Target family: Cholecystokinin receptors (type: gpcr)
Target: CCK<sub>1</sub> receptor

Ligand: YM-022 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Pharmacological profile of (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo- 5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (YM022), a new potent and selective gastrin/cholecystokinin-B receptor antagonist, in vitro and in vivo.
Published in: J Pharmacol Exp Ther

Ligand: YF-476 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
Published in: J Med Chem

Ligand: VL-0395 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Anthranilic acid derivatives: a new class of non-peptide CCK1 receptor antagonists.
Published in: Bioorg Med Chem

Ligand: TP-680 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pKi
Reference (Journal): Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist.
Published in: Br J Pharmacol

Ligand: T-0632 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pIC50
Reference (Journal): Pharmacological profile of T-0632, a novel potent and selective CCKA receptor antagonist, in vitro.
Published in: Eur J Pharmacol

Ligand: [3H]devazepide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pKd
Reference (Journal): Characterization of the binding of [3H]-(+/-)-L-364,718: a new potent, nonpeptide cholecystokinin antagonist radioligand selective for peripheral receptors.
Published in: Mol Pharmacol

Ligand: [125I]DTyr-Gly-[(Nle28,31)CCK-26-33 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Use of N,O-bis-Fmoc-D-Tyr-ONSu for introduction of an oxidative iodination site into cholecystokinin family peptides.
Published in: Int J Pept Protein Res

Ligand: SR146131 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pIC50
Reference (Journal): SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies.
Published in: J Pharmacol Exp Ther

Ligand: SC-50998 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): 1,3,4-trisubstituted pyrrolidinones as scaffolds for construction of peptidomimetic cholecystokinin antagonists.
Published in: Bioorg Med Chem Lett

Ligand: rebamipide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Median affinity: 4.4 pIC50
Reference (Journal): Pharmacological characterization of rebamipide: its cholecystokinin CCK1 receptor binding profile and effects on Ca2+ mobilization and amylase release in rat pancreatic acinar cells.
Published in: Eur J Pharmacol

Ligand: proglumide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 2.2 pIC50
Reference (Journal): Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists.
Published in: Arzneimittelforschung

Ligand: pranazepide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.4 pIC50
Reference (Journal): Pharmacological profile of FK480, a novel cholecystokinin type-A receptor antagonist: comparison to loxiglumide.
Published in: J Pharmacol Exp Ther

Ligand: pentagastrin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974)
Median affinity: 6.2 pIC50
Reference (Journal): Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity.
Published in: Proc Natl Acad Sci USA