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 | [528058] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | Ki = 3800 nM | [528058] | ||
PD-137342 | Drug Info | IC50 = 63 nM | |||
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 | Drug Info | IC50 = 5 nM | [532617] | ||
Tyr-D-Nle-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | Ki = 2200 nM | [528193] | ||
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 1.6 nM | [528193] | ||
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 1.1 nM | [528193] | ||
PD-134308 | Drug Info | IC50 = 1.7 nM | |||
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | Ki = 1700 nM | [528193] | ||
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 | [527234] | ||
PD-136621 | Drug Info | IC50 = 43 nM | |||
IQM-95333 | Drug Info | Ki = 2910 nM | [534494] | ||
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe | Drug Info | IC50 = 0.3 nM | |||
Pentagastrin | Drug Info | IC50 = 2.9 nM | [552753] | ||
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 1100 nM | [528193] | ||
PD-134308 | Drug Info | IC50 = 30 nM | [534527] | ||
Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 0.22 nM | [528193] | ||
Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 3.8 nM | [528193] | ||
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | Ki = 150 nM | [528193] | ||
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | Ki = 26 nM | [528193] | ||
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | Ki = 15 nM | [528193] | ||
Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 2.7 nM | [528193] | ||
PD-140547 | Drug Info | IC50 = 13.2 nM | |||
PD-170292 | Drug Info | EC50 = 5 nM | [552343] | ||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | Ki < 1000 nM | [531079] | ||
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 | [528193] | ||
SNF-9007 | Drug Info | Ki = 2.1 nM | [528193] | ||
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 15 nM | [528193] | ||
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 1.5 nM | [528193] | ||
Tyr-Gly-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | Ki = 4.8 nM | [528193] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | Ki = 9300 nM | [528058] | ||
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Drug Info | Ki = 7700 nM | [528606] | ||
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | Ki = 1500 nM | [528058] | ||
Tetragastrin | Drug Info | Ki = 3 nM | [533465] | ||
Dexloxiglumide | Drug Info | Ki = 2.8 nM | [534494] | ||
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 | [528606] | ||
References | |||||
Ref 528058 | J 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 528058 | J 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 532617 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 527234 | J 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 534494 | J 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 552753 | Progress 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 528193 | J 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 534527 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 552343 | CCK1R agonists: a promising target for the pharmacological treatment of obesity. Curr Top Med Chem. 2003;3(8):837-54. | ||||
Ref 531079 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 528193 | J 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 528058 | J 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 528606 | J 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 528058 | J 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 533465 | J 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. | ||||
Ref 534494 | J 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 528606 | J 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. |
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