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Target
Glucagon-like peptide 1 receptor
Ligand
BDBM50324732
Substrate
n/a
Meas. Tech.
ChEMBL_651180 (CHEMBL1227945)
EC50
0.6±n/a nM
Citation
 Day, JW; Ottaway, N; Patterson, JT; Gelfanov, V; Smiley, D; Gidda, J; Findeisen, H; Bruemmer, D; Drucker, DJ; Chaudhary, N; Holland, J; Hembree, J; Abplanalp, W; Grant, E; Ruehl, J; Wilson, H; Kirchner, H; Lockie, SH; Hofmann, S; Woods, SC; Nogueiras, R; Pfluger, PT; Perez-Tilve, D; DiMarchi, R; Tschöp, MH A new glucagon and GLP-1 co-agonist eliminates obesity in rodents. Nat Chem Biol 5:749-57 (2009) [PubMed]  Article 
Target
Name:
Glucagon-like peptide 1 receptor
Synonyms:
GLP-1 receptor | GLP-1-R | GLP-1R | GLP1R | GLP1R_HUMAN | Glucagon-like peptide 1 receptor | Glucagon-like peptide 1 receptor (GLP-1)
Type:
Enzyme
Mol. Mass.:
53035.78
Organism:
Homo sapiens (Human)
Description:
P43220
Residue:
463
Sequence:
MAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDLFCNRTFDEYACWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPWRDLSECEESKRGERSSPEEQLLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIHLNLFASFILRALSVFIKDAALKWMYSTAAQQHQWDGLLSYQDSLSCRLVFLLMQYCVAANYYWLLVEGVYLYTLLAFSVLSEQWIFRLYVSIGWGVPLLFVVPWGIVKYLYEDEGCWTRNSNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLAKSTLTLIPLLGTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERWRLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS
  
Inhibitor
Name:
BDBM50324732
Synonyms:
CHEMBL1222075
Type:
Small organic molecule
Emp. Form.:
C153H225N43O49S
Mol. Mass.:
3482.747
SMILES:
CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(O)=O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(N)=O |r,wU:205.213,177.190,167.174,147.160,132.141,112.119,98.103,76.86,62.70,43.53,30.37,8.12,231.237,wD:196.207,188.194,219.227,173.178,222.230,159.168,141.147,120.132,104.111,87.97,71.74,54.61,39.41,16.28,4.4,239.245,240.248,209.214,(21.88,-5.16,;20.57,-4.37,;20.57,-2.78,;19.27,-1.98,;19.27,-.39,;17.96,.41,;16.65,-.39,;16.65,-1.98,;15.33,.41,;15.33,2,;16.65,2.8,;16.65,4.38,;17.96,2,;14.03,-.38,;12.72,.41,;12.72,2,;11.41,-.38,;11.41,-1.97,;12.72,-2.77,;14.09,-2.12,;15.11,-3.31,;14.35,-4.69,;14.81,-6.2,;13.79,-7.38,;12.32,-7.04,;11.85,-5.52,;12.87,-4.35,;10.1,.42,;8.79,-.38,;8.79,-1.97,;7.48,.42,;7.48,2,;8.79,2.81,;8.79,4.39,;7.48,5.18,;10.11,5.18,;6.17,-.37,;4.86,.42,;4.86,2.01,;3.55,-.37,;2.24,.42,;.94,-.37,;.94,-1.96,;-.38,.43,;-.38,2.01,;.94,2.82,;2.24,2.01,;3.55,2.81,;3.55,4.4,;2.25,5.19,;.94,4.4,;-1.68,-.37,;-3.01,.43,;-3.01,2.02,;-4.3,-.36,;-4.3,-1.95,;-3.01,-2.75,;-1.69,-1.95,;-3.01,-4.34,;-5.61,.43,;-6.92,-.36,;-6.92,-1.95,;-8.24,.44,;-8.24,2.02,;-6.92,2.83,;-6.92,4.41,;-8.23,5.2,;-5.61,5.2,;-9.55,-.36,;-10.85,.44,;-10.85,2.03,;-12.17,-.35,;-12.17,-1.95,;-13.46,.44,;-14.79,-.34,;-14.79,-1.94,;-16.1,.45,;-16.1,2.03,;-14.79,2.84,;-14.79,4.42,;-13.47,5.21,;-13.47,6.81,;-14.78,7.61,;-12.17,7.61,;-17.41,-.34,;-18.72,.45,;-18.72,2.04,;-20.03,-.34,;-20.03,-1.94,;-18.72,-2.73,;-18.72,-4.32,;-17.4,-5.11,;-17.4,-6.71,;-18.73,-7.51,;-16.11,-7.51,;-21.35,.46,;-22.63,-.33,;-22.63,-1.93,;-23.96,.46,;-23.96,2.05,;-22.63,2.85,;-25.26,-.32,;-26.57,.47,;-26.57,2.05,;-27.89,-.32,;-27.89,-1.92,;-26.57,-2.71,;-25.28,-1.92,;-26.57,-4.3,;-29.2,.47,;-30.5,-.32,;-30.5,-1.92,;-31.82,.47,;-31.82,2.06,;-30.5,2.86,;-30.5,4.45,;-29.18,2.06,;-33.12,-.31,;-34.44,.47,;-34.44,2.06,;-35.73,-.31,;-35.73,-1.91,;-34.44,-2.7,;-33.13,-1.91,;-31.82,-2.71,;-31.81,-4.3,;-30.5,-5.09,;-33.12,-5.09,;-34.43,-4.3,;-37.06,.48,;-38.37,-.31,;-38.37,-1.91,;-39.67,.48,;-39.67,2.07,;-38.37,2.87,;-38.37,4.46,;-37.06,5.26,;-37.06,6.85,;-40.98,-.3,;-42.29,.48,;-42.29,2.07,;-43.59,-.3,;-43.59,-1.9,;-42.29,-2.69,;-44.92,.49,;-46.22,-.3,;-46.22,-1.89,;-47.53,.49,;-47.53,2.08,;-46.22,2.88,;-44.91,2.07,;-43.59,2.87,;-43.6,4.46,;-42.28,5.26,;-44.91,5.27,;-46.22,4.47,;-48.84,-.29,;-50.15,.49,;-50.15,2.08,;-51.46,-.29,;-51.46,-1.88,;-50.15,-2.69,;-48.85,-1.88,;-50.15,-4.28,;-52.76,.5,;-54.08,-.29,;-54.08,-1.88,;-55.39,.5,;-55.39,2.09,;-54.08,2.89,;-56.69,-.29,;-58.02,.5,;-58.02,2.09,;-59.31,-.28,;-60.63,.51,;-61.93,-.28,;-61.93,-1.87,;-63.25,.51,;-63.25,2.09,;-61.93,2.9,;-60.63,2.09,;-59.31,2.89,;-59.31,4.48,;-60.62,5.29,;-61.92,4.48,;-64.55,-.28,;-65.86,.51,;-65.86,2.1,;-67.17,-.27,;-68.49,.51,;-69.79,-.27,;-69.79,-1.86,;-71.09,.52,;-72.42,-.27,;-73.73,.52,;-73.73,2.11,;-75.03,-.27,;-75.03,-1.86,;-73.73,-2.66,;-73.73,-4.25,;-75.02,-5.05,;-72.43,-5.04,;-76.34,.52,;-77.65,-.27,;-77.65,-1.85,;-78.97,.52,;-78.97,2.11,;-77.63,2.92,;-80.26,-.26,;-81.63,.51,;-81.63,2.05,;-82.95,2.82,;-84.22,1.95,;-85.46,2.88,;-84.95,4.35,;-83.41,4.32,;-82.97,-.26,;-84.31,.52,;-82.97,-1.82,;-67.17,-1.87,;-68.49,-2.67,;-65.86,-2.67,;-59.31,-1.88,;-60.63,-2.68,;-58.02,-2.68,;3.55,-1.96,;4.86,-2.76,;2.24,-2.76,;20.57,.4,;20.57,1.99,;21.89,-.39,;23.19,.4,;23.19,1.99,;24.51,2.79,;25.82,1.99,;24.51,4.38,;24.51,-.4,;24.51,-1.99,;25.81,.4,;27.12,-.4,;27.12,-1.99,;25.81,-2.79,;28.44,-2.78,;28.44,.39,;29.75,-.4,;28.44,1.98,)|
Structure:
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