Reaction Details Report a problem with these data
Target
Glucagon receptor
Ligand
BDBM29133
Substrate
125I-Glucagon
Meas. Tech.
SPA Receptor Binding Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
119±n/a nM
Citation
 Madsen, P; Kodra, JT; Behrens, C; Nishimura, E; Jeppesen, CB; Pridal, L; Andersen, B; Knudsen, LB; Valcarce-Aspegren, C; Guldbrandt, M; Christensen, IT; Jørgensen, AS; Ynddal, L; Brand, CL; Bagger, MA; Lau, J Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties. J Med Chem 52:2989-3000 (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:
BDBM29133
Synonyms:
thiazole, 30
Type:
Small organic molecule
Emp. Form.:
C29H22F6N2O5S
Mol. Mass.:
624.551
SMILES:
O[C@H](CNC(=O)c1ccc(CC(c2nc(cs2)-c2ccc(cc2)C(F)(F)F)c2ccc(OC(F)(F)F)cc2)cc1)C(O)=O |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
125I-Glucagon
Synonyms:
n/a
Type:
radiolabeled peptide substrate
Mol. Mass.:
3483.25
Organism:
Sus scrofa (Pig)
Description:
n/a
Residue:
29
Sequence:
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT