Target
Glucagon receptor
Ligand
BDBM50324705
Substrate
n/a
Meas. Tech.
ChEMBL_651179 (CHEMBL1227944)
EC50
0.071±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 receptor
Synonyms:
GCGR | GL-R | GLR_HUMAN | Glucagon Receptor (GCGR) | Glucagon receptor (GlucR)
Type:
Enzyme
Mol. Mass.:
54026.92
Organism:
Homo sapiens (Human)
Description:
P47871
Residue:
477
Sequence:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
  
Inhibitor
Name:
BDBM50324705
Synonyms:
CHEMBL1222079
Type:
Small organic molecule
Emp. Form.:
C155H228N44O49S
Mol. Mass.:
3523.799
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(N)=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(N)=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,(49.72,-5.28,;48.42,-4.48,;48.42,-2.89,;47.11,-2.1,;47.11,-.51,;45.8,.29,;44.5,-.5,;44.5,-2.1,;43.18,.29,;43.18,1.88,;44.5,2.68,;44.5,4.27,;45.81,1.88,;41.87,-.5,;40.55,.3,;40.55,1.88,;39.26,-.5,;39.26,-2.09,;40.55,-2.88,;41.94,-2.24,;42.96,-3.42,;42.19,-4.81,;42.63,-6.25,;41.6,-7.35,;40.12,-7.01,;39.69,-5.56,;40.72,-4.46,;37.95,.3,;36.63,-.49,;36.63,-2.09,;35.32,.3,;35.32,1.89,;36.63,2.69,;36.63,4.28,;35.33,5.06,;37.95,5.07,;34.01,-.49,;32.71,.31,;32.71,1.89,;31.39,-.49,;30.08,.31,;28.78,-.48,;28.78,-2.08,;27.46,.31,;27.46,1.9,;28.78,2.7,;30.09,1.89,;31.39,2.7,;31.39,4.28,;30.09,5.07,;28.78,4.29,;26.16,-.48,;24.84,.31,;24.84,1.9,;23.54,-.48,;23.54,-2.07,;24.84,-2.86,;26.16,-2.07,;24.84,-4.46,;22.23,.32,;20.91,-.48,;20.91,-2.07,;19.6,.32,;19.6,1.91,;20.91,2.71,;20.91,4.3,;19.61,5.08,;22.23,5.08,;18.29,-.47,;16.98,.32,;16.98,1.91,;15.67,-.47,;15.67,-2.06,;14.37,.33,;13.05,-.46,;13.05,-2.06,;11.75,.33,;11.75,1.92,;13.05,2.73,;13.05,4.31,;14.37,5.09,;14.37,6.69,;13.06,7.48,;15.67,7.48,;10.44,-.46,;9.12,.33,;9.12,1.93,;7.81,-.45,;7.81,-2.05,;9.16,-2.83,;9.16,-4.38,;10.5,-5.15,;10.5,-6.7,;11.85,-7.48,;9.16,-7.48,;6.49,.34,;5.21,-.44,;5.21,-2.05,;3.88,.35,;3.88,1.93,;5.23,2.71,;5.23,4.26,;3.88,5.03,;6.56,5.03,;2.59,-.44,;1.27,.35,;1.27,1.94,;-.05,-.44,;-.05,-2.04,;1.27,-2.83,;2.57,-2.04,;1.27,-4.42,;-1.36,.35,;-2.67,-.43,;-2.67,-2.03,;-3.98,.36,;-3.98,1.94,;-2.67,2.75,;-2.67,4.33,;-1.34,1.94,;-5.27,-.43,;-6.6,.36,;-6.6,1.94,;-7.89,-.43,;-7.89,-2.03,;-6.6,-2.82,;-5.28,-2.03,;-3.97,-2.83,;-3.97,-4.42,;-2.66,-5.21,;-5.28,-5.21,;-6.59,-4.41,;-9.21,.36,;-10.53,-.42,;-10.53,-2.02,;-11.83,.36,;-11.83,1.95,;-10.53,2.75,;-10.53,4.34,;-9.22,5.14,;-9.22,6.73,;-13.14,-.42,;-14.45,.37,;-14.45,1.95,;-15.75,-.42,;-15.75,-2.02,;-14.45,-2.81,;-17.08,.37,;-18.38,-.41,;-18.38,-2.01,;-19.68,.37,;-19.68,1.96,;-18.38,2.76,;-17.07,1.96,;-15.75,2.76,;-15.75,4.35,;-14.44,5.14,;-17.07,5.14,;-18.38,4.35,;-21,-.41,;-22.3,.38,;-22.3,1.96,;-23.62,-.41,;-23.62,-2,;-22.3,-2.8,;-21.01,-2,;-22.3,-4.39,;-24.92,.38,;-26.24,-.41,;-26.24,-2,;-27.55,.38,;-27.55,1.97,;-26.24,2.77,;-28.85,-.4,;-30.18,.39,;-30.18,1.97,;-31.46,-.4,;-32.79,.39,;-34.09,-.4,;-34.09,-1.99,;-35.41,.39,;-35.41,1.98,;-34.09,2.78,;-32.79,1.98,;-31.47,2.78,;-31.47,4.37,;-32.78,5.16,;-34.08,4.37,;-36.71,-.39,;-38.03,.4,;-38.03,1.98,;-39.33,-.39,;-40.65,.4,;-41.95,-.39,;-41.95,-1.98,;-43.25,.4,;-44.58,-.38,;-45.88,.4,;-45.88,1.99,;-47.19,-.38,;-47.19,-1.97,;-45.88,-2.77,;-45.88,-4.37,;-47.18,-5.16,;-44.59,-5.16,;-48.5,.41,;-49.81,-.38,;-49.81,-1.97,;-51.13,.41,;-51.13,2,;-49.79,2.8,;-52.42,-.38,;-53.77,.39,;-53.77,1.92,;-55.09,2.69,;-56.35,1.82,;-57.58,2.75,;-57.09,4.22,;-55.54,4.18,;-55.1,-.38,;-56.43,.39,;-55.1,-1.93,;-39.33,-1.98,;-40.65,-2.79,;-38.03,-2.78,;-31.46,-1.99,;-32.79,-2.8,;-30.18,-2.79,;31.39,-2.08,;32.71,-2.87,;30.08,-2.88,;48.42,.29,;48.42,1.87,;49.74,-.51,;51.03,.28,;51.03,1.87,;52.35,2.67,;53.66,1.87,;52.35,4.26,;52.35,-.51,;52.35,-2.1,;53.66,.28,;54.97,-.52,;54.97,-2.11,;53.66,-2.9,;56.28,-2.9,;56.28,.28,;57.58,-.52,;56.28,1.86,)|
Structure:
Search PDB for entries with ligand similarity: