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TargetGastrin/cholecystokinin type B receptor
LigandBDBM21135
Substrate/Competitor[125I]CCK-8
Meas. Tech.Radioligand Labeled Binding Assay and Phosphatidylinositol Hydrolysis Assay for the CCK Receptor
Ki 0.22±n/a nM
Citation Agnes, RSLee, YSDavis, PMa, SWBadghisi, HPorreca, FLai, JHruby, VJ Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem49:2868-75 (2006) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Gastrin/cholecystokinin type B receptor
Name:Gastrin/cholecystokinin type B receptor
Synonyms:CCK-2 receptor | CCK-B receptor | CCK-BR | CCKBR | CCKRB | Cholecystokinin A | Cholecystokinin receptor | Cholecystokinin-2 Receptor | GASR_HUMAN | Gastrin/cholecystokinin type B receptor
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:48445.79
Organism:Homo sapiens (Human)
Description:Stable expression of human CCK-2 receptors in HEK 293 cells.
Residue:447
Sequence:
MELLKLNRSVQGTGPGPGASLCRPGAPLLNSSSVGNLSCEPPRIRGAGTRELELAIRITL
YAVIFLMSVGGNMLIIVVLGLSRRLRTVTNAFLLSLAVSDLLLAVACMPFTLLPNLMGTF
IFGTVICKAVSYLMGVSVSVSTLSLVAIALERYSAICRPLQARVWQTRSHAARVIVATWL
LSGLLMVPYPVYTVVQPVGPRVLQCVHRWPSARVRQTWSVLLLLLLFFIPGVVMAVAYGL
ISRELYLGLRFDGDSDSDSQSRVRNQGGLPGAVHQNGRCRPETGAVGEDSDGCYVQLPRS
RPALELTALTAPGPGSGSRPTQAKLLAKKRVVRMLLVIVVLFFLCWLPVYSANTWRAFDG
PGAHRALSGAPISFIHLLSYASACVNPLVYCFMHRRFRQACLETCARCCPRPPRARPRAL
PDEDPPTPSIASLSRLSYTTISTLGPG
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BDBM21135
[125I]CCK-8
NameBDBM21135
Synonyms:(3S)-3-[(2S)-2-[(2S)-2-(2-{[(2S)-1-[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]pyrrolidin-2-yl]formamido}acetamido)-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid | CCK-Opioid Peptide, 5 | Tyr-Pro-Gly-Trp-NMeNle-Asp-Phe-NH2
TypePeptide
Emp. Form.C47H59N9O10
Mol. Mass.910.0257
SMILESCCCC[C@H](N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
Structure
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