Target
Glucagon-like peptide 1 receptor
Ligand
BDBM50324703
Substrate
n/a
Meas. Tech.
ChEMBL_651180 (CHEMBL1227945)
EC50
1.1±n/a nM
Citation
 Day, JWOttaway, NPatterson, JTGelfanov, VSmiley, DGidda, JFindeisen, HBruemmer, DDrucker, DJChaudhary, NHolland, JHembree, JAbplanalp, WGrant, ERuehl, JWilson, HKirchner, HLockie, SHHofmann, SWoods, SCNogueiras, RPfluger, PTPerez-Tilve, DDiMarchi, RTschöp, 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:
BDBM50324703
Synonyms:
CHEMBL1222077
Type:
Small organic molecule
Emp. Form.:
C155H226N42O51S
Mol. Mass.:
3525.769
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](CCC(O)=O)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(O)=O |r,wU:208.216,180.193,170.177,150.163,135.144,115.122,98.106,76.86,62.70,43.53,30.37,8.12,234.240,wD:199.210,191.197,222.230,176.181,225.233,162.171,144.150,123.135,107.114,87.97,71.74,54.61,39.41,16.28,4.4,242.248,243.251,212.217,(49.71,-5.26,;48.4,-4.46,;48.4,-2.87,;47.1,-2.08,;47.1,-.49,;45.79,.31,;44.48,-.48,;44.48,-2.08,;43.16,.31,;43.16,1.9,;44.48,2.7,;44.48,4.29,;45.79,1.9,;41.86,-.48,;40.55,.32,;40.55,1.9,;39.24,-.48,;39.24,-2.07,;40.55,-2.86,;41.92,-2.22,;42.95,-3.4,;42.18,-4.79,;42.64,-6.29,;41.63,-7.47,;40.15,-7.14,;39.68,-5.63,;40.7,-4.45,;37.93,.32,;36.62,-.47,;36.62,-2.07,;35.31,.32,;35.31,1.91,;36.62,2.71,;36.62,4.3,;35.32,5.08,;37.94,5.09,;34,-.47,;32.69,.32,;32.69,1.91,;31.38,-.47,;30.07,.33,;28.77,-.47,;28.77,-2.06,;27.45,.33,;27.45,1.92,;28.77,2.72,;30.07,1.91,;31.38,2.71,;31.39,4.3,;30.08,5.09,;28.77,4.31,;26.15,-.46,;24.82,.33,;24.82,1.92,;23.53,-.46,;23.53,-2.05,;24.82,-2.84,;26.15,-2.05,;24.82,-4.44,;22.22,.34,;20.91,-.46,;20.91,-2.05,;19.58,.34,;19.58,1.93,;20.91,2.73,;20.91,4.32,;19.59,5.1,;22.22,5.1,;18.28,-.45,;16.98,.34,;16.98,1.93,;15.66,-.45,;15.66,-2.04,;14.37,.35,;13.04,-.44,;13.04,-2.04,;11.73,.35,;11.73,1.93,;13.04,2.75,;13.04,4.32,;14.38,5.11,;14.38,6.71,;13.05,7.5,;15.67,7.5,;10.43,-.44,;9.1,.35,;9.1,1.95,;7.81,-.43,;7.81,-2.03,;9.1,-2.83,;9.1,-4.42,;10.45,-5.19,;10.45,-6.73,;11.78,-7.5,;9.1,-7.5,;6.49,.36,;5.2,-.42,;5.2,-2.03,;3.88,.37,;3.88,1.95,;5.21,2.72,;5.21,4.27,;3.88,5.04,;6.55,5.04,;2.57,-.42,;1.25,.37,;1.25,1.96,;-.07,-.42,;-.07,-2.02,;1.25,-2.81,;2.57,-2.02,;1.25,-4.4,;-1.37,.37,;-2.66,-.41,;-2.66,-2.01,;-3.99,.38,;-3.99,1.96,;-2.66,2.77,;-2.66,4.35,;-1.35,1.96,;-5.29,-.41,;-6.6,.38,;-6.6,1.96,;-7.91,-.41,;-7.91,-2.01,;-6.6,-2.8,;-5.3,-2.01,;-3.99,-2.81,;-3.99,-4.4,;-2.67,-5.19,;-5.3,-5.19,;-6.61,-4.39,;-9.23,.38,;-10.54,-.4,;-10.54,-2,;-11.84,.38,;-11.84,1.97,;-10.54,2.77,;-10.54,4.36,;-9.22,5.16,;-9.22,6.74,;-13.14,-.4,;-14.46,.39,;-14.46,1.97,;-15.77,-.4,;-15.77,-2,;-14.46,-2.79,;-17.08,.39,;-18.39,-.4,;-18.39,-1.99,;-19.7,.39,;-19.7,1.98,;-18.39,2.78,;-17.08,1.98,;-15.77,2.78,;-15.77,4.37,;-14.45,5.16,;-17.07,5.16,;-18.38,4.37,;-21.01,-.39,;-22.32,.4,;-22.32,1.98,;-23.62,-.39,;-23.62,-1.98,;-22.32,-2.78,;-21.01,-1.98,;-22.32,-4.37,;-24.94,.4,;-26.24,-.39,;-26.24,-1.98,;-27.55,.4,;-27.55,1.99,;-26.24,2.79,;-28.86,-.38,;-30.18,.41,;-30.18,1.99,;-31.48,-.38,;-32.8,.41,;-34.11,-.38,;-34.11,-1.97,;-35.42,.41,;-35.42,2,;-34.11,2.8,;-32.81,1.99,;-31.48,2.8,;-31.47,4.38,;-32.79,5.18,;-34.09,4.39,;-36.71,-.37,;-38.03,.41,;-38.03,2,;-39.35,-.37,;-40.64,.42,;-41.96,-.37,;-41.96,-1.96,;-43.26,.42,;-44.59,-.36,;-45.9,.42,;-45.9,2.01,;-47.19,-.36,;-47.19,-1.95,;-45.9,-2.75,;-45.9,-4.35,;-47.2,-5.14,;-44.59,-5.14,;-48.5,.42,;-49.81,-.36,;-49.81,-1.95,;-51.13,.43,;-51.13,2.02,;-49.81,2.82,;-52.43,-.36,;-53.78,.41,;-53.78,1.95,;-55.1,2.71,;-56.37,1.85,;-57.61,2.77,;-57.1,4.25,;-55.55,4.21,;-55.11,-.37,;-56.45,.41,;-55.11,-1.92,;-39.35,-1.96,;-40.64,-2.77,;-38.03,-2.76,;-31.48,-1.97,;-32.8,-2.78,;-30.18,-2.77,;31.38,-2.06,;32.69,-2.85,;30.07,-2.86,;48.4,.31,;48.4,1.89,;49.72,-.49,;51.02,.3,;51.02,1.89,;52.34,2.69,;53.65,1.89,;52.34,4.28,;52.34,-.49,;52.34,-2.09,;53.64,.3,;54.95,-.5,;54.95,-2.09,;53.64,-2.88,;56.27,-2.88,;56.27,.3,;57.61,-.46,;56.27,1.88,)|
Structure:
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