Target family: Somatostatin receptors (type: gpcr)
Target: SST<sub>4</sub> receptor

Ligand: analog 32 [PMID:18543899] (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.340000152587891 pIC50
Reference (Journal): Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.
Published in: J Med Chem

Ligand: β3-tetrapeptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Beta(2)/beta(3)-di- and alpha/beta(3)-tetrapeptide derivatives as potent agonists at somatostatin sst(4) receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: β3-tetrapeptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Beta(2)/beta(3)-di- and alpha/beta(3)-tetrapeptide derivatives as potent agonists at somatostatin sst(4) 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): [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: 8.100000381469727 pIC50
Reference (Journal): Differential expression of multiple somatostatin receptors in the rat cerebellum during development.
Published in: J Neurochem

Ligand: BIM 23068 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1-5).
Published in: Endocrinology

Ligand: BIM 23295 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): The elucidation of somatostatin receptor functions: a current view.
Published in: Rev Physiol Biochem Pharmacol

Ligand: BIM 23454 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 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: 6.400000095367432 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): 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): [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: 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: 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: [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: H-c[Cys-Phe-LAgl(NβMe,benzoyl)-DTrp-Lys-Thr-Phe-Cys]-OH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
Published in: J Med Chem

Ligand: H-c[Cys-Phe-LAgl(NβMe,benzoyl)-Trp-Lys-Thr-Phe-Cys]-OH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
Published in: J Med Chem

Ligand: H-c[DCys-Phe-LAgl(NβMe,benzoyl)-DTrp-Lys-Thr-Phe-Cys]-OH (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
Published in: J Med Chem

Ligand: J-2156 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.920000076293945 pKi
Reference (Journal): Superagonism at the human somatostatin receptor subtype 4.
Published in: J Pharmacol Exp Ther

Ligand: KE 108 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 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): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
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): [125I]Tyr10-cortistatin14 labels all five somatostatin receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: L-803,087 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 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
Median affinity:  pKi
Reference (Journal): Functional characterisation of the putative somatostatin sst2 receptor antagonist CYN 154806.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: NNC269100 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Nonpeptide somatostatin agonists with sst4 selectivity: synthesis and structure-activity relationships of thioureas.
Published in: J Med Chem

Ligand: PRL-2915 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Highly potent cyclic disulfide antagonists of somatostatin.
Published in: J Med Chem

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:  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): 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): [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): 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: 8.2 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): 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-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): 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): 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): [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): 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): 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: 9.399999618530273 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: 9.6 pIC50
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: 8.4 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: 9.4 pKd
Reference (Journal): Characterisation of human recombinant somatostatin receptors. 1. Radioligand binding studies.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: [125I]Tyr11-SRIF-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Cloning and characterization of a fourth human somatostatin receptor.
Published in: Proc Natl Acad Sci USA

Ligand: veldoreotide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Novel long-acting somatostatin analog with endocrine selectivity: potent suppression of growth hormone but not of insulin.
Published in: Endocrinology