Reaction Details |
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Target | Growth hormone secretagogue receptor type 1 |
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Ligand | BDBM19388 |
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Substrate/Competitor | 125I-His9-ghrelin |
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Meas. Tech. | Receptor Binding Studies and GHS-R Ca2+ Flux Assay |
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pH | 7.4±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 1.0±n/a nM |
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EC50 | 85±89 nM |
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Citation | Serby, MD; Zhao, H; Szczepankiewicz, BG; Kosogof, C; Xin, Z; Liu, B; Liu, M; Nelson, LT; Kaszubska, W; Falls, HD; Schaefer, V; Bush, EN; Shapiro, R; Droz, BA; Knourek-Segel, VE; Fey, TA; Brune, ME; Beno, DW; Turner, TM; Collins, CA; Jacobson, PB; Sham, HL; Liu, G 2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists. J Med Chem49:2568-78 (2006) [PubMed] Article |
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More Info.: | Get all data from this article, Solution Info, Assay Method |
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Growth hormone secretagogue receptor type 1 |
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Name: | Growth hormone secretagogue receptor type 1 |
Synonyms: | GH-releasing peptide receptor | GHRP | GHS-R | GHSR | GHSR_HUMAN | Ghrelin Receptor (Growth Hormone Secretagogue Receptor Type 1) | Ghrelin receptor | Ghrelin receptor 1a (GHS-R1a) |
Type: | Receptor |
Mol. Mass.: | 41334.57 |
Organism: | Homo sapiens (Human) |
Description: | Receptor binding studies use plasma membranes from LLC PK-1 cells transiently transfected with hGHSR1a. |
Residue: | 366 |
Sequence: | MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG
NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ
FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV
LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW
RRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQI
SQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWT
ESSINT
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BDBM19388 |
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125I-His9-ghrelin |
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Name: | 125I-His9-ghrelin |
Synonyms: | radiolabeled peptide ligand |
Type: | Peptide |
Mol. Mass.: | 9033.11 |
Organism: | n/a |
Description: | n/a |
Residue: | 82 |
Sequence: | GLYSERSERCTANYLPHELESERPRGLHISGLNARGVALGLNGLNARGLYSGLSERLYSL
YSPRPRALALYSLEGLNPRARG
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