Reaction Details |
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Target | Gastrin/cholecystokinin type B receptor |
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Ligand | BDBM50002895 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_439002 (CHEMBL889348) |
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Ki | 1.1±n/a nM |
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Citation | McDonald, IM; Black, JW; Buck, IM; Dunstone, DJ; Griffin, EP; Harper, EA; Hull, RA; Kalindjian, SB; Lilley, EJ; Linney, ID; Pether, MJ; Roberts, SP; Shaxted, ME; Spencer, J; Steel, KI; Sykes, DA; Walker, MK; Watt, GF; Wright, L; Wright, PT; Xun, W Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion. J Med Chem50:3101-12 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Gastrin/cholecystokinin type B receptor |
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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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BDBM50002895 |
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n/a |
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Name | BDBM50002895 |
Synonyms: | CHEMBL226726 |
Type | Small organic molecule |
Emp. Form. | C31H39N5O5 |
Mol. Mass. | 561.6719 |
SMILES | CN(CC(O)=O)c1cccc(NC(=O)CN2N=C(C3CCCCC3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 |t:16| |
Structure |
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