Target Validation Information
TTD ID T05849
Target Name Gastrin/cholecystokinin type B receptor (CCKBR)
Type of Target
Successful
Drug Potency against Target Pentagastrin Drug Info IC50 = 2.9 nM [11]
PD-170292 Drug Info EC50 = 5 nM [10]
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Drug Info Ki < 1000 nM [5]
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe Drug Info IC50 = 0.3 nM
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 Drug Info IC50 = 5 nM [6]
Cholecystokinin-9 Drug Info IC50 = 3688 nM [1]
Dexloxiglumide Drug Info Ki = 2.8 nM [8]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo Drug Info Ki = 71 nM [4]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info Ki = 7700 nM [4]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info Ki = 9300 nM [2]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac Drug Info Ki = 1300 nM [2]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info Ki = 3800 nM [2]
IQM-95333 Drug Info Ki = 2910 nM [8]
L-365260 Drug Info IC50 = 8.5 nM
PD-134308 Drug Info IC50 = 1.7 nM
PD-134308 Drug Info IC50 = 30 nM [9]
PD-135118 Drug Info IC50 = 4.2 nM
PD-135666 Drug Info IC50 = 0.15 nM
PD-136621 Drug Info IC50 = 43 nM
PD-137337 Drug Info IC50 = 160 nM
PD-137342 Drug Info IC50 = 63 nM
PD-138915 Drug Info IC50 = 170 nM
PD-138916 Drug Info IC50 = 23 nM
PD-138917 Drug Info IC50 = 180 nM
PD-140547 Drug Info IC50 = 13.2 nM
PD-140548 Drug Info IC50 = 259 nM
PD-140723 Drug Info IC50 = 9.3 nM
SNF-9007 Drug Info Ki = 2.1 nM [3]
Tetragastrin Drug Info Ki = 3 nM [7]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 2700 nM [3]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1.5 nM [3]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info Ki = 1500 nM [2]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 150 nM [3]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1.6 nM [3]
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 2200 nM [3]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1100 nM [3]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 15 nM [3]
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 3.8 nM [3]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 1700 nM [3]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1.1 nM [3]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 26 nM [3]
Tyr-D-Phe-Gly-Trp-NMeNle-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]
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 4.8 nM [3]
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 0.22 nM [3]
References
REF 1 5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectiv... J Med Chem. 2004 Oct 7;47(21):5318-29.
REF 2 Design and synthesis of novel hydrazide-linked bifunctional peptides as delta/mu opioid receptor agonists and CCK-1/CCK-2 receptor antagonists. J Med Chem. 2006 Mar 9;49(5):1773-80.
REF 3 Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem. 2006 May 18;49(10):2868-75.
REF 4 Partial retro-inverso, retro, and inverso modifications of hydrazide linked bifunctional peptides for opioid and cholecystokinin (CCK) receptors. J Med Chem. 2007 Jan 11;50(1):165-8.
REF 5 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 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.
REF 6 Synthesis and biological activities of pseudopeptide analogues of the C-terminal heptapeptide of cholecystokinin. On the importance of the peptide ... J Med Chem. 1987 Aug;30(8):1366-73.
REF 7 Synthesis and binding affinities of analogues of cholecystokinin-(30-33) as probes for central nervous system cholecystokinin receptors. J Med Chem. 1987 Apr;30(4):729-32.
REF 8 Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecy... J Med Chem. 1997 Oct 10;40(21):3402-7.
REF 9 Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfecte... J Med Chem. 1997 Nov 21;40(24):3947-56.
REF 10 CCK1R agonists: a promising target for the pharmacological treatment of obesity. Curr Top Med Chem. 2003;3(8):837-54.
REF 11 Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Curr Opin Pharmacol. 2007 Dec;7(6):583-92.

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