Reaction Details
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Report a problem with these dataTarget
Growth hormone secretagogue receptor type 1
Ligand
BDBM50260273
Substrate
n/a
Meas. Tech.
ChEMBL_509093 (CHEMBL1007237)
IC50
210±n/a nM
Citation
Holst, B; Mokrosinski, J; Lang, M; Brandt, E; Nygaard, R; Frimurer, TM; Beck-Sickinger, AG; Schwartz, TW Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism. J Biol Chem 282:15799-811 (2007) [PubMed] Article More Info.:
Target
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:
MWNATPSEEPGFNLTLADLDWDASPGNDSLGDELLQLFPAPLLAGVTATCVALFVVGIAGNLLTMLVVSRFRELRTTTNLYLSSMAFSDLLIFLCMPLDLVRLWQYRPWNFGDLLCKLFQFVSESCTYATVLTITALSVERYFAICFPLRAKVVVTKGRVKLVIFVIWAVAFCSAGPIFVLVGVEHENGTDPWDTNECRPTEFAVRSGLLTVMVWVSSIFFFLPVFCLTVLYSLIGRKLWRRRRGDAVVGASLRDQNHKQTVKMLAVVVFAFILCWLPFHVGRYLFSKSFEPGSLEIAQISQYCNLVSFVLFYLSAAINPILYNIMSKKYRVAVFRLLGFEPFSQRKLSTLKDESSRAWTESSINT
Inhibitor
Name:
BDBM50260273
Synonyms:
CHEMBL507636 | DprwFwLL-NH2
Type:
Small organic molecule
Emp. Form.:
C58H78N14O10
Mol. Mass.:
1131.3277
SMILES:
CC(C)C[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CC(O)=O)C(N)=O |r,wU:66.70,41.56,30.40,16.28,73.79,8.12,wD:55.67,4.4,(17.4,-13.08,;17.4,-11.54,;18.72,-10.77,;16.07,-10.78,;16.05,-9.24,;14.72,-8.47,;14.71,-6.93,;16.04,-6.16,;13.37,-6.17,;13.36,-4.63,;14.69,-3.86,;14.69,-2.32,;16.04,-4.62,;12.04,-6.94,;10.71,-6.18,;10.69,-4.64,;9.38,-6.95,;9.39,-8.49,;10.72,-9.25,;12.12,-8.63,;13.15,-9.77,;12.39,-11.1,;12.87,-12.57,;11.85,-13.72,;10.34,-13.4,;9.86,-11.94,;10.89,-10.79,;8.04,-6.19,;6.71,-6.97,;6.71,-8.51,;5.37,-6.2,;5.36,-4.67,;6.69,-3.89,;8.03,-4.65,;9.36,-3.88,;9.35,-2.34,;8.02,-1.58,;6.69,-2.35,;4.04,-6.98,;2.7,-6.23,;2.69,-4.69,;1.37,-7,;1.38,-8.54,;2.71,-9.3,;4.12,-8.67,;5.15,-9.82,;4.38,-11.15,;4.87,-12.62,;3.84,-13.76,;2.33,-13.45,;1.85,-11.98,;2.88,-10.84,;.04,-6.23,;-1.29,-7,;-1.28,-8.55,;-2.63,-6.24,;-2.64,-4.7,;-1.31,-3.92,;-1.31,-2.39,;.02,-1.61,;.01,-.07,;-1.32,.7,;1.35,.71,;-3.96,-7.01,;-5.29,-6.25,;-5.31,-4.71,;-6.63,-7.02,;-7.53,-8.29,;-9.03,-7.52,;-8.76,-5.86,;-7.07,-5.61,;-6.08,-3.87,;-4.52,-3.86,;-6.94,-2.62,;-8.43,-2.61,;-6.19,-1.21,;-4.65,-1.2,;-3.89,.14,;-3.87,-2.53,;17.38,-8.46,;17.37,-6.93,;18.72,-9.22,)|
Structure:
