Reaction Details |
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Target | Gastrin/cholecystokinin type B receptor |
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Ligand | BDBM50056102 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_439002 (CHEMBL889348) |
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Ki | 0.14±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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BDBM50056102 |
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n/a |
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Name | BDBM50056102 |
Synonyms: | (R)-1-(1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-3-(3-(methylamino)phenyl)urea | 1-[(R)-1-(3,3-Dimethyl-2-oxo-butyl)-2-oxo-5-pyridin-2-yl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-3-(3-methylamino-phenyl)-urea | CHEMBL324547 | YF-476 |
Type | Small organic molecule |
Emp. Form. | C28H30N6O3 |
Mol. Mass. | 498.5762 |
SMILES | CNc1cccc(NC(=O)N[C@@H]2N=C(c3ccccn3)c3ccccc3N(CC(=O)C(C)(C)C)C2=O)c1 |t:12| |
Structure |
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