Target family: Somatostatin receptors (type: gpcr)
Target: SST<sub>2</sub> receptor

Ligand: AC-178,335 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pKi
Reference (Journal): A linear hexapeptide somatostatin antagonist blocks somatostatin activity in vitro and influences growth hormone release in rats.
Published in: Mol Pharmacol

Ligand: AM3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.640000343322754 pIC50
Reference (Journal): Radiolabeled bicyclic somatostatin-based analogs: a novel class of potential radiotracers for SPECT/PET of neuroendocrine tumors.
Published in: J Nucl Med

Ligand: analog 30 [PMID:18543899] (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pIC50
Reference (Journal): Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
Published in: J Med Chem

Ligand: analog 31 [PMID:18543899] (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Journal): Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
Published in: J Med Chem

Ligand: analog 32 [PMID:18543899] (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.920000076293945 pIC50
Reference (Journal): Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
Published in: J Med Chem

Ligand: analog 3 [PMID:18543899] (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.119999885559082 pIC50
Reference (Journal): Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
Published in: J Med Chem

Ligand: BASS antagonist (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.52 pKi
Reference (Journal): Identification and characterization of novel somatostatin antagonists.
Published in: Mol Pharmacol

Ligand: BIM 23023 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: BIM 23023 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: BIM 23023 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: BIM 23027 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: BIM 23027 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.850000381469727 pIC50
Reference (Journal): Differences in the operational characteristics of the human recombinant somatostatin receptor types, sst1 and sst2, in mouse fibroblast (Ltk-) cells.
Published in: Br J Pharmacol

Ligand: BIM 23027 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Molecular and functional properties of somatostain receptor subtypes.
Published in: Metab Clin Exp

Ligand: BIM 23030 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: BIM 23030 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: BIM 23030 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: BIM 23030 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: BIM 23034 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: BIM 23034 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 11.699999809265137 pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: BIM 23052 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: BIM 23052 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: BIM 23052 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: BIM 23052 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: BIM 23056 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: BIM 23056 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: BIM 23056 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: BIM 23056 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: BIM 23059 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 11.100000381469727 pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: BIM 23059 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: BIM 23060 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: BIM 23060 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.899999618530273 pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: BIM 23066 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: BIM 23068 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: BIM 23068 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: BIM 23197 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation.
Published in: J Clin Invest

Ligand: BIM 23454 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): Characterization of new selective somatostatin receptor subtype-2 (sst2) antagonists, BIM-23627 and BIM-23454. Effects of BIM-23627 on GH release in anesthetized male rats after short-term high-dose dexamethasone treatment.
Published in: Endocrinology

Ligand: BIM 23627 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Characterization of new selective somatostatin receptor subtype-2 (sst2) antagonists, BIM-23627 and BIM-23454. Effects of BIM-23627 on GH release in anesthetized male rats after short-term high-dose dexamethasone treatment.
Published in: Endocrinology

Ligand: BOC-ATE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pIC50
Reference (Journal): Preclinical evaluation of new and highly potent analogues of octreotide for predictive imaging and targeted radiotherapy.
Published in: Clin Cancer Res

Ligand: CGP 23996 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: CGP 23996 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: CGP 23996 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: CGP 23996 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: cortistatin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: cortistatin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: cortistatin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: CST-17 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: CST-17 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: CST-17 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Superagonism at the human somatostatin receptor subtype 4.
Published in: J Pharmacol Exp Ther

Ligand: DC 23-60 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: DC 23-60 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: demotate 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.489999771118164 pIC50
Reference (Journal): [(99m)Tc]Demotate 2 in the detection of sst(2)-positive tumours: a preclinical comparison with [(111)In]DOTA-tate.
Published in: Eur J Nucl Med Mol Imaging

Ligand: DOTA-BASS (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.819999694824219 pIC50
Reference (Journal): Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
Published in: J Med Chem

Ligand: DOTA-JR11 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
Published in: J Med Chem

Ligand: [D-Tyr8]CYN 154806 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Functional characterisation of the putative somatostatin sst2 receptor antagonist CYN 154806.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: EC 5-21 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: EC 5-21 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.600000381469727 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: edotreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2016)
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Affinity profiles for human somatostatin receptor subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use.
Published in: Eur J Nucl Med

Ligand: Ga-DOTA-NOC (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.720000267028809 pIC50
Reference (Journal): Are radiogallium-labelled DOTA-conjugated somatostatin analogues superior to those labelled with other radiometals?
Published in: Eur J Nucl Med Mol Imaging

Ligand: [Ga-DOTA,Tyr3,Thr8]octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Are radiogallium-labelled DOTA-conjugated somatostatin analogues superior to those labelled with other radiometals?
Published in: Eur J Nucl Med Mol Imaging

Ligand: [Ga-DOTA,Tyr3,Thr8]octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Affinity profiles for human somatostatin receptor subtypes SST1-SST5 of somatostatin radiotracers selected for scintigraphic and radiotherapeutic use.
Published in: Eur J Nucl Med

Ligand: Ga-KE88 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.390000343322754 pIC50
Reference (Journal): New pansomatostatin ligands and their chelated versions: affinity profile, agonist activity, internalization, and tumor targeting.
Published in: Clin Cancer Res

Ligand: Ga-NODAGA-LM3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.890000343322754 pIC50
Reference (Journal): PET of somatostatin receptor-positive tumors using 64Cu- and 68Ga-somatostatin antagonists: the chelate makes the difference.
Published in: J Nucl Med

Ligand: In-NODAGATOC (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pIC50
Reference (Journal): NODAGATOC, a new chelator-coupled somatostatin analogue labeled with [67/68Ga] and [111In] for SPECT, PET, and targeted therapeutic applications of somatostatin receptor (hsst2) expressing tumors.
Published in: Bioconjug Chem

Ligand: KE 108 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): A new peptidic somatostatin agonist with high affinity to all five somatostatin receptors.
Published in: Eur J Pharmacol

Ligand: KE 108 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.630000114440918 pEC50
Reference (Journal): Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists.
Published in: Mol Endocrinol

Ligand: KE 108 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.
Published in: Mol Endocrinol

Ligand: KE 108 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists.
Published in: Mol Endocrinol

Ligand: KE 108 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.
Published in: Mol Endocrinol

Ligand: L-054,522 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 11 pKi
Reference (Journal): Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
Published in: Proc Natl Acad Sci USA

Ligand: L-362,855 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: L-362,855 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: L-362,855 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: L-362,855 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: L-362,855 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: L-363,301 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: L-363,301 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: L-363,301 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: L-363,301 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Molecular and functional properties of somatostain receptor subtypes.
Published in: Metab Clin Exp

Ligand: L-363,377 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Molecular and functional properties of somatostain receptor subtypes.
Published in: Metab Clin Exp

Ligand: L-363,377 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
Published in: Proc Natl Acad Sci USA

Ligand: L-363,377 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
Published in: Science

Ligand: L-363,409 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 12 pIC50
Reference (Journal): Molecular and functional properties of somatostain receptor subtypes.
Published in: Metab Clin Exp

Ligand: L-779,976 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.25 pEC50
Reference (Journal): Receptor signaling and endocytosis are differentially regulated by somatostatin analogs.
Published in: Mol Pharmacol

Ligand: L-779,976 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.050000190734863 pEC50
Reference (Journal): Receptor signaling and endocytosis are differentially regulated by somatostatin analogs.
Published in: Mol Pharmacol

Ligand: L-779,976 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.300000190734863 pKi
Reference (Journal): Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
Published in: Science

Ligand: lanreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: UK (2001), FDA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: lanreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: UK (2001), FDA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: lanreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: UK (2001), FDA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: lanreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: UK (2001), FDA (2007)
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: lanreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: UK (2001), FDA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: lanreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: UK (2001), FDA (2007)
Primary target: yes
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: lanreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: UK (2001), FDA (2007)
Primary target: no
Median affinity:  pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: [L-Tyr8]CYN 154806 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Functional characterisation of the putative somatostatin sst2 receptor antagonist CYN 154806.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: maltotriose-[125I][Tyr3,Thr8]octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.020000457763672 pIC50
Reference (Journal): Comparison of radioiodinated TOC, TOCA and Mtr-TOCA: the effect of carbohydration on the pharmacokinetics.
Published in: Eur J Nucl Med Mol Imaging

Ligand: NC 4-28B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: NC 4-28B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: NC 4-28B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Molecular and functional properties of somatostain receptor subtypes.
Published in: Metab Clin Exp

Ligand: NC 8-12 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pIC50
Reference (Journal): Molecular and functional properties of somatostain receptor subtypes.
Published in: Metab Clin Exp

Ligand: NC 8-12 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.600000381469727 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: NOC-ATE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Preclinical evaluation of new and highly potent analogues of octreotide for predictive imaging and targeted radiotherapy.
Published in: Clin Cancer Res

Ligand: NODAGA-[Tyr3]-octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.489999771118164 pIC50
Reference (Journal): NODAGATOC, a new chelator-coupled somatostatin analogue labeled with [67/68Ga] and [111In] for SPECT, PET, and targeted therapeutic applications of somatostatin receptor (hsst2) expressing tumors.
Published in: Bioconjug Chem

Ligand: octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988), EMA (2022)
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
Published in: Proc Natl Acad Sci USA

Ligand: octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1988), EMA (2022)
Primary target: no
Median affinity:  pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: pasireotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Functional activity of the multiligand analog SOM230 at human recombinant somatostatin receptor subtypes supports its usefulness in neuroendocrine tumors.
Published in: Neuroendocrinology

Ligand: pasireotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Median affinity:  pEC50
Reference (Journal): Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.
Published in: Mol Endocrinol

Ligand: pasireotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Median affinity:  pEC50
Reference (Journal): Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists.
Published in: Mol Endocrinol

Ligand: pasireotide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity: 5 pEC50
Reference (Journal): Agonist-biased signaling at the sst2A receptor: the multi-somatostatin analogs KE108 and SOM230 activate and antagonize distinct signaling pathways.
Published in: Mol Endocrinol

Ligand: pasireotide (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity: 7.630000114440918 pEC50
Reference (Journal): Ligand-dependent mechanisms of sst2A receptor trafficking: role of site-specific phosphorylation and receptor activation in the actions of biased somatostatin agonists.
Published in: Mol Endocrinol

Ligand: PRL-2915 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKi
Reference (Journal): Potent antagonists of somatostatin: synthesis and biology.
Published in: J Med Chem

Ligand: PRL-2970 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Journal): Potent antagonists of somatostatin: synthesis and biology.
Published in: J Med Chem

Ligand: seglitide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: seglitide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: seglitide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: seglitide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: seglitide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
Published in: Proc Natl Acad Sci USA

Ligand: seglitide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: seglitide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: seglitide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SiFA-Asn(AcNH-β-Glc)-PEG-Tyr3-octreotate (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.479999542236328 pIC50
Reference (Journal): One-step ¹⁸F-labeling of carbohydrate-conjugated octreotate-derivatives containing a silicon-fluoride-acceptor (SiFA): in vitro and in vivo evaluation as tumor imaging agents for positron emission tomography (PET).
Published in: Bioconjug Chem

Ligand: SiFA-Asn(AcNH-β-Glc)-Tyr3-octreotate (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.359999656677246 pIC50
Reference (Journal): One-step ¹⁸F-labeling of carbohydrate-conjugated octreotate-derivatives containing a silicon-fluoride-acceptor (SiFA): in vitro and in vivo evaluation as tumor imaging agents for positron emission tomography (PET).
Published in: Bioconjug Chem

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Receptor signaling and endocytosis are differentially regulated by somatostatin analogs.
Published in: Mol Pharmacol

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Superagonism at the human somatostatin receptor subtype 4.
Published in: J Pharmacol Exp Ther

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of potent non-peptide somatostatin antagonists with sst(3) selectivity.
Published in: J Med Chem

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
Published in: Science

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.
Published in: Proc Natl Acad Sci USA

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Superagonism at the human somatostatin receptor subtype 4.
Published in: J Pharmacol Exp Ther

Ligand: [111In]DOTA-BOC-ATE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pIC50
Reference (Journal): Preclinical evaluation of new and highly potent analogues of octreotide for predictive imaging and targeted radiotherapy.
Published in: Clin Cancer Res

Ligand: [111In]DOTA-NOC (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals.
Published in: Eur J Nucl Med Mol Imaging

Ligand: [111In]DOTA-NOC-ATE (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Preclinical evaluation of new and highly potent analogues of octreotide for predictive imaging and targeted radiotherapy.
Published in: Clin Cancer Res

Ligand: [111In,90Y]DOTA-LAN (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals.
Published in: Eur J Nucl Med Mol Imaging

Ligand: [111In,90Y]DOTA-NOC (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals.
Published in: Eur J Nucl Med Mol Imaging

Ligand: [111In,90Y]DOTA-OC (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals.
Published in: Eur J Nucl Med Mol Imaging

Ligand: [111In,90Y]DOTA-TOC (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pIC50
Reference (Journal): DOTA-NOC, a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5 for labelling with various radiometals.
Published in: Eur J Nucl Med Mol Imaging

Ligand: [125I]BIM23027 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): A quantitative autoradiographical study on the distribution of somatostatin sst2 receptors in the rat central nervous system using [125I]-BIM-23027.
Published in: Neuropharmacology

Ligand: [125I]CGP 23996 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pKd
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [125I]CGP 23996 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pKd
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: [125I]LTT-SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: [125I]LTT-SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [125I]LTT-SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
Published in: Science

Ligand: [125I]LTT-SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): High affinity binding sites for a somatostatin-28 analog in rat brain.
Published in: Life Sci

Ligand: [125I]LTT-SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): High affinity binding sites for somatostatin to rat pituitary.
Published in: Biochem Biophys Res Commun

Ligand: [125I]MK-678 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKd
Reference (Journal): Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides.
Published in: Mol Pharmacol

Ligand: [125I]Tyr10-CST14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [125I]Tyr10-CST14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [125I]Tyr11-SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pKd
Reference (Journal): High affinity binding sites for somatostatin to rat pituitary.
Published in: Biochem Biophys Res Commun

Ligand: [125I]Tyr11-SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKd
Reference (Journal): Molecular and functional properties of somatostain receptor subtypes.
Published in: Metab Clin Exp

Ligand: [125I]Tyr3 SMS 201-995 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.539999961853027 pKd
Reference (Journal): New specific radioligand for one subpopulation of brain somatostatin receptors.
Published in: Life Sci

Ligand: [125I]Tyr3 SMS 201-995 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.89 pIC50
Reference (Journal): Comparison of radioiodinated TOC, TOCA and Mtr-TOCA: the effect of carbohydration on the pharmacokinetics.
Published in: Eur J Nucl Med Mol Imaging

Ligand: [125I]Tyr3 SMS 201-995 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.899999618530273 pKd
Reference (Journal): [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors.
Published in: Eur J Pharmacol

Ligand: [125I]Tyr3 SMS 201-995 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.899999618530273 pKd
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [125I][Tyr3,Thr8]octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.33 pIC50
Reference (Journal): Comparison of radioiodinated TOC, TOCA and Mtr-TOCA: the effect of carbohydration on the pharmacokinetics.
Published in: Eur J Nucl Med Mol Imaging

Ligand: [67Ga]NODAGA-[Tyr3]octreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.460000038146973 pIC50
Reference (Journal): NODAGATOC, a new chelator-coupled somatostatin analogue labeled with [67/68Ga] and [111In] for SPECT, PET, and targeted therapeutic applications of somatostatin receptor (hsst2) expressing tumors.
Published in: Bioconjug Chem

Ligand: Tyr3-octreotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity:  -

Ligand: vapreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Binding properties of somatostatin receptor subtypes.
Published in: Metab Clin Exp

Ligand: vapreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: vapreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: vapreotide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: veldoreotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Novel long-acting somatostatin analog with endocrine selectivity: potent suppression of growth hormone but not of insulin.
Published in: Endocrinology

Ligand: Y-KE88 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): New pansomatostatin ligands and their chelated versions: affinity profile, agonist activity, internalization, and tumor targeting.
Published in: Clin Cancer Res