Target Information
| Target General Information | Top | |||||
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| Target ID |
T05849
(Former ID: TTDS00043)
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| Target Name |
Gastrin/cholecystokinin type B receptor (CCKBR)
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| Synonyms |
Cholecystokinin-2 receptor; CCKRB; CCK2-R; CCK-BR; CCK-B receptor
Click to Show/Hide
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| Gene Name |
CCKBR
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 2 Target-related Diseases | + | ||||
| 1 | Diagnostic imaging [ICD-11: N.A.] | |||||
| 2 | Pancreatic internal secretion disorder [ICD-11: 5A4Y] | |||||
| Function |
The CCK-B receptors occur throughout the central nervous system where they modulate anxiety, analgesia, arousal, and neuroleptic activity. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Receptor for gastrin and cholecystokinin.
Click to Show/Hide
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| BioChemical Class |
GPCR rhodopsin
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| UniProt ID | ||||||
| Sequence |
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL PDEDPPTPSIASLSRLSYTTISTLGPG Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| ADReCS ID | BADD_A01437 | |||||
| HIT2.0 ID | T44C7S | |||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Pentagastrin | Drug Info | Approved | Diagnostic imaging | [3], [4] | |
| Clinical Trial Drug(s) | [+] 9 Clinical Trial Drugs | + | ||||
| 1 | GASTRAZOLE | Drug Info | Phase 3 | Duodenal ulcer | [5] | |
| 2 | Dexloxiglumide | Drug Info | Phase 2 | Pancreatic malfunction | [2] | |
| 3 | Itriglumide | Drug Info | Phase 2 | Anxiety disorder | [6], [7] | |
| 4 | S-0509 | Drug Info | Phase 2 | Ulcerative colitis | [8] | |
| 5 | Spiroglumide | Drug Info | Phase 2 | Stomach disease | [9] | |
| 6 | TT-223 | Drug Info | Phase 2 | Type-1 diabetes | [10] | |
| 7 | YF-476 | Drug Info | Phase 2 | Stomach ulcer | [11], [12] | |
| 8 | Z 360 | Drug Info | Phase 2 | Discovery agent | [13], [14] | |
| 9 | Demogastrin | Drug Info | Phase 1 | Thyroid cancer | [15] | |
| Discontinued Drug(s) | [+] 6 Discontinued Drugs | + | ||||
| 1 | CR-2093 | Drug Info | Discontinued in Phase 1 | Intestine cancer | [21] | |
| 2 | AG-041R | Drug Info | Terminated | Ulcerative colitis | [25], [26] | |
| 3 | FR-208419 | Drug Info | Terminated | Dyspepsia | [27] | |
| 4 | GR-199114X | Drug Info | Terminated | Stomach ulcer | [28] | |
| 5 | LY288513 | Drug Info | Terminated | Anxiety disorder | [29], [30] | |
| 6 | YM-022 | Drug Info | Terminated | Gastrointestinal disease | [31], [32] | |
| Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
| 1 | JNJ-26070109 | Drug Info | Preclinical | Gastroesophageal reflux disease | [23], [24] | |
| 2 | PD-170292 | Drug Info | Preclinical | Obesity | [22] | |
| Mode of Action | [+] 4 Modes of Action | + | ||||
| Agonist | [+] 8 Agonist drugs | + | ||||
| 1 | Pentagastrin | Drug Info | [1], [33], [34], [35] | |||
| 2 | PD-170292 | Drug Info | [22] | |||
| 3 | CCK-33 | Drug Info | [56] | |||
| 4 | CCK-8 | Drug Info | [56] | |||
| 5 | desulfated cholecystokinin-8 | Drug Info | [35] | |||
| 6 | PBC-264 | Drug Info | [62] | |||
| 7 | RB-400 | Drug Info | [65] | |||
| 8 | [3H]PBC-264 | Drug Info | [73] | |||
| Antagonist | [+] 17 Antagonist drugs | + | ||||
| 1 | GASTRAZOLE | Drug Info | [36], [2] | |||
| 2 | Itriglumide | Drug Info | [38] | |||
| 3 | S-0509 | Drug Info | [39], [2] | |||
| 4 | Spiroglumide | Drug Info | [40] | |||
| 5 | JNJ-26070109 | Drug Info | [45] | |||
| 6 | LY288513 | Drug Info | [49] | |||
| 7 | PD136450 | Drug Info | [51] | |||
| 8 | YM-022 | Drug Info | [52] | |||
| 9 | CI-1015 | Drug Info | [58] | |||
| 10 | GW-5823 | Drug Info | [59] | |||
| 11 | PD-135158 | Drug Info | [63] | |||
| 12 | PD-149164 | Drug Info | [64] | |||
| 13 | tetronothiodin | Drug Info | [69] | |||
| 14 | TP-680 | Drug Info | [70] | |||
| 15 | [125I]PD142308 | Drug Info | [67] | |||
| 16 | [3H]JB-93182 | Drug Info | [72] | |||
| 17 | [3H]PD140376 | Drug Info | [74] | |||
| Inhibitor | [+] 36 Inhibitor drugs | + | ||||
| 1 | Dexloxiglumide | Drug Info | [37] | |||
| 2 | YF-476 | Drug Info | [42] | |||
| 3 | IQM-95333 | Drug Info | [37] | |||
| 4 | PD-135666 | Drug Info | [50] | |||
| 5 | 4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [53] | |||
| 6 | Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe | Drug Info | [54] | |||
| 7 | Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 | Drug Info | [55] | |||
| 8 | Cholecystokinin-9 | Drug Info | [57] | |||
| 9 | H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-Bo | Drug Info | [60] | |||
| 10 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H | Drug Info | [61] | |||
| 11 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Ac | Drug Info | [61] | |||
| 12 | H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc | Drug Info | [61] | |||
| 13 | PD-135118 | Drug Info | [50] | |||
| 14 | PD-136621 | Drug Info | [50] | |||
| 15 | PD-137337 | Drug Info | [50] | |||
| 16 | PD-137342 | Drug Info | [50] | |||
| 17 | PD-138915 | Drug Info | [50] | |||
| 18 | PD-138916 | Drug Info | [50] | |||
| 19 | PD-138917 | Drug Info | [50] | |||
| 20 | PD-140547 | Drug Info | [50] | |||
| 21 | PD-140548 | Drug Info | [50] | |||
| 22 | PD-140723 | Drug Info | [50] | |||
| 23 | Tetragastrin | Drug Info | [68] | |||
| 24 | Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 25 | Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 26 | Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc | Drug Info | [61] | |||
| 27 | Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 28 | Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 29 | Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 30 | Tyr-D-Nle-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 31 | Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 32 | Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 33 | Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 34 | Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 35 | Tyr-D-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [71] | |||
| 36 | Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2 | Drug Info | [71] | |||
| Modulator | [+] 10 Modulator drugs | + | ||||
| 1 | TT-223 | Drug Info | [41] | |||
| 2 | Z 360 | Drug Info | [13], [14] | |||
| 3 | Demogastrin | Drug Info | [43] | |||
| 4 | CR-2093 | Drug Info | [44] | |||
| 5 | AG-041R | Drug Info | [46] | |||
| 6 | FR-208419 | Drug Info | [47] | |||
| 7 | GR-199114X | Drug Info | [48] | |||
| 8 | RP-71483 | Drug Info | [66] | |||
| 9 | RP-72540 | Drug Info | [66] | |||
| 10 | RPR-107836 | Drug Info | [67] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
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| Calcium signaling pathway | hsa04020 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
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| Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
| Gastric acid secretion | hsa04971 | Affiliated Target |
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| Class: Organismal Systems => Digestive system | Pathway Hierarchy | ||
| Degree | 2 | Degree centrality | 2.15E-04 | Betweenness centrality | 0.00E+00 |
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| Closeness centrality | 1.56E-01 | Radiality | 1.22E+01 | Clustering coefficient | 1.00E+00 |
| Neighborhood connectivity | 4.50E+00 | Topological coefficient | 6.43E-01 | Eccentricity | 13 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| 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 | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
|---|---|---|---|---|---|---|
| KEGG Pathway | [+] 3 KEGG Pathways | + | ||||
| 1 | Calcium signaling pathway | |||||
| 2 | Neuroactive ligand-receptor interaction | |||||
| 3 | Gastric acid secretion | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | CCKR signaling map ST | |||||
| Pathwhiz Pathway | [+] 1 Pathwhiz Pathways | + | ||||
| 1 | Gastric Acid Production | |||||
| Reactome | [+] 3 Reactome Pathways | + | ||||
| 1 | Peptide ligand-binding receptors | |||||
| 2 | G alpha (q) signalling events | |||||
| 3 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| WikiPathways | [+] 7 WikiPathways | + | ||||
| 1 | GPCRs, Class A Rhodopsin-like | |||||
| 2 | Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| 3 | Secretion of Hydrochloric Acid in Parietal Cells | |||||
| 4 | Peptide GPCRs | |||||
| 5 | GPCR ligand binding | |||||
| 6 | GPCR downstream signaling | |||||
| 7 | GPCRs, Other | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
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| REF 1 | Functional interactions between endocannabinoid and CCK neurotransmitter systems may be critical for extinction learning. Neuropsychopharmacology. 2009 Jan;34(2):509-21. | |||||
| REF 2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
| REF 3 | 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: 870). | |||||
| REF 4 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 017048. | |||||
| REF 5 | Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 Apr 24;94(8):1107-15. | |||||
| 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: 909). | |||||
| 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 800010503) | |||||
| REF 8 | ClinicalTrials.gov (NCT00243074) S0509: AZD2171 in Treating Patients With Malignant Pleural Mesothelioma That Cannot Be Removed By Surgery. U.S. National Institutes of Health. | |||||
| REF 9 | Progress medicinal chem PMC37H. Page(48). | |||||
| REF 10 | ClinicalTrials.gov (NCT00743002) A Trial of TT223 in Patients With Type 2 Diabetes Who Are Taking Metformin and/or Thiazolidinedione. U.S. National Institutes of Health. | |||||
| 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: 887). | |||||
| REF 12 | ClinicalTrials.gov (NCT01339169) YF476 and Type I Gastric Carcinoids. U.S. National Institutes of Health. | |||||
| REF 13 | Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gen... Biol Pharm Bull. 2010;33(2):216-22. | |||||
| REF 14 | Z-360, a novel therapeutic agent for pancreatic cancer, prevents up-regulation of ephrin B1 gene expression and phosphorylation of NR2B via suppression of interleukin-1 production in a cancer-induced pain model in mice.Mol Pain.2010 Oct 28;6:72. | |||||
| REF 15 | 99mTc-Demogastrin 2 for CCK 2-receptor scintigraphy in medullary thyroid carcinoma. J Nucl Med. 2008; 49 (Supplement 1):115P. | |||||
| REF 16 | 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: 3503). | |||||
| REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005803) | |||||
| REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000702) | |||||
| REF 19 | 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: 879). | |||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001138) | |||||
| 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 800001442) | |||||
| REF 22 | Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60. | |||||
| REF 23 | 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: 6665). | |||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026533) | |||||
| REF 25 | 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: 901). | |||||
| 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 800005071) | |||||
| REF 27 | 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 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009210) | |||||
| REF 29 | 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: 902). | |||||
| REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002176) | |||||
| REF 31 | 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: 888). | |||||
| REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004033) | |||||
| REF 33 | Molecular cloning of the human brain and gastric cholecystokinin receptor: structure, functional expression and chromosomal localization. Biochem Biophys Res Commun. 1992 Nov 30;189(1):296-303. | |||||
| REF 34 | The effects of central administration of the CCK-B receptor agonist pentagastrin on feeding and cortisol release in sheep. Methods Find Exp Clin Pharmacol. 1996 May;18(4):235-8. | |||||
| REF 35 | The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization. J Biol Chem. 1993 Apr 15;268(11):8164-9. | |||||
| REF 36 | Gastrazole (JB95008), a novel CCK2/gastrin receptor antagonist, in the treatment of advanced pancreatic cancer: results from two randomised controlled trials. Br J Cancer. 2006 April 24; 94(8): 1107-1115. | |||||
| REF 37 | 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 38 | Role of CCK/gastrin receptors in gastrointestinal/metabolic diseases and results of human studies using gastrin/CCK receptor agonists/antagonists in these diseases. Curr Top Med Chem. 2007; 7(12): 1211-1231. | |||||
| REF 39 | Selective action of a CCK-B/gastrin receptor antagonist, S-0509, on pentagastrin-, peptone meal- and beer-stimulated gastric acid secretion in dogs. Aliment Pharmacol Ther. 2000 Apr;14(4):479-88. | |||||
| REF 40 | Effect of dexloxiglumide and spiroglumide, two new CCK-receptor antagonists, on gastric emptying and secretion in the rat: evaluation of their receptor selectivity in vivo. Aliment Pharmacol Ther. 1996 Jun;10(3):411-9. | |||||
| REF 41 | The effect of glucagon-like peptide-1 on energy expenditure and substrate metabolism in humans. Int J Obes Relat Metab Disord. 2000 Mar;24(3):288-98. | |||||
| REF 42 | CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs. Scand J Gastroenterol. 2004 Sep;39(9):886-90. | |||||
| REF 43 | Demonstration of new sites of expression of the CCK-B/gastrin receptor in pancreatic acinar AR42J cells using immunoelectron microscopy. Regul Pept. 1999 Oct 22;84(1-3):81-9. | |||||
| REF 44 | Inhibitory effects of the gastrin receptor antagonist CR2093 on basal, gastrin-stimulated and growth factor-stimulated growth of the rat pancreatic cell line AR42J. Anticancer Drugs. 1994 Oct;5(5):591-7. | |||||
| REF 45 | The cholecystokinin CCK2 receptor antagonist, JNJ-26070109, inhibits gastric acid secretion and prevents omeprazole-induced acid rebound in the rat. Br J Pharmacol. 2012 Jul;166(5):1684-93. | |||||
| REF 46 | AG-041R, a gastrin/CCK-B antagonist, stimulates chondrocyte proliferation and metabolism in vitro. Biochem Biophys Res Commun. 2001 May 25;283(5):1118-23. | |||||
| REF 47 | 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 48 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009210) | |||||
| REF 49 | Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73. | |||||
| REF 50 | 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 51 | Cholecystokinin type B receptor antagonist PD-136,450 is a partial secretory agonist in the stomach and a full agonist in the pancreas of the rat. Gut. 1994 Feb;35(2):270-4. | |||||
| REF 52 | YM022, a potent and selective gastrin/CCK-B receptor antagonist, inhibits peptone meal-induced gastric acid secretion in Heidenhain pouch dogs. Dig Dis Sci. 1997 Apr;42(4):707-14. | |||||
| REF 53 | 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 54 | The rational design and synthesis of non-peptide hegnylogues of CCK-26-33 - a novel series of CCK-A selective ligands, Bioorg. Med. Chem. Lett. 3(5):889-894 (1993). | |||||
| REF 55 | 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. | |||||
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