Capture-Western), PRMT5 (Reconstituted Complex), SSTR1 (Protein-peptide)

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: A1ZAX0, B2ZI34, E7F7V7, F1MV99, F1R332, O08726, O08786, O43603, O54798, O54799, O62709, O88626, O88854, O97666, O97772, O97967, P05363, P08911, P08912, P21451, P21729, P22270, P24053, P24530, P25101, P26684, P28088, P28336, P28646, P30550, P30551, P30552, P30553, P30796, P30872, P30873, P30937, P30974, P31391, P32238

SIGNOR signaling

5 interactions.

A	Effect	B	Mechanism
EZH2	“down-regulates quantity by repression”	SSTR1	“transcriptional regulation”
SSTR1	“up-regulates activity”	GNAI1	binding
SSTR1	“up-regulates activity”	GNAI3	binding
SSTR1	“up-regulates activity”	GNA12	binding
somatostatin	“up-regulates activity”	SSTR1	“chemical activation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	52
Likely benign	1
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

317 predictions. Top by Δscore:

Variant	Effect	Δscore
14:38208217:G:GT	donor_gain	0.9900
14:38208593:G:GT	donor_gain	0.9800
14:38208608:GG:G	donor_gain	0.9700
14:38208609:GG:G	donor_gain	0.9700
14:38208609:GGTA:G	donor_loss	0.9700
14:38208610:G:GA	donor_loss	0.9700
14:38208611:T:TC	donor_loss	0.9700
14:38208610:G:GG	donor_gain	0.9600
14:38208122:G:T	donor_gain	0.9500
14:38208106:TACA:T	donor_gain	0.9400
14:38208107:ACAA:A	donor_gain	0.9400
14:38208108:CAAA:C	donor_gain	0.9300
14:38208597:T:TA	donor_gain	0.9200
14:38208111:A:AG	donor_gain	0.9000
14:38208112:G:GG	donor_gain	0.9000
14:38208182:G:GA	donor_gain	0.9000
14:38208204:C:T	donor_gain	0.9000
14:38208612:AAG:A	donor_loss	0.9000
14:38208103:GG:G	donor_gain	0.8900
14:38208104:GG:G	donor_gain	0.8900
14:38208184:A:G	donor_gain	0.8700
14:38208654:C:T	donor_gain	0.8600
14:38208246:C:G	donor_gain	0.8500
14:38208598:T:TA	donor_gain	0.8500
14:38208102:AG:A	donor_gain	0.8400
14:38209432:A:AG	acceptor_gain	0.8400
14:38209432:AGCCC:A	acceptor_gain	0.8400
14:38209433:G:GG	acceptor_gain	0.8400
14:38208103:G:A	donor_gain	0.8300
14:38208943:T:G	donor_gain	0.8300

AlphaMissense

2555 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
14:38209603:G:A	G72R	1.000
14:38209603:G:C	G72R	1.000
14:38209604:G:A	G72E	1.000
14:38209617:C:A	N76K	1.000
14:38209617:C:G	N76K	1.000
14:38209686:T:A	N99K	1.000
14:38209686:T:G	N99K	1.000
14:38209688:T:C	L100P	1.000
14:38209699:G:C	D104H	1.000
14:38209700:A:C	D104A	1.000
14:38209700:A:T	D104V	1.000
14:38209758:G:C	W123C	1.000
14:38209758:G:T	W123C	1.000
14:38209819:A:C	S144R	1.000
14:38209821:C:A	S144R	1.000
14:38209821:C:G	S144R	1.000
14:38209843:A:C	S152R	1.000
14:38209845:C:A	S152R	1.000
14:38209845:C:G	S152R	1.000
14:38209853:G:C	R155P	1.000
14:38210227:T:C	F280L	1.000
14:38210229:T:A	F280L	1.000
14:38210229:T:G	F280L	1.000
14:38209594:T:C	C69R	0.999
14:38209603:G:T	G72W	0.999
14:38209612:G:A	G75R	0.999
14:38209612:G:C	G75R	0.999
14:38209613:G:A	G75E	0.999
14:38209615:A:C	N76H	0.999
14:38209615:A:G	N76D	0.999

dbSNP variants (sampled 300 via entrez): RS1000372493 (14:38211626 C>T), RS1000730866 (14:38206324 A>G), RS1001157299 (14:38211932 A>C), RS1001204367 (14:38206114 C>G), RS1001377547 (14:38211774 G>T), RS1001730634 (14:38206175 A>G), RS1001870422 (14:38208889 T>A), RS1002167854 (14:38210714 C>G,T), RS1002808352 (14:38207879 T>C), RS1002938491 (14:38207268 C>G), RS1003798371 (14:38207505 C>A,T), RS1004503283 (14:38210732 C>A,T), RS1004564428 (14:38206063 C>A), RS1005911812 (14:38206434 C>T), RS1006110361 (14:38212233 G>A)

Disease associations

OMIM: gene MIM:182451 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

3 associations (top):

Study	Trait	p-value
GCST001821_11	Metabolite levels (5-HIAA/ MHPG Ratio)	5.000000e-08
GCST002929_15	Chromium levels	6.000000e-07
GCST003192_2	Coronary artery aneurysm in Kawasaki disease	9.000000e-06

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0005132	5-HIAA measurement
EFO:0005133	MHPG measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (2): CHEMBL1917 (SINGLE PROTEIN), CHEMBL2111436 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

5 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 17,306 (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
CHEMBL3696475	MK-7145	1	8

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 (28 total), top 25:

Ligand	Action	Affinity	Parameter
[125I]LTT-SRIF-28	Full agonist	10.0	pKd
[125I]Tyr10-CST14	Full agonist	10.0	pKd
[125I]CGP 23996	Full agonist	9.6	pKd
CST-17	Full agonist	9.6	pKi
SRIF-14	Full agonist	9.5	pKi
SRIF-28	Full agonist	9.4	pKi
[125I]Tyr11-SRIF-14	Full agonist	9.2	pKd
cortistatin-14	Full agonist	9.1	pKi
Des-AA5-[D-Trp8]SRIF	Full agonist	9.1	pIC50
L-797,591	Full agonist	8.8	pKi
CH 275	Full agonist	8.7	pIC50
KE 108	Full agonist	8.6	pIC50
BIM 23052	Full agonist	8.6	pKi
L-817,818	Full agonist	8.5	pKi
CGP 23996	Full agonist	8.4	pKi
Des-AA1,2,5,12,13-[D-Trp8]SRIF	Full agonist	8.3	pIC50
cyclo(7-12) Des-AA1,2,5-[Glu7,D-Trp8,IAmp9,m-I-Tyr11,hhLys12]SRIF	Full agonist	8.2	pIC50
SRA880	Antagonist	8.1	pKd
pasireotide	Full agonist	8.0	pIC50
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF	Full agonist	7.8	pIC50
Des-Ala1,2,5-[D-Trp8,IAmp9]SRIF	Full agonist	7.5	pIC50
NC 4-28B	Full agonist	7.4	pKi
BIM 23050	Full agonist	6.4	pIC50
L-362,855	Full agonist	6.2	pKi
BIM 23454	Antagonist	6.0	pIC50

Binding affinities (BindingDB)

126 measured of 138 human assays (138 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
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-14	KI	0.63 nM
SS-25	KI	0.79 nM
Cortistatin(1-14)	KI	0.85 nM
Tyr10-cortistatin	KI	0.91 nM
CST14-Tyr10	KI	0.91 nM
L-797591	KI	1.4 nM
CH-275	KI	1.8 nM
L-817,818	KI	3.3 nM
octreotide	KI	12 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)-6-[(1R)-1-hydroxyethyl]-3-[(4-hydroxyphenyl)methyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]acetamide	KI	15 nM	US-8952128: Somatostatin-dopamine chimeric analogs
BIM 23268	KI	18.4 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)-3,15,18-tribenzyl-21-(3-carbamimidamidopropyl)-6-[(1R)-1-hydroxyethyl]-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17,20,23-octaoxo-1,4,7,10,13,16,19,22-octazacyclooctacos-24-yl]amino]-3-(4-hydroxyphenyl)propan-2-yl]acetamide	KI	24.2 nM	US-8952128: Somatostatin-dopamine chimeric analogs
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-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfinyl]-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	32.5 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-[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-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfinyl]-N-[(5S)-5-[[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfinyl]acetyl]amino]-6-[[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-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	67.6 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]methylsulfinyl]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	76.5 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
c[Aha-Phe-D-Trp-Lys-Ser(Bzl)]	KI	80 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)-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]hexyl]acetamide	KI	84.2 nM	US-8952128: Somatostatin-dopamine chimeric analogs
BIM 23295	KI	86.8 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
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-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	115 nM	US-8952128: Somatostatin-dopamine chimeric analogs
1-[3-[(2S,5S,8S,11R,14S,17S,20S,27R)-14-(4-aminobutyl)-5,20-dibenzyl-27-[bis[2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]ethyl]amino]-17-[(1R)-1-hydroxyethyl]-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	135 nM	US-8952128: Somatostatin-dopamine chimeric analogs
c[Aha-Phe-D-Trp-Lys-Thr(Bzl)]	KI	141 nM
D-Phe-AIa-Tyr-D-Trp-Lys-Val-Ala-D-Nal-NH2	KI	145 nM
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfinyl]-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	149 nM	US-8952128: Somatostatin-dopamine chimeric analogs
BIM 23313	KI	151 nM
2-[[(6aR,9R,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]methylsulfanyl]-N-[(3S,6S,9S,12R,15S,18S,21S,24R)-9-(4-aminobutyl)-3,18-dibenzyl-21-[3-(diaminomethylideneamino)propyl]-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]acetamide	KI	175 nM	US-8952128: Somatostatin-dopamine chimeric analogs
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
c[Ahx-Phe-D-Trp-Lys-Thr(Bzl)]	KI	183 nM
L-803,087	KI	199 nM

ChEMBL bioactivities

689 potent at pChembl≥5 of 750 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.85	IC50	0.14	nM	SOMATOSTATIN
9.80	Ki	0.1585	nM	CHEMBL3349516
9.72	IC50	0.19	nM	CHEMBL558161
9.70	IC50	0.2	nM	CHEMBL437296
9.70	Ki	0.1995	nM	CHEMBL3349522
9.60	Ki	0.2512	nM	CHEMBL3349521
9.54	Ki	0.29	nM	SOMATOSTATIN
9.54	Kd	0.29	nM	CHEMBL440072
9.51	Ki	0.31	nM	CHEMBL3098601
9.49	Ki	0.32	nM	CHEMBL1823873
9.46	IC50	0.35	nM	CHEMBL376485
9.44	Ki	0.36	nM	SOMATOSTATIN
9.43	EC50	0.37	nM	CHEMBL558161
9.42	Ki	0.38	nM	CHEMBL408362
9.42	Ki	0.38	nM	SOMATOSTATIN
9.37	Ki	0.43	nM	SOMATOSTATIN
9.34	IC50	0.46	nM	SANDOSTATIN
9.30	IC50	0.5	nM	CHEMBL376484
9.30	Ki	0.5012	nM	CHEMBL3349517
9.20	Ki	0.631	nM	SOMATOSTATIN
9.20	Ki	0.631	nM	CHEMBL3349518
9.19	IC50	0.64	nM	CHEMBL426548
9.10	IC50	0.8	nM	CHEMBL555977
9.10	Ki	0.7943	nM	CHEMBL3349513
9.08	IC50	0.83	nM	SOMATOSTATIN
9.03	EC50	0.93	nM	CHEMBL563125
9.01	IC50	0.98	nM	CHEMBL408338
9.00	IC50	1	nM	CHEMBL409100
9.00	IC50	1	nM	CHEMBL553655
9.00	IC50	1	nM	CHEMBL555977
8.96	IC50	1.1	nM	CHEMBL3350037
8.92	IC50	1.2	nM	CHEMBL2021559
8.91	Kd	1.23	nM	CHEMBL251835
8.80	IC50	1.6	nM	CHEMBL222699
8.80	IC50	1.6	nM	CHEMBL268060
8.80	Ki	1.6	nM	CHEMBL71723
8.80	Ki	1.585	nM	CHEMBL3349605
8.80	Ki	1.585	nM	CHEMBL3349606
8.80	IC50	1.6	nM	SOMATOSTATIN
8.79	Kd	1.622	nM	CHEMBL460542
8.76	Kd	1.738	nM	ERGOLINE
8.72	IC50	1.9	nM	SOMATOSTATIN
8.72	Ki	1.9	nM	CHEMBL442494
8.72	IC50	1.9	nM	CHEMBL442494
8.70	IC50	2	nM	CHEMBL442494
8.70	Ki	2	nM	CHEMBL1794035
8.67	Kd	2.138	nM	CHEMBL540705
8.66	IC50	2.21	nM	CAMPTOTHECIN
8.66	IC50	2.2	nM	CHEMBL442494
8.64	Ki	2.3	nM	SOMATOSTATIN

PubChem BioAssay actives

532 with measured affinity, of 890 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	752208: Binding affinity to Somatostatin receptor type 1 (unknown origin) by radioligand displacement assay	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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) 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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0002	uM
(4R,7S,10S,13R,16S,19R)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]-7,16-dibenzyl-13-[methyl(naphthalene-2-carbonyl)amino]-6,9,12,15,18-pentaoxo-10-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	423836: Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography	ic50	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,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	1061947: Displacement of [125I]-somatostatin from human SSTR1 expressed in CHO-K1 cells	ki	0.0003	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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0003	uM
(4R,7S,10R,13S,16R,19S,22R,25S,28R,31S)-13,28-bis(4-aminobutyl)-25-(2-amino-2-oxoethyl)-31-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-19,22-dibenzyl-10-[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-16-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30-nonaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29-nonazacyclodotriacontane-4-carboxylic acid	1638705: Displacement of [125I]somatostatin from human SSTR1 expressed in CHO-K1 cell membranes after 120 mins	kd	0.0003	uM
(2S)-6-amino-2-[[(2S)-2-amino-3-[[2-[2-[(2R,5S,8S,11S,14S,17S)-11-(4-aminobutyl)-17-benzyl-14-[(1R)-1-hydroxyethyl]-5-[(4-hydroxyphenyl)methyl]-8-(1H-indol-3-ylmethyl)-1-methyl-3,6,9,12,15,18-hexaoxo-1,4,7,10,13,16-hexazacyclooctadec-2-yl]ethylsulfanyl]acetyl]amino]propanoyl]amino]-N-[(2R)-1-[[(2R,3R)-1,3-dihydroxybutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]hexanamide	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0003	uM
(2S,5S,8S,11S,14S,17S,20S,23S,26S,29S,32S,34Z,37S)-2,17-bis(4-aminobutyl)-5-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-8,11,23-tribenzyl-20,26-bis[(1R)-1-hydroxyethyl]-29-(hydroxymethyl)-14-(1H-indol-3-ylmethyl)-3,6,9,12,15,18,21,24,27,30,38-undecaoxo-1,4,7,10,13,16,19,22,25,28,31-undecazacyclooctatriacont-34-ene-32-carboxamide	1061947: Displacement of [125I]-somatostatin from human SSTR1 expressed in CHO-K1 cells	ki	0.0003	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	203079: Binding affinity towards human sst1 receptor expressed in CHO-K1 cells	ki	0.0004	uM
(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-16-[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-10-methyl-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxamide	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0005	uM
(2S)-2-[[(2S)-2-amino-3-[[2-[2-[(2R,5S,8S,11S,14S,17S)-11-(4-aminobutyl)-17-benzyl-14-[(1R)-1-hydroxyethyl]-5-[(4-hydroxyphenyl)methyl]-8-(1H-indol-3-ylmethyl)-1-methyl-3,6,9,12,15,18-hexaoxo-1,4,7,10,13,16-hexazacyclooctadec-2-yl]ethylsulfanyl]acetyl]amino]propanoyl]amino]-3-(4-aminophenyl)-N-[(2R)-1-[[(2R,3R)-1,3-dihydroxybutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]propanamide	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0005	uM
(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]-25,28-dibenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-13-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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) 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
(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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0008	uM
(4R,7S,10S,13R,16S,19R)-19-[[(2S)-2-amino-3-(4-hydroxy-2-iodophenyl)propanoyl]amino]-N-[(2R,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-7,16-dibenzyl-13-[methyl(naphthalene-2-carbonyl)amino]-6,9,12,15,18-pentaoxo-10-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	423836: Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography	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-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-yl)-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	423840: Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14	ec50	0.0009	uM
(4R,7S,10S,13R,16S,19R)-19-amino-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-7,16-dibenzyl-13-[methyl(naphthalene-2-carbonyl)amino]-6,9,12,15,18-pentaoxo-10-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	423836: Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography	ic50	0.0010	uM
(4S,7R,10S,13R,16S,19R,22S,25R,28S,31R,34S)-19,31-bis(4-aminobutyl)-34-[[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-decaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid	203259: Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.	ic50	0.0010	uM
(4R,7S,10R,13S,16R,19S,22S,25S,28R,31R,34S)-19,31-bis(4-aminobutyl)-34-[[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-decaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid	242515: Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1	ic50	0.0010	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
[(6aR,9R,10aR)-5-bromo-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]-[4-(2,1,3-benzoxadiazol-5-yl)piperazin-1-yl]methanone	313961: Binding affinity to human recombinant sst1 receptor	kd	0.0012	uM
(4R,7S,10S,13R,16S,19R)-19-amino-N-[(2S)-1-amino-3-naphthalen-2-yl-1-oxopropan-2-yl]-7,16-dibenzyl-13-[methyl(naphthalene-2-carbonyl)amino]-6,9,12,15,18-pentaoxo-10-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	423836: Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography	ic50	0.0012	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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0016	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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0016	uM
1-[4-(3,4-difluorophenyl)piperazin-1-yl]-3-[methyl-[2-(9H-xanthen-9-yl)ethyl]amino]propan-1-one	418533: Binding affinity to human sst1 receptor	kd	0.0016	uM
N-[(2S)-1-[[(1S,3R)-3-(aminomethyl)cyclohexyl]methylamino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]spiro[indene-1,4’-piperidine]-1’-carboxamide	203079: Binding affinity towards human sst1 receptor expressed in CHO-K1 cells	ki	0.0016	uM
(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]-N-[(2S)-1-[[(2R)-1-[[(2R,3R)-1,3-dihydroxybutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]propanamide	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0016	uM
(2S,3R)-2-[[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]-N-[2-[[2-[[(2R)-1-amino-1-oxo-3-sulfanylpropan-2-yl]amino]-2-oxoethyl]amino]-2-oxoethyl]-3-hydroxybutanamide	280425: Displacement of [125I-Tyr-11]-SRIF from SSTR of human NCI-H69 cell membranes	ic50	0.0016	uM
6-[4-[(6aR,9R,10aR)-5-bromo-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinoline-9-carbonyl]piperazin-1-yl]-1-methylpyridin-2-one	313961: Binding affinity to human recombinant sst1 receptor	kd	0.0017	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	203261: Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells	ki	0.0019	uM
(4R,7S,10R,13S,16R,19S,22R,25S,28R,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-16-[(1S)-1-hydroxyethyl]-10-[(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	203261: Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 receptor expressed on CHO cells	ki	0.0020	uM
1-[4-(2,1,3-benzoxadiazol-5-yl)piperazin-1-yl]-3-[methyl-[2-(9H-xanthen-9-yl)ethyl]amino]propan-1-one	418533: Binding affinity to human sst1 receptor	kd	0.0021	uM
(19S)-19-ethyl-19-hydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione	91553: Cytotoxic activity against human neuroblastoma IMR32 cells which over-express somatostatin receptors	ic50	0.0022	uM
(4R,7S,10R,13S,16R,19S,22R,25S,28R,31R,34S)-31-(4-aminobutyl)-25,28-dibenzyl-34-(carbamoylamino)-10,16-bis[(1R)-1-hydroxyethyl]-13-[(4-hydroxy-3-iodophenyl)methyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid	203259: Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.	ic50	0.0025	uM
(4R,7S,10R,13S,16R,19S,22S,25S,28R,31R,34S)-34-amino-31-(4-aminobutyl)-25,28-dibenzyl-10,16-bis[(1R)-1-hydroxyethyl]-13-[(4-hydroxy-2-iodophenyl)methyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxamide	242515: Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1	ic50	0.0025	uM
(4R,7S,10S,13S,16S,19S,22R,25S,28S,31S,34R)-34-amino-31-(4-aminobutyl)-25,28-dibenzyl-10,16-bis[(1R)-1-hydroxyethyl]-13-[(4-hydroxy-3-(125I)iodophenyl)methyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxamide	423836: Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography	ic50	0.0025	uM
1-[4-(2,1,3-benzoxadiazol-5-yl)piperazin-1-yl]-3-[2-(9H-fluoren-9-yl)ethyl-methylamino]propan-1-one;hydrochloride	418533: Binding affinity to human sst1 receptor	kd	0.0026	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	616817: Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiography	ic50	0.0027	uM
[2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl] N-(2-aminoethyl)-N-[2-[[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2R)-1-[[(4S,7S,10S,13R,16S,19S)-4-[[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]carbamoyl]-10-(3-aminopropyl)-16-benzyl-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-2-oxoethyl]carbamate	91553: Cytotoxic activity against human neuroblastoma IMR32 cells which over-express somatostatin receptors	ic50	0.0028	uM
(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-37-[[2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-4-amino-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]propanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxypropanoyl]amino]-4-oxobutanoyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-4-carboxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]hexanoyl]amino]propanoyl]amino]acetyl]amino]-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-10,16-bis[(1S)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-2-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid	203257: Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	ic50	0.0032	uM
(4R,7S,10S,13S,16S,19S,22R,25S,28S,31S,34R)-34-amino-31-(4-aminobutyl)-25,28-dibenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-13-[(4-hydroxyphenyl)methyl]-22-[methyl(naphthalene-2-carbonyl)amino]-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid	423836: Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography	ic50	0.0033	uM
(4R,7S,10R,13S,16R,19S,22S,25S,28R,31R,34S)-34-amino-31-(4-aminobutyl)-25,28-dibenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-13-[(4-hydroxyphenyl)methyl]-22-[methyl(naphthalene-2-carbonyl)amino]-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid	242515: Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 1	ic50	0.0033	uM
(4R,7S,10R,13S,16R,19S,22R,25S,28R,31R,34S)-34-amino-31-(4-aminobutyl)-25,28-dibenzyl-10,16-bis[(1R)-1-hydroxyethyl]-13-[(4-hydroxy-3-iodophenyl)methyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid	203259: Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 1.	ic50	0.0036	uM
(4R,7S,10S,13S,16S,19S,22R,25S,28S,31S,34R)-34-amino-31-(4-aminobutyl)-25,28-dibenzyl-10,16-bis[(1R)-1-hydroxyethyl]-13-[(4-hydroxy-3-(125I)iodophenyl)methyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-19-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decazacyclopentatriacontane-4-carboxylic acid	423836: Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography	ic50	0.0036	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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0040	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	203390: Binding affinity towards human Somatostatin receptor type 1 (sst1) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells	ki	0.0040	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	616817: Displacement of 125I-[LTT]-SRIF-28 from human sst1 receptor in CHO cells after 2 hrs by autoradiography	ic50	0.0041	uM
(4R,7S,10S,13R,16S,19R)-19-amino-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-[methyl(naphthalene-2-carbonyl)amino]-6,9,12,15,18-pentaoxo-10-[[4-[(propan-2-ylamino)methyl]phenyl]methyl]-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide	423836: Displacement of [125I]LTT-SRIF-28 from human sst1 receptor by autoradiography	ic50	0.0047	uM

CTD chemical–gene interactions

29 total (human), top 29 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Ethanol	affects cotreatment, increases expression	2
Nickel	decreases expression	2
bisphenol A	affects cotreatment, decreases expression	1
trichostatin A	increases expression	1
arsenite	increases methylation	1
mono-(2-ethylhexyl)phthalate	increases expression	1
sodium arsenite	decreases expression	1
potassium chromate(VI)	increases expression	1
CGP 52608	affects binding, increases reaction	1
trans-10,cis-12-conjugated linoleic acid	decreases expression	1
pasireotide	affects binding	1
licochalcone B	decreases expression	1
bisphenol S	decreases expression	1
(+)-JQ1 compound	decreases expression	1
N-(3-aminopropyl)-N-(1-(5-benzyl-3-methyl-4-oxo-(1,2)thiazolo(5,4-d)pyrimidin-6-yl)-2-methylpropyl)-4-methylbenzamide	decreases activity	1
Resveratrol	affects cotreatment, decreases expression	1
Zoledronic Acid	decreases expression	1
Air Pollutants	decreases expression, increases abundance	1
Benzo(a)pyrene	affects methylation, increases methylation	1
Copper	affects cotreatment, decreases expression	1
Dexamethasone	affects cotreatment, decreases expression	1
Folic Acid	affects cotreatment, increases expression	1
Indomethacin	affects cotreatment, decreases expression	1
Progesterone	decreases expression	1
Somatostatin	increases expression	1
Valproic Acid	increases expression	1
Vanadates	decreases expression	1
1-Methyl-3-isobutylxanthine	affects cotreatment, decreases expression	1
Particulate Matter	decreases expression, increases abundance	1

ChEMBL screening assays

135 unique, capped per target: 121 binding, 13 functional, 1 admet

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1009178	Binding	Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst1 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
CHEMBL1024531	Functional	Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14	Novel, potent, and radio-iodinatable somatostatin receptor 1 (sst1) selective analogues. — J Med Chem
CHEMBL4195973	ADMET	Drug uptake in HEK293 cells co-expressing SSTR1 (unknown origin) and RFP assessed as SSTR1-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

6 cell lines: 3 cancer cell line, 2 spontaneously immortalized cell line, 1 transformed cell line

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

Cellosaurus	Name	Category	Sex
CVCL_E0PZ	Ubigene HeLa SSTR1 KO	Cancer cell line	Female
CVCL_H499	CHO-K1/SST1/Gqi5	Spontaneously immortalized cell line	Female
CVCL_LB33	PathHunter U2OS SSTR1 beta-arrestin	Cancer cell line	Female
CVCL_T382	Psi-CRIP-hSSR-bsr	Transformed cell line	Male
CVCL_U009	CHO-SSTR1	Spontaneously immortalized cell line	Female
CVCL_ZK21	Tango SSTR1-bla U2OS	Cancer cell line	Female

Clinical trials (associated diseases)

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