Reaction Details |
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Target | Growth hormone secretagogue receptor type 1/Isoform 1B of Growth hormone secretagogue receptor type 1 (1B) |
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Ligand | BDBM212436 |
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Substrate/Competitor | n/a |
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Meas. Tech. | GHS Ligand Binding Assay |
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Ki | 19.3±3.3 nM |
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Citation | Mary, S; Fehrentz, JA; Damian, M; Gaibelet, G; Orcel, H; Verdié, P; Mouillac, B; Martinez, J; Marie, J; Banères, JL Heterodimerization with Its splice variant blocks the ghrelin receptor 1a in a non-signaling conformation: a study with a purified heterodimer assembled into lipid discs. J Biol Chem288:24656-65 (2013) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Growth hormone secretagogue receptor type 1/Isoform 1B of Growth hormone secretagogue receptor type 1 (1B) |
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Name: | Growth hormone secretagogue receptor type 1/Isoform 1B of Growth hormone secretagogue receptor type 1 (1B) |
Synonyms: | GHS-R1a:GHS-R1b | Growth hormone secretagogue receptor type 1 (1B) |
Type: | Dimeric receptor |
Mol. Mass.: | n/a |
Description: | n/a |
Components: | This complex has 2 components. |
Component 1 |
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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Component 2 |
Name: | Isoform 1B of Growth hormone secretagogue receptor type 1 (1B) |
Synonyms: | GHSR | GHSR_HUMAN | Ghrelin receptor 1b (GHS-R1b) | Growth hormone secretagogue receptor type 1 (1B) |
Type: | Protein |
Mol. Mass.: | 32156.55 |
Organism: | Homo sapiens (Human) |
Description: | Q92847-2 |
Residue: | 289 |
Sequence: | MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAG
NLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQ
FVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFV
LVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLW
RRRRGDAVVGASLRDQNHKQTVKMLGGSQRALRLSLAGPILSLCLLPSL
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BDBM212436 |
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n/a |
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Name | BDBM212436 |
Synonyms: | JMV 3002 | N-[1-[4-[(2,4-dimethoxyphenyl)methyl]-5-(2-phenylethyl)-1,2,4-triazol-3-yl]-2-(1H-indol-3-yl)ethyl]pyridine-2-carboxamide |
Type | Small organic molecule |
Emp. Form. | C35H34N6O3 |
Mol. Mass. | 586.6829 |
SMILES | COc1ccc(Cn2c(CCc3ccccc3)nnc2C(Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)c(OC)c1 |
Structure |
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