Target family: Somatostatin receptors (type: gpcr)
Target: SST<sub>1</sub> receptor

Ligand: BIM 23050 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 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
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
Median affinity:  pKi
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: BIM 23052 (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 23454 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 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: 5.599999904632568 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: 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: 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: CH 275 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Journal): Differential expression of multiple somatostatin receptors in the rat cerebellum during development.
Published in: J Neurochem

Ligand: CH 275 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem 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: 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: 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: cyclo(7-12) Des-AA1,2,5-[Glu7,D-Trp8,IAmp9,m-I-Tyr11,hhLys12]SRIF (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Published in: J Med Chem

Ligand: Des-AA1,2,5,12,13-[D-Trp8]SRIF (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Published in: J Med Chem

Ligand: Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Somatostatin receptor 1 selective analogues: 3. Dicyclic peptides.
Published in: J Med Chem

Ligand: Des-AA5-[D-Trp8]SRIF (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Published in: J Med Chem

Ligand: Des-Ala1,2,5-[D-Trp8,IAmp9]SRIF (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Somatostatin receptor 1 selective analogues: 2. N(alpha)-Methylated scan.
Published in: J Med Chem

Ligand: [D-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: KE 108 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): A new peptidic somatostatin agonist with high affinity to all five somatostatin 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): [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): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: L-797,591 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
Published in: Science

Ligand: L-817,818 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
Published in: Science

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: NC 4-28B (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 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: 8 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: SRA880 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): SRA880, in vitro characterization of the first non-peptide somatostatin sst(1) receptor antagonist.
Published in: Neurosci Lett

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): 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: 8.4 pIC50
Reference (Journal): Differential expression of multiple somatostatin receptors in the rat cerebellum during development.
Published in: J Neurochem

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-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: 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
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
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): [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): 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): 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): 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): 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): 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): Superagonism at the human somatostatin receptor subtype 4.
Published in: J Pharmacol Exp Ther

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

Ligand: [125I]LTT-SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [125I]LTT-SRIF-28 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 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: 8.8 pKd
Reference (Journal): Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
Published in: Science

Ligand: [125I]Tyr10-CST14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 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: 10 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
Median affinity: 9.2 pKd
Reference (Journal): Molecular and functional properties of somatostain receptor subtypes.
Published in: Metab Clin Exp