Proteins > Cholecystokinin receptor type A
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Cholecystokinin receptor type A
A cholecystokinin receptor 1 that is encoded in the genome of rat. [OMA:P30551, PRO:DNx]
Synonyms
CCK-A receptor;
CCK-AR;
Cholecystokinin-1 receptor;
CCK1-R
Research
Bioassay Publications (44)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 8 (18.18) | 18.7374 |
| 1990's | 25 (56.82) | 18.2507 |
| 2000's | 11 (25.00) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (34)
Drugs with Potency Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| lithium chloride | Rattus norvegicus (Norway rat) | Potency | 710.0000 | 1 | 0 |
Drugs with Inhibition Measurements
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:12, 1988
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:12, 1988
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:12, 1988
Design of nonpeptidal ligands for a peptide receptor: cholecystokinin antagonists.Journal of medicinal chemistry, , Volume: 30, Issue:7, 1987
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Novel glutamic acid derived cholecystokinin receptor ligands.Journal of medicinal chemistry, , Volume: 33, Issue:2, 1990
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
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.Journal of medicinal chemistry, , Jan-01, Volume: 41, Issue:1, 1998
Amide bond replacements incorporated into CCK-B selective "dipeptoids".Journal of medicinal chemistry, , Apr-17, Volume: 35, Issue:8, 1992
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Synthesis, biological evaluation, and quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Analogs of CCK incorporating conformationally constrained replacements for Asp32.Journal of medicinal chemistry, , Oct-30, Volume: 35, Issue:22, 1992
Three-dimensional molecular shape analysis-quantitative structure-activity relationship of a series of cholecystokinin-A receptor antagonists.Journal of medicinal chemistry, , Oct-14, Volume: 37, Issue:21, 1994
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:12, 1988
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Development of peptide 3D structure mimetics: rational design of novel peptoid cholecystokinin receptor antagonists.Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
beta-Turned dipeptoids as potent and selective CCK(1) receptor antagonists.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.Journal of medicinal chemistry, , Nov-04, Volume: 42, Issue:22, 1999
Three-dimensional molecular shape analysis-quantitative structure-activity relationship of a series of cholecystokinin-A receptor antagonists.Journal of medicinal chemistry, , Oct-14, Volume: 37, Issue:21, 1994
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993
Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.Journal of medicinal chemistry, , Mar-20, Volume: 35, Issue:6, 1992
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.Journal of medicinal chemistry, , Volume: 33, Issue:1, 1990
Novel glutamic acid derived cholecystokinin receptor ligands.Journal of medicinal chemistry, , Volume: 33, Issue:2, 1990
Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted benzolactams.Journal of medicinal chemistry, , Volume: 32, Issue:8, 1989
Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.Journal of medicinal chemistry, , Volume: 31, Issue:12, 1988
Combination of molecular modeling, site-directed mutagenesis, and SAR studies to delineate the binding site of pyridopyrimidine antagonists on the human CCK1 receptor.Journal of medicinal chemistry, , Jul-28, Volume: 48, Issue:15, 2005
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1)receptor antagonists: structure-activity relationship studies on the substituent at N2-position.Journal of medicinal chemistry, , Jun-21, Volume: 44, Issue:13, 2001
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.Journal of medicinal chemistry, , Nov-04, Volume: 42, Issue:22, 1999
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.Journal of medicinal chemistry, , Oct-10, Volume: 40, Issue:21, 1997
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Development of peptide 3D structure mimetics: rational design of novel peptoid cholecystokinin receptor antagonists.Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
Novel nonpeptide CCK-B antagonists: design and development of quinazolinone derivatives as potent, selective, and orally active CCK-B antagonists.Journal of medicinal chemistry, , Mar-26, Volume: 41, Issue:7, 1998
5-(Piperidin-2-yl)- and 5-(homopiperidin-2-yl)-1,4-benzodiazepines: high-affinity, basic ligands for the cholecystokinin-B receptor.Journal of medicinal chemistry, , Aug-01, Volume: 40, Issue:16, 1997
Controlled modification of acidity in cholecystokinin B receptor antagonists: N-(1,4-benzodiazepin-3-yl)-N'-[3-(tetrazol-5-ylamino) phenyl]ureas.Journal of medicinal chemistry, , Feb-16, Volume: 39, Issue:4, 1996
High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.Journal of medicinal chemistry, , Mar-18, Volume: 37, Issue:6, 1994
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
Rationally designed "dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Novel glutamic acid derived cholecystokinin receptor ligands.Journal of medicinal chemistry, , Volume: 33, Issue:2, 1990
Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.Bioorganic & medicinal chemistry letters, , Jun-05, Volume: 10, Issue:11, 2000
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.Journal of medicinal chemistry, , Nov-04, Volume: 42, Issue:22, 1999
Structurally similar small molecule photoaffinity CCK-A agonists and antagonists as novel tools for directly probing 7TM receptors-ligand interactions.Bioorganic & medicinal chemistry letters, , Nov-17, Volume: 8, Issue:22, 1998
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.Journal of medicinal chemistry, , Oct-10, Volume: 40, Issue:21, 1997
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Rationally designed "dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993
Rationally designed "dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.Journal of medicinal chemistry, , Jul-10, Volume: 35, Issue:14, 1992
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.Journal of medicinal chemistry, , Volume: 35, Issue:1, 1992
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.Journal of medicinal chemistry, , Volume: 34, Issue:1, 1991
Development of peptide 3D structure mimetics: rational design of novel peptoid cholecystokinin receptor antagonists.Journal of medicinal chemistry, , Sep-21, Volume: 43, Issue:19, 2000
Development of 1,4-benzodiazepine cholecystokinin type B antagonists.Journal of medicinal chemistry, , Dec-24, Volume: 36, Issue:26, 1993
Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Highly constrained dipeptoid analogues containing a type II' beta-turn mimic as novel and selective CCK-A receptor ligands.Bioorganic & medicinal chemistry letters, , Jan-04, Volume: 9, Issue:1, 1999
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993