Target Validation Information
TTD ID T28330
Target Name Cholecystokinin receptor type A (CCKAR)
Type of Target
Clinical trial
Drug Potency against Target Drug Info IC50 = 120 nM [17]
A-71378 Drug Info IC50 = 0.5 nM [17]
PD-170292 Drug Info EC50 = 2 nM [16]
Drug Info Ki = 0.64 nM [11]
1-(3,3-Diphenyl-allyl)-3-m-tolyl-urea Drug Info Ki = 800 nM [1]
1-(4-Chloro-phenyl)-3-(3,3-diphenyl-allyl)-urea Drug Info Ki = 90 nM [1]
1-(4-Chloro-phenyl)-3-(3-pentyl-oct-2-enyl)-urea Drug Info Ki = 200 nM [1]
3,4-Dichloro-N-(3,3-diphenyl-allyl)-benzamide Drug Info Ki = 400 nM [1]
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe Drug Info IC50 = 0.28 nM
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 Drug Info IC50 = 5 nM [9]
Boc-cyclo-(Glu-Tyr-Nle-D-Lys)-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 1997 nM [11]
Boc-D-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 1550 nM [11]
Boc-D-Glu-Tyr(SO3H)-Nle-D-Nle-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 1600 nM [11]
Boc-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 1996 nM [11]
Boc-Tyr(SO3H)-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 0.93 nM [11]
CR-1795 Drug Info IC50 = 30 nM
CR-2345 Drug Info IC50 = 6600 nM
Dexloxiglumide Drug Info Ki = 0.64 nM [10]
FR-175985 Drug Info IC50 = 62 nM
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H Drug Info Ki = 7000 nM [5]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H Drug Info Ki = 10000 nM [2]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc Drug Info Ki = 4100 nM [2]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H Drug Info Ki = 1900 nM [5]
IQM-95333 Drug Info Ki = 2890 nM [14]
L-365260 Drug Info IC50 = 280 nM
L-708474 Drug Info IC50 = 1797 nM [13]
L-740093 Drug Info IC50 = 1604 nM
PD-134308 Drug Info IC50 = 4300 nM
PD-135118 Drug Info IC50 = 950 nM
PD-135666 Drug Info IC50 = 25.5 nM
PD-136621 Drug Info IC50 = 3100 nM
PD-137337 Drug Info IC50 = 2500 nM
PD-137342 Drug Info IC50 = 18000 nM
PD-138915 Drug Info IC50 = 580 nM
PD-138916 Drug Info IC50 = 850 nM
PD-140547 Drug Info IC50 = 539 nM
PD-140548 Drug Info IC50 = 2.8 nM
PD-140723 Drug Info IC50 = 186 nM
Pranazepide Drug Info IC50 = 0.67 nM
SNF-9007 Drug Info Ki = 3200 nM [4]
Tetragastrin Drug Info Ki = 3 nM [12]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 6500 nM [4]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 320 nM [4]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc Drug Info Ki = 1900 nM [2]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 5700 nM [4]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 5100 nM [4]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 910 nM [4]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 9.6 nM [4]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 2000 nM [4]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 1100 nM [4]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 Drug Info Ki = 98 nM [4]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 Drug Info Ki = 3600 nM [4]
VL-0395 Drug Info IC50 = 197 nM [8]
VL-0494 Drug Info IC50 = 197 nM [6]
VL-0699 Drug Info IC50 = 12700 nM [3]
VL-1499 Drug Info IC50 = 4010 nM [8]
VL-2799 Drug Info IC50 = 3240 nM [7]
Action against Disease Model Drug Info Dexloxigl uMide, the active enantiomer of loxigl uMide, interacts competitively with CCK(1) receptors as determined in preclinical studies, such as specific radioligand binding assays or functional studies on isolated guinea pig gallbladder, where it inhibited smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8), the most prominent active forms of cholecystokinin. Dexloxigl uMide has a potent antagonistic effect, of a competitive nature, on h uMan gallbladder cholecystokinin type 1 receptors. In isolated h uMan gallbladder, dexloxigl uMide produced a concentration-dependent rightward shift of the cholecystokinin-octapeptide curve, without affecting its maximal response [15]
References
REF 1 Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718. J Med Chem. 1992 Mar 20;35(6):1042-9.
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 Anthranilic acid based CCK1 receptor antagonists and CCK-8 have a common step in their "receptor desmodynamic processes". J Med Chem. 2006 Apr 20;49(8):2456-62.
REF 4 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 5 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 6 Synthesis and evaluation of novel benzimidazole derivative [Bz-Im] and its radio/biological studies. Bioorg Med Chem Lett. 2007 May 15;17(10):2749-55.
REF 7 Anthranilic acid based CCK1 receptor antagonists: blocking the receptor with the same 'words' of the endogenous ligand. Bioorg Med Chem. 2009 Mar 15;17(6):2336-50.
REF 8 2D-QSAR and 3D-QSAR/CoMFA analyses of the N-terminal substituted anthranilic acid based CCK(1) receptor antagonists: 'Hic Rhodus, hic saltus'. Bioorg Med Chem. 2009 Jul 15;17(14):5198-206.
REF 9 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 10 Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. J Med Chem. 1989 Feb;32(2):445-9.
REF 11 Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors. J Med Chem. 1989 Jun;32(6):1184-90.
REF 12 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 13 High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group. J Med Chem. 1994 Mar 18;37(6):719-21.
REF 14 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 15 Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 as a promising therapeutic target. Drug Discov Today. 2007 Jul;12(13-14):504-20.
REF 16 NPY Y1 and Y5 receptor selective antagonists as anti-obesity drugs. Curr Top Med Chem. 2007;7(17):1721-33.
REF 17 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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