Target Validation Information
Target ID T05849
Target Name Gastrin/cholecystokinin type B receptor
Target Type
Successful
Drug Potency against Target PD-140723 Drug Info IC50 = 9.3 nM
PD-138917 Drug Info IC50 = 180 nM
PD-138916 Drug Info IC50 = 23 nM
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac Drug Info Ki = 1300 nM [1]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info Ki = 3800 nM [1]
PD-137342 Drug Info IC50 = 63 nM
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 Drug Info IC50 = 5 nM [2]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 2200 nM [3]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1.6 nM [3]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1.1 nM [3]
PD-134308 Drug Info IC50 = 1.7 nM
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 1700 nM [3]
PD-140548 Drug Info IC50 = 259 nM
L-365260 Drug Info IC50 = 8.5 nM
PD-135118 Drug Info IC50 = 4.2 nM
Cholecystokinin-9 Drug Info IC50 = 3688 nM [4]
PD-136621 Drug Info IC50 = 43 nM
IQM-95333 Drug Info Ki = 2910 nM [5]
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe Drug Info IC50 = 0.3 nM
Pentagastrin Drug Info IC50 = 2.9 nM [6]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1100 nM [3]
PD-134308 Drug Info IC50 = 30 nM [7]
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 0.22 nM [3]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 3.8 nM [3]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 150 nM [3]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 26 nM [3]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 15 nM [3]
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 2.7 nM [3]
PD-140547 Drug Info IC50 = 13.2 nM
PD-170292 Drug Info EC50 = 5 nM [8]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [9]
PD-137337 Drug Info IC50 = 160 nM
PD-135666 Drug Info IC50 = 0.15 nM
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 2700 nM [3]
SNF-9007 Drug Info Ki = 2.1 nM [3]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 15 nM [3]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1.5 nM [3]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 4.8 nM [3]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info Ki = 9300 nM [1]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info Ki = 7700 nM [10]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info Ki = 1500 nM [1]
Tetragastrin Drug Info Ki = 3 nM [11]
Dexloxiglumide Drug Info Ki = 2.8 nM [5]
PD-138915 Drug Info IC50 = 170 nM
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo Drug Info Ki = 71 nM [10]
References
REF 1J Med Chem. 2006 Mar 9;49(5):1773-80.Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists.
REF 2J Med Chem. 1987 Aug;30(8):1366-73.Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide bonds.
REF 3J Med Chem. 2006 May 18;49(10):2868-75.Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
REF 4J Med Chem. 2004 Oct 7;47(21):5318-29.5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.
REF 5J Med Chem. 1997 Oct 10;40(21):3402-7.Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
REF 6Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Curr Opin Pharmacol. 2007 Dec;7(6):583-92. Epub 2007 Nov 9.
REF 7J Med Chem. 1997 Nov 21;40(24):3947-56.Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.
REF 8CCK1R agonists: a promising target for the pharmacological treatment of obesity. Curr Top Med Chem. 2003;3(8):837-54.
REF 9J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
REF 10J Med Chem. 2007 Jan 11;50(1):165-8.Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors.
REF 11J Med Chem. 1987 Apr;30(4):729-32.Synthesis and binding affinities of analogues of cholecystokinin-(30-33) as probes for central nervous system cholecystokinin receptors.

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