Target Information
Target General Information | Top | |||||
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Target ID |
T28330
(Former ID: TTDC00082)
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Target Name |
Cholecystokinin receptor type A (CCKAR)
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Synonyms |
CCKAR; CCK-AR; CCK-A receptor
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Gene Name |
CCKAR
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Target Type |
Clinical trial target
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[1] | ||||
Disease | [+] 2 Target-related Diseases | + | ||||
1 | Influenza [ICD-11: 1E30-1E32] | |||||
2 | Pancreatic malfunction [ICD-11: DC30-DC3Z] | |||||
Function |
Receptor forcholecystokinin. Mediates pancreatic growth and enzyme secretion, smooth muscle contraction of the gall bladder and stomach. Has a 1000-fold higher affinity for CCK rather than for gastrin. It modulates feeding and dopamine-induced behavior in the central and peripheral nervous system. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system.
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BioChemical Class |
GPCR rhodopsin
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UniProt ID | ||||||
Sequence |
MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNT
LVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYF MGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYS NLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGI KFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNS SAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSY TSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSH MSASVPPQ Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold |
Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
1 | Dexloxiglumide | Drug Info | Phase 2 | Pancreatic malfunction | [2] | |
2 | proglumide | Drug Info | Phase 2 | Influenza virus infection | [3] | |
Discontinued Drug(s) | [+] 15 Discontinued Drugs | + | ||||
1 | CE-326597 | Drug Info | Discontinued in Phase 2 | Obesity | [4] | |
2 | GI 181771 | Drug Info | Discontinued in Phase 2 | Obesity | [5] | |
3 | Lintitript | Drug Info | Discontinued in Phase 2 | Obesity | [6], [7] | |
4 | Pranazepide | Drug Info | Discontinued in Phase 2 | Pancreatic malfunction | [8], [9] | |
5 | Tarazepide | Drug Info | Discontinued in Phase 2 | Gastrointestinal disease | [10] | |
6 | SR-146131 | Drug Info | Discontinued in Phase 1 | Obesity | [11], [12] | |
7 | SSR-125180 | Drug Info | Discontinued in Phase 1 | Obesity | [13] | |
8 | T-0632 | Drug Info | Discontinued in Phase 1 | Pancreatic malfunction | [14], [15] | |
9 | UCL-2000; butabindide | Drug Info | Discontinued in Phase 1 | Obesity | [16] | |
10 | A-70276 | Drug Info | Terminated | Gastrointestinal disease | [19] | |
11 | A-71623 | Drug Info | Terminated | Obesity | [20], [21] | |
12 | FR-208419 | Drug Info | Terminated | Dyspepsia | [22] | |
13 | GI-248573 | Drug Info | Terminated | Bladder disease | [23] | |
14 | Lorglumide | Drug Info | Terminated | Pancreatic malfunction | [24], [25] | |
15 | SR-27950 | Drug Info | Terminated | Eating disorder | [26] | |
Preclinical Drug(s) | [+] 6 Preclinical Drugs | + | ||||
1 | A-71378 | Drug Info | Preclinical | Obesity | [17], [18] | |
2 | A-74498 | Drug Info | Preclinical | Obesity | [18] | |
3 | AR-R-1589 | Drug Info | Preclinical | Eating disorder | [18] | |
4 | FPL-14294 | Drug Info | Preclinical | Obesity | [18] | |
5 | GG-8573 | Drug Info | Preclinical | Obesity | [18] | |
6 | PD-170292 | Drug Info | Preclinical | Obesity | [18] | |
Mode of Action | [+] 4 Modes of Action | + | ||||
Inhibitor | [+] 51 Inhibitor drugs | + | ||||
1 | Dexloxiglumide | Drug Info | [27] | |||
2 | Pranazepide | Drug Info | [32] | |||
3 | CR-1795 | Drug Info | [41] | |||
4 | IQM-95333 | Drug Info | [43] | |||
5 | PD-135666 | Drug Info | [45] | |||
6 | SNF-9007 | Drug Info | [46] | |||
7 | 1-(3,3-Diphenyl-allyl)-3-m-tolyl-urea | Drug Info | [48] | |||
8 | 1-(4-Chloro-phenyl)-3-(3,3-diphenyl-allyl)-urea | Drug Info | [48] | |||
9 | 1-(4-Chloro-phenyl)-3-(3-pentyl-oct-2-enyl)-urea | Drug Info | [48] | |||
10 | 3,4-Dichloro-N-(3,3-diphenyl-allyl)-benzamide | Drug Info | [48] | |||
11 | Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe | Drug Info | [50] | |||
12 | Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 | Drug Info | [53] | |||
13 | Boc-cyclo-(Glu-Tyr-Nle-D-Lys)-Trp-Nle-Asp-Phe-NH2 | Drug Info | [54] | |||
14 | Boc-D-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 | Drug Info | [54] | |||
15 | Boc-D-Glu-Tyr(SO3H)-Nle-D-Nle-Trp-Nle-Asp-Phe-NH2 | Drug Info | [54] | |||
16 | Boc-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 | Drug Info | [54] | |||
17 | Boc-Tyr(SO3H)-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [54] | |||
18 | CR-2345 | Drug Info | [41] | |||
19 | FR-175985 | Drug Info | [32] | |||
20 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H | Drug Info | [60] | |||
21 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | [61] | |||
22 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | [61] | |||
23 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H | Drug Info | [60] | |||
24 | L-708474 | Drug Info | [66] | |||
25 | L-740093 | Drug Info | [68] | |||
26 | PD-135118 | Drug Info | [45] | |||
27 | PD-136621 | Drug Info | [45] | |||
28 | PD-137337 | Drug Info | [45] | |||
29 | PD-137342 | Drug Info | [45] | |||
30 | PD-138915 | Drug Info | [45] | |||
31 | PD-138916 | Drug Info | [45] | |||
32 | PD-140547 | Drug Info | [45] | |||
33 | PD-140548 | Drug Info | [45] | |||
34 | PD-140723 | Drug Info | [45] | |||
35 | Tetragastrin | Drug Info | [69] | |||
36 | Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [46] | |||
37 | Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [46] | |||
38 | Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | [61] | |||
39 | Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [46] | |||
40 | Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [46] | |||
41 | Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [46] | |||
42 | Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [46] | |||
43 | Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [46] | |||
44 | Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [46] | |||
45 | Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [46] | |||
46 | Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [46] | |||
47 | VL-0395 | Drug Info | [71] | |||
48 | VL-0494 | Drug Info | [72] | |||
49 | VL-0699 | Drug Info | [73] | |||
50 | VL-1499 | Drug Info | [71] | |||
51 | VL-2799 | Drug Info | [74] | |||
Antagonist | [+] 18 Antagonist drugs | + | ||||
1 | proglumide | Drug Info | [1] | |||
2 | Lintitript | Drug Info | [30], [31] | |||
3 | Tarazepide | Drug Info | [33], [34], [35] | |||
4 | T-0632 | Drug Info | [38] | |||
5 | Lorglumide | Drug Info | [44] | |||
6 | 2-NAP | Drug Info | [49] | |||
7 | Asperlicin | Drug Info | [51] | |||
8 | Bis(31/31')[[Cys(31), Nva(34)]NPY(27-36)-NH(2)] | Drug Info | [52] | |||
9 | CI-1015 | Drug Info | [57] | |||
10 | Devazepide | Drug Info | [51] | |||
11 | IQM-97423 | Drug Info | [62] | |||
12 | JNJ-17156516 | Drug Info | [64] | |||
13 | KSG-504 | Drug Info | [65] | |||
14 | L-736380 | Drug Info | [67] | |||
15 | PD-135158 | Drug Info | [56] | |||
16 | SC-50998 | Drug Info | [47] | |||
17 | TP-680 | Drug Info | [70] | |||
18 | [3H]devazepide | Drug Info | [75] | |||
Agonist | [+] 16 Agonist drugs | + | ||||
1 | CE-326597 | Drug Info | [28] | |||
2 | GI 181771 | Drug Info | [29] | |||
3 | SR-146131 | Drug Info | [36] | |||
4 | SSR-125180 | Drug Info | [37] | |||
5 | UCL-2000; butabindide | Drug Info | [18] | |||
6 | A-71378 | Drug Info | [18] | |||
7 | A-74498 | Drug Info | [18] | |||
8 | AR-R-1589 | Drug Info | [18] | |||
9 | FPL-14294 | Drug Info | [18] | |||
10 | GG-8573 | Drug Info | [18] | |||
11 | PD-170292 | Drug Info | [18] | |||
12 | CCK-33 | Drug Info | [55] | |||
13 | CCK-8 | Drug Info | [56] | |||
14 | Glaxo-11p | Drug Info | [58] | |||
15 | GW-5823 | Drug Info | [59] | |||
16 | JMV180 | Drug Info | [63] | |||
Modulator | [+] 5 Modulator drugs | + | ||||
1 | A-70276 | Drug Info | [39] | |||
2 | A-71623 | Drug Info | [40] | |||
3 | FR-208419 | Drug Info | [42] | |||
4 | GI-248573 | Drug Info | [37] | |||
5 | SR-27950 | Drug Info | [47] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target Affiliated Biological Pathways | Top | |||||
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KEGG Pathway | [+] 4 KEGG Pathways | + | ||||
1 | Calcium signaling pathway | |||||
2 | Neuroactive ligand-receptor interaction | |||||
3 | Insulin secretion | |||||
4 | Pancreatic secretion | |||||
Reactome | [+] 2 Reactome Pathways | + | ||||
1 | Peptide ligand-binding receptors | |||||
2 | G alpha (q) signalling events | |||||
WikiPathways | [+] 5 WikiPathways | + | ||||
1 | GPCRs, Class A Rhodopsin-like | |||||
2 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
3 | Peptide GPCRs | |||||
4 | GPCR ligand binding | |||||
5 | GPCR downstream signaling |
Target-Related Models and Studies | Top | |||||
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Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
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REF 1 | Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8. | |||||
REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 3 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 4 | ClinicalTrials.gov (NCT00542009) A Trial In Diabetic Patients To Assess Effect Of CE-326,597 On Glucose Control And Body Weight. U.S. National Institutes of Health. | |||||
REF 5 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013294) | |||||
REF 6 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 890). | |||||
REF 7 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004912) | |||||
REF 8 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 874). | |||||
REF 9 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003071) | |||||
REF 10 | Cholecystokinin receptor-1 mediates the inhibitory effects of exogenous cholecystokinin octapeptide on cellular morphine dependence. BMC Neurosci. 2012 Jun 8;13:63. | |||||
REF 11 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 868). | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010439) | |||||
REF 13 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015967) | |||||
REF 14 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 884). | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007781) | |||||
REF 16 | Clinical pipeline report, company report or official report of University College London. | |||||
REF 17 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 894). | |||||
REF 18 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | |||||
REF 19 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003433) | |||||
REF 20 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 858). | |||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003438) | |||||
REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010485) | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008844) | |||||
REF 24 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 891). | |||||
REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000580) | |||||
REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001260) | |||||
REF 27 | Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue. J Med Chem. 1989 Feb;32(2):445-9. | |||||
REF 28 | Obesity Pharmacotherapy: Current Perspectives and Future Directions. Curr Cardiol Rev. 2013 February; 9(1): 33-54. | |||||
REF 29 | Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506. | |||||
REF 30 | A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15. | |||||
REF 31 | A novel role for cholecystokinin: regulation of mesenteric vascular resistance. Regul Pept. 2004 Sep 15;121(1-3):145-53. | |||||
REF 32 | Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines, Bioorg. Med. Chem. Lett. 7(2):169-174 (1997). | |||||
REF 33 | Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80. | |||||
REF 34 | The ghrelin pentapeptide inhibits the secretion of pancreatic juice in rats. J Physiol Pharmacol. 2006 Dec;57(4):691-700. | |||||
REF 35 | Effects of intraduodenal administration of tarazepide on pancreatic secretion and duodenal EMG in neonatal calves. Regul Pept. 1998 Nov 30;78(1-3):113-23. | |||||
REF 36 | SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther. 1999 May;289(2):742-51. | |||||
REF 37 | US patent application no. 8,748,419, Antagonists. | |||||
REF 38 | Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12. | |||||
REF 39 | Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors. J Med Chem. 1991 Dec;34(12):3350-9. | |||||
REF 40 | Characterization of two novel cholecystokinin tetrapeptide (30-33) analogues, A-71623 and A-70874, that exhibit high potency and selectivity for cholecystokinin-A receptors. Mol Pharmacol. 1991 Mar;39(3):346-51. | |||||
REF 41 | Biological properties of (R)-4-benzamido-5-oxopentanoic basic derivatives as CCK-antagonists, Bioorg. Med. Chem. Lett. 3(5):861-866 (1993). | |||||
REF 42 | Dual CCK-A and CCK-B receptor antagonists (II). Preparation and structure activity relationships of 5-alkyl-9-methyl-1,4-benzodiazepines and discovery of FR208419. Chem Pharm Bull (Tokyo). 2000 Jan;48(1):1-15. | |||||
REF 43 | 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 44 | Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73. | |||||
REF 45 | Selective ligands for cholecystokinin receptor subtypes CCK-A and CCK-B within a single structural class, Bioorg. Med. Chem. Lett. 3(5):881-884 (1993). | |||||
REF 46 | 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 47 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 76). | |||||
REF 48 | 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 49 | Unexpected relationship between plasma protein binding and the pharmacodynamics of 2-NAP, a CCK1-receptor antagonist. Br J Clin Pharmacol. 2007 May;63(5):618-22. | |||||
REF 50 | Toward developing peptidomimetics: Successful replacement of backbone amide bonds in tetrapeptide-based CCK-A receptor agonists, Bioorg. Med. Chem. Lett. 3(5):855-860 (1993). | |||||
REF 51 | Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19. | |||||
REF 52 | Role of CCK(A) receptors in postprandial lower esophageal sphincter function in morbidly obese subjects. Dig Dis Sci. 2002 Nov;47(11):2531-7. | |||||
REF 53 | 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 54 | 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 55 | Distinct cholecystokinin receptors in brain and pancreas. Proc Natl Acad Sci U S A. 1980 Nov;77(11):6917-21. | |||||
REF 56 | Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci U S A. 1990 Sep;87(17):6728-32. | |||||
REF 57 | Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile. J Med Chem. 1998 Jan 1;41(1):38-45. | |||||
REF 58 | Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger". J Med Chem. 1996 Jan 19;39(2):562-9. | |||||
REF 59 | Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists. J Med Chem. 1997 Aug 15;40(17):2706-25. | |||||
REF 60 | 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 61 | 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 62 | Pharmacological study of IQM-97,423, a potent and selective CCK1 receptor antagonist with protective effect in experimental acute pancreatitis. Pharmacology. 2004 Oct;72(2):68-76. | |||||
REF 63 | Identification of a region of the N-terminal of the human CCKA receptor essential for the high affinity interaction with agonist CCK. Biochem Biophys Res Commun. 1995 Aug 24;213(3):845-52. | |||||
REF 64 | 3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokini... J Pharmacol Exp Ther. 2007 Nov;323(2):562-9. | |||||
REF 65 | Effects of KSG-504, a new CCK-A receptor antagonist, on gallbladder and gastrointestinal functions. Nihon Yakurigaku Zasshi. 1996 Jan;107(1):33-44. | |||||
REF 66 | 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 67 | Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas. J Med Chem. 1996 Feb 16;39(4):842-9. | |||||
REF 68 | C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists, Bioorg. Med. Chem. Lett. 5(24):3023-3026 (1995). | |||||
REF 69 | 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 70 | Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Br J Pharmacol. 1996 Apr;117(7):1558-64. | |||||
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