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

Ligand: PD-140548 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Peptoid CCK receptor antagonists: pharmacological evaluation of CCKA, CCKB and mixed CCKA/B receptor antagonists.
Published in: Eur J Pharmacol

Ligand: PD136450 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Characterization of cholecystokininA receptor agonist activity by a family of cholecystokininB receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: PD-135158 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.9 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

Ligand: loxiglumide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Pharmacological characterisation of a new potent and specific nonpolypeptidic cholecystokinin antagonist.
Published in: Arzneimittelforschung

Ligand: lorglumide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): CR-1409: a potent inhibitor of cholecystokinin-stimulated amylase release and cholecystokinin binding in rat pancreatic acini.
Published in: Pancreas

Ligand: lorglumide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  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

Ligand: lintitript (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pIC50
Reference (Journal): The agonist SR 146131 and the antagonist SR 27897 occupy different sites on the human CCK(1) receptor.
Published in: Eur J Pharmacol

Ligand: lintitript (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Peripheral biological activity of SR 27897: a new potent non-peptide antagonist of CCKA receptors.
Published in: Eur J Pharmacol

Ligand: L-740093 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.8 pKi
Reference (Journal): Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo.
Published in: Mol Pharmacol

Ligand: L-736380 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.
Published in: J Med Chem

Ligand: L-365260 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 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

Ligand: JNJ-17156516 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): 3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide.
Published in: J Pharmacol Exp Ther

Ligand: JMV180 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Identification of a region of the N-terminal of the human CCKA receptor essential for the high affinity interaction with agonist CCK.
Published in: Biochem Biophys Res Commun

Ligand: IQM-97423 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Pharmacological study of IQM-97,423, a potent and selective CCK1 receptor antagonist with protective effect in experimental acute pancreatitis.
Published in: Pharmacology

Ligand: GW-5823 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
Published in: J Med Chem

Ligand: Glaxo-11p (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
Published in: J Med Chem

Ligand: gastrin-17 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.1 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

Ligand: dexloxiglumide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.5 pKi
Reference (Journal): 3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide.
Published in: J Pharmacol Exp Ther

Ligand: devazepide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.720000267028809 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

Ligand: CI-988 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 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

Ligand: CI-1015 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Second generation &quot;peptoid&quot; CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
Published in: J Med Chem

Ligand: CE-326597 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.5 pIC50
Reference (Journal): Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.
Published in: Bioorg Med Chem Lett

Ligand: CCK-8 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.899999618530273 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

Ligand: CCK-8 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.2 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

Ligand: CCK-8 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: CCK-58 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pIC50
Reference (Journal): Differences in receptor binding and stability to enzymatic digestion between CCK-8 and CCK-58.
Published in: Pancreas

Ligand: CCK-58 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: CCK-4 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 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

Ligand: CCK-39 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: CCK-33 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: CCK-33 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKd
Reference (Journal): Distinct cholecystokinin receptors in brain and pancreas.
Published in: Proc Natl Acad Sci USA

Ligand: ARL-15849 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.5 pKi
Reference (Journal): ARL 15849: a selective CCK-A agonist with anorectic activity in the rat and dog.
Published in: Pharmacol Biochem Behav

Ligand: A-71623 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Behavioral effects of A71623, a highly selective CCK-A agonist tetrapeptide.
Published in: Am J Physiol