General Information of DTT (ID: TTCG0AL)

DTT Name Cholecystokinin receptor type A (CCKAR) DTT Info
Gene Name CCKAR

Molecule-Related Drug & Molecule List

Molecule-Related Drug List
Molecule Type:
DTT
DTP
DME
Drug Status:
Discontinued Drug(s)
Clinical Trial Drug(s)
Preclinical Drug(s)
Investigative Drug(s)
2 Clinical Trial Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexloxiglumide DM52HUD Pancreatic malfunction DC30-DC3Z Phase 2 [1]
proglumide DM4MF9V Influenza virus infection 1E30-1E32 Phase 2 [2]
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19 Discontinued Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
CE-326597 DMXO49B Obesity 5B81 Discontinued in Phase 2 [3]
GI 181771 DMIUFS4 Obesity 5B81 Discontinued in Phase 2 [4]
Lintitript DMS5X94 Obesity 5B81 Discontinued in Phase 2 [5]
Pranazepide DMP43IR Pancreatic malfunction DC30-DC3Z Discontinued in Phase 2 [6]
Tarazepide DMX6ZYE Gastrointestinal disease DE2Z Discontinued in Phase 2 [7]
SR-146131 DML7KCO Obesity 5B81 Discontinued in Phase 1 [8]
SSR-125180 DMSOBW2 Obesity 5B81 Discontinued in Phase 1 [9]
T-0632 DML4M5K Pancreatic malfunction DC30-DC3Z Discontinued in Phase 1 [10]
UCL-2000; butabindide DML51D0 Obesity 5B81 Discontinued in Phase 1 [11]
A-70276 DM9KNFZ Gastrointestinal disease DE2Z Terminated [12]
A-71623 DMKZNTY Obesity 5B81 Terminated [13]
CR-1795 DM8NVZQ N. A. N. A. Terminated [14]
FR-208419 DMLG426 Dyspepsia MD92 Terminated [15]
GI-248573 DMT6J1E Bladder disease DC11-DC1Z Terminated [9]
IQM-95333 DMYCPFU N. A. N. A. Terminated [16]
Lorglumide DM904B6 Pancreatic malfunction DC30-DC3Z Terminated [17]
PD-135666 DMLEVNC N. A. N. A. Terminated [18]
SNF-9007 DM4CNM9 N. A. N. A. Terminated [19]
SR-27950 DMZ8SXP Eating disorder 6B82 Terminated [20]
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⏷ Show the Full List of 19 Discontinued Drug(s)
6 Preclinical Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
A-71378 DMZ4HMP Obesity 5B81 Preclinical [11]
A-74498 DMAK6H3 Obesity 5B81 Preclinical [11]
AR-R-1589 DMMD8VY Eating disorder 6B82 Preclinical [11]
FPL-14294 DMUHVEA Obesity 5B81 Preclinical [11]
GG-8573 DMFQI38 Obesity 5B81 Preclinical [11]
PD-170292 DMEOVDQ Obesity 5B81 Preclinical [11]
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⏷ Show the Full List of 6 Preclinical Drug(s)
63 Investigative Drug(s) Transported by This DTP
Drug Name Drug ID Indication ICD 11 Highest Status REF
1-(3,3-Diphenyl-allyl)-3-m-tolyl-urea DM6RO2L Discovery agent N.A. Investigative [21]
1-(4-Chloro-phenyl)-3-(3,3-diphenyl-allyl)-urea DM3YI5G Discovery agent N.A. Investigative [21]
1-(4-Chloro-phenyl)-3-(3-pentyl-oct-2-enyl)-urea DMUW1GI Discovery agent N.A. Investigative [21]
2-NAP DM2FTIC Gastrointestinal disease DE2Z Investigative [22]
3,4-Dichloro-N-(3,3-diphenyl-allyl)-benzamide DMWOMVF Discovery agent N.A. Investigative [21]
Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe DMKAHYQ Discovery agent N.A. Investigative [23]
Asperlicin DMAY2N3 Gastrointestinal disease DE2Z Investigative [24]
Bis(31/31')[[Cys(31), Nva(34)]NPY(27-36)-NH(2)] DMKANOH Discovery agent N.A. Investigative [25]
Boc-Asp-Tyr(So3-)-Nle-Gly-Trp-Asp-Phe-NH2 DMPJR98 Discovery agent N.A. Investigative [26]
Boc-cyclo-(Glu-Tyr-Nle-D-Lys)-Trp-Nle-Asp-Phe-NH2 DMRQVME Discovery agent N.A. Investigative [27]
Boc-D-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 DMBCPKF Discovery agent N.A. Investigative [27]
Boc-D-Glu-Tyr(SO3H)-Nle-D-Nle-Trp-Nle-Asp-Phe-NH2 DM1IXOG Discovery agent N.A. Investigative [27]
Boc-Glu-Tyr(SO3H)-Nle-D-Lys-Trp-Nle-Asp-Phe-NH2 DMN3EU9 Discovery agent N.A. Investigative [27]
Boc-Tyr(SO3H)-Nle-Gly-Trp-Nle-Asp-Phe-NH2 DMAYWTI Discovery agent N.A. Investigative [27]
CCK-33 DM1N0ED Discovery agent N.A. Investigative [28]
CCK-8 DMN0J4W N. A. N. A. Investigative [29]
CI-1015 DMQ5CE1 Discovery agent N.A. Investigative [30]
CR-2345 DMFG0XS Discovery agent N.A. Investigative [14]
Devazepide DMD4N2F Gastrointestinal disease DE2Z Investigative [24]
FR-175985 DMQDP23 Discovery agent N.A. Investigative [6]
Glaxo-11p DM4QJPU Discovery agent N.A. Investigative [31]
GW-5823 DMCOYF9 Discovery agent N.A. Investigative [32]
H-Tyr-D-Ala-Gly-Phe-NH-NH-D-Trp-Nle-Asp-Phe-H DMF82C1 Discovery agent N.A. Investigative [33]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-D-Trp-H DMSXD63 Discovery agent N.A. Investigative [34]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-Nle-Trp-Boc DMIPXCZ Discovery agent N.A. Investigative [34]
H-Tyr-D-Ala-Gly-Phe-NH-NH-Trp-D-Nle-D-Asp-D-Phe-H DMFSKDM Discovery agent N.A. Investigative [33]
IQM-97423 DM2MXIK Discovery agent N.A. Investigative [35]
JMV180 DM5G0IM Discovery agent N.A. Investigative [36]
JNJ-17156516 DMIXUNB Discovery agent N.A. Investigative [37]
KSG-504 DMC92ER Pancreatic malfunction DC30-DC3Z Investigative [38]
L-708474 DM3QUCS Discovery agent N.A. Investigative [39]
L-736380 DMM5AYL Discovery agent N.A. Investigative [40]
L-740093 DMVA2D0 Discovery agent N.A. Investigative [41]
PD-135118 DMUTEWI Discovery agent N.A. Investigative [18]
PD-135158 DMA7YJV Discovery agent N.A. Investigative [29]
PD-136621 DM8N3RB Discovery agent N.A. Investigative [18]
PD-137337 DMJWK0T Discovery agent N.A. Investigative [18]
PD-137342 DMH2OV9 Discovery agent N.A. Investigative [18]
PD-138915 DMLVRU7 Discovery agent N.A. Investigative [18]
PD-138916 DMIAFN5 Discovery agent N.A. Investigative [18]
PD-140547 DMF86P3 Discovery agent N.A. Investigative [18]
PD-140548 DMNO2EP Discovery agent N.A. Investigative [18]
PD-140723 DMWTOJN Discovery agent N.A. Investigative [18]
SC-50998 DMBQ16F Discovery agent N.A. Investigative [20]
Tetragastrin DMDWUCX Discovery agent N.A. Investigative [42]
TP-680 DMM41O9 Discovery agent N.A. Investigative [43]
Tyr-D-Ala-Gly-D-Trp-Nle-Asp-Phe-NH2 DM0D1Z5 Discovery agent N.A. Investigative [19]
Tyr-D-Ala-Gly-D-Trp-NMeNle-Asp-Phe-NH2 DMPH1G0 Discovery agent N.A. Investigative [19]
Tyr-D-Ala-Gly-Phe-NH-NH-Phe-Asp-NMeNle-D-Trp-Boc DMB2TCF Discovery agent N.A. Investigative [34]
Tyr-D-Ala-Gly-Trp-Nle-Asp-Phe-NH2 DMUXMVQ Discovery agent N.A. Investigative [19]
Tyr-D-Ala-Gly-Trp-NMeNle-Asp-Phe-NH2 DMREJ69 Discovery agent N.A. Investigative [19]
Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 DMQREP2 Discovery agent N.A. Investigative [19]
Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 DMZ24LN Discovery agent N.A. Investigative [19]
Tyr-D-Phe-Gly-D-Trp-Nle-Asp-Phe-NH2 DMIWMN6 Discovery agent N.A. Investigative [19]
Tyr-D-Phe-Gly-D-Trp-NMeNle-Asp-Phe-NH2 DM2CEWT Discovery agent N.A. Investigative [19]
Tyr-D-Phe-Gly-Trp-Nle-Asp-Phe-NH2 DMKM81A Discovery agent N.A. Investigative [19]
Tyr-D-Phe-Gly-Trp-NMeNle-Asp-Phe-NH2 DMZOTGM Discovery agent N.A. Investigative [19]
VL-0395 DMKW5YL Discovery agent N.A. Investigative [44]
VL-0494 DM2XAUY Discovery agent N.A. Investigative [45]
VL-0699 DMCZNB3 Discovery agent N.A. Investigative [46]
VL-1499 DMU9VQJ Discovery agent N.A. Investigative [44]
VL-2799 DMBEV4W Discovery agent N.A. Investigative [47]
[3H]devazepide DM4NXRO Discovery agent N.A. Investigative [48]
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⏷ Show the Full List of 63 Investigative Drug(s)
Molecule Interaction Atlas

References

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2 Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8.
3 Obesity Pharmacotherapy: Current Perspectives and Future Directions. Curr Cardiol Rev. 2013 February; 9(1): 33-54.
4 Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 Jul-Aug;25(6):483-506.
5 A cholecystokinin-1 receptor agonist (CCK-8) mediates increased permeability of brain barriers to leptin. Br J Pharmacol. 2008 Jul;154(5):1009-15.
6 Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines, Bioorg. Med. Chem. Lett. 7(2):169-174 (1997).
7 Melatonin as modulator of pancreatic enzyme secretion and pancreatoprotector. J Physiol Pharmacol. 2007 Dec;58 Suppl 6:65-80.
8 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.
9 US patent application no. 8,748,419, Antagonists.
10 Effect of T-0632, a cholecystokininA receptor antagonist, on experimental acute pancreatitis. Jpn J Pharmacol. 1997 Feb;73(2):105-12.
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12 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.
13 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.
14 Biological properties of (R)-4-benzamido-5-oxopentanoic basic derivatives as CCK-antagonists, Bioorg. Med. Chem. Lett. 3(5):861-866 (1993).
15 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.
16 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.
17 Behavioral and neurochemical study on the role of the brain cholecystokinin system in anxiety. Hokkaido Igaku Zasshi. 1998 Sep;73(5):463-73.
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19 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.
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. (Target id: 76).
21 Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718. J Med Chem. 1992 Mar 20;35(6):1042-9.
22 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.
23 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).
24 Privileged structures: a useful concept for the rational design of new lead drug candidates. Mini Rev Med Chem. 2007 Nov;7(11):1108-19.
25 Role of CCK(A) receptors in postprandial lower esophageal sphincter function in morbidly obese subjects. Dig Dis Sci. 2002 Nov;47(11):2531-7.
26 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.
27 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.
28 Distinct cholecystokinin receptors in brain and pancreas. Proc Natl Acad Sci U S A. 1980 Nov;77(11):6917-21.
29 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.
30 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.
31 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.
32 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.
33 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.
34 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.
35 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.
36 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.
37 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.
38 Effects of KSG-504, a new CCK-A receptor antagonist, on gallbladder and gastrointestinal functions. Nihon Yakurigaku Zasshi. 1996 Jan;107(1):33-44.
39 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.
40 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.
41 C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists, Bioorg. Med. Chem. Lett. 5(24):3023-3026 (1995).
42 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.
43 Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist. Br J Pharmacol. 1996 Apr;117(7):1558-64.
44 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.
45 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.
46 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.
47 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.
48 Characterization of the binding of [3H]-(+/-)-L-364,718: a new potent, nonpeptide cholecystokinin antagonist radioligand selective for peripheral receptors. Mol Pharmacol. 1986 Sep;30(3):212-7.