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Reaction Details
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TargetGastrin/cholecystokinin type B receptor
LigandBDBM21280
Substrate/Competitorn/a
Ki>10000±n/a nM
CommentsPDSP_1751
Citation Rinaldi-Carmona, MBarth, FMillan, JDerocq, JMCasellas, PCongy, COustric, DSarran, MBouaboula, MCalandra, BPortier, MShire, DBrelière, JCLe Fur, GL SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J Pharmacol Exp Ther284:644-50 (1998) [PubMed]
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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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BDBM21280
n/a
NameBDBM21280
Synonyms:5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S)-1,3,3-trimethylbicyclo[2.2.1]heptan-2-yl]-1H-pyrazole-3-carboxamide | N-(1,3,3-trimethylbicyclo(2.2.1)heptan-2-yl)-5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)pyrazole-3-carboxamide | SR 144528 | SR-144528 | SR144528
TypeSmall organic molecule
Emp. Form.C29H34ClN3O
Mol. Mass.476.053
SMILESCc1ccc(Cn2nc(cc2-c2ccc(Cl)c(C)c2)C(=O)NC2[C@@]3(C)CCC(C3)C2(C)C)cc1 |r,TLB:21:22:28:26.25|
Structure
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