Target family: Cholecystokinin receptors (type: gpcr)
Target: CCK<sub>2</sub> receptor

Ligand: Z-360 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.3 pKi
Reference (Journal): Effect of Z-360, a novel orally active CCK-2/gastrin receptor antagonist on tumor growth in human pancreatic adenocarcinoma cell lines in vivo and mode of action determinations in vitro.
Published in: Cancer Chemother Pharmacol

Ligand: YM-022 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pIC50
Reference (Journal): Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor.
Published in: Regul Pept

Ligand: YF-476 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo.
Published in: Aliment Pharmacol Ther

Ligand: YF-476 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.6 pKi
Reference (Journal): Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor.
Published in: Regul Pept

Ligand: YF-476 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): Single oral doses of netazepide (YF476), a gastrin receptor antagonist, cause dose-dependent, sustained increases in gastric pH compared with placebo and ranitidine in healthy subjects.
Published in: Aliment Pharmacol Ther

Ligand: TP-680 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist.
Published in: Br J Pharmacol

Ligand: tetronothiodin (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Species specificity of pharmacological characteristics of CCK-B receptors.
Published in: Neurosci Lett

Ligand: [3H]PD140376 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): [3H]PD 140376: a novel and highly selective antagonist radioligand for the cholecystokininB/gastrin receptor in guinea pig cerebral cortex and gastric mucosa.
Published in: Mol Pharmacol

Ligand: [3H]PBC-264 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pKd
Reference (Journal): [3H]pBC 264, a suitable probe for studying cholecystokinin-B receptors: binding characteristics in rodent brains and comparison with [3H]SNF 8702.
Published in: Mol Pharmacol

Ligand: [3H]L365260 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor.
Published in: Regul Pept

Ligand: [3H]JB-93182 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKd
Reference (Journal): Characterization of the binding of a novel radioligand to CCKB/gastrin receptors in membranes from rat cerebral cortex.
Published in: Br J Pharmacol

Ligand: [3H]gastrin (Peptide)
Interaction type: Agonist
Action: Full agonist
Primary target: no
Median affinity: 9 pIC50

Ligand: [125I]PD142308 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKd
Reference (Journal): Synthesis of novel iodinated radioligands with high affinity and selectivity for CCK-B/gastrin receptors.
Published in: Bioorg Med Chem Lett

Ligand: [125I]gastrin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50

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: [125I]-BDZ2 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Synthesis and in vitro characterization of radioiodinatable benzodiazepines selective for type 1 and type 2 cholecystokinin receptors.
Published in: J Med Chem

Ligand: RP73870 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Pharmacological analysis of CCK2 receptor antagonists using isolated rat stomach ECL cells.
Published in: Br J Pharmacol

Ligand: RP-69758 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Pharmacological properties of ureido-acetamides, new potent and selective non-peptide CCKB/gastrin receptor antagonists.
Published in: Eur J Pharmacol

Ligand: RB-400 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pKi
Reference (Journal): Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
Published in: Bioorg Med Chem Lett

Ligand: pentagastrin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974)
Median affinity: 9.1 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: PD-149164 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 10.1 pIC50
Reference (Journal): Cholecystokinin B antagonists. Synthesis and quantitative structure-activity relationships of a series of C-terminal analogues of CI-988.
Published in: Bioorg Med Chem

Ligand: PD-140548 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 pIC50
Reference (Journal): Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.
Published in: J Med Chem

Ligand: PD-135666 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.8 pIC50
Reference (Journal): Peptoid CCK receptor antagonists: pharmacological evaluation of CCKA, CCKB and mixed CCKA/B receptor antagonists.
Published in: Eur J Pharmacol

Ligand: PD-135158 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pIC50
Reference (Journal): Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor gene.
Published in: Neuropeptides

Ligand: PBC-264 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pIC50
Reference (Journal): His381 of the rat CCKB receptor is essential for CCKB versus CCKA receptor antagonist selectivity.
Published in: Eur J Pharmacol

Ligand: LY-288513 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor gene.
Published in: Neuropeptides

Ligand: LY262691 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Structure of a nanobody-stabilized active state of the β(2) adrenoceptor.
Published in: Nature

Ligand: lorglumide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor gene.
Published in: Neuropeptides

Ligand: L-740093 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pIC50
Reference (Journal): Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor.
Published in: Regul Pept

Ligand: L-365260 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization.
Published in: J Biol Chem

Ligand: JNJ-26070109 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): JNJ-26070109 [(R)4-bromo-N-[1-(2,4-difluoro-phenyl)-ethyl]-2-(quinoxaline-5-sulfonylamino)-benzamide]: a novel, potent, and selective cholecystokinin 2 receptor antagonist with good oral bioavailability.
Published in: J Pharmacol Exp Ther

Ligand: JMV310 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): Cyclic cholecystokinin analogues that are highly selective for rat and guinea pig central cholecystokinin receptors.
Published in: Mol Pharmacol

Ligand: itriglumide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): Characterization of antisecretory and antiulcer activity of CR 2945, a new potent and selective gastrin/CCK(B) receptor antagonist.
Published in: Eur J Pharmacol

Ligand: GW-5823 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 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: GV150013 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.40999984741211 pIC50
Reference (Journal): Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
Published in: J Med Chem

Ligand: gastrin-71 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: gastrin-34 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: gastrin-17 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 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: gastrin-14 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: devazepide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization.
Published in: J Biol Chem

Ligand: desulfated gastrin-71 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: desulfated gastrin-34 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: desulfated gastrin-17 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: desulfated gastrin-14 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: desulfated cholecystokinin-8 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization.
Published in: J Biol Chem

Ligand: CI-988 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.8 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: 9.1 pIC50
Reference (Journal): Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor gene.
Published in: Neuropeptides

Ligand: CI-1015 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
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: CCK-8 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization.
Published in: J Biol Chem

Ligand: CCK-8 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin.
Published in: J Biol Chem

Ligand: CCK-58 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Differences in receptor binding and stability to enzymatic digestion between CCK-8 and CCK-58.
Published in: Pancreas

Ligand: CCK-4 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin.
Published in: J Biol Chem

Ligand: CCK-33 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pIC50
Reference (Journal): Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin.
Published in: J Biol Chem

Ligand: BC-264 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
Published in: Bioorg Med Chem Lett

Ligand: BC-254 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pKi
Reference (Journal): [3H]pBC 264, a suitable probe for studying cholecystokinin-B receptors: binding characteristics in rodent brains and comparison with [3H]SNF 8702.
Published in: Mol Pharmacol

Ligand: BBL-454 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
Published in: Bioorg Med Chem Lett

Ligand: ARL-15849 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): ARL 15849: a selective CCK-A agonist with anorectic activity in the rat and dog.
Published in: Pharmacol Biochem Behav

Ligand: AG-041R (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor.
Published in: Regul Pept

Ligand: A-71378 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.5 pIC50
Reference (Journal): Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor gene.
Published in: Neuropeptides